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HK1002279A - Heterocyclic compounds having tachykinin receptor antagonist activity, their preparation and their use - Google Patents

Heterocyclic compounds having tachykinin receptor antagonist activity, their preparation and their use Download PDF

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HK1002279A
HK1002279A HK98101290.8A HK98101290A HK1002279A HK 1002279 A HK1002279 A HK 1002279A HK 98101290 A HK98101290 A HK 98101290A HK 1002279 A HK1002279 A HK 1002279A
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single bond
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西刚秀
石桥公树
中岛胜义
深沢彻也
藏田等司
山口武
伊藤一洋
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三共株式会社
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Description

Heterocyclic compounds having tachykinin receptor antagonistic activity, their preparation and use
Background
The present invention relates to a series of novel heterocyclic compounds having tachykinin receptor antagonistic activity. Also provided are methods and compositions for using them in the treatment and prevention of disease, as well as methods for preparing them and intermediates useful in their preparation.
The various forms of tachykinins present in mammals are associated with a variety of diseases and disorders, including respiratory diseases such as asthma, bronchitis, rhinitis and cough; (ii) an allergic reaction; ocular inflammations such as conjunctivitis and vernal conjunctivitis; skin diseases such as contact dermatitis, allergic dermatitis and urticaria; diseases related to rheumatism, such as rheumatoid arthritis; pain, such as migraine, headache and toothache; central nervous system disorders such as anxiety and alzheimer's disease; and gastrointestinal diseases such as colitis; and cystitis; and so on. Thus, inhibition of the activity of these forms of tachykinin would lead to novel treatments and/or prevention of these diseases and disorders.
The compounds of the invention are generally antagonistic to the tachykinin receptor but also to the substance P receptor (this receptor is generally referred to as the "neurokinin 1 receptor" -NK1) And the neurokinin A receptor (this receptor is generally referred to as the "neurokinin 2 receptor" -NK2) Has special antagonistic effect. The compounds of the invention are particularly advantageous in that they can simultaneously antagonize these receptors, also known as "dual action".
Compounds structurally related to the compounds of the present invention are disclosed in FR2729952, FR2729953 and FR 2729954. However, they are selectivelyActing on NK1None of the compounds have the dual role of the compounds of the present invention.
Non-peptide compounds of low molecular weight are known to have antagonistic effects on these two receptors, for example, certain compounds disclosed in WO 9429309(1994), WO 9417045(1994), WO 9426735(1994) and WO 9528389 (1995). Typical examples of compounds disclosed in these documents include:compound AWO 9429309Compound BWO 9417045Compound CWO 9426735
However, these compounds are poorly absorbed orally. Thus, these prior art compounds cannot be administered orally and must be administered parenterally, e.g., by injection. As is common knowledge in the medical field, administration of any drug by injection is undesirable because it requires either training of the patient (and some patients are not trainable themselves) or administration by experienced medical personnel, which adds to the expense and inconvenience to both the patient and the medical personnel.
Therefore, there is a need to develop novel tachykinin receptor antagonists having the above dual effects, good oral absorption effect and low toxicity.
We have found a series of novel compounds which have antagonistic NK activity at least equivalent to those of the compounds of the prior art1Are active and have a dual effect and they surprisingly have a tailored strong antagonistic NK2The activity of the receptor.
Summary of The Invention
It is therefore an object of the present invention to provide a series of novel heterocyclic compounds.
It is another more specific object of the present invention to provide compounds having tachykinin receptor antagonistic activity.
It is another more specific object of the present invention to provide a toolSuch as NK1And NK2The tachykinin receptor antagonistic activity of a compound of (a).
It is another more specific object of the invention to provide compounds with greatly increased activity.
Other objects and advantages of the present invention will become apparent as the description proceeds.
The compounds of the present invention are compounds of formula (I) and its quaternary ammonium derivatives of formula (Ia), and their pharmaceutically acceptable salts and esters:wherein: r1And R2Which may be the same or different, each represents a carbocyclic aryl or an aromatic heterocyclic group, the aryl and heterocyclic groups being unsubstituted or substituted by at least one substituent preferably selected from the group consisting of α, A represents a methylene group, a carbonyl group or a sulfonyl group, B represents the groups A and R1An alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 4 carbon atoms; drepresents an oxygen or sulfur atom; e represents an alkylene group having 1 to 6 carbon atoms, a haloalkylene group having 1 to 6 carbon atoms, a cycloalkane-1, 1-diyl group having 3 to 6 carbon atoms, a cycloalkane-1, 1-diyl methyl group having 3 to 6 carbon atoms in the cycloalkane moiety or a cycloalkane-1, 1-di (ylmethyl) group having 3 to 6 carbon atoms in the cycloalkane moiety; g represents an alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 4 carbon atoms; l represents orGroup or formulaGroup wherein R3Denotes a carbocyclic aryl or aromatic heterocyclic radical, which aryl and aromatic heterocyclic radicals are unsubstituted or substituted by at least one substituent preferably selected from the group of substituents α4Represents a hydrogen atom, a carbocyclic aryl or aromatic heterocyclic group which is unsubstituted or substituted by at least one substituent preferably selected from the group consisting of α5Expression formula (I)A group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an amino group, an amido group, a C1-C6 alkyl groupAn alkyl group substituted with an amido group, an amido group in which the nitrogen atom is substituted with an alkyl group having 1 to 6 carbon atoms, a hydroxyl group, a hydroxyalkyl group having 1 to 6 carbon atoms, an alkoxyalkyl group in which the alkoxy moiety and the alkyl moiety each have 1 to 6 carbon atoms, or an aralkyloxyalkyl group in which the oxyalkyl moiety has 1 to 6 carbon atoms, the alkyl moiety of the aralkyl moiety has 1 to 4 carbon atoms and is substituted with 1 to 3 carbocyclic aryl groups which are unsubstituted or substituted with at least one substituent α preferably custom defined wherein R is6Represents an alkyl group having 1 to 6carbon atoms, an alkoxy group having 1 to 6 carbon atoms, orA group, a carbocyclic aryl or heterocyclic group, the aryl and heterocyclic groups being unsubstituted or substituted by at least one substituent preferably selected from the group consisting of α
Wherein R isaRepresents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, having 1 to 6 carbons
Alkoxy of an atom, aliphatic carboxylic acid acyl having 1 to 6 carbon atoms, having 1 to 6 carbons
Alkanesulfonyl of an atom, haloalkanesulfonyl having 1 to 6 carbon atoms, having 3 to 8
Cycloalkyl of carbon atoms, unsubstituted or substituted by at least one substituent preferably self-defined
α or wherein the alkyl moiety has from 1 to 4 carbon atoms and
aralkyl substituted by 1 to 3 carbocyclic aryl groups as defined above, and
wherein R isbRepresents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, having 1 to 6 carbons
Alkoxy of an atom, aliphatic carboxylic acid acyl having 1 to 6 carbon atoms, having 1 to 6 carbons
Alkanesulfonyl of an atom, haloalkanesulfonyl having 1 to 6 carbon atoms, having 3 to 8
Cycloalkyl radicals, carbocyclic aryl radicals or aromatic heterocyclic radicals of carbon atoms, the aryl and aromatic heterocyclic radicals not being
Substituted or substituted by at least one substituent preferably selected from the group consisting of α
Wherein the alkyl moiety has from 1 to 4 carbon atoms and is taken up by from 1 to 3 carbocyclic aryl groups as defined above
A substituted aralkyl group,
or
RaAnd RbTogether with the nitrogen atom to which they are attached represent a nitrogen-containing heterocyclic group, R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent selected from the group consisting of substituents β as defined below, and which has one heteroatom selected from nitrogen, oxygen and sulfur atoms, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above and fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl and aromatic heterocyclyl group are unsubstituted or substituted by at least one substituent preferably defined as substituent α7Represents an alkyl group having 1 to 6 carbon atoms, and the above-mentioned substituent α is selected from the group consisting of a halogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxylic acid acyl group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, a hydroxyl group, a carboxyl group, an alkoxycarbonyl group having 1 to 6 carbon atoms in the alkoxy moiety, an acylaliphatic carboxylic acid amino group having 1 to 6 carbon atoms, an alkylsulfonylamino group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, an amino group, a cyano group, and an alkylene group having 1 to 8 carbon atoms (forming a cycloalkyl group fused with an aryl group or a heterocyclic group), the above-mentioned substituent β is:
when substituting carbon atoms, oxo
When substituted for a nitrogen atom, selected from alkylsulfonyl groups of 1 to 6 carbon atoms, having 1 to 6 carbon atoms
Alkyl which is unsubstituted or substituted by at least one substituent which is preferably defined by the following substituents γ,
aliphatic acyl radicals, unsubstituted or substituted by at least one substituent, preferably defined as substituent α above
Carbocyclic aryl radicals in which the alkyl part has from 1 to 4 carbon atoms and is interrupted by from 1 to 3 carbocyclic rings as defined above
An aryl-substituted aralkyl group, a substituted aralkyl group,
and when substituting the sulfur atom, one or two oxygen atoms to form a sulfoxide or sulfone group; and the above-mentioned substituent γ is selected from the group consisting of a halogen atom, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxylic acid group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, a hydroxyl group, a carboxyl group, an alkoxycarbonyl group having 1 to 6 carbon atoms in the alkoxy moiety, an aliphatic acylamino group having 1 to 6 carbon atoms, an amino group, and a cyano group.
The present invention also provides a composition for treating or preventing central nervous system disorders, neurodegenerative disorders, respiratory disorders, inflammatory disorders, allergy, allergic disorders, ophthalmic disorders, skin disorders, drug addiction, physical disorders caused by stress, sympathetically-reflective dystrophy, dysthymia, unwanted immune responses, disorders associated with increased immunity, digestive disorders, emesis, bladder disorders, eosinophilia, disorders caused by abnormal blood flow, and pain, comprising an effective amount of a compound of formula (I) or (Ia), or a pharmaceuticallyacceptable salt or ester thereof, in admixture with a pharmaceutically acceptable carrier or diluent.
The invention further provides a method of treatment or prophylaxis of diseases or disorders of the central nervous system, neurodegenerative diseases, respiratory diseases, inflammatory diseases, allergy, allergic diseases, ophthalmic diseases, dermatological diseases, drug addiction, physical disorders caused by stress, sympatholytic dystrophy, dysthymia, unwanted immune responses, diseases associated with increased immunity, diseases of the digestive system, emesis, bladder function disorders, eosinophilia, diseases caused by abnormal blood flow, and pain, which comprises administering to an animal, which may be a human, suffering from or susceptible to such a disease or disorder an effective amount of a compound of formula (I) or (Ia), or a pharmaceutically acceptable salt or ester thereof.
The present invention also provides compounds of formula (Iz):wherein:
j represents an alkylene group having 1 to 6 carbon atoms;
ar represents a fused ring of a carbocyclic aryl or aromatic heterocyclic group, the aryl and aromatic heterocyclic groups being unsubstituted or
Substituted with at least one substituent preferably customized to substituent α as above;
R14represents a hydrogen atom or an amino protecting group; and
represents a sulfoxide group in which the sulfur atom has the S-configuration.
Detailed description of the invention
When R is1,R2,R3,R4,R6,Ra,RbAr or the substituent β represents a carbocyclic aryl group having 5 to 14, preferably 6 to 14, more preferably 6 to 10, most preferably 6 or 10 ring carbon atoms, these groups may have a single aromatic ring or may have two or more fused aromatic rings, these groups may be unsubstituted or may be substituted with one or more substituents selected from the group consisting of the substituents α as defined above and listed below, except for the number of substitutable positions, sometimes sterically restricting the rings, the number of substituents is not limited, however, when the groups are substituted, we generally prefer 1 to 3 substituents.
Examples of substituted groups include 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, 2, 4-dimethoxyphenyl, 2, 3-dimethoxyphenyl, 2, 5-dimethoxyphenyl, 3, 4-dimethoxyphenyl, 3, 5-dimethoxyphenyl, 2, 6-dimethoxyphenyl, 3, 4, 5-trimethoxyphenyl, 2, 3, 4-trimethoxyphenyl, 2, 3, 5-trimethoxyphenyl, 2, 3, 6-trimethoxyphenyl, 2, 4, 6-trimethoxyphenyl, 2-ethoxyphenyl, 3-ethoxyphenyl, 4-ethoxyphenyl, 2-isopropoxyphenyl, 3-isopropoxyphenyl, 4-isopropoxyphenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2, 4-dimethylphenyl, 2, 3-dimethylphenyl, 2, 5-dimethylpropyl, 3, 4-dimethylphenyl, 3, 5-dimethylphenyl, 2, 6-dimethylphenyl, 3, 4, 5-trimethylphenyl, 2, 3, 4-trimethylphenyl, 2, 3, 5-trimethylphenyl, 2, 3, 6-trimethylphenyl, 2, 4, 6-trimethylphenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2, 4-dichlorophenyl, 2, 3-dichlorophenyl, 2, 5-dichlorophenyl, 3, 4-dichlorophenyl, 3, 5-dichlorophenyl, 2, 6-dichlorophenyl, 3, 4, 5-trichlorophenyl group, 2, 3, 4-trichlorophenyl group, 2, 3, 5-trichlorophenyl group, 2, 3, 6-trichlorophenyl group, 2, 4, 6-trichlorophenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2, 4-difluorophenyl group, 2, 3-difluorophenyl group, 3, 4-difluorophenyl group, 3, 5-difluorophenyl group, 2, 6-difluorophenyl group, 3, 4, 5-trifluorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 2, 4-bis (trifluoromethyl) phenyl group, 2, 3-bis (trifluoromethyl) phenyl group, 3, 4-bis (trifluoromethyl) phenyl group, 3, 5-bis (trifluoromethyl) phenyl, 2, 6-bis (trifluoromethyl) phenyl, 3, 4, 5-tris (trifluoromethyl) phenyl, 2-acetamidophenyl, 3-acetamidophenyl, 4-acetamidophenyl, 2-methoxycarbonylphenyl, 3-methoxycarbonylphenyl, and 4-methoxycarbonylphenyl.
When substituent α is an alkylene group having 1 to 8 carbon atoms, it forms, together with the two carbon atoms of the aryl group to which it is attached, a cycloalkyl fused to the aryl group an example of a fused ring is 2, 3-indanyl.
When R is1,R2,R3,R4,R6,RbOr Ar represents an aromatic heterocyclic group, they have 5 to 7 ring atoms. A monocyclic ring in which 1 to 3 atoms are hetero atoms selected from nitrogen, oxygen and sulfur atoms, or in which at least one is as defined aboveThe other rings are fused ring systems of aromatic heterocyclic or carbocyclic aryl as defined above. When there are 3 heteroatoms in the heteroaromatic ring, they are preferably all nitrogen atoms, or have one or two nitrogen atoms, respectively two or one oxygen and/or sulfur atoms.
Examples of aryl heterocyclic groups include furyl, thienyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1, 2, 3-oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl. Preferably a 5-to 7-membered aromatic heterocycle containing at least one nitrogen atom, optionally with additional nitrogen, oxygen or sulphur atoms, examples of such groups include pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1, 2, 3-oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl. Of these groups, pyridyl, imidazolyl, oxazolyl, pyrazinyl and thiazolyl are more preferable.
These heteroaryl groups may form fused rings with other cyclic groups, and examples of such fused ring systems include thienylyl, benzofuranyl, benzothienyl, benzoxazolyl, benzimidazolyl, isoquinolyl, quinolyl and quinoxalinyl.
These heteroaryl groups may be unsubstituted or substituted with one or more substituents selected from the group consisting of the substituents α defined above and exemplified below, the number of substituents being not particularly limited except for the limitation by steric hindrance at the substitution position.
Optionally, R6May represent non-aromatic (preferably saturated) heterocyclic groups which may have 5 to 7 ring atoms of which 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur atoms, preferably at least one of which is nitrogen. Examples of such groups include pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinyl, morpholinyl, thioxolinyl, oxazolidinyl, thiazolidinyl, diazolidinyl, oxolanyl, thiolanyl and perhydropyridinyl.
When B or G represents an alkylene group having 1 to 4 carbon atoms, they may be a linear or branched group having 1 to 4 carbon atoms, and examples thereof include methylene, methylmethylene, 1, 2-ethylene, 1, 2-propylene, 1, 3-propylene, 1, 4-butylene, 1-methyl-1, 3-propylene, 2-methyl-1, 3-propylene and 3-methyl-1, 3-propylene, among which a linear or branched alkylene group having 1 to 3 carbon atoms is preferred, a linear or branched alkylene group having 2 or 3 carbon atoms is more preferred, and a 1, 2-ethylene group or a 1, 3-propylene group is most preferred.
When B or G represents an alkenylene group having 2 to 4 carbon atoms, they may be a straight chain or branched group having 2 to 4 carbon atoms, and examples thereof include a vinylenegroup, a 2-propenylene group, a 1-methyl-2-propenylene group, a 2-ethyl-2-propenylene group and a 2-butenylene group, of which the vinylene group, the 2-propenylene group and the 3-butenylene group are preferred, and the vinylene group or the 2-propenylene group is more preferred.
When E or J represents an alkylene group having 1 to 6 carbon atoms, it may be a straight or branched chain group having 1 to 6 carbon atoms, examples thereof include methylene, methylmethylene, 1, 2-ethylene, 1, 2-propylene, 1, 3-propylene, 1, 4-butylene, 1-methyl-1, 3-propylene, 2-methyl-1, 3-propylene, 3-methyl-1, 3-propylene, 1, 5-pentylene, 1, 6-hexylene, 1, 1-dimethyl-1, 3-propylene, 2, 2-dimethyl-1, 3-propylene, 1, 1-dimethyl-1, 4-butylene, and 2, 2-dimethyl-1, 4-butylene. Among them, a linear or branched alkylene group having 1 to 4 carbon atoms is preferable, and a methylene group or a 1, 2-ethylene group is more preferable.
E may also represent a haloalkylene group having 1 to 6 carbon atoms substituted with 1 to 3 halogen atoms, preferably fluorine, chlorine, bromine and iodine atoms, wherein the alkylene group may be any of the unsubstituted alkylene groups exemplified above.
When E represents a cycloalkane-1, 1-diyl group having 3 to 6 carbon atoms, it is a group of the formulaWherein m is an integer from 2 to 5. When E represents a cycloalkane having a cycloalkyl moiety of 3 to 6 carbon atomsWhen the radical is a 1, 1-diyl methyl radical, it is a radical of the formulaWherein m is as defined above. When E represents cycloalkane-1, 1-bis (ylmethyl) group having 3 to 6 carbon atoms in the cycloalkyl moiety, it is a group of formulaWherein m is as defined above.
Examples of such groups include cyclopropane-1, 1-diyl, cyclobutane-1, 1-diyl, cyclopentane-1, 1-diyl, cyclohexane-1, 1-diyl, cyclopropane-1, 1-diyl methyl, cyclobutane-1, 1-diyl methyl, cyclopentane-1, 1-diyl methyl, cyclohexane-1, 1-diyl methyl, cyclopropane-1, 1-di (ylmethyl), cyclobutane-1, 1-di (ylmethyl), cyclopentane-1, 1-di (ylmethyl), cyclohexane-1, 1-di (ylmethyl), wherein cyclopropane-1, 1-diyl, cyclobutane-1, 1-diyl, cyclopropane-1, 1-diyl methyl and cyclobutane-1 are preferred, 1-diyl methyl group.
When R is5,R6,R7,Ra,RbWhen the substituent α or the substituent β represents an alkyl group having 1 to 6 carbon atoms, it may be a straight-chain or branched-chain alkyl group having 1 to 6 carbon atoms, and examples thereof include methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, 2-methylbutyl, neopentyl, 1-ethylpropyl, hexyl, isohexyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 3, 3-dimethylbutyl, 2, 2-dimethylbutyl, 1, 1-dimethylbutyl, 1, 2-dimethylbutyl, 1, 3-dimethylbutyl, 2, 3-dimethylbutyl and 2-ethylbutyl groups, preferably straight-chain or branched-chain alkyl groups having 1 to 4 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl and tert-butyl groups, of which methyl and ethyl groups are preferred.
When R is5,R6,Ra,RbWhen the substituent γ or the substituent α represents an alkoxy group having 1 to 6 carbon atoms, it may be a straight-chain or branched alkoxy group having 1 to 6 carbon atoms, and examples thereof include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxyA group selected from the group consisting of a sec-butoxy group, a tert-butoxy group, a pentyloxy group, an isopentyloxy group, a 2-methylbutyloxy group, a neopentyloxy group, a 1-ethylpropoxy group, a hexyloxy group, an isohexyloxy group, a 4-methylpentyloxy group, a 3-methylpentyloxy group, a 2-methylpentyloxy group, a 1-methylpentyloxy group, a3, 3-dimethylbutoxy group, a2, 2-dimethylbutoxy group, a 1, 1-dimethylbutoxy group, a 1, 2-dimethylbutoxy group, a 1, 3-dimethylbutoxy group, a2, 3-dimethylbutyl group, and a 2-ethylbutyl group, preferably a straight-chain or branched-chain alkoxy group having 1 to 4 carbon atoms, such as a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group.
When R is5When representing an acylamino group, the acyl moiety may be selected from a variety of acyl groups known in the art. For example, it may be: aliphatic acyl, such as alkanoyl, preferably having 1 to 21 carbon atoms, more preferably 1 to 6 carbon atoms, most preferably 2 to 6 carbon atoms, for example formyl, acetyl, propionyl, butyryl, isobutyryl, pivaloyl, valeryl, isovaleryl, octanoyl, nonanoyl, decanoyl, 3-methylnonanoyl, 8-methylnonanoyl, 3-ethyloctanoyl, 3, 7-dimethyloctanoyl, undecanoyl, dodecanoyl, tridecanoyl, tetradecanoyl, pentadecanoyl, hexadecanoyl, 1-methylpenecanoyl, 14-methylpenecanoyl, 13, 13-dimethyltetradecanoyl, heptadecanoyl, 15-methylhexadecanoyl, octadecanoyl, 1-methyldecadecanoylHeptaalkanoyl, nonadecanoyl, eicosanoyl or heneicosanoyl; haloalkanoyl, wherein the alkanoyl moiety may be any of the alkanoyl exemplified above except formyl, but is preferably alkanoyl having 2 to 6 carbon atoms, of which haloalkanoyl having 1 to 3 halogen atoms is preferred, such as chloroacetyl, dichloroacetyl, trichloroacetyl or trifluoroacetyl; an alkoxyalkyl group in which the alkoxy moiety has 1 to 6 carbon atoms and may be any of the alkoxy groups exemplified for R5 etc., as mentioned above, and the alkanoyl moiety may be any of the alkanoyl groups exemplified above except formyl, but preferably a group having 2 to 6 carbon atoms, for example, a methoxyacetyl group; alkenoylAn alkyl or alkanoyl group, preferably having 3 to 6 carbon atoms, e.g., acryloyl, propioloyl, methacryloyl, butyroyl, methacryloyl or (E) -2-methyl-2-butenoyl; aromatic acyl groups in which the aryl moiety may be R as defined above1Aryl groups as defined and exemplified in (a) and (b) such as unsubstituted arylcarbonyl, e.g., benzoyl, 1-naphthoyl or 2-naphthoyl; haloarylcarbonyl groups in which the aryl moiety can be R as described above1Aryl groups as defined and exemplified in (i) and (ii) such as 2-bromobenzoyl or 4-chlorobenzoyl; alkyl-substituted arylcarbonyl groups in which the aryl moiety can be R as described above1Aryl as defined and exemplified in (1), and alkyl moieties can be R as described above5Alkyl as defined and exemplified in (1) and (b) such as 2, 4, 6-trimethylbenzoyl or 4-toluoyl; alkoxy-substituted arylcarbonyl groups in which the aryl moiety can be R as described above1Aryl defined and exemplified in the above and alkoxy moieties can be R as described above5Alkoxy groups as defined and exemplified in (1) and (b) such as 4-methoxybenzoyl; nitro-substituted arylcarbonyl groups in which the aryl moiety may be R as described above1Aryl groups as defined and exemplified in (1) and (2) such as 4-nitro-benzoyl or 2-nitrobenzoyl; alkoxycarbonyl-substituted arylcarbonyl groups in which the aryl moiety can be R as described above1The alkoxy moiety of the arylalkoxycarbonyl group as defined and exemplified in (a) and (b) may be R as described above5Alkoxy as defined and exemplified in (1) and (b), such as 2- (methoxycarbonyl) benzoyl; aryl-substituted arylcarbonyl groups in which each aryl moiety can be R as described above1Aryl groups as defined and exemplified in (1), (b), (c) and (d), etc., such as 4-phenylbenzoyl; alkoxycarbonyl having from 1 to 6, preferably from 1 to 4, carbon atoms in the alkoxy moiety (i.e.having from 2 to 7, preferably from 2 to 5, carbon atoms in total), such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl, sec-butoxycarbonyl, tert-butoxycarbonyl, pentyloxycarbonyl, isopentyloxycarbonyl, 2-methylbutoxycarbonyl, neopentyloxycarbonyl, 1-ethylpropoxycarbonyl, hexyloxycarbonyl,iso-hexyloxycarbonyl, 4-methylpentyloxycarbonyl, 3-methylpentyloxycarbonyl, 2-methylpentyloxycarbonyl, 1-methylpentyloxycarbonyl, 3, 3-dimethylbutyloxycarbonyl, 2, 2-dimethylbutyloxycarbonyl, 11-dimethylbutoxycarbonyl, 1, 2-dimethylbutoxycarbonyl, 1, 3-dimethylbutoxycarbonyl, 2, 3-dimethylbutoxycarbonyl and 2-ethylbutyloxycarbonyl, preferably methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl, sec-butoxycarbonyl and tert-butoxycarbonyl, with methoxycarbonyl, ethoxycarbonyl, tert-butoxycarbonyl and isobutoxycarbonyl being preferred; alkoxycarbonyl substituted by a halogen atom or trialkylsilyl group, wherein each alkyl moiety has 1 to 6 carbon atoms, such as 2, 2, 2-trichloroethoxycarbonyl or 2-trimethylsilylethoxycarbonyl; alkenylcarbonyl, the alkenyl moiety having from 2 to 6 carbon atoms, such as vinylcarbonyl and allylcarbonyl; aralkylcarbonyl in which the aromatic ring may be substituted by 1 or 2 alkoxy groups having 1 to 6 carbon atoms or by nitro groups, such as benzylcarbonyl, phenacylcarbonyl, 4-methoxybenzylcarbonyl, 3, 4-dimethoxybenzylcarbonyl, 2-nitrobenzylcarbonyl and 4-nitrobenzylcarbonyl; alkylsulfonyl groups having 1 to 6 carbon atoms such as methylsulfonyl group, ethylsulfonyl group and 1-propylsulfonyl group; fluoroalkanesulfonyl groups having 1 to 6 carbon atoms such as trifluoromethanesulfonyl and pentafluoroethanesulfonyl; arylsulfonyl wherein the aryl moiety is as above R1Etc., such as phenylsulfonyl and p-toluenesulfonyl.
Among them, aliphatic acyl groups, aromatic acyl groups and alkylsulfonyl groups are preferred.
When R is5When an alkyl group having 1 to 6 carbon atoms is represented and substituted with an amido group, the alkyl moiety can be any of the above R5The alkyl, acyl substituents defined and exemplified in (A) can be any of the above R5Acyl groups as defined and exemplified in (1).
When R is5When representing an acylamino group in which a nitrogen atom is substituted with an alkyl group having 1 to 6 carbon atoms, the acyl substituent may be any of the above R5The acyl, alkyl moieties defined and exemplified in (A) can be any of the above R5Alkyl groups as defined and exemplified in (1).
When R is5When a hydroxyalkyl group having 1 to 6 carbon atoms is represented, it may be any of the above-mentioned alkyl groups substituted with at least one hydroxyl group,for example hydroxymethyl, hydroxyethyl, hydroxypropyl, hydroxybutyl, hydroxypentyl, or hydroxyhexyl.
When R is5When alkoxyalkyl is represented, the alkoxy and alkyl moieties can each be selected from the group consisting of R described above5The corresponding groups as defined and exemplified in (a). Examples of alkoxyalkyl groups include: methoxymethyl, ethoxymethyl, propoxymethyl, isopropoxymethyl, butoxymethyl, isobutoxymethyl, sec-butoxymethyl, tert-butoxymethyl, pentoxymethyl, isopentyloxymethyl, neopentyloxymethyl, hexyloxymethyl, isohexyloxymethyl, methoxyethyl, ethoxyethyl, propoxyethyl, isopropoxyethyl, butoxyethyl, isobutoxyethyl, sec-butoxyethyl, tert-butoxyethyl, pentyloxyethylOxyethyl, isopentyloxyethyl, neopentyloxyethyl, hexyloxyethyl, isohexyloxyethyl, methoxypropyl, ethoxypropyl, propoxypropyl, isopropyl, butoxypropyl, isobutoxypropyl, sec-butoxypropyl, tert-butoxypropyl, pentyloxypropyl, isopentyloxypropyl, neopentyloxypropyl, hexyloxypropyl, isohexyloxypropyl, methoxybutyl, ethoxybutyl, propoxybutyl, isopropoxybutyl, butoxybutyl, isobutoxybutyl, sec-butoxybutyl, tert-butoxybutyl, pentyloxybutyl, isopentoxybutyl, neopentyoxybutyl, hexyloxybutyl, isohexyloxybutyl, methoxypentyl, ethoxypentyl, propoxypentyl, isopropoxypentyl, butoxypentyl, isobutoxypentyl, sec-butoxypentyl, tert-butoxypentyl, pentyloxypentyl, isopentyloxypentyl, neopentyloxypentyl, hexyloxypentyl, isohexyl, methoxyhexyl, propoxyhexyl, isopropyloxyhexyl, butyloxyhexyl, isobutyloxyhexyl, sec-butyloxyhexyl, tert-butyloxyhexyl, pentyloxyhexyl, isopentyloxyhexyl, neopentyloxyhexyl, hexyloxyhexyl and isohexyloxyhexyl.
When R is5When representing aralkyloxyalkyl, the aralkyi moiety is an alkyl group having from 1 to 4 carbon atoms and substituted with from 1 to 3 carbocyclic aryl groups, the carbocyclic aryl groups being unsubstituted or substituted with at least one substituent preferably selected from the group defined above or exemplified below by α, and the alkyl group of the oxyalkyl moiety has from 1 to 6 carbon atoms the alkyl moiety can be any of the R's described above5The aralkyl moiety of (a) may be any of those defined and exemplified for substituent βSpecific examples of such a group include benzyloxymethyl, α -naphthylmethoxymethyl, β -naphthylmethoxymethyl, phenethoxymethyl, 2-benzyloxyethyl, 2- β -naphthylmethoxyethyl, 2- β -naphthylmethoxyethyl, 2-phenylethoxyethyl, 3-benzyloxypropyl, 3- β -naphthylmethoxypropyl, 3- β -naphthylmethoxypropyl, 3-phenylethoxypropyl, 4-benzyloxybutyl, 4- α -naphthylmethoxybutyl, 4- β -naphthylmethoxybutyl, 4-phenylethoxybutyl, 5-benzyloxypentyl, 5- α -naphthylmethoxypentyl, 5- β -naphthylmethoxypentyl, 5-phenylethoxypentyl, 6-benzyloxyhexyl, 6- α -naphthylmethoxyhexyl, 6- β -naphthylmethoxyhexyl and 6-phenylethoxyhexyl.
When R isaAnd RbWhen the substituent α or the substituent gamma represents an aliphatic carboxylic acid group, it may be R as described above5Any of the aliphatic acyl groups, haloalkanoyl groups, alkoxyalkanoyl groups, alkenoyl groups, acyl groups, alkoxycarbonyl groups substituted with a halogen atom, and alkenylcarbonyl groups, particularly formyl group, acetyl group, propionyl group, butyryl group, isobutyryl group, Valeryl group (Pentanoyl group), pivaloyl group, Valeryl group (Valeryl group) and isovaleryl group, preferably acetyl group and propionyl group, defined and exemplified in (a).
When R isaAnd RbWhen the substituent α or the substituent γ represents an alkylsulfonyl group or a haloalkylsulfonyl group, it may be any of the above-mentioned R5And those defined and exemplified for substituent β.
When R isaAnd RbWhen a cycloalkyl group is represented, it may have 3 to 8 ring carbon atoms, and examples thereof include ringsPropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl, with cyclopentyl and cyclohexyl being preferred.
When R isaAnd RbWhen it represents a nitrogen-containing heterocyclic group together with the nitrogen atom to which they are attached, it may have 5 to 7 ring atoms of which 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, at least one of which is nitrogen. The heterocyclic group is preferably a saturated (non-aromatic) group. Examples include pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinyl, morpholinyl and thioxolinyl.
When R is4And R5When taken together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms or a heterocyclyl group, which group is unsubstituted or substituted with at least one substituent selected from the group consisting of substituents β as defined above4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, the aryl and aromatic heterocyclyl groups being unsubstituted or substituted by at least one substituent preferably defined as substituent α aboveaAnd RbAnd R1And R6Etc. and the above RaAnd RbThe cycloalkyl groups exemplified in (1).
From R4And R5One particularly preferred group represented together is a group of the formula:wherein Ar, J andas defined above.
When the substituent α or the substituent γ represents a halogen atom, it may be fluorine, chlorine, bromine or iodine, preferably a fluorine or chlorine atom.
When the substituent α represents a haloalkyl group, the alkyl moiety may be a straight-chain or branched-chain alkyl group having 1 to 6, preferably 1 to 3 carbon atoms, the number of halogen atoms is not limited except for the limitation of the number of substitution positions, and 1 to 3 halogen atoms are generally preferred examples of the group include trifluoromethyl, trichloromethyl, difluoromethyl, dichloromethyl, dibromomethyl, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, 2, 2, 2-trichloroethyl, 2, 2, 2-trifluoroethyl, 2-bromoethyl, 2-chloroethyl, 2-fluoroethyl, 2-iodoethyl, 2, 2-dibromoethyl, 3-bromopropyl, 3-chloropropyl, 3-fluoropropyl, 3-iodopropyl, 4-bromobutyl, 4-chlorobutyl, 4-fluorobutyl, 4-iodobutyl, 5-bromopentyl, 5-chloropentyl, 5-fluoropentyl, 5-iodopentyl, 6-bromohexyl, 6-chlorohexyl, 6-fluorohexyl and 6-iodohexyl, wherein trifluoromethyl, 2-bromoethyl and 2-chloroethyl are preferred.
When the substituent α or the substituent γ represents an alkoxycarbonyl group having 1 to 6 carbon atoms in the alkoxy moiety, it may be R as described above5Any such groups as defined and exemplified in (a).
When the substituent α or the substituent γ represents an amido group, the acyl moiety may be R as described above5Etc. of any such groups exemplified therein. Particularly preferred examples of such groups include aliphatic carboxamido groups such as carboxamido, acetylamino, propionylamino, butyrylamino, isobutyrylamino, pentanoylamino (pentanoylamino), pivaloylamino, pentanoylamino (valrylamino) and isovalerylamino, preferably acetylamino and propionylamino.
When substituent β represents an alkylsulfonyl group having 1 to 6 carbon atoms, it may be a straight-chain or branched-chain group having 1 to 6, preferably 1 to 4 carbon atoms, and examples include a methylsulfonyl group, an ethylsulfonyl group, a propylsulfonyl group, an isopropylsulfonyl group, a butylsulfonyl group, an isobutylsulfonyl group, a sec-butylsulfonyl group, a tert-butylsulfonyl group, a pentylsulfonyl group, an isopentylsulfonyl group, a neopentylsulfonyl group, a 2-methylbutylsulfonyl group, a 1-ethylpropylsulfonyl group, a 4-methylpentylsulfonyl group, a 3-methylpentylsulfonyl group, a 2-methylpentylsulfonyl group, a 1-methylpentylsulfonyl group, a3, 3-dimethylbutylsulfonyl group, a2, 2-dimethylbutylsulfonyl group, a 1, 1-dimethylbutylsulfonyl group, a 1, 2-dimethylbutylsulfonyl group, a 1, 3-dimethylbutylsulfonyl group, a 2-ethylbutylsulfonyl group, a hexylsulfonyl group and an isohexylsulfonyl group.
When R isaAnd RbOr the substituent β represents an aralkyl group in which the alkyl group has 1 to 4 carbon atoms and is substituted by 1 to 3 carbocyclic aromatic groups as defined above, and examples thereof include benzyl group, α -naphthylmethyl group, α 0-naphthylmethyl group, indenylmethyl group, phenanthryl group, anthracenylmethyl group, benzhydryl group, trityl group, 1-phenylethyl group, 2-phenylethyl group, 1- α -naphthylethyl group, 2- α -naphthylethyl group, 1- β -naphthylethyl group, 2- β -naphthylethyl group,1-phenylpropyl group, 2-phenylpropyl group, 3-phenylpropyl group, 1- α -naphthylpropyl group, 2- α -naphthylpropyl group, 3- α -naphthylpropyl group, 1- β -naphthylpropyl group2- β -naphthylpropyl, 3- β -naphthylpropyl, 1-phenylbutyl, 2-phenylbutyl, 3-phenylbutyl, 4-phenylbutyl, 1- β 0-naphthylbutyl, 2- β 1-naphthylbutyl, 3- α -naphthylbutyl, 4- α -naphthylbutyl, 1- β -naphthylbutyl, 2- β -naphthylbutyl, 3- β -naphthylbutyl, 4- β -naphthylbutyl, 1-phenylpentyl, 2-phenylpentyl, 3-phenylpentyl, 4-phenylpentyl, 5-phenylpentyl, 1- α -naphthylpentyl, 2- α -naphthylpentyl, 3-α -naphthylpentyl group, 4- α -naphthylpentyl group, 5- α 0-naphthylpentyl group, 1- α 4-naphthylpentyl group, 2- α 5-naphthylpentyl group, 3- α 7-naphthylpentyl group, 4- α 8-naphthylpentyl group, 5- α 9-naphthylpentyl group, 1-phenylhexyl group, 2-phenylhexyl group, 3-phenylhexyl group, 4-phenylhexyl group, 5-phenylhexyl group, 6-phenylhexyl group, 1- α 1-naphthylhexyl group, 2- α 2-naphthylhexyl group, 3- α 3-naphthylhexyl group, 4- α -naphthylhexyl group, 5- α -naphthylhexyl group, 6- α -naphthylhexyl group, 1- β -naphthylhexyl group, 2- β -naphthylhexyl group, 3- α 6-naphthylhexyl group, 4- β -naphthylhexyl group, 5- β -naphthylhexyl group and 6- β -naphthylhexyl group, wherein we prefer an aralkyl group in which the base is benzene and the alkyl group has 1 to 4 carbon atoms, more preferably benzyl group or benzene ethyl group.
When R is14'When an amino protecting group is represented, it is represented by the above-mentioned R5Any of the aliphatic ester groups, aromatic acyl groups and alkoxycarbonyl groups defined and exemplified in the above, or alkenyloxycarbonyl groups, aralkyloxycarbonyl groups and silyl groups defined and exemplified in the following ester groups. Among them, t-butoxycarbonyl is preferred.
Each compound of the present invention contains a base in its molecule, and thuscan form an acid addition salt. Examples of acid addition salts include: salts with inorganic acids, in particular hydrohalic acids (such as hydrofluoric, hydrobromic, hydroiodidic or hydrochloric acid), nitric acid, perchloric acid, carbonic acid, sulfuric acid or phosphoric acid; salts with lower alkylsulfonic acids, such as methanesulfonic acid, trifluoromethanesulfonic acid and ethanesulfonic acid, salts with arylsulfonic acid, benzenesulfonic acid or p-toluenesulfonic acid; salts with organic carboxylic acids, such as acetic acid, fumaric acid, tartaric acid, oxalic acid, maleic acid, malic acid, succinic acid, benzoic acid, mandelic acid, ascorbic acid, lactic acid, gluconic acid or citric acid; and salts with amino acids such as glycine, arginine, ornithine, lysine, glutamic acid or aspartic acid.
Since the compounds of the formula (I) according to the invention can be prepared by reacting R with7Radical modified piperazineThe nitrogen atom of the pyridino or piperazinyl group is converted to a quaternary ammonium and the invention therefore also includes salts of compounds of formula (I) having a cation or anion which may be any atomic group capable of forming an anion, for example a halogen atom such as chloride, and iodide.
The compounds of formula (I) according to the invention may sometimes be converted into hydrates by already absorbed water or by adhering absorbed water when placed in the atmosphere, and the invention also includes such hydrates.
As part of the present invention, the compounds of formula (I) of the present invention may form esters. When the compound is used for therapeutic purposes, its ester may be a pharmaceutically acceptable ester, and obviously, it should not be more toxic (or have unacceptably higher toxicity) than the parent compound, and it should not be less active (or have unacceptably lower activity) than the parent compound. The esters may be either "normal"or "biodissociable" esters, both of which may be used as protecting groups.
"typical" esters are esters that can be cleaved by chemical means such as hydrogenolysis, hydrolysis, electrolysis, photolysis, and the like. Examples of groups that can form esters with hydroxyl groups include:
the above-mentioned aliphatic acyl group;the above aromatic acyl group; tetrahydropyranyl or tetrahydrothiopyranyl groups such as tetrahydropyran-2-yl, 3-bromotetrahydropyran-2-yl, 4-methoxytetrahydropyran-4-yl, tetrahydrothiopyran-2-yl and 4-methoxytetrahydrothiopyran-4-yl; tetrahydrofuranyl or tetrahydrothienyl, such as tetrahydrofuran-2-yl or tetrahydrothiophen-2-yl; silyl groups, trialkylsilyl groups having 1 to 6 carbon atoms in each alkyl group (e.g. trimethylsilyl, triethylsilyl, isopropyldimethylsilyl, tert-butyldimethylsilyl, methyldiisopropylsilyl, methyl di-tert-butylsilyl and triisopropylsilyl), in which one or two alkyl groups are substituted by the above-mentioned R1The aryl-substituted trialkylsilyl groups defined and exemplified above having 1 to 6 carbon atoms in each alkyl group (e.g., diphenylmethylsilyl, diphenylbutylsilyl, diphenylisopropylsilyl and phenylisopropylsilyl); optionally substituted alkanes having 1 to 6 carbon atoms in the alkoxy moietyOxymethyl groups, such as alkoxymethyl (e.g., methoxymethyl, 1, 1-dimethyl-1-methoxymethyl, ethoxymethyl, propoxymethyl, isopropoxymethyl, butoxymethyl and tert-butoxymethyl, alkoxyalkoxymethyl groups having 1 to 6 carbon atoms in each alkoxy moiety (e.g., 2-methoxyethoxymethyl), haloalkoxymethyl groups having 1 to 6 carbon atoms in the alkoxy moiety [ e.g., 2, 2, 2-trichloroethoxymethyl and bis (2-chloroethoxy) methyl]Substituted ethyl groups such as alkoxyethyl groups having 1 to 6 carbon atoms in the alkoxy moiety (e.g. 1-ethoxyethyl and 1-isopropoxyethyl), haloethyl groups (e.g. 2, 2, 2-trichloroethyl), aralkyl groups as defined above for substituent β, preferably alkyl groups substituted with 1 to 3 aryl groups (e.g. benzyl, α -naphthylmethyl, β -naphthylmethyl, benzhydryl, trityl, α -naphthyldiphenylmethyl and 9-naphthylmethyl), lower alkyl groups substituted with 1 to 3 aryl groups, wherein the aryl groups are substituted with lower alkyl groups, lower alkoxy groups, nitro, halogen or cyano groups, (e.g. 4-methylbenzyl, 2, 4, 6-trimethylbenzyl, 3, 4, 5-trimethylbenzyl, 4-methoxybenzyl, 4-methoxyphenyldiphenylmethyl, 2-nitrobenzyl, 4-chlorobenzyl, 4-bromobenzyl and 4-cyanobenzyl), alkoxycarbonyl groups such as vinyloxycarbonyl and allyloxycarbonyl groups, aralkyloxycarbonyl groups which may be substituted with 1 or 2 lower alkoxy groups or nitro groups such as benzyloxycarbonyl, 4-nitrobenzyl and 4-cyanobenzyl and 2-nitrobenzyl groups.
The biologically cleavable esters contain groups which can be cleaved by biological means, such as biodegradation, to form the free acid or salt thereof. Whether an ester is biodegraded can be determined by injecting the ester intravenously into a test animal (e.g., a rat or mouse), examining the body fluids of the animal after administration and testing the original, compound or pharmaceutically acceptable salt thereof.
Examples of biodissociable esters include:
1- (acyloxy) lower alkyl, e.g. 1- (aliphatic acyloxy) lower alkyl (e.g. formyloxy)
Methyl, acetoxymethyl, dimethylaminoacetoxymethyl, propionyloxymethyl, butyryloxymethyl, nov
Valeryloxymethyl, isovaleryloxymethyl, hexanoyloxymethyl, 1-formyloxyethyl,
1-acetoxyethyl group, 1-propionyloxyethyl group, 1-butyryloxyethyl group, 1-pivaloyloxyethyl group,
1-valeryloxyethyl group, 1-isovaleryloxyethyl group, 1-hexanoyloxyethyl group, 1-formyloxypropyl group,
1-acetoxypropyl group, 1-propionyloxypropyl group, 1-butyryloxypropyl group, 1-pivaloyloxypropyl group,
1-valeryloxypropyl group, 1-isovaleryloxypropyl group, 1-hexanoyloxypropyl group, 1-acetoxybutyl group,
1-propionyloxybutyl, 1-butyryloxybutyl, 1-pivaloyloxybutyl, 1-acetoxypentyl,
1-propionyloxypentyl, 1-butyryloxypentyl, 1-pivaloyloxypentyl and 1-pivaloyloxyhexyl
Radical);
1- (Cycloalkylcarbonyloxy) lower alkyl (e.g. cyclopentylcarbonyloxymethyl, cyclohexylcarbonyloxymethyl)
1-cyclopentylcarbonyloxyethyl group, 1-cyclohexylcarbonyloxyethyl group, 1-cyclopentylcarbonyloxypropyl group,
1-cyclohexylcarbonyloxypropyl, 1-cyclopentylcarbonyloxybutyl and 1-cyclohexylcarbonyloxybutyl);
1- (aroyloxy) lower alkyl (e.g., benzoyloxymethyl);
carbonyloxyalkyl radicals, e.g. (alkoxycarbonyloxy) alkyl and (cycloalkyloxycarbonyloxy) alkyl (e.g. methoxy)
Carbonyloxymethyl, ethoxycarbonyloxymethyl, propoxycarbonyloxymethyl, isopropoxycarbonyloxymethyl, butanes
Oxycarbonyloxymethyl, isobutoxycarbonyloxymethyl, pentyloxycarbonyloxymethyl, hexyloxycarbonyloxymethyl,
cyclohexyloxycarbonyloxymethyl, cyclohexyloxycarbonyloxy (cyclohexyl) methyl, 1- (methoxycarbonyl)
Oxy) ethyl, 1- (ethoxycarbonyloxy) ethyl, 1- (propoxycarbonyloxy) ethyl, 1
- (isopropyloxycarbonyloxy) ethyl, 1- (butyloxycarbonyloxy) ethyl, 1- (isobutyloxycarbonyloxy)
Ethyl, 1- (tert-butoxycarbonyloxy) ethyl, 1- (pentyloxycarbonyloxy) ethyl, 1- (hexyloxy)
Oxycarbonyloxy) ethyl group, 1- (cyclopentoxycarbonyloxy) propyl group,
1- (cyclohexyloxycarbonyloxy) propyl, 1- (cyclopentyloxycarbonyloxy) butyl, 1- (cyclohexyloxy)
Carbonyl oxygen) butyl, 1- (cyclohexyloxycarbonyloxy) ethyl, 1- (ethoxycarbonyloxy) propyl,
2- (methoxycarbonyloxy) ethyl, 2- (ethoxycarbonyloxy) ethyl, 2- (propoxycarbonyloxy)
Ethyl, 2- (isopropyloxycarbonyloxy) ethyl, 2- (butyloxycarbonyloxy) ethyl, 2- (iso
Butoxycarbonyloxy) ethyl, 2- (pentyloxycarbonyloxy) ethyl 2- (hexyloxycarbonyloxy) -ethyl,
1- (methoxycarbonyloxy) propyl, 1- (ethoxycarbonyloxy) propyl, 1- (propoxycarbonyl)
Oxy) propyl, 1- (isopropyloxycarbonyloxy) propyl, 1- (butyloxycarbonyloxy) propyl, 1-
(isobutoxycarbonyloxy) propyl, 1- (pentyloxycarbonyloxy) propyl, 1- (hexyloxycarbonyloxy)
Propyl, 1- (methoxycarbonyloxy) butyl, 1- (ethoxycarbonyloxy) butyl, 1- (propoxyl)
Carbonyloxy) butyl, 1- (isopropyloxycarbonyloxy) butyl, 1- (butyloxycarbonyloxy) butyl,
1- (isobutoxycarbonyloxy) butyl, 1- (methoxycarbonyloxy) pentyl, 1- (ethoxycarbonyl)
Oxygen) pentyl, 1- (methoxycarbonyloxy) hexyl and 1- (ethoxycarbonyloxy) hexyl);
oxodioxolyl methyl (e.g., (5-phenyl-2-oxo-1, 3-dioxan)
Cyclopenten-4-yl) methyl, [5- (4-tolyl) -2-oxo-1, 3-di
Oxopenen-4-yl]methyl, [5- (4-methoxyphenyl) -2-oxo-1, 3
-dioxol-4-yl]methyl, [5- (4-fluorophenyl) -2-oxo-1,
3-dioxolen-4-yl]methyl, [5- (4-chlorophenyl) -2-oxo-1
3-dioxolen-4-yl methyl group, (2-oxo-1, 3-dioxolen-
4-yl) methyl, 5-methyl-2-oxo-1, 3-dioxolen-4-yl) methyl
Radical, (5-ethyl-2-oxo-1, 3-dioxol-4-yl) methyl, (5)
-propyl-2-oxo-1, 3-dioxolen-4-yl) methyl group, (5-propyl-
2-oxo-1, 3-dioxolen-4-yl) methyl, (5-isopropyl-2-oxy
1, 3-dioxolen-4-yl) methyl and (5-butyl-2-oxo-1,
3-dioxolen-4-yl) methyl);
2-benzo [ c]furanones, e.g. 2-benzo [ c]furanone, dimethyl 2-benzo [ c]
Furyl and dimethoxy 2-benzo [ c]furanonyl;
the above-mentioned aliphatic acyl group;
the above aromatic acyl group;
a succinic acid half-ester salt residue;
a phosphate residue;
ester-forming residues derived from e.g. amino acids;
1- (acyloxy) alkoxycarbonyl, such as pivaloyloxymethoxycarbonyl.
Among them, we prefer a carbonyloxyalkyl group.
The compound of formula (I) has asymmetric atoms in the molecule, and stereoisomers with asymmetric carbon atoms having R or S configuration exist. Stereoisomers whose asymmetric carbon atoms have the R or S configuration and mixtures thereof in any proportion are also included in the scope of the present invention.
Preferred compounds of the invention are compounds of the formula (I) wherein E represents methylene, and salts and esters thereof
(A1)R1And R2The same or different, each represents an aryl group, an aromatic heterocyclic group or an aryl group substituted with 1 to 3 groups selected from the substituent α;
(B1)R2represents aryl or aryl substituted by 1 to 3 groups selected from substituent α;
(C1) a represents a carbonyl group;
(D1) b represents a single bond;
(E1) d is an oxygen atom;
(F1) g is an alkylene group having 1 to 4 carbon atoms;
(G1) g is an alkylene group having 2 or 3 carbon atoms;
(H1)R3represents an aromatic heterocyclic group or an aryl group substituted with 1 to 3 groups selected from the group consisting of substituents α;
(I1) l representsA group;
(J1)R4represents an aryl group or an aromatic heterocyclic group;
(K1)R5expression formula (I)Group (wherein R6Represents an alkyl group having 1 to 6 carbon atoms or an amine residue);
(L1)R5represents amino, amido or hydroxyl;
(M1)R4and R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent selected from the group consisting of substituent β, or a heterocyclyl group having a single nitrogen and/or oxygen and/or sulfur heteroatom, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl and aromatic heterocyclyl group is unsubstituted or substituted by at least one substituent selected from the group consisting of substituents α.
Further preferred compounds of the invention are compounds of the formula (I) wherein E represents a formula wherein n is an integer from 2 to 4, and salts and esters thereofA group, and (A2) R1And R2The same or different, each represents an aryl group, an aromatic heterocyclic group or an aryl group substituted with 1 to 3 groups selected from the group consisting of the substituent α, (B2) R2Represents aryl or is represented byAryl substituted with 1 to 3 substituents selected from the group consisting of substituent α, (C2) A represents carbonyl;(D2) b represents a single bond; (E2) d represents an oxygen atom; (F2) g represents an alkylene group having 1 to 4 carbon atoms; (G2) g represents an alkylene group having 2 to 3 carbon atoms; (H2) r3Represents an aromatic heterocycle or an aryl group substituted with 1 to 3 substituents selected from the group consisting of the substituent α (I2) L represents a general formulaA group; (J2) r4Represents an aryl group or an aromatic heterocyclic group; (K2) r5Is represented by the general formulaRadical (in which R is6Represents an alkyl group having 1 to 6 carbon atoms or an amine residue); (L2) R5Represents amino, amido or hydroxyl; (M2) n is 2 or 3; (N2) N is 2; (O2) R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent selected from the group consisting of substituent β, or a heterocyclyl group having a single nitrogen and/or oxygen and/or sulfur heteroatom, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl and aromatic heterocyclyl group is unsubstituted or substituted by at least one substituent selected from the group consisting of substituents α.
Further preferred compounds of the invention are compounds of the formula (I) wherein R is4And R5Together represent a group of the formulaAnd (A3) R1Represents an aryl group, an aromatic heterocyclic group, or an aryl group substituted with 1 to 3 groups selected from the group consisting of the substituent α (B3)1Represents aryl or from 1 to 3 substituents α1Aryl substituted by the group of (1), substituent α1Selected from the group consisting of alkyl groups having 1 to 6 carbon atoms, haloalkyl groups having 1 to 6 carbon atoms, and alkoxy groups having 1 to 6 carbon atoms; (C3) r2Represents an aryl group or an aryl group substituted with 1 to 3 groups selected from the group consisting of the substituent α, (D3) R2Represents an aryl group or an aryl group substituted by 1 to 3 halogen atoms;(E3) a represents a carbonyl group; (F3) B represents a single bond; (G3) D represents an oxygen atom; (H3) e represents C1-4Alkylene or including C3-6C of cycloalkane-1, 1-diyl group3-8An alkylene group; (I3) e represents methylene, ethylene, dimethylmethylene, 1, 1-dimethylethylene, 2, 2-dimethylethylene, cyclopropane-1, 1-diyl, cyclobutane-1, 1-diyl, cyclopentane-1, 1-diyl, cyclohexane-1, 1-diyl, cyclopropane-1, 1-diyl methyl, cyclobutane-1, 1-diyl methyl, cyclopentane-1, 1-diyl methyl or cyclohexane-1, 1-diyl methyl; (J3) g represents C1-4An alkylene group; (K3) g represents C2-3An alkylene group; (L3) J represents C1-4Alkylene, (M3) J represents methylene or ethylene, (N3) Ring Ar represents aryl, aryl substituted with 1to 3 substituents selected from the group consisting of a substituent α or aromatic heterocyclic group, (O3) Ring Ar represents aryl or aryl substituted with 1 to 3 substituents selected from the group consisting of a substituent α.
Examples of certain compounds of the present invention shown by the following formulas (I-1), (I-2) and (I-3) can be prepared as shown in the examples described below. The definitions of the substituents of these compounds correspond to tables 1, 2 and 3, that is, Table 1 relates to formula (I-1) and the like.
Each compound number in these tables includes 2 compounds, with G in one representing 1, 2-ethylene (which may be represented by the number and suffix "a" as specified in the tables) and G in the other representing 1, 3-propylene (which may be represented by the number and suffix "b" as specified in the tables).
Further, the compound Nos. 2-1537 to 2-3072 include those in which B may represent a single bond orCompounds of the groups which may be indicated by the suffix, α or β respectively, for example, Compound No.2-1537a α is Compound No.2-1537 in which G represents 1, 2-ethylene and B represents a single bond, Compound 2-537 αβ is Compound in which G represents 1, 2-ethylene and B represents a single bondCompound No.2-1537 of the groups, Compound No.2-1537B α is Compound No.2-1537 in which G represents 1, 3-propylene and B represents a single bond, Compound No.2-1537B β is Compound No.2-1537 in which G represents 1, 3-propylene and B represents a single bondCompound No.2-1537 of the group.
Names representing certain substituents are abbreviated as follows:
cBu cyclobutyl-1,1-diyl
cHx cyclohexyl-1, 1-diyl
Me methyl group
Ph phenyl
cPn cyclopentyl-1, 1-diyl
cPr cyclopropyl-1, 1-diyl
Single bond Single bond
Furthermore, the radical formula corresponding to the substituent symbol Sub-xx is as indicated on page 624 of the text
Page 631 shows:
TABLE 1
Compound (I) Serial number R1 R2 A B Z
1-1 Sub-33 3,4-diClPh CH2 Single bond Sub-1
1-2 Sub-33 3,4-diClPh CH2 Single bond Sub-2
1-3 Sub-33 3,4-diClPh CH2 Single bond Sub-3
1-4 Sub-33 3,4-diClPh CH2 Single bond Sub-4
1-5 Sub-33 3,4-diClPh CH2 Single bond Sub-5
1-6 Sub-33 3,4-diClPh CH2 Single bond Sub-6
1-7 Sub-33 3,4-diClPh CH2 Single bond Sub-7
1-8 Sub-33 3,4-diClPh CH2 Single bond Sub-8
1-9 Sub-33 3,4-diClPh CH2 Single bond Sub-9
1-10 Sub-33 3,4-diClPh CH2 Single bond Sub-10
1-11 Sub-33 3,4-diClPh CH2 Single bond Sub-11
1-12 Sub-33 3,4-diClPh CH2 Single bond Sub-12
1-13 Sub-33 3,4-diClPh CH2 Single bond Sub-13
1-14 Sub-33 3,4-diClPh CH2 Single bond Sub-14
1-15 Sub-33 3,4-diClPh CH2 Single bond Sub-15
1-16 Sub-33 3,4-diClPh CH2 Single bond Sub-16
1-17 Sub-33 3,4-diClPh CH2 Single bond Sub-17
1-18 Sub-33 3,4-diClPh CH2 Single bond Sub-18
1-19 Sub-33 3,4-diClPh CH2 Single bond Sub-19
1-20 Sub-33 3,4-diClPh CH2 Single bond Sub-20
1-21 Sub-33 3,4-diClPh CH2 Single bond Sub-21
1-22 Sub-33 3,4-diClPh CH2 Single bond Sub-22
1-23 Sub-33 3,4-diClPh CH2 Single bond Sub-23
1-24 Sub-33 3,4-diClPh CH2 Single bond Sub-24
1-25 Sub-33 3,4-diClPh CH2 Single bond Sub-25
1-26 Sub-33 3,4-diClPh CH2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-27 Sub-33 3,4-diClPh CH2 Single bond Sub-27
1-28 Sub-33 3,4-diClPh CH2 Single bond Sub-28
1-29 Sub-33 3,4-diClPh CH2 Single bond Sub-29
1-30 Sub-33 3,4-diClPh CH2 Single bond Sub-30
1-31 Sub-33 3,4-diClPh CH2 Single bond Sub-31
1-32 Sub-33 3,4-diClPh CH2 Single bond Sub-32
1-33 Sub-34 3,4-diClPh CH2 Single bond Sub-1
1-34 Sub-34 3,4-diClPh CH2 Single bond Sub-2
1-35 Sub-34 3,4-diClPh CH2 Single bond Sub-3
1-36 Sub-34 3,4-diClPh CH2 Single bond Sub-4
1-37 Sub-34 3,4-diClPh CH2 Single bond Sub-5
1-38 Sub-34 3,4-diClPh CH2 Single bond Sub-6
1-39 Sub-34 3,4-diClPh CH2 Single bond Sub-7
1-40 Sub-34 3,4-diClPh CH2 Single bond Sub-8
1-41 Sub-34 3,4-diClPh CH2 Single bond Sub-9
1-42 Sub-34 3,4-diClPh CH2 Single bond Sub-10
1-43 Sub-34 3,4-diClPh CH2 Single bond Sub-11
1-44 Sub-34 3,4-diClPh CH2 Single bond Sub-12
1-45 Sub-34 3,4-diClPh CH2 Single bond Sub-13
1-46 Sub-34 3,4-diClPh CH2 Single bond Sub-14
1-47 Sub-34 3,4-diClPh CH2 Single bond Sub-15
1-48 Sub-34 3,4-diClPh CH2 Single bond Sub-16
1-49 Sub-34 3,4-diClPh CH2 Single bond Sub-17
1-50 Sub-34 3,4-diClPh CH2 Single bond Sub-18
1-51 Sub-34 3,4-diClPh CH2 Single bond Sub-19
1-52 Sub-34 3,4-diClPh CH2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-53 Sub-34 3,4-diClPh CH2 Single bond Sub-21
1-54 Sub-34 3,4-diClPh CH2 Single bond Sub-22
1-55 Sub-34 3,4-diClPh CH2 Single bond Sub-23
1-56 Sub-34 3,4-diClPh CH2 Single bond Sub-24
1-57 Sub-34 3,4-diClPh CH2 Single bond Sub-25
1-58 Sub-34 3,4-diClPh CH2 Single bond Sub-26
1-59 Sub-34 3,4-diClPh CH2 Single bond Sub-27
1-60 Sub-34 3,4-diClPh CH2 Single bond Sub-28
1-61 Sub-34 3,4-diClPh CH2 Single bond Sub-29
1-62 Sub-34 3,4-diClPh CH2 Single bond Sub-30
1-63 Sub-34 3,4-diClPh CH2 Single bond Sub-31
1-64 Sub-34 3,4-diClPh CH2 Single bond Sub-32
1-65 Sub-35 3,4-diClPh CH2 Single bond Sub-1
1-66 Sub-35 3,4-diClPh CH2 Single bond Sub-2
1-67 Sub-35 3,4-diClPh CH2 Single bond Sub-3
1-68 Sub-35 3,4-diClPh CH2 Single bond Sub-4
1-69 Sub-35 3,4-diClPh CH2 Single bond Sub-5
1-70 Sub-35 3,4-diClPh CH2 Single bond Sub-6
1-71 Sub-35 3,4-diClPh CH2 Single bond Sub-7
1-72 Sub-35 3,4-diClPh CH2 Single bond Sub-8
1-73 Sub-35 3,4-diClPh CH2 Single bond Sub-9
1-74 Sub-35 3,4-diClPh CH2 Single bond Sub-10
1-75 Sub-35 3,4-diClPh CH2 Single bond Sub-11
1-76 Sub-35 3,4-diClPh CH2 Single bond Sub-12
1-77 Sub-35 3,4-diClPh CH2 Single bond Sub-13
1-78 Sub-35 3,4-diClPh CH2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-79 Sub-35 3,4-diClPh CH2 Single bond Sub-15
1-80 Sub-35 3,4-diClPh CH2 Single bond Sub-16
1-81 Sub-35 3,4-diClPh CH2 Single bond Sub-17
1-82 Sub-35 3,4-diClPh CH2 Single bond Sub-18
1-83 Sub-35 3,4-diClPh CH2 Single bond Sub-19
1-84 Sub-35 3,4-diClPh CH2 Single bond Sub-20
1-85 Sub-35 3,4-diClPh CH2 Single bond Sub-21
1-86 Sub-35 3,4-diClPh CH2 Single bond Sub-22
1-87 Sub-35 3,4-diClPh CH2 Single bond Sub-23
1-88 Sub-35 3,4-diClPh CH2 Single bond Sub-24
1-89 Sub-35 3,4-diClPh CH2 Single bond Sub-25
1-90 Sub-35 3,4-diClPh CH2 Single bond Sub-26
1-91 Sub-35 3,4-diClPh CH2 Single bond Sub-27
1-92 Sub-35 3,4-diClPh CH2 Single bond Sub-28
1-93 Sub-35 3,4-diClPh CH2 Single bond Sub-29
1-94 Sub-35 3,4-diClPh CH2 Single bond Sub-30
1-95 Sub-35 3,4-diClPh CH2 Single bond Sub-31
1-96 Sub-35 3,4-diClPh CH2 Single bond Sub-32
1-97 Sub-36 3,4-diClPh CH2 Single bond Sub-1
1-98 Sub-36 3,4-diClPh CH2 Single bond Sub-2
1-99 Sub-36 3,4-diClPh CH2 Single bond Sub-3
1-100 Sub-36 3,4-diClPh CH2 Single bond Sub-4
1-101 Sub-36 3,4-diClPh CH2 Single bond Sub-5
1-102 Sub-36 3,4-diClPh CH2 Single bond Sub-6
1-103 Sub-36 3,4-diClPh CH2 Single bond Sub-7
1-104 Sub-36 3,4-diClPh CH2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-105 Sub-36 3,4-diClPh CH2 Single bond Sub-9
1-106 Sub-36 3,4-diClPh CH2 Single bond Sub-10
1-107 Sub-36 3,4-diClPh CH2 Single bond Sub-11
1-108 Sub-36 3,4-diClPh CH2 Single bond Sub-12
1-109 Sub-36 3,4-diClPh CH2 Single bond Sub-13
1-110 Sub-36 3,4-diClPh CH2 Single bond Sub-14
1-111 Sub-36 3,4-diClPh CH2 Single bond Sub-15
1-112 Sub-36 3,4-diClPh CH2 Single bond Sub-16
1-113 Sub-36 3,4-diClPh CH2 Single bond Sub-17
1-114 Sub-36 3,4-diClPh CH2 Single bond Sub-18
1-115 Sub-36 3,4-diClPh CH2 Single bond Sub-19
1-116 Sub-36 3,4-diClPh CH2 Single bond Sub-20
1-117 Sub-36 3,4-diClPh CH2 Single bond Sub-21
1-118 Sub-36 3,4-diClPh CH2 Single bond Sub-22
1-119 Sub-36 3,4-diClPh CH2 Single bond Sub-23
1-120 Sub-36 3,4-diClPh CH2 Single bond Sub-24
1-121 Sub-36 3,4-diClPh CH2 Single bond Sub-25
1-122 Sub-36 3,4-diClPh CH2 Single bond Sub-26
1-123 Sub-36 3,4-diClPh CH2 Single bond Sub-27
1-124 Sub-36 3,4-diClPh CH2 Single bond Sub-28
1-125 Sub-36 3,4-diClPh CH2 Single bond Sub-29
1-126 Sub-36 3,4-diClPh CH2 Single bond Sub-30
1-127 Sub-36 3,4-diClPh CH2 Single bond Sub-31
1-128 Sub-36 3,4-diClPh CH2 Single bond Sub-32
1-129 Sub-37 3,4-diClPh CH2 Single bond Sub-1
1-130 Sub-37 3,4-diClPh CH2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-131 Sub-37 3,4-diClPh CH2 Single bond Sub-3
1-132 Sub-37 3,4-diClPh CH2 Single bond Sub-4
1-133 Sub-37 3,4-diClPh CH2 Single bond Sub-5
1-134 Sub-37 3,4-diClPh CH2 Single bond Sub-6
1-135 Sub-37 3,4-diClPh CH2 Single bond Sub-7
1-136 Sub-37 3,4-diClPh CH2 Single bond Sub-8
1-137 Sub-37 3,4-diClPh CH2 Single bond Sub-9
1-138 Sub-37 3,4-diClPh CH2 Single bond Sub-10
1-139 Sub-37 3,4-diClPh CH2 Single bond Sub-11
1-140 Sub-37 3,4-diClPh CH2 Single bond Sub-12
1-141 Sub-37 3,4-diClPh CH2 Single bond Sub-13
1-142 Sub-37 3,4-diClPh CH2 Single bond Sub-14
1-143 Sub-37 3,4-diClPh CH2 Single bond Sub-15
1-144 Sub-37 3,4-diClPh CH2 Single bond Sub-16
1-145 Sub-37 3,4-diClPh CH2 Single bond Sub-17
1-146 Sub-37 3,4-diClPh CH2 Single bond Sub-18
1-147 Sub-37 3,4-diClPh CH2 Single bond Sub-19
1-148 Sub-37 3,4-diClPh CH2 Single bond Sub-20
1-149 Sub-37 3,4-diClPh CH2 Single bond Sub-21
1-150 Sub-37 3,4-diClPh CH2 Single bond Sub-22
1-151 Sub-37 3,4-diClPh CH2 Single bond Sub-23
1-152 Sub-37 3,4-diClPh CH2 Single bond Sub-24
1-153 Sub-37 3,4-diClPh CH2 Single bond Sub-25
1-154 Sub-37 3,4-diClPh CH2 Single bond Sub-26
1-155 Sub-37 3,4-diClPh CH2 Single bond Sub-27
1-156 Sub-37 3,4-diClPh CH2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-157 Sub-37 3,4-diClPh CH2 Single bond Sub-29
1-158 Sub-37 3,4-diClPh CH2 Single bond Sub-30
1-159 Sub-37 3,4-diClPh CH2 Single bond Sub-31
1-160 Sub-37 3,4-diClPh CH2 Single bond Sub-32
1-161 Sub-38 3,4-diClPh CH2 Single bond Sub-1
1-162 Sub-38 3,4-diClPh CH2 Single bond Sub-2
1-163 Sub-38 3,4-diClPh CH2 Single bond Sub-3
1-164 Sub-38 3,4-diClPh CH2 Single bond Sub-4
1-165 Sub-38 3,4-diClPh CH2 Single bond Sub-5
1-166 Sub-38 3,4-diClPh CH2 Single bond Sub-6
1-167 Sub-38 3,4-diClPh CH2 Single bond Sub-7
1-168 Sub-38 3,4-diClPh CH2 Single bond Sub-8
1-169 Sub-38 3,4-diClPh CH2 Single bond Sub-9
1-170 Sub-38 3,4-diClPh CH2 Single bond Sub-10
1-171 Sub-38 3,4-diClPh CH2 Single bond Sub-11
1-172 Sub-38 3,4-diClPh CH2 Single bond Sub-12
1-173 Sub-38 3,4-diClPh CH2 Single bond Sub-13
1-174 Sub-38 3,4-diClPh CH2 Single bond Sub-14
1-175 Sub-38 3,4-diClPh CH2 Single bond Sub-15
1-176 Sub-38 3,4-diClPh CH2 Single bond Sub-16
1-177 Sub-38 3,4-diClPh CH2 Single bond Sub-17
1-178 Sub-38 3,4-diClPh CH2 Single bond Sub-18
1-179 Sub-38 3,4-diClPh CH2 Single bond Sub-19
1-180 Sub-38 3,4-diClPh CH2 Single bond Sub-20
1-181 Sub-38 3,4-diClPh CH2 Single bond Sub-21
1-182 Sub-38 3,4-diClPh CH2 Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-183 Sub-38 3,4-diClPh CH2 Single bond Sub-23
1-184 Sub-38 3,4-diClPh CH2 Single bond Sub-24
1-185 Sub-38 3,4-diClPh CH2 Single bond Sub-25
1-186 Sub-38 3,4-diClPh CH2 Single bond Sub-26
1-187 Sub-38 3,4-diClPh CH2 Single bond Sub-27
1-188 Sub-38 3,4-diClPh CH2 Single bond Sub-28
1-189 Sub-38 3,4-diClPh CH2 Single bond Sub-29
1-190 Sub-38 3,4-diClPh CH2 Single bond Sub-30
1-191 Sub-38 3,4-diClPh CH2 Single bond Sub-31
1-192 Sub-38 3,4-diClPh CH2 Single bond Sub-32
1-193 Sub-39 3,4-diClPh CH2 Single bond Sub-1
1-194 Sub-39 3,4-diClPh CH2 Single bond Sub-2
1-195 Sub-39 3,4-diClPh CH2 Single bond Sub-3
1-196 Sub-39 3,4-diClPh CH2 Single bond Sub-4
1-197 Sub-39 3,4-diClPh CH2 Single bond Sub-5
1-198 Sub-39 3,4-diClPh CH2 Single bond Sub-6
1-199 Sub-39 3,4-diClPh CH2 Single bond Sub-7
1-200 Sub-39 3,4-diClPh CH2 Single bond Sub-8
1-201 Sub-39 3,4-diClPh CH2 Single bond Sub-9
1-202 Sub-39 3,4-diClPh CH2 Single bond Sub-10
1-203 Sub-39 3,4-diClPh CH2 Single bond Sub-11
1-204 Sub-39 3,4-diClPh CH2 Single bond Sub-12
1-205 Sub-39 3,4-diClPh CH2 Single bond Sub-13
1-206 Sub-39 3,4-diClPh CH2 Single bond Sub-14
1-207 Sub-39 3,4-diClPh CH2 Single bond Sub-15
1-208 Sub-39 3,4-diClPh CH2 Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-209 Sub-39 3,4-diClPh CH2 Single bond Sub-17
1-210 Sub-39 3,4-diClPh CH2 Single bond Sub-18
1-211 Sub-39 3,4-diClPh CH2 Single bond Sub-19
1-212 Sub-39 3,4-diClPh CH2 Single bond Sub-20
1-213 Sub-39 3,4-diClPh CH2 Single bond Sub-21
1-214 Sub-39 3,4-diClPh CH2 Single bond Sub-22
1-215 Sub-39 3,4-diClPh CH2 Single bond Sub-23
1-216 Sub-39 3,4-diClPh CH2 Single bond Sub-24
1-217 Sub-39 3,4-diClPh CH2 Single bond Sub-25
1-218 Sub-39 3,4-diClPh CH2 Single bond Sub-26
1-219 Sub-39 3,4-diClPh CH2 Single bond Sub-27
1-220 Sub-39 3,4-diClPh CH2 Single bond Sub-28
1-221 Sub-39 3,4-diClPh CH2 Single bond Sub-29
1-222 Sub-39 3,4-diClPh CH2 Single bond Sub-30
1-223 Sub-39 3,4-diClPh CH2 Single bond Sub-31
1-224 Sub-39 3,4-diClPh CH2 Single bond Sub-32
1-225 Sub-40 3,4-diClPh CH2 Single bond Sub-1
1-226 Sub-40 3,4-diClPh CH2 Single bond Sub-2
1-227 Sub-40 3,4-diClPh CH2 Single bond Sub-3
1-228 Sub-40 3,4-diClPh CH2 Single bond Sub-4
1-229 Sub-40 3,4-diClPh CH2 Single bond Sub-5
1-230 Sub-40 3,4-diClPh CH2 Single bond Sub-6
1-231 Sub-40 3,4-diClPh CH2 Single bond Sub-7
1-232 Sub-40 3,4-diClPh CH2 Single bond Sub-8
1-233 Sub-40 3,4-diClPh CH2 Single bond Sub-9
1-234 Sub-40 3,4-diClPh CH2 Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-235 Sub-40 3,4-diClPh CH2 Single bond Sub-11
1-236 Sub-40 3,4-diClPh CH2 Single bond Sub-12
1-237 Sub-40 3,4-diClPh CH2 Single bond Sub-13
1-238 Sub-40 3,4-diClPh CH2 Single bond Sub-14
1-239 Sub-40 3,4-diClPh CH2 Single bond Sub-15
1-240 Sub-40 3,4-diClPh CH2 Single bond Sub-16
1-241 Sub-40 3,4-diClPh CH2 Single bond Sub-17
1-242 Sub-40 3,4-diClPh CH2 Single bond Sub-18
1-243 Sub-40 3,4-diClPh CH2 Single bond Sub-19
1-244 Sub-40 3,4-diClPh CH2 Single bond Sub-20
1-245 Sub-40 3,4-diClPh CH2 Single bond Sub-21
1-246 Sub-40 3,4-diClPh CH2 Single bond Sub-22
1-247 Sub-40 3,4-diClPh CH2 Single bond Sub-23
1-248 Sub-40 3,4-diClPh CH2 Single bond Sub-24
1-249 Sub-40 3,4-diClPh CH2 Single bond Sub-25
1-250 Sub-40 3,4-diClPh CH2 Single bond Sub-26
1-251 Sub-40 3,4-diClPh CH2 Single bond Sub-27
1-252 Sub-40 3,4-diClPh CH2 Single bond Sub-28
1-253 Sub-40 3,4-diClPh CH2 Single bond Sub-29
1-254 Sub-40 3,4-diClPh CH2 Single bond Sub-30
1-255 Sub-40 3,4-diClPh CH2 Single bond Sub-31
1-256 Sub-40 3,4-diClPh CH2 Single bond Sub-32
1-257 Sub-41 3,4-diClPh CH2 Single bond Sub-1
1-258 Sub-41 3,4-diClPh CH2 Single bond Sub-2
1-259 Sub-41 3,4-diClPh CH2 Single bond Sub-3
1-260 Sub-41 3,4-diClPh CH2 Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-261 Sub-41 3,4-diClPh CH2 Single bond Sub-5
1-262 Sub-41 3,4-diClPh CH2 Single bond Sub-6
1-263 Sub-41 3,4-diClPh CH2 Single bond Sub-7
1-264 Sub-41 3,4-diClPh CH2 Single bond Sub-8
1-265 Sub-41 3,4-diClPh CH2 Single bond Sub-9
1-266 Sub-41 3,4-diClPh CH2 Single bond Sub-10
1-267 Sub-41 3,4-diClPh CH2 Single bond Sub-11
1-268 Sub-41 3,4-diClPh CH2 Single bond Sub-12
1-269 Sub-41 3,4-diClPh CH2 Single bond Sub-13
1-270 Sub-41 3,4-diClPh CH2 Single bond Sub-14
1-271 Sub-41 3,4-diClPh CH2 Single bond Sub-15
1-272 Sub-41 3,4-diClPh CH2 Single bond Sub-16
1-273 Sub-41 3,4-diClPh CH2 Single bond Sub-17
1-274 Sub-41 3,4-diClPh CH2 Single bond Sub-18
1-275 Sub-41 3,4-diClPh CH2 Single bond Sub-19
1-276 Sub-41 3,4-diClPh CH2 Single bond Sub-20
1-277 Sub-41 3,4-diClPh CH2 Single bond Sub-21
1-278 Sub-41 3,4-diClPh CH2 Single bond Sub-22
1-279 Sub-41 3,4-diClPh CH2 Single bond Sub-23
1-280 Sub-41 3,4-diClPh CH2 Single bond Sub-24
1-281 Sub-41 3,4-diClPh CH2 Single bond Sub-25
1-282 Sub-41 3,4-diClPh CH2 Single bond Sub-26
1-283 Sub-41 3,4-diClPh CH2 Single bond Sub-27
1-284 Sub-41 3,4-diClPh CH2 Single bond Sub-28
1-285 Sub-41 3,4-diClPh CH2 Single bond Sub-29
1-286 Sub-41 3,4-diClPh CH2 Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-287 Sub-41 3,4-diClPh CH2 Single bond Sub-31
1-288 Sub-41 3,4-diClPh CH2 Single bond Sub-32
1-289 Sub-42 3,4-diClPh CH2 Single bond Sub-1
1-290 Sub-42 3,4-diClPh CH2 Single bond Sub-2
1-291 Sub-42 3,4-diClPh CH2 Single bond Sub-3
1-292 Sub-42 3,4-diClPh CH2 Single bond Sub-4
1-293 Sub-42 3,4-diClPh CH2 Single bond Sub-5
1-294 Sub-42 3,4-diClPh CH2 Single bond Sub-6
1-295 Sub-42 3,4-diClPh CH2 Single bond Sub-7
1-296 Sub-42 3,4-diClPh CH2 Single bond Sub-8
1-297 Sub-42 3,4-diClPh CH2 Single bond Sub-9
1-298 Sub-42 3,4-diClPh CH2 Single bond Sub-10
1-299 Sub-42 3,4-diClPh CH2 Single bond Sub-11
1-300 Sub-42 3,4-diClPh CH2 Single bond Sub-12
1-301 Sub-42 3,4-diClPh CH2 Single bond Sub-13
1-302 Sub-42 3,4-diClPh CH2 Single bond Sub-14
1-303 Sub-42 3,4-diClPh CH2 Single bond Sub-15
1-304 Sub-42 3,4-diClPh CH2 Single bond Sub-16
1-305 Sub-42 3,4-diClPh CH2 Single bond Sub-17
1-306 Sub-42 3,4-diClPh CH2 Single bond Sub-18
1-307 Sub-42 3,4-diClPh CH2 Single bond Sub-19
1-308 Sub-42 3,4-diClPh CH2 Single bond Sub-20
1-309 Sub-42 3,4-diClPh CH2 Single bond Sub-21
1-310 Sub-42 3,4-diClPh CH2 Single bond Sub-22
1-311 Sub-42 3,4-diClPh CH2 Single bond Sub-23
1-312 Sub-42 3,4-diClPh CH2 Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-313 Sub-42 3,4-diClPh CH2 Single bond Sub-25
1-314 Sub-42 3,4-diClPh CH2 Single bond Sub-26
1-315 Sub-42 3,4-diClPh CH2 Single bond Sub-27
1-316 Sub-42 3,4-diClPh CH2 Single bond Sub-28
1-317 Sub-42 3,4-diClPh CH2 Single bond Sub-29
1-318 Sub-42 3,4-diClPh CH2 Single bond Sub-30
1-319 Sub-42 3,4-diClPh CH2 Single bond Sub-31
1-320 Sub-42 3,4-diClPh CH2 Single bond Sub-32
1-321 Sub-43 3,4-diClPh CH2 Single bond Sub-1
1-322 Sub-43 3,4-diClPh CH2 Single bond Sub-2
1-323 Sub-43 3,4-diClPh CH2 Single bond Sub-3
1-324 Sub-43 3,4-diClPh CH2 Single bond Sub-4
1-325 Sub-43 3,4-diClPh CH2 Single bond Sub-5
1-326 Sub-43 3,4-diClPh CH2 Single bond Sub-6
1-327 Sub-43 3,4-diClPh CH2 Single bond Sub-7
1-328 Sub-43 3,4-diClPh CH2 Single bond Sub-8
1-329 Sub-43 3,4-diClPh CH2 Single bond Sub-9
1-330 Sub-43 3,4-diClPh CH2 Single bond Sub-10
1-331 Sub-43 3,4-diClPh CH2 Single bond Sub-11
1-332 Sub-43 3,4-diClPh CH2 Single bond Sub-12
1-333 Sub-43 3,4-diClPh CH2 Single bond Sub-13
1-334 Sub-43 3,4-diClPh CH2 Single bond Sub-14
1-335 Sub-43 3,4-diClPh CH2 Single bond Sub-15
1-336 Sub-43 3,4-diClPh CH2 Single bond Sub-16
1-337 Sub-43 3,4-diClPh CH2 Single bond Sub-17
1-338 Sub-43 3,4-diClPh CH2 Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-339 Sub-43 3,4-diClPh CH2 Single bond Sub-19
1-340 Sub-43 3,4-diClPh CH2 Single bond Sub-20
1-341 Sub-43 3,4-diClPh CH2 Single bond Sub-21
1-342 Sub-43 3,4-diClPh CH2 Single bond Sub-22
1-343 Sub-43 3,4-diClPh CH2 Single bond Sub-23
1-344 Sub-43 3,4-diClPh CH2 Single bond Sub-24
1-345 Sub-43 3,4-diClPh CH2 Single bond Sub-25
1-346 Sub-43 3,4-diClPh CH2 Single bond Sub-26
1-347 Sub-43 3,4-diClPh CH2 Single bond Sub-27
1-348 Sub-43 3,4-diClPh CH2 Single bond Sub-28
1-349 Sub-43 3,4-diClPh CH2 Single bond Sub-29
1-350 Sub-43 3,4-diClPh CH2 Single bond Sub-30
1-351 Sub-43 3,4-diClPh CH2 Single bond Sub-31
1-352 Sub-43 3,4-diClPh CH2 Single bond Sub-32
1-353 Sub-44 3,4-diClPh CH2 Single bond Sub-1
1-354 Sub-44 3,4-diClPh CH2 Single bond Sub-2
1-355 Sub-44 3,4-diClPh CH2 Single bond Sub-3
1-356 Sub-44 3,4-diClPh CH2 Single bond Sub-4
1-357 Sub-44 3,4-diClPh CH2 Single bond Sub-5
1-358 Sub-44 3,4-diClPh CH2 Single bond Sub-6
1-359 Sub-44 3,4-diClPh CH2 Single bond Sub-7
1-360 Sub-44 3,4-diClPh CH2 Single bond Sub-8
1-361 Sub-44 3,4-diClPh CH2 Single bond Sub-9
1-362 Sub44 3,4-diClPh CH2 Single bond Sub-10
1-363 Sub-44 3,4-diClPh CH2 Single bond Sub-11
1-364 Sub-44 3,4-diClPh CH2 Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-365 Sub-44 3,4-diClPh CH2 Single bond Sub-13
1-366 Sub-44 3,4-diClPh CH2 Single bond Sub-14
1-367 Sub-44 3,4-diClPh CH2 Single bond Sub-15
1-368 Sub-44 3,4-diClPh CH2 Single bond Sub-16
1-369 Sub-44 3,4-diClPh CH2 Single bond Sub-17
1-370 Sub-44 3,4-diClPh CH2 Single bond Sub-18
1-371 Sub-44 3,4-diClPh CH2 Single bond Sub-19
1-372 Sub-44 3,4-diClPh CH2 Single bond Sub-20
1-373 Sub-44 3,4-diClPh CH2 Single bond Sub-21
1-374 Sub-44 3,4-diClPh CH2 Single bond Sub-22
1-375 Sub-44 3,4-diClPh CH2 Single bond Sub-23
1-376 Sub-44 3,4-diClPh CH2 Single bond Sub-24
1-377 Sub-44 3,4-diClPh CH2 Single bond Sub-25
1-378 Sub-44 3,4-diClPh CH2 Single bond Sub-26
1-379 Sub-44 3,4-diClPh CH2 Single bond Sub-27
1-380 Sub-44 3,4-diClPh CH2 Single bond Sub-28
1-381 Sub-44 3,4-diClPh CH2 Single bond Sub-29
1-382 Sub-44 3,4-diClPh CH2 Single bond Sub-30
1-383 Sub-44 3,4-diClPh CH2 Single bond Sub-31
1-384 Sub-44 3,4-diClPh CH2 Single bond Sub-32
1-385 Sub-45 3,4-diClPh CH2 Single bond Sub-1
1-386 Sub-45 3,4-diClPh CH2 Single bond Sub-2
1-387 Sub-45 3,4-diClPh CH2 Single bond Sub-3
1-388 Sub-45 3,4-diClPh CH2 Single bond Sub-4
1-389 Sub-45 3,4-diClPh CH2 Single bond Sub-5
1-390 Sub-45 3,4-diClPh CH2 Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-391 Sub-45 3,4-diClPh CH2 Single bond Sub-7
1-392 Sub-45 3,4-diClPh CH2 Single bond Sub-8
1-393 Sub-45 3,4-diClPh CH2 Single bond Sub-9
1-394 Sub-45 3,4-diClPh CH2 Single bond Sub-10
1-395 Sub-45 3,4-diClPh CH2 Single bond Sub-11
1-396 Sub-45 3,4-diClPh CH2 Single bond Sub-12
1-397 Sub-45 3,4-diClPh CH2 Single bond Sub-13
1-398 Sub-45 3,4-diClPh CH2 Single bond Sub-14
1-399 Sub-45 3,4-diClPh CH2 Single bond Sub-15
1-400 Sub-45 3,4-diClPh CH2 Single bond Sub-16
1-401 Sub-45 3,4-diClPh CH2 Single bond Sub-17
1-402 Sub-45 3,4-diClPh CH2 Single bond Sub-18
1-403 Sub-45 3,4-diClPh CH2 Single bond Sub-19
1-404 Sub-45 3,4-diClPh CH2 Single bond Sub-20
1-405 Sub-45 3,4-diClPh CH2 Single bond Sub-21
1-406 Sub-45 3,4-diClPh CH2 Single bond Sub-22
1-407 Sub-45 3,4-diClPh CH2 Single bond Sub-23
1-408 Sub-45 3,4-diClPh CH2 Single bond Sub-24
1-409 Sub-45 3,4-diClPh CH2 Single bond Sub-25
1-410 Sub-45 3,4-diClPh CH2 Single bond Sub-26
1-411 Sub-45 3,4-diClPh CH2 Single bond Sub-27
1-412 Sub-45 3,4-diClPh CH2 Single bond Sub-28
1-413 Sub-45 3,4-diClPh CH2 Single bond Sub-29
1-414 Sub-45 3,4-diClPh CH2 Single bond Sub-30
1-415 Sub-45 3,4-diClPh CH2 Single bond Sub-31
1-416 Sub-45 3,4-diClPh CH2 Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-417 Sub-46 3,4-diClPh CH2 Single bond Sub-1
1-418 Sub-46 3,4-diClPh CH2 Single bond Sub-2
1-419 Sub-46 3,4-diClPh CH2 Single bond Sub-3
1-420 Sub-46 3,4-diClPh CH2 Single bond Sub-4
1-421 Sub-46 3,4-diClPh CH2 Single bond Sub-5
1-422 Sub-46 3,4-diClPh CH2 Single bond Sub-6
1-423 Sub-46 3,4-diClPh CH2 Single bond Sub-7
1-424 Sub-46 3,4-diClPh CH2 Single bond Sub-8
1-425 Sub-46 3,4-diClPh CH2 Single bond Sub-9
1-426 Sub-46 3,4-diClPh CH2 Single bond Sub-10
1-427 Sub-46 3,4-diClPh CH2 Single bond Sub-11
1-428 Sub-46 3,4-diClPh CH2 Single bond Sub-12
1-429 Sub-46 3,4-diClPh CH2 Single bond Sub-13
1-430 Sub-46 3,4-diClPh CH2 Single bond Sub-14
1-431 Sub-46 3,4-diClPh CH2 Single bond Sub-15
1-432 Sub-46 3,4-diClPh CH2 Single bond Sub-16
1-433 Sub-46 3,4-diClPh CH2 Single bond Sub-17
1-434 Sub-46 3,4-diClPh CH2 Single bond Sub-18
1-435 Sub-46 3,4-diClPh CH2 Single bond Sub-19
1-436 Sub-46 3,4-diClPh CH2 Single bond Sub-20
1-437 Sub-46 3,4-diClPh CH2 Single bond Sub-21
1-438 Sub-46 3,4-diClPh CH2 Single bond Sub-22
1-439 Sub-46 3,4-diClPh CH2 Single bond Sub-23
1-440 Sub-46 3,4-diClPh CH2 Single bond Sub-24
1-441 Sub-46 3,4-diClPh CH2 Single bond Sub-25
1-442 Sub-46 3,4-diClPh CH2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-443 Sub-46 3,4-diClPh CH2 Single bond Sub-27
1-444 Sub-46 3,4-diClPh CH2 Single bond Sub-28
1-445 Sub-46 3,4-diClPh CH2 Single bond Sub-29
1-446 Sub-46 3,4-diClPh CH2 Single bond Sub-30
1-447 Sub-46 3,4-diClPh CH2 Single bond Sub-31
1-448 Sub-46 3,4-diClPh CH2 Single bond Sub-32
1-449 Sub-47 3,4-diClPh CH2 Single bond Sub-1
1-450 Sub-47 3,4-diClPh CH2 Single bond Sub-2
1-451 Sub-47 3,4-diClPh CH2 Single bond Sub-3
1-452 Sub-47 3,4-diClPh CH2 Single bond Sub-4
1-453 Sub-47 3,4-diClPh CH2 Single bond Sub-5
1-454 Sub-47 3,4-diClPh CH2 Single bond Sub-6
1-455 Sub-47 3,4-diClPh CH2 Single bond Sub-7
1-456 Sub-47 3,4-diClPh CH2 Single bond Sub-8
1-457 Sub-47 3,4-diClPh CH2 Single bond Sub-9
1-458 Sub-47 3,4-diClPh CH2 Single bond Sub-10
1-459 Sub-47 3,4-diClPh CH2 Single bond Sub-11
1-460 Sub-47 3,4-diClPh CH2 Single bond Sub-12
1-461 Sub-47 3,4-diClPh CH2 Single bond Sub-13
1-462 Sub-47 3,4-diClPh CH2 Single bond Sub-14
1-463 Sub-47 3,4-diClPh CH2 Single bond Sub-15
1-464 Sub-47 3,4-diClPh CH2 Single bond Sub-16
1-465 Sub-47 3,4-diClPh CH2 Single bond Sub-17
1-466 Sub-47 3,4-diClPh CH2 Single bond Sub-18
1-467 Sub-47 3,4-diClPh CH2 Single bond Sub-19
1-468 Sub-47 3,4-diClPh CH2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-469 Sub-47 3,4-diClPh CH2 Single bond Sub-21
1-470 Sub-47 3,4-diClPh CH2 Single bond Sub-22
1-471 Sub-47 3,4-diClPh CH2 Single bond Sub-23
1-472 Sub-47 3,4-diClPh CH2 Single bond Sub-24
1-473 Sub-47 3,4-diClPh CH2 Single bond Sub-25
1-474 Sub-47 3,4-diClPh CH2 Single bond Sub-26
1-475 Sub-47 3,4-diClPh CH2 Single bond Sub-27
1-476 Sub-47 3,4-diClPh CH2 Single bond Sub-28
1-477 Sub-47 3,4-diClPh CH2 Single bond Sub-29
1-478 Sub-47 3,4-diClPh CH2 Single bond Sub-30
1-479 Sub-47 3,4-diClPh CH2 Single bond Sub-31
1-480 Sub-47 3,4-diClPh CH2 Single bond Sub-32
1-481 Sub-48 3,4-diClPh CH2 Single bond Sub-1
1-482 Sub-48 3,4-diClPh CH2 Single bond Sub-2
1-483 Sub-48 3,4-diClPh CH2 Single bond Sub-3
1-484 Sub-48 3,4-diClPh CH2 Single bond Sub-4
1-485 Sub-48 3,4-diClPh CH2 Single bond Sub-5
1-486 Sub-48 3,4-diClPh CH2 Single bond Sub-6
1-487 Sub-48 3,4-diClPh CH2 Single bond Sub-7
1-488 Sub-48 3,4-diClPh CH2 Single bond Sub-8
1-489 Sub-48 3,4-diClPh CH2 Single bond Sub-9
1-490 Sub-48 3,4-diClPh CH2 Single bond Sub-10
1-491 Sub-48 3,4-diClPh CH2 Single bond Sub-11
1-492 Sub-48 3,4-diClPh CH2 Single bond Sub-12
1-493 Sub-48 3,4-diClPh CH2 Single bond Sub-13
1-494 Sub-48 3,4-diClPh CH2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-495 Sub-48 3,4-diClPh CH2 Single bond Sub-15
1-496 Sub-48 3,4-diClPh CH2 Single bond Sub-16
1-497 Sub-48 3,4-diClPh CH2 Single bond Sub-17
1-498 Sub-48 3,4-diClPh CH2 Single bond Sub-18
1-499 Sub-48 3,4-diClPh CH2 Single bond Sub-19
1-500 Sub-48 3,4-diClPh CH2 Single bond Sub-20
1-501 Sub-48 3,4-diClPh CH2 Single bond Sub-21
1-502 Sub-48 3,4-diClPh CH2 Single bond Sub-22
1-503 Sub-48 3,4-diClPh CH2 Single bond Sub-23
1-504 Sub-48 3,4-diClPh CH2 Single bond Sub-24
1-505 Sub-48 3,4-diClPh CH2 Single bond Sub-25
1-506 Sub-48 3,4-diClPh CH2 Single bond Sub-26
1-507 Sub-48 3,4-diClPh CH2 Single bond Sub-27
1-508 Sub-48 3,4-diClPh CH2 Single bond Sub-28
1-509 Sub-48 3,4-diClPh CH2 Single bond Sub-29
1-510 Sub-48 3,4-diClPh CH2 Single bond Sub-30
1-511 Sub-48 3,4-diClPh CH2 Single bond Sub-31
1-512 Sub-48 3,4-diClPh CH2 Single bond Sub-32
1-513 Sub-49 3,4-diClPh CH2 Single bond Sub-1
1-514 Sub-49 3,4-diClPh CH2 Single bond Sub-2
1-515 Sub-49 3,4-diClPh CH2 Single bond Sub-3
1-516 Sub-49 3,4-diClPh CH2 Single bond Sub-4
1-517 Sub-49 3,4-diClPh CH2 Single bond Sub-5
1-518 Sub-49 3,4-diClPh CH2 Single bond Sub-6
1-519 Sub-49 3,4-diClPh CH2 Single bond Sub-7
1-520 Sub-49 3,4-diClPh CH2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-521 Sub-49 3,4-diClPh CH2 Single bond Sub-9
1-522 Sub-49 3,4-diClPh CH2 Single bond Sub-10
1-523 Sub-49 3,4-diClPh CH2 Single bond Sub-11
1-524 Sub-49 3,4-diClPh CH2 Single bond Sub-12
1-525 Sub-49 3,4-diClPh CH2 Single bond Sub-13
1-526 Sub-49 3,4-diClPh CH2 Single bond Sub-14
1-527 Sub-49 3,4-diClPh CH2 Single bond Sub-15
1-528 Sub-49 3,4-diClPh CH2 Single bond Sub-16
1-529 Sub-49 3,4-diClPh CH2 Single bond Sub-17
1-530 Sub-49 3,4-diClPh CH2 Single bond Sub-18
1-531 Sub-49 3,4-diClPh CH2 Single bond Sub-19
1-532 Sub-49 3,4-diClPh CH2 Single bond Sub-20
1-533 Sub-49 3,4-diClPh CH2 Single bond Sub-21
1-534 Sub-49 3,4-diClPh CH2 Single bond Sub-22
1-535 Sub-49 3,4-diClPh CH2 Single bond Sub-23
1-536 Sub-49 3,4-diClPh CHl2 Single bond Sub-24
1-537 Sub-49 3,4-diClPh CH2 Single bond Sub-25
1-538 Sub-49 3,4-diClPh CH2 Single bond Sub-26
1-539 Sub-49 3,4-diClPh CH2 Single bond Sub-27
1-540 Sub-49 3,4-diClPh CH2 Single bond Sub-28
1-541 Sub-49 3,4-diClPh CH2 Single bond Sub-29
1-542 Sub-49 3,4-diClPh CH2 Single bond Sub-30
1-543 Sub-49 3,4-diClPh CH2 Single bond Sub-31
1-544 Sub-49 3,4-diClPh CH2 Single bond Sub-32
1-545 Sub-50 3,4-diClPh CH2 SheetKey with a key body Sub-1
1-546 Sub-50 3,4-diClPh CH2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-547 Sub-50 3,4-diClPh CH2 Single bond Sub-3
1-548 Sub-50 3,4-diClPh CH2 Single bond Sub-4
1-549 Sub-50 3,4-diClPh CH2 Single bond Sub-5
1-550 Sub-50 3,4-diClPh CH2 Single bond Sub-6
1-551 Sub-50 3,4-diCiPh CH2 Single bond Sub-7
1-552 Sub-50 3,4-diClPh CH2 Single bond Sub-8
1-553 Sub-50 3,4-diClPh CH2 Single bond Sub-9
1-554 Sub-50 3,4-diClPh CH2 Single bond Sub-10
1-555 Sub-50 3,4-diClPh CH2 Single bond Sub-11
1-556 Sub-50 3,4-diClPh CH2 Single bond Sub-12
1-557 Sub-50 3,4-diClPh CH2 Single bond Sub-13
1-558 Sub-50 3,4-diClPh CH2 Single bond Sub-14
1-559 Sub-50 3,4-diClPh CH2 Single bond Sub-15
1-560 Sub-50 3,4-diClPh CH2 Single bond Sub-16
1-561 Sub-50 3,4-diClPh CH2 Single bond Sub-17
1-562 Sub-50 3,4-diClPh CH2 Single bond Sub-18
1-563 Sub-50 3,4-diClPh CH2 Single bond Sub-19
1-564 Sub-50 3,4-diClPh CH2 Single bond Sub-20
1-565 Sub-50 3,4-diClPh CH2 Single bond Sub-21
1-566 Sub-50 3,4-diClPh CH2 Single bond Sub-22
1-567 Sub-50 3,4-diClPh CH2 Single bond Sub-23
1-568 Sub-50 3,4-diClPh CH2 Single bond Sub-24
1-569 Sub-50 3,4-diClPh CH2 Single bond Sub-25
1-570 Sub-50 3,4-diClPh CH2 Single bond Sub-26
1-571 Sub-50 3,4-diClPh CH2 Single bond Sub-27
1-572 Sub-50 3,4-diClPh CH2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-573 Sub-50 3,4-diClPh CH2 Single bond Sub-29
1-574 Sub-50 3,4-diClPh CH2 Single bond Sub-30
1-575 Sub-50 3,4-diClPh CH2 Single bond Sub-31
1-576 Sub-50 3,4-diClPh CH2 Single bond Sub-32
1-577 Sub-51 3,4-diClPh CH2 Single bond Sub-1
1-578 Sub-51 3,4-diClPh CH2 Single bond Sub-2
1-579 Sub-51 3,4-diClPh CH2 Single bond Sub-3
1-580 Sub-51 3,4-diClPh CH2 Single bond Sub-4
1-581 Sub-51 3,4-diClPh CH2 Single bond Sub-5
1-582 Sub-51 3,4-diClPh CH2 Single bond Sub-6
1-583 Sub-51 3,4-diClPh CH2 Single bond Sub-7
1-584 Sub-51 3,4-diClPh CH2 Single bond Sub-8
1-585 Sub-51 3,4-diClPh CH2 Single bond Sub-9
1-586 Sub-51 3,4-diClPh CH2 Single bond Sub-10
1-587 Sub-51 3,4-diClPh CH2 Single bond Sub-11
1-588 Sub-51 3,4-diClPh CH2 Single bond Sub-12
1-589 Sub-51 3,4-diClPh CH2 Single bond Sub-13
1-590 Sub-51 3,4-diClPh CH2 Single bond Sub-14
1-591 Sub-51 3,4-diClPh CH2 Single bond Sub-15
1-592 Sub-51 3,4-diClPh CH2 Single bond Sub-16
1-593 Sub-51 3,4-diClPh CH2 Single bond Sub-17
1-594 Sub-51 3,4-diClPh CH2 Single bond Sub-18
1-595 Sub-51 3,4-diClPh CH2 Single bond Sub-19
1-596 Sub-51 3,4-diClPh CH2 Single bond Sub-20
1-597 Sub-51 3,4-diClPh CH2 Single bond Sub-21
1-598 Sub-51 3,4-diClPh CH2 Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-599 Sub-51 3,4-diClPh CH2 Single bond Sub-23
1-600 Sub-51 3,4-diClPh CH2 Single bond Sub-24
1-601 Sub-51 3,4-diClPh CH2 Single bond Sub-25
1-602 Sub-51 3,4-diClPh CH2 Single bond Sub-26
1-603 Sub-51 3,4-diClPh CH2 Single bond Sub-27
1-604 Sub-51 3,4-diClPh CH2 Single bond Sub-28
1-605 Sub-51 3,4-diClPh CH2 Single bond Sub-29
1-606 Sub-51 3,4-diClPh CH2 Single bond Sub-30
1-607 Sub-51 3,4-diClPh CH2 Single bond Sub-31
1-608 Sub-51 3,4-diClPh CH2 Single bond Sub-32
1-609 Sub-52 3,4-diClPh CH2 Single bond Sub-1
1-610 Sub-52 3,4-diClPh CH2 Single bond Sub-2
1-611 Sub-52 3,4-diClPh CH2 Single bond Sub-3
1-612 Sub-52 3,4-diClPh CH2 Single bond Sub-4
1-613 Sub-52 3,4-diClPh CH2 Single bond Sub-5
1-614 Sub-52 3,4-diClPh CH2 Single bond Sub-6
1-615 Sub-52 3,4-diClPh CH2 Single bond Sub-7
1-616 Sub-52 3,4-diClPh CH2 Single bond Sub-8
1-617 Sub-52 3,4-diClPh CH2 Single bond Sub-9
1-618 Sub-52 3,4-diClPh CH2 Single bond Sub-10
1-619 Sub-52 3,4-diClPh CH2 Single bond Sub-11
1-620 Sub-52 3,4-diClPh CH2 Single bond Sub-12
1-621 Sub-52 3,4-diClPh CH2 Single bond Sub-13
1-622 Sub-52 3,4-diClPh CH2 Single bond Sub-14
1-623 Sub-52 3,4-diClPh CH2 Single bond Sub-15
1-624 Sub-52 3,4-diClPh CH2 Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-625 Sub-52 3,4-diClPh CH2 Single bond Sub-17
1-626 Sub-52 3,4-diClPh CH2 Single bond Sub-18
1-627 Sub-52 3,4-diClPh CH2 Single bond Sub-19
1-628 Sub-52 3,4-diClPh CH2 Single bond Sub-20
1-629 Sub-52 3,4-diClPh CH2 Single bond Sub-21
1-630 Sub-52 3,4-diClPh CH2 Single bond Sub-22
1-631 Sub-52 3,4-diClPh CH2 Single bond Sub-23
1-632 Sub-52 3,4-diClPh CH2 Single bond Sub-24
1-633 Sub-52 3,4-diClPh CH2 Single bond Sub-25
1-634 Sub-52 3,4-diClPh CH2 Single bond Sub-26
1-635 Sub-52 3,4-diClPh CH2 Single bond Sub-27
1-636 Sub-52 3,4-diClPh CH2 Single bond Sub-28
1-637 Sub-52 3,4-diClPh CH2 Single bond Sub-29
1-638 Sub-52 3,4-diClPh CH2 Single bond Sub-30
1-639 Sub-52 3,4-diClPh CH2 Single bond Sub-31
1-640 Sub-52 3,4-diClPh CH2 Single bond Sub-32
1-641 Sub-53 3,4-diClPh CH2 Single bond Sub-1
1-642 Sub-53 3,4-diClPh CH2 Single bond Sub-2
1-643 Sub-53 3,4-diClPh CH2 Single bond Sub-3
1-644 Sub-53 3,4-diClPh CH2 Single bond Sub-4
1-645 Sub-53 3,4-diClPh CH2 Single bond Sub-5
1-646 Sub-53 3,4-diClPh CH2 Single bond Sub-6
1-647 Sub-53 3,4-diClPh CH2 Single bond Sub-7
1-648 Sub-53 3,4-diClPh CH2 Single bond Sub-8
1-649 Sub-53 3,4-diClPh CH2 Single bond Sub-9
1-650 Sub-53 3,4-diClPh CH2 Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-651 Sub-53 3,4-diClPh CH2 Single bond Sub-11
1-652 Sub-53 3,4-diClPh CH2 Single bond Sub-12
1-653 Sub-53 3,4-diClPh CH2 Single bond Sub-13
1-654 Sub-53 3,4-diClPh CH2 Single bond Sub-14
1-655 Sub-53 3,4-diClPh CH2 Single bond Sub-15
1-656 Sub-53 3,4-diClPh CH2 Single bond Sub-16
1-657 Sub-53 3,4-diClPh CH2 Single bond Sub-17
1-658 Sub-53 3,4-diClPh CH2 Single bond Sub-18
1-659 Sub-53 3,4-diClPh CH2 Single bond Sub-19
1-660 Sub-53 3,4-diClPh CH2 Single bond Sub-20
1-661 Sub-53 3,4-diClPh CH2 Single bond Sub-21
1-662 Sub-53 3,4-diClPh CH2 Single bond Sub-22
1-663 Sub-53 3,4-diClPh CH2 Single bond Sub-23
1-664 Sub-53 3,4-diClPh CH2 Single bond Sub-24
1-665 Sub-53 3,4-diClPh CH2 Single bond Sub-25
1-666 Sub-53 3,4-diClPh CH2 Single bond Sub-26
1-667 Sub-53 3,4-diClPh CH2 Single bond Sub-27
1-668 Sub-53 3,4-diClPh CH2 Single bond Sub-28
1-669 Sub-53 3,4-diClPh CH2 Single bond Sub-29
1-670 Sub-53 3,4-diClPh CH2 Single bond Sub-30
1-671 Sub-53 3,4-diClPh CH2 Single bond Sub-31
1-672 Sub-53 3,4-diClPh CH2 Single bond Sub-32
1-673 Sub-54 3,4-diClPh CH2 Single bond Sub-1
1-674 Sub-54 3,4-diClPh CH2 Single bond Sub-2
1-675 Sub-54 3,4-diClPh CH2 Single bond Sub-3
1-676 Sub-54 3,4-diClPh CH2 Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-677 Sub-54 3,4-diClPh CH2 Single bond Sub-5
1-678 Sub-54 3,4-diClPh CH2 Single bond Sub-6
1-679 Sub-54 3,4-diClPh CH2 Single bond Sub-7
1-680 Sub-54 3,4-diClPh CH2 Single bond Sub-8
1-681 Sub-54 3,4-diClPh CH2 Single bond Sub-9
1-682 Sub-54 3,4-diClPh CH2 Single bond Sub-10
1-683 Sub-54 3,4-diClPh CH2 Single bond Sub-11
1-684 Sub-54 3,4-diClPh CH2 Single bond Sub-12
1-685 Sub-54 3,4-diClPh CH2 Single bond Sub-13
1-686 Sub-54 3,4-diClPh CH2 Single bond Sub-14
1-687 Sub-54 3,4-diClPh CH2 Single bond Sub-15
1-688 Sub-54 3,4-diClPh CH2 Single bond Sub-16
1-689 Sub-54 3,4-diClPh CH2 Single bond Sub-17
1-690 Sub-54 3,4-diClPh CH2 Single bond Sub-18
1-691 Sub-54 3,4-diClPh CH2 Single bond Sub-19
1-692 Sub-54 3,4-diClPh CH2 Single bond Sub-20
1-693 Sub-54 3,4-diClPh CH2 Single bond Sub-21
1-694 Sub-54 3,4-diClPh CH2 Single bond Sub-22
1-695 Sub-54 3,4-diClPh CH2 Single bond Sub-23
1-696 Sub-54 3,4-diClPh CH2 Single bond Sub-24
1-697 Sub-54 3,4-diClPh CH2 Single bond Sub-25
1-698 Sub-54 3,4-diClPh CH2 Single bond Sub-26
1-699 Sub-54 3,4-diClPh CH2 Single bond Sub-27
1-700 Sub-54 3,4-diClPh CH2 Single bond Sub-28
1-701 Sub-54 3,4-diClPh CH2 Single bond Sub-29
1-702 Sub-54 3,4-diClPh CH2 Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-703 Sub-54 3,4-diClPh CH2 Single bond Sub-31
1-704 Sub-54 3,4-diClPh CH2 Single bond Sub-32
1-705 Sub-55 3,4-diClPh CH2 Single bond Sub-1
1-706 Sub-55 3,4-diClPh CH2 Single bond Sub-2
1-707 Sub-55 3,4-diClPh CH2 Single bond Sub-3
1-708 Sub-55 3,4-diClPh CH2 Single bond Sub-4
1-709 Sub-55 3,4-diClPh CH2 Single bond Sub-5
1-710 Sub-55 3,4-diClPh CH2 Single bond Sub-6
1-711 Sub-55 3,4-diClPh CH2 Single bond Sub-7
1-712 Sub-55 3,4-diClPh CH2 Single bond Sub-8
1-713 Sub-55 3,4-diClPh CH2 Single bond Sub-9
1-714 Sub-55 3,4-diClPh CH2 Single bond Sub-10
1-715 Sub-55 3,4-diClPh CH2 Single bond Sub-11
1-716 Sub-55 3,4-diClPh CH2 Single bond Sub-12
1-717 Sub-55 3,4-diClPh CH2 Single bond Sub-13
1-718 Sub-55 3,4-diClPh CH2 Single bond Sub-14
1-719 Sub-55 3,4-diClPh CH2 Single bond Sub-15
1-720 Sub-55 3,4-diClPh CH2 Single bond Sub-16
1-721 Sub-55 3,4-diClPh CH2 Single bond Sub-17
1-722 Sub-55 3,4-diClPh CH2 Single bond Sub-18
1-723 Sub-55 3,4-diClPh CH2 Single bond Sub-19
1-724 Sub-55 3,4-diClPh CH2 Single bond Sub-20
1-725 Sub-55 3,4-diClPh CH2 Single bond Sub-21
1-726 Sub-55 3,4-diClPh CH2 Single bond Sub-22
1-727 Sub-55 3,4-diClPh CH2 Single bond Sub-23
1-728 Sub-55 3,4-diClPh CH2 Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-729 Sub-55 3,4-diClPh CH2 Single bond Sub-25
1-730 Sub-55 3,4-diClPh CH2 Single bond Sub-26
1-731 Sub-55 3,4-diClPh CH2 Single bond Sub-27
1-732 Sub-55 3,4-diClPh CH2 Single bond Sub-28
1-733 Sub-55 3,4-diClPh CH2 Single bond Sub-29
1-734 Sub-55 3,4-diClPh CH2 Single bond Sub-30
1-735 Sub-55 3,4-diClPh CH2 Single bond Sub-31
1-736 Sub-55 3,4-diClPh CH2 Single bond Sub-32
1-737 Sub-56 3,4-diClPh CH2 Single bond Sub-1
1-738 Sub-56 3,4-diClPh CH2 Single bond Sub-2
1-739 Sub-56 3,4-diClPh CH2 Single bond Sub-3
1-740 Sub-56 3,4-diClPh CH2 Single bond Sub-4
1-741 Sub-56 3,4-diClPh CH2 Single bond Sub-5
1-742 Sub-56 3,4-diClPh CH2 SheetKey with a key body Sub-6
1-743 Sub-56 3,4-diClPh CH2 Single bond Sub-7
1-744 Sub-56 3,4-diClPh CH2 Single bond Sub-8
1-745 Sub-56 3,4-diClPh CH2 Single bond Sub-9
1-746 Sub-56 3,4-diClPh CH2 Single bond Sub-10
1-747 Sub-56 3,4-diClPh CH2 Single bond Sub-11
1-748 Sub-56 3,4-diClPh CH2 Single bond Sub-12
1-749 Sub-56 3,4-diClPh CH2 Single bond Sub-13
1-750 Sub-56 3,4-diClPh CH2 Single bond Sub-14
1-751 Sub-56 3,4-diClPh CH2 Single bond Sub-15
1-752 Sub-56 3,4-diClPh CH2 Single bond Sub-16
1-753 Sub-56 3,4-diClPh CH2 Single bond Sub-17
1-754 Sub-56 3,4-diClPh CH2 Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-755 Sub-56 3,4-diClPh CH2 Single bond Sub-19
1-756 Sub-56 3,4-diClPh CH2 Single bond Sub-20
1-757 Sub-56 3,4-diClPh CH2 Single bond Sub-21
1-758 Sub-56 3,4-diClPh CH2 Single bond Sub-22
1-759 Sub-56 3,4-diClPh CH2 Single bond Sub-23
1-760 Sub-56 3,4-diClPh CH2 Single bond Sub-24
1-761 Sub-56 3,4-diClPh CH2 Single bond Sub-25
1-762 Sub-56 3,4-diClPh CH2 Single bond Sub-26
1-763 Sub-56 3,4-diClPh CH2 Single bond Sub-27
1-764 Sub-56 3,4-diClPh CH2 Single bond Sub-28
1-765 Sub-56 3,4-diClPh CH2 Single bond Sub-29
1-766 Sub-56 3,4-diClPh CH2 Single bond Sub-30
1-767 Sub-56 3,4-diClPh CH2 Single bond Sub-31
1-768 Sub-56 3,4-diClPh CH2 Single bond Sub-32
1-769 Sub-57 3,4-diClPh CH2 Single bond Sub-1
1-770 Sub-57 3,4-diClPh CH2 Single bond Sub-2
1-771 Sub-57 3,4-diClPh CH2 Single bond Sub-3
1-772 Sub-57 3,4-diClPh CH2 Single bond Sub-4
1-773 Sub-57 3,4-diClPh CH2 Single bond Sub-5
1-774 Sub-57 3,4-diClPh CH2 Single bond Sub-6
1-775 Sub-57 3,4-diClPh CH2 Single bond Sub-7
1-776 Sub-57 3,4-diClPh CH2 Single bond Sub-8
1-777 Sub-57 3,4-diClPh CH2 Single bond Sub-9
1-778 Sub-57 3,4-diClPh CH2 Single bond Sub-10
1-779 Sub-57 3,4-diClPh CH2 Single bond Sub-11
1-780 Sub-57 3,4-diClPh CH2 Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-781 Sub-57 3,4-diClPh CH2 Single bond Sub-13
1-782 Sub-57 3,4-diClPh CH2 Single bond Sub-14
1-783 Sub-57 3,4-diClPh CH2 Single bond Sub-15
1-784 Sub-57 3,4-diClPh CH2 Single bond Sub-16
1-785 Sub-57 3,4-diClPh CH2 Single bond Sub-17
1-786 Sub-57 3,4-diClPh CH2 Single bond Sub-18
1-787 Sub-57 3,4-diClPh CH2 Single bond Sub-19
1-788 Sub-57 3,4-diClPh CH2 Single bond Sub-20
1-789 Sub-57 3,4-diClPh CH2 Single bond Sub-21
1-790 Sub-57 3,4-diClPh CH2 Single bond Sub-22
1-791 Sub-57 3,4-diClPh CH2 Single bond Sub-23
1-792 Sub-57 3,4-diClPh CH2 Single bond Sub-24
1-793 Sub-57 3,4-diClPh CH2 Single bond Sub-25
1-794 Sub-57 3,4-diClPh CH2 Single bond Sub-26
1-795 Sub-57 3,4-diClPh CH2 Single bond Sub-27
1-796 Sub-57 3,4-diClPh CH2 Single bond Sub-28
1-797 Sub-57 3,4-diClPh CH2 Single bond Sub-29
1-798 Sub-57 3,4-diClPh CH2 Single bond Sub-30
1-799 Sub-57 3,4-diClPh CH2 Single bond Sub-31
1-800 Sub-57 3,4-diClPh CH2 Single bond Sub-32
1-801 Sub-58 3,4-diClPh CH2 Single bond Sub-1
1-802 Sub-58 3,4-diClPh CH2 Single bond Sub-2
1-803 Sub-58 3,4-diClPh CH2 Single bond Sub-3
1-804 Sub-58 3,4-diClPh CH2 Single bond Sub-4
1-805 Sub-58 3,4-diClPh CH2 Single bond Sub-5
1-806 Sub-58 3,4-diClPh CH2 Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-807 Sub-58 3,4-diClPh CH2 Single bond Sub-7
1-808 Sub-58 3,4-diClPh CH2 Single bond Sub-8
1-809 Sub-58 3,4-diClPh CH2 Single bond Sub-9
1-810 Sub-58 3,4-diClPh CH2 Single bond Sub-10
1-811 Sub-58 3,4-diClPh CH2 Single bond Sub-11
1-812 Sub-58 3,4-diClPh CH2 Single bond Sub-12
1-813 Sub-58 3,4-diClPh CH2 Single bond Sub-13
1-814 Sub-58 3,4-diClPh CH2 Single bond Sub-14
1-815 Sub-58 3,4-diClPh CH2 Single bond Sub-15
1-816 Sub-58 3,4-diClPh CH2 Single bond Sub-16
1-817 Sub-58 3,4-diClPh CH2 Single bond Sub-17
1-818 Sub-58 3,4-diClPh CH2 Single bond Sub-18
1-819 Sub-58 3,4-diClPh CH2 Single bond Sub-19
1-820 Sub-58 3,4-diClPh CH2 Single bond Sub-20
1-821 Sub-58 3,4-diClPh CH2 Single bond Sub-21
1-822 Sub-58 3,4-diClPh CH2 Single bond Sub-22
1-823 Sub-58 3,4-diClPh CH2 Single bond Sub-23
1-824 Sub-58 3,4-diClPh CH2 Single bond Sub-24
1-825 Sub-58 3,4-diClPh CH2 Single bond Sub-25
1-826 Sub-58 3,4-diClPh CH2 Single bond Sub-26
1-827 Sub-58 3,4-diClPh CH2 Single bond Sub-27
1-828 Sub-58 3,4-diClPh CH2 Single bond Sub-28
1-829 Sub-58 3,4-diClPh CH2 Single bond Sub-29
1-830 Sub-58 3,4-diClPh CH2 Single bond Sub-30
1-831 Sub-58 3,4-diClPh CH2 Single bond Sub-31
1-832 Sub-58 3,4-diClPh CH2 Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-833 Sub-59 3,4-diClPh CH2 Single bond Sub-1
1-834 Sub-59 3,4-diClPh CH2 Single bond Sub-2
1-835 Sub-59 3,4-diClPh CH2 Single bond Sub-3
1-836 Sub-59 3,4-diClPh CH2 Single bond Sub-4
1-837 Sub-59 3,4-diClPh CH2 Single bond Sub-5
1-838 Sub-59 3,4-diClPh CH2 Single bond Sub-6
1-839 Sub-59 3,4-diClPh CH2 Single bond Sub-7
1-840 Sub-59 3,4-diClPh CH2 Single bond Sub-8
1-841 Sub-59 3,4-diClPh CH2 Single bond Sub-9
1-842 Sub-59 3,4-diClPh CH2 Single bond Sub-10
1-843 Sub-59 3,4-diClPh CH2 Single bond Sub-11
1-844 Sub-59 3,4-diClPh CH2 Single bond Sub-12
1-845 Sub-59 3,4-diClPh CH2 Single bond Sub-13
1-846 Sub-59 3,4-diClPh CH2 Single bond Sub-14
1-847 Sub-59 3,4-diClPh CH2 Single bond Sub-15
1-848 Sub-59 3,4-diClPh CH2 Single bond Sub-16
1-849 Sub-59 3,4-diClPh CH2 Single bond Sub-17
1-850 Sub-59 3,4-diClPh CH2 Single bond Sub-18
1-851 Sub-59 3,4-diClPh CH2 Single bond Sub-19
1-852 Sub-59 3,4-diClPh CH2 Single bond Sub-20
1-853 Sub-59 3,4-diClPh CH2 Single bond Sub-21
1-854 Sub-59 3,4-diClPh CH2 Single bond Sub-22
1-855 Sub-59 3,4-diClPh CH2 Single bond Sub-23
1-856 Sub-59 3,4-diClPh CH2 Single bond Sub-24
1-857 Sub-59 3,4-diClPh CH2 Single bond Sub-25
1-858 Sub-59 3,4-diClPh CH2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-859 Sub-59 3,4-diClPh CH2 Single bond Sub-27
1-860 Sub-59 3,4-diClPh CH2 Single bond Sub-28
1-861 Sub-59 3,4-diClPh CH2 Single bond Sub-29
1-862 Sub-59 3,4-diClPh CH2 Single bond Sub-30
1-863 Sub-59 3,4-diClPh CH2 Single bond Sub-31
1-864 Sub-59 3,4-diClPh CH2 Single bond Sub-32
1-865 Sub-60 3,4-diClPh CH2 Single bond Sub-1
1-866 Sub-60 3,4-diClPh CH2 Single bond Sub-2
1-867 Sub-60 3,4-diClPh CH2 Single bond Sub-3
1-868 Sub-60 3,4-diClPh CH2 Single bond Sub-4
1-869 Sub-60 3,4-diClPh CH2 Single bond Sub-5
1-870 Sub-60 3,4-diClPh CH2 Single bond Sub-6
1-871 Sub-60 3,4-diClPh CH2 Single bond Sub-7
1-872 Sub-60 3,4-diClPh CH2 Single bond Sub-8
1-873 Sub-60 3,4-diClPh CH2 Single bond Sub-9
1-874 Sub-60 3,4-diClPh CH2 Single bond Sub-10
1-875 Sub-60 3,4-diClPh CH2 Single bond Sub-11
1-876 Sub-60 3,4-diClPh CH2 Single bond Sub-12
1-877 Sub-60 3,4-diClPh CH2 Single bond Sub-13
1-878 Sub-60 3,4-diClPh CH2 Single bond Sub-14
1-879 Sub-60 3,4-diClPh CH2 Single bond Sub-15
1-880 Sub-60 3,4-diClPh CH2 Single bond Sub-16
1-881 Sub-60 3,4-diClPh CH2 Single bond Sub-17
1-882 Sub-60 3,4-diClPh CH2 Single bond Sub-18
1-883 Sub-60 3,4-diClPh CH2 Single bond Sub-19
1-884 Sub-60 3,4-diClPh CH2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-885 Sub-60 3,4-diClPh CH2 Single bond Sub-21
1-886 Sub-60 3,4-diClPh CH2 Single bond Sub-22
1-887 Sub-60 3,4-diClPh CH2 Single bond Sub-23
1-888 Sub-60 3,4-diClPh CH2 Single bond Sub-24
1-889 Sub-60 3,4-diClPh CH2 Single bond Sub-25
1-890 Sub-60 3,4-diClPh CH2 Single bond Sub-26
1-891 Sub-60 3,4-diClPh CH2 Single bond Sub-27
1-892 Sub-60 3,4-diClPh CH2 Single bond Sub-28
1-893 Sub-60 3,4-diClPh CH2 Single bond Sub-29
1-894 Sub-60 3,4-diClPh CH2 Single bond Sub-30
1-895 Sub-60 3,4-diClPh CH2 Single bond Sub-31
1-896 Sub-60 3,4-diClPh CH2 Single bond Sub-32
1-897 Sub-61 3,4-diClPh CH2 Single bond Sub-1
1-898 Sub-61 3,4-diClPh CH2 Single bond Sub-2
1-899 Sub-61 3,4-diClPh CH2 Single bond Sub-3
1-900 Sub-61 3,4-diClPh CH2 Single bond Sub-4
1-901 Sub-61 3,4-diClPh CH2 Single bond Sub-5
1-902 Sub-61 3,4-diClPh CH2 Single bond Sub-6
1-903 Sub-61 3,4-diClPh CH2 Single bond Sub-7
1-904 Sub-61 3,4-diClPh CH2 Single bond Sub-8
1-905 Sub-61 3,4-diClPh CH2 Single bond Sub-9
1-906 Sub-61 3,4-diClPh CH2 Single bond Sub-10
1-907 Sub-61 3,4-diClPh CH2 Single bond Sub-11
1-908 Sub-61 3,4-diClPh CH2 Single bond Sub-12
1-909 Sub-61 3,4-diClPh CH2 Single bond Sub-13
1-910 Sub-61 3,4-diClPh CH2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-911 Sub-61 3,4-diClPh CH2 Single bond Sub-15
1-912 Sub-61 3,4-diClPh CH2 Single bond Sub-16
1-913 Sub-61 3,4-diClPh CH2 Single bond Sub-17
1-914 Sub-61 3,4-diClPh CH2 Single bond Sub-18
1-915 Sub-61 3,4-diClPh CH2 Single bond Sub-19
1-916 Sub-61 3,4-diClPh CH2 Single bond Sub-20
1-917 Sub-61 3,4-diClPh CH2 Single bond Sub-21
1-918 Sub-61 3,4-diClPh CH2 Single bond Sub-22
1-919 Sub-61 3,4-diClPh CH2 Single bond Sub-23
1-920 Sub-61 3,4-diClPh CH2 Single bond Sub-24
1-921 Sub-61 3,4-diClPh CH2 Single bond Sub-25
1-922 Sub-61 3,4-diClPh CH2 Single bond Sub-26
1-923 Sub-61 3,4-diClPh CH2 Single bond Sub-27
1-924 Sub-61 3,4-diClPh CH2 Single bond Sub-28
1-925 Sub-61 3,4-diClPh CH2 Single bond Sub-29
1-926 Sub-61 3,4-diClPh CH2 Single bond Sub-30
1-927 Sub-61 3,4-diClPh CH2 Single bond Sub-31
1-928 Sub-61 3,4-diClPh CH2 Single bond Sub-32
1-929 Sub-62 3,4-diClPh CH2 Single bond Sub-1
1-930 Sub-62 3,4-diClPh CH2 Single bond Sub-2
1-931 Sub-62 3,4-diClPh CH2 Single bond Sub-3
1-932 Sub-62 3,4-diClPh CH2 Single bond Sub-4
1-933 Sub-62 3,4-diClPh CH2 Single bond Sub-5
1-934 Sub-62 3,4-diClPh CH2 Single bond Sub-6
1-935 Sub-62 3,4-diClPh CH2 Single bond Sub-7
1-936 Sub-62 3,4-diClPh CH2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-937 Sub-62 3,4-diClPh CH2 Single bond Sub-9
1-938 Sub-62 3,4-diClPh CH2 Single bond Sub-10
1-939 Sub-62 3,4-diClPh CH2 Single bond Sub-11
1-940 Sub-62 3,4-diClPh CH2 Single bond Sub-12
1-941 Sub-62 3,4-diClPh CH2 Single bond Sub-13
1-942 Sub-62 3,4-diClPh CH2 Single bond Sub-14
1-943 Sub-62 3,4-diClPh CH2 Single bond Sub-15
1-944 Sub-62 3,4-diClPh CH2 Single bond Sub-16
1-945 Sub-62 3,4-diClPh CH2 Single bond Sub-17
1-946 Sub-62 3,4-diClPh CH2 Single bond Sub-18
1-947 Sub-62 3,4-diClPh CH2 Single bond Sub-19
1-948 Sub-62 3,4-diClPh CH2 Single bond Sub-20
1-949 Sub-62 3,4-diClPh CH2 Single bond Sub-21
1-950 Sub-62 3,4-diClPh CH2 Single bond Sub-22
1-951 Sub-62 3,4-diClPh CH2 Single bond Sub-23
1-952 Sub-62 3,4-diClPh CH2 Single bond Sub-24
1-953 Sub-62 3,4-diClPh CH2 Single bond Sub-25
1-954 Sub-62 3,4-diClPh CH2 Single bond Sub-26
1-955 Sub-62 3,4-diClPh CH2 Single bond Sub-27
1-956 Sub-62 3,4-diClPh CH2 Single bond Sub-28
1-957 Sub-62 3,4-diClPh CH2 Single bond Sub-29
1-958 Sub-62 3,4-diClPh CH2 Single bond Sub-30
1-959 Sub-62 3,4-diClPh CH2 Single bond Sub-31
1-960 Sub-62 3,4-diClPh CH2 Single bond Sub-32
1-961 Sub-63 3,4-diClPh CH2 Single bond Sub-1
1-962 Sub-63 3,4-diClPh CH2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-963 Sub-63 3,4-diClPh CH2 Single bond Sub-3
1-964 Sub-63 3,4-diClPh CH2 Single bond Sub-4
1-965 Sub-63 3,4-diClPh CH2 Single bond Sub-5
1-966 Sub-63 3,4-diClPh CH2 Single bond Sub-6
1-967 Sub-63 3,4-diClPh CH2 Single bond Sub-7
1-968 Sub-63 3,4-diClPh CH2 Single bond Sub-8
1-969 Sub-63 3,4-diClPh CH2 Single bond Sub-9
1-970 Sub-63 3,4-diClPh CH2 Single bond Sub-10
1-971 Sub-63 3,4-diClPh CH2 Single bond Sub-11
1-972 Sub-63 3,4-diClPh CH2 Single bond Sub-12
1-973 Sub-63 3,4-diClPh CH2 Single bond Sub-13
1-974 Sub-63 3,4-diClPh CH2 Single bond Sub-14
1-975 Sub-63 3,4-diClPh CH2 Single bond Sub-15
1-976 Sub-63 3,4-diClPh CH2 Single bond Sub-16
1-977 Sub-63 3,4-diClPh CH2 Single bond Sub-17
1-978 Sub-63 3,4-diClPh CH2 Single bond Sub-18
1-979 Sub-63 3,4-diClPh CH2 Single bond Sub-19
1-980 Sub-63 3,4-diClPh CH2 Single bond Sub-20
1-981 Sub-63 3,4-diClPh CH2 Single bond Sub-21
1-982 Sub-63 3,4-diClPh CH2 Single bond Sub-22
1-983 Sub-63 3,4-diClPh CH2 Single bond Sub-23
1-984 Sub-63 3,4-diClPh CH2 Single bond Sub-24
1-985 Sub-63 3,4-diClPh CH2 Single bond Sub-25
1-986 Sub-63 3,4-diClPh CH2 Single bond Sub-26
1-987 Sub-63 3,4-diClPh CH2 Single bond Sub-27
1-988 Sub-63 3,4-diClPh CH2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-989 Sub-63 3,4-diClPh CH2 Single bond Sub-29
1-990 Sub-63 3,4-diClPh CH2 Single bond Sub-30
1-991 Sub-63 3,4-diClPh CH2 Single bond Sub-31
1-992 Sub-63 3,4-diClPh CH2 Single bond Sub-32
1-993 Sub-64 3,4-diClPh CH2 Single bond Sub-1
1-994 Sub-64 3,4-diClPh CH2 Single bond Sub-2
1-995 Sub-64 3,4-diClPh CH2 Single bond Sub-3
1-996 Sub-64 3,4-diClPh CH2 Single bond Sub-4
1-997 Sub-64 3,4-diClPh CH2 Single bond Sub-5
1-998 Sub-64 3,4-diClPh CH2 Single bond Sub-6
1-999 Sub-64 3,4-diClPh CH2 Single bond Sub-7
1-1000 Sub-64 3,4-diClPh CH2 Single bond Sub-8
1-1001 Sub-64 3,4-diClPh CH2 Single bond Sub-9
1-1002 Sub-64 3,4-diClPh CH2 Single bond Sub-10
1-1003 Sub-64 3,4-diClPh CH2 Single bond Sub-11
1-1004 Sub-64 3,4-diClPh CH2 Single bond Sub-12
1-1005 Sub-64 3,4-diClPh CH2 Single bond Sub-13
1-1006 Sub-64 3,4-diClPh CH2 Single bond Sub-14
1-1007 Sub-64 3,4-diClPh CH2 Single bond Sub-15
1-1008 Sub-64 3,4-diClPh CH2 Single bond Sub-16
1-1009 Sub-64 3,4-diClPh CH2 Single bond Sub-17
1-1010 Sub-64 3,4-diClPh CH2 Single bond Sub-18
1-1011 Sub-64 3,4-diClPh CH2 Single bond Sub-19
1-1012 Sub-64 3,4-diClPh CH2 Single bond Sub-20
1-1013 Sub-64 3,4-diClPh CH2 Single bond Sub-21
1-1014 Sub-64 3,4-diClPh CH2 Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1015 Sub-64 3,4-diClPh CH2 Single bond Sub-23
1-1016 Sub-64 3,4-diClPh CH2 Single bond Sub-24
1-1017 Sub-64 3,4-diClPh CH2 Single bond Sub-25
1-1018 Sub-64 3,4-diClPh CH2 Single bond Sub-26
1-1019 Sub-64 3,4-diClPh CH2 Single bond Sub-27
1-1020 Sub-64 3,4-diClPh CH2 Single bond Sub-28
1-1021 Sub-64 3,4-diClPh CH2 Single bond Sub-29
1-1022 Sub-64 3,4-diClPh CH2 Single bond Sub-30
1-1023 Sub-64 3,4-diClPh CH2 Single bond Sub-31
1-1024 Sub-64 3,4-diClPh CH2 Single bond Sub-32
1-1025 Sub-33 3,4-diClPh CO Single bond Sub-1
1-1026 Sub-33 3,4-diClPh CO Single bond Sub-2
1-1027 Sub-33 3,4-diClPh CO Single bond Sub-3
1-1028 Sub-33 3,4-diClPh CO Single bond Sub-4
1-1029 Sub-33 3,4-diClPh CO Single bond Sub-5
1-1030 Sub-33 3,4-diClPh CO Single bond Sub-6
1-1031 Sub-33 3,4-diClPh CO Single bond Sub-7
1-1032 Sub-33 3,4-diClPh CO Single bond Sub-8
1-1033 Sub-33 3,4-diClPh CO Single bond Sub-9
1-1034 Sub-33 3,4-diClPh CO Single bond Sub-10
1-1035 Sub-33 3,4-diClPh CO Single bond Sub-11
1-1036 Sub-33 3,4-diClPh CO Single bond Sub-12
1-1037 Sub-33 3,4-diClPh CO Single bond Sub-13
1-1038 Sub-33 3,4-diClPh CO Single bond Sub-14
1-1039 Sub-33 3,4-diClPh CO Single bond Sub-15
1-1040 Sub-33 3,4-diClPh CO Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1041 Sub-33 3,4-diClPh CO Single bond Sub-17
1-1042 Sub-33 3,4-diClPh CO Single bond Sub-18
1-1043 Sub-33 3,4-diClPh CO Single bond Sub-19
1-1044 Sub-33 3,4-diClPh CO Single bond Sub-20
1-1045 Sub-33 3,4-diClPh CO Single bond Sub-21
l-1046 Sub-33 3,4-diClPh CO Single bond Sub-22
1-1047 Sub-33 3,4-diClPh CO Single bond Sub-23
1-1048 Sub-33 3,4-diClPh CO Single bond Sub-24
1-1049 Sub-33 3,4-diClPh CO Single bond Sub-25
1-1050 Sub-33 3,4-diClPh CO Single bond Sub-26
1-1051 Sub-33 3,4-diClPh CO Single bond Sub-27
1-1052 Sub-33 3,4-diClPh CO Single bond Sub-28
1-1053 Sub-33 3,4-diClPh CO Single bond Sub-29
1-1054 Sub-33 3,4-diClPh CO Single bond Sub-30
1-1055 Sub-33 3,4-diClPh CO Single bond Sub-31
1-1056 Sub-33 3,4-diClPh CO Single bond Sub-32
1-1057 Sub-34 3,4-diClPh CO Single bond Sub-1
1-1058 Sub-34 3,4-diClPh CO Single bond Sub-2
1-1059 Sub-34 3,4-diClPh CO Single bond Sub-3
1-1060 Sub-34 3,4-diClPh CO Single bond Sub-4
1-1061 Sub-34 3,4-diClPh CO Single bond Sub-5
1-1062 Sub-34 3,4-diClPh CO Single bond Sub-6
1-1063 Sub-34 3,4-diClPh CO Single bond Sub-7
1-1064 Sub-34 3,4-diClPh CO Single bond Sub-8
1-1065 Sub-34 3,4-diClPh CO Single bond Sub-9
1-1066 Sub-34 3,4-diClPh CO Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1067 Sub-34 3,4-diClPh CO Single bond Sub-11
1-1068 Sub-34 3,4-diClPh CO Single bond Sub-12
1-1069 Sub-34 3,4-diClPh CO Single bond Sub-13
1-1070 Sub-34 3,4-diClPh CO Single bond Sub-14
1-1071 Sub-34 3,4-diClPh CO Single bond Sub-15
1-1072 Sub-34 3,4-diClPh CO Single bond Sub-16
1-1073 Sub-34 3,4-diClPh CO Single bond Sub-17
1-1074 Sub-34 3,4-diClPh CO Single bond Sub-18
1-1075 Sub-34 3,4-diClPh CO Single bond Sub-19
1-1076 Sub-34 3,4-diClPh CO Single bond Sub-20
1-1077 Sub-34 3,4-diClPh CO Single bond Sub-21
1-1078 Sub-34 3,4-diClPh CO Single bond Sub-22
1-1079 Sub-34 3,4-diClPh CO Single bond Sub-23
1-1080 Sub-34 3,4-diClPh CO Single bond Sub-24
1-1081 Sub-34 3,4-diClPh CO Single bond Sub-25
1-1082 Sub-34 3,4-diClPh CO Single bond Sub-26
1-1083 Sub-34 3,4-diClPh CO Single bond Sub-27
1-1084 Sub-34 3,4-diClPh CO Single bond Sub-28
1-1085 Sub-34 3,4-diClPh CO Single bond Sub-29
1-1086 Sub-34 3,4-diClPh CO Single bond Sub-30
1-1087 Sub-34 3,4-diClPh CO Single bond Sub-31
1-1088 Sub-34 3,4-diClPh CO Single bond Sub-32
1-1089 Sub-35 3,4-diClPh CO Single bond Sub-1
1-1090 Sub-35 3,4-diClPh CO Single bond Sub-2
1-1091 Sub-35 3,4-diClPh CO Single bond Sub-3
1-1092 Sub-35 3,4-diClPh CO Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1093 Sub-35 3,4-diClPh CO Single bond Sub-5
1-1094 Sub-35 3,4-diClPh CO Single bond Sub-6
1-1095 Sub-35 3,4-diClPh CO Single bond Sub-7
1-1096 Sub-35 3,4-diClPh CO Single bond Sub-8
1-1097 Sub-35 3,4-diClPh CO Single bond Sub-9
1-1098 Sub-35 3,4-diClPh CO Single bond Sub-10
1-1099 Sub-35 3,4-diClPh CO Single bond Sub-11
1-1100 Sub-35 3,4-diClPh CO Single bond Sub-12
1-1101 Sub-35 3,4-diClPh CO Single bond Sub-13
1-1102 Sub-35 3,4-diClPh CO Single bond Sub-14
1-1103 Sub-35 3,4-diClPh CO Single bond Sub-15
1-1104 Sub-35 3,4-diClPh CO Single bond Sub-16
1-1105 Sub-35 3,4-diClPh CO Single bond Sub-17
1-1106 Sub-35 3,4-diClPh CO Single bond Sub-18
1-1107 Sub-35 3,4-diClPh CO Single bond Sub-19
1-1108 Sub-35 3,4-diClPh CO Single bond Sub-20
1-1109 Sub-35 3,4-diClPh CO Single bond Sub-21
1-1110 Sub-35 3,4-diClPh CO Single bond Sub-22
1-1111 Sub-35 3,4-diClPh CO Single bond Sub-23
1-1112 Sub-35 3,4-diClPh CO Single bond Sub-24
1-1113 Sub-35 3,4-diClPh CO Single bond Sub-25
1-1114 Sub-35 3,4-diClPh CO Single bond Sub-26
1-1115 Sub-35 3,4-diClPh CO Single bond Sub-27
1-1116 Sub-35 3,4-diClPh CO Single bond Sub-28
1-1117 Sub-35 3,4-diClPh CO Single bond Sub-29
1-1118 Sub-35 3,4-diClPh CO Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1119 Sub-35 3,4-diClPh CO Single bond Sub-31
1-1120 Sub-35 3,4-diClPh CO Single bond Sub-32
1-1121 Sub-36 3,4-diClPh CO Single bond Sub-1
1-1122 Sub-36 3,4-diClPh CO Single bond Sub-2
1-1123 Sub-36 3,4-diClPh CO Single bond Sub-3
1-1124 Sub-36 3,4-diClPh CO Single bond Sub-4
1-1125 Sub-36 3,4-diClPh CO Single bond Sub-5
1-1126 Sub-36 3,4-diClPh CO Single bond Sub-6
1-1127 Sub-36 3,4-diClPh CO Single bond Sub-7
1-1128 Sub-36 3,4-diClPh CO Single bond Sub-8
1-1129 Sub-36 3,4-diClPh CO Single bond Sub-9
1-1130 Sub-36 3,4-diClPh CO Single bond Sub-10
1-1131 Sub-36 3,4-diClPh CO Single bond Sub-11
1-1132 Sub-36 3,4-diClPh CO Single bond Sub-12
1-1133 Sub-36 3,4-diClPh CO Single bond Sub-13
1-1134 Sub-36 3,4-diClPh CO Single bond Sub-14
1-1135 Sub-36 3,4-diClPh CO Single bond Sub-15
1-1136 Sub-36 3,4-diClPh CO Single bond Sub-16
1-1137 Sub-36 3,4-diClPh CO Single bond Sub-17
1-1138 Sub-36 3,4-diClPh CO Single bond Sub-18
1-1139 Sub-36 3,4-diClPh CO Single bond Sub-19
1-1140 Sub-36 3,4-diClPh CO Single bond Sub-20
1-1141 Sub-36 3,4-diClPh CO Single bond Sub-21
1-1142 Sub-36 3,4-diClPh CO Single bond Sub-22
1-1143 Sub-36 3,4-diClPh CO Single bond Sub-23
1-1144 Sub-36 3,4-diClPh CO Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1145 Sub-36 3,4-diClPh CO Single bond Sub-25
1-1146 Sub-36 3,4-diClPh CO Single bond Sub-26
1-1147 Sub-36 3,4-diClPh CO Single bond Sub-27
1-1148 Sub-36 3,4-diClPh CO Single bond Sub-28
1-1149 Sub-36 3,4-diClPh CO Single bond Sub-29
1-1150 Sub-36 3,4-diClPh CO Single bond Sub-30
1-1151 Sub-36 3,4-diClPh CO Single bond Sub-31
1-1152 Sub-36 3,4-diClPh CO Single bond Sub-32
1-1153 Sub-37 3,4-diClPh CO Single bond Sub-1
1-1154 Sub-37 3,4-diClPh CO Single bond Sub-2
1-1155 Sub-37 3,4-diClPh CO Single bond Sub-3
1-1156 Sub-37 3,4-diClPh CO Single bond Sub-4
1-1157 Sub-37 3,4-diClPh CO Single bond Sub-5
1-1158 Sub-37 3,4-diClPh CO Single bond Sub-6
1-1159 Sub-37 3,4-diClPh CO Single bond Sub-7
1-1160 Sub-37 3,4-diClPh CO Single bond Sub-8
1-1161 Sub-37 3,4-diClPh CO Single bond Sub-9
1-1162 Sub-37 3,4-diClPh CO Single bond Sub-10
1-1163 Sub-37 3,4-diClPh CO Single bond Sub-11
1-1164 Sub-37 3,4-diClPh CO Single bond Sub-12
1-1165 Sub-37 3,4-diClPh CO Single bond Sub-13
1-1166 Sub-37 3,4-diClPh CO Single bond Sub-14
1-1167 Sub-37 3,4-diClPh CO Single bond Sub-15
1-1168 Sub-37 3,4-diClPh CO Single bond Sub-16
1-1169 Sub-37 3,4-diClPh CO Single bond Sub-17
1-1170 Sub-37 3,4-diClPh CO Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1171 Sub-37 3,4-diClPh CO Single bond Sub-19
1-1172 Sub-37 3,4-diClPh CO Single bond Sub-20
1-1173 Sub-37 3,4-diClPh CO Single bond Sub-21
1-1174 Sub-37 3,4-diClPh CO Single bond Sub-22
1-1175 Sub-37 3,4-diClPh CO Single bond Sub-23
1-1176 Sub-37 3,4-diClPh CO Single bond Sub-24
1-1177 Sub-37 3,4-diClPh CO Single bond Sub-25
1-1178 Sub-37 3,4-diClPh CO Single bond Sub-26
1-1179 Sub-37 3,4-diClPh CO Single bond Sub-27
1-1180 Sub-37 3,4-diClPh CO Single bond Sub-28
1-1181 Sub-37 3,4-diClPh CO Single bond Sub-29
1-1182 Sub-37 3,4-diClPh CO Single bond Sub-30
1-1183 Sub-37 3,4-diClPh CO Single bond Sub-31
1-1184 Sub-37 3,4-diClPh CO Single bond Sub-32
1-1185 Sub-38 3,4-diClPh CO Single bond Sub-1
1-1186 Sub-38 3,4-diClPh CO Single bond Sub-2
1-1187 Sub-38 3,4-diClPh CO Single bond Sub-3
1-1188 Sub-38 3,4-diClPh CO Single bond Sub-4
1-1189 Sub-38 3,4-diClPh CO Single bond Sub-5
1-1190 Sub-38 3,4-diClPh CO Single bond Sub-6
1-1191 Sub-38 3,4-diClPh CO Single bond Sub-7
1-1192 Sub-38 3,4-diClPh CO Single bond Sub-8
1-1193 Sub-38 3,4-diClPh CO Single bond Sub-9
1-1194 Sub-38 3,4-diClPh CO Single bond Sub-10
1-1195 Sub-38 3,4-diClPh CO Single bond Sub-11
1-1196 Sub-38 3,4-diClPh CO Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1197 Sub-38 3,4-diClPh CO Single bond Sub-13
1-1198 Sub-38 3,4-diClPh CO Single bond Sub-14
1-1199 Sub-38 3,4-diClPh CO Single bond Sub-15
1-1200 Sub-38 3,4-diClPh CO Single bond Sub-16
1-1201 Sub-38 3,4-diClPh CO Single bond Sub-17
1-1202 Sub-38 3,4-diClPh CO Single bond Sub-18
1-1203 Sub-38 3,4-diClPh CO Single bond Sub-19
1-1204 Sub-38 3,4-diClPh CO Single bond Sub-20
1-1205 Sub-38 3,4-diClPh CO Single bond Sub-21
1-1206 Sub-38 3,4-diClPh CO Single bond Sub-22
1-1207 Sub-38 3,4-diClPh CO Single bond Sub-23
1-1208 Sub-38 3,4-diClPh CO Single bond Sub-24
1-1209 Sub-38 3,4-diClPh CO Single bond Sub-25
1-1210 Sub-38 3,4-diClPh CO Single bond Sub-26
1-1211 Sub-38 3,4-diClPh CO Single bond Sub-27
1-1212 Sub-38 3,4-diClPh CO Single bond Sub-28
1-1213 Sub-38 3,4-diClPh CO Single bond Sub-29
1-1214 Sub-38 3,4-diClPh CO Single bond Sub-30
1-1215 Sub-38 3,4-diClPh CO Single bond Sub-31
1-1216 Sub-38 3,4-diClPh CO Single bond Sub-32
1-1217 Sub-39 3,4-diClPh CO Single bond Sub-1
1-1218 Sub-39 3,4-diClPh CO Single bond Sub-2
1-1219 Sub-39 3,4-diClPh CO Single bond Sub-3
1-1220 Sub-39 3,4-diClPh CO Single bond Sub-4
1-1221 Sub-39 3,4-diClPh CO Single bond Sub-5
1-1222 Sub-39 3,4-diClPh CO Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1223 Sub-39 3,4-diClPh CO Single bond Sub-7
1-1224 Sub-39 3,4-diClPh CO Single bond Sub-8
1-1225 Sub-39 3,4-diClPh CO Single bond Sub-9
1-1226 Sub-39 3,4-diClPh CO Single bond Sub-10
1-1227 Sub-39 3,4-diClPh CO Single bond Sub-11
1-1228 Sub-39 3,4-diClPh CO Single bond Sub-12
1-1229 Sub-39 3,4-diClPh CO Single bond Sub-13
1-1230 Sub-39 3,4-diClPh CO Single bond Sub-14
1-1231 Sub-39 3,4-diClPh CO Single bond Sub-15
1-1232 Sub-39 3,4-diClPh CO Single bond Sub-16
1-1233 Sub-39 3,4-diClPh CO Single bond Sub-17
1-1234 Sub-39 3,4-diClPh CO Single bond Sub-18
1-1235 Sub-39 3,4-diClPh CO Single bond Sub-19
1-1236 Sub-39 3,4-diClPh CO Single bond Sub-20
1-1237 Sub-39 3,4-diClPh CO Single bond Sub-21
1-1238 Sub-39 3,4-diClPh CO Single bond Sub-22
1-1239 Sub-39 3,4-diClPh CO Single bond Sub-23
1-1240 Sub-39 3,4-diClPh CO Single bond Sub-24
1-1241 Sub-39 3,4-diClPh CO Single bond Sub-25
1-1242 Sub-39 3,4-diClPh CO Single bond Sub-26
1-1243 Sub-39 3,4-diClPh CO Single bond Sub-27
1-1244 Sub-39 3,4-diClPh CO Single bond Sub-28
1-1245 Sub-39 3,4-diClPh CO Single bond Sub-29
1-1246 Sub-39 3,4-diClPh CO Single bond Sub-30
1-1247 Sub-39 3,4-diClPh CO Single bond Sub-31
1-1248 Sub-39 3,4-diClPh CO Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1249 Sub-40 3,4-diClPh CO Single bond Sub-1
1-1250 Sub-40 3,4-diClPh CO Single bond Sub-2
1-1251 Sub-40 3,4-diClPh CO Single bond Sub-3
1-1252 Sub-40 3,4-diClPh CO Single bond Sub-4
1-1253 Sub-40 3,4-diClPh CO Single bond Sub-5
1-1254 Sub-40 3,4-diClPh CO Single bond Sub-6
1-1255 Sub-40 3,4-diClPh CO Single bond Sub-7
1-1256 Sub-40 3,4-diClPh CO Single bond Sub-8
1-1257 Sub-40 3,4-diClPh CO Single bond Sub-9
1-1258 Sub-40 3,4-diClPh CO Single bond Sub-10
1-1259 Sub-40 3,4-diClPh CO Single bond Sub-11
1-1260 Sub-40 3,4-diClPh CO Single bond Sub-12
1-1261 Sub-40 3,4-diClPh CO Single bond Sub-13
1-1262 Sub-40 3,4-diClPh CO Single bond Sub-14
1-1263 Sub-40 3,4-diClPh CO Single bond Sub-15
1-1264 Sub-40 3,4-diClPh CO Single bond Sub-16
1-1265 Sub-40 3,4-diClPh CO Single bond Sub-17
1-1266 Sub-40 3,4-diClPh CO Single bond Sub-18
1-1267 Sub-40 3,4-diClPh CO Single bond Sub-19
1-1268 Sub-40 3,4-diClPh CO Single bond Sub-20
1-1269 Sub-40 3,4-diClPh CO Single bond Sub-21
1-1270 Sub-40 3,4-diClPh CO Single bond Sub-22
1-1271 Sub-40 3,4-diClPh CO Single bond Sub-23
1-1272 Sub-40 3,4-diClPh CO Single bond Sub-24
1-1273 Sub-40 3,4-diClPh CO Single bond Sub-25
1-1274 Sub-40 3,4-diClPh CO Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1275 Sub-40 3,4-diClPh CO Single bond Sub-27
1-1276 Sub-40 3,4-diClPh CO Single bond Sub-28
1-1277 Sub-40 3,4-diClPh CO Single bond Sub-29
1-1278 Sub-40 3,4-diClPh CO Single bond Sub-30
1-1279 Sub-40 3,4-diClPh CO Single bond Sub-31
1-1280 Sub-40 3,4-diClPh CO Single bond Sub-32
1-1281 Sub-41 3,4-diClPh CO Single bond Sub-1
1-1282 Sub-41 3,4-diClPh CO Single bond Sub-2
1-1283 Sub-41 3,4-diClPh CO Single bond Sub-3
1-1284 Sub-41 3,4-diClPh CO Single bond Sub-4
1-1285 Sub-41 3,4-diClPh CO Single bond Sub-5
1-1286 Sub-41 3,4-diClPh CO Single bond Sub-6
1-1287 Sub-41 3,4-diClPh CO Single bond Sub-7
1-1288 Sub-41 3,4-diClPh CO Single bond Sub-8
1-1289 Sub-41 3,4-diClPh CO Single bond Sub-9
1-1290 Sub-41 3,4-diClPh CO Single bond Sub-10
1-1291 Sub-41 3,4-diClPh CO Single bond Sub-11
1-1292 Sub-41 3,4-diClPh CO Single bond Sub-12
1-1293 Sub-41 3,4-diClPh CO Single bond Sub-13
1-1294 Sub-41 3,4-diClPh CO Single bond Sub-14
1-1295 Sub-41 3,4-diClPh CO Single bond Sub-15
1-1296 Sub-41 3,4-diClPh CO Single bond Sub-16
1-1297 Sub-41 3,4-diClPh CO Single bond Sub-17
1-1298 Sub-41 3,4-diClPh CO Single bond Sub-18
1-1299 Sub-41 3,4-diClPh CO Single bond Sub-19
1-1300 Sub-41 3,4-diClPh CO Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1301 Sub-41 3,4-diClPh CO Single bond Sub-21
1-1302 Sub-41 3,4-diClPh CO Single bond Sub-22
1-1303 Sub-41 3,4-diClPh CO Single bond Sub-23
1-1304 Sub-41 3,4-diClPh CO Single bond Sub-24
1-1305 Sub-41 3,4-diClPh CO Single bond Sub-25
1-1306 Sub-41 3,4-diClPh CO Single bond Sub-26
1-1307 Sub-41 3,4-diClPh CO Single bond Sub-27
1-1308 Sub-41 3,4-diClPh CO Single bond Sub-28
1-1309 Sub-41 3,4-diClPh CO Single bond Sub-29
1-1310 Sub-41 3,4-diClPh CO Single bond Sub-30
1-1311 Sub-41 3,4-diClPh CO Single bond Sub-31
1-1312 Sub-41 3,4-diClPh CO Single bond Sub-32
1-1313 Sub-42 3,4-diClPh CO Single bond Sub-1
1-1314 Sub-42 3,4-diClPh CO Single bond Sub-2
1-1315 Sub-42 3,4-diClPh CO Single bond Sub-3
1-1316 Sub-42 3,4-diClPh CO Single bond Sub-4
1-1317 Sub-42 3,4-diClPh CO Single bond Sub-5
1-1318 Sub-42 3,4-diClPh CO Single bond Sub-6
1-1319 Sub-42 3,4-diClPh CO Single bond Sub-7
1-1320 Sub-42 3,4-diClPh CO Single bond Sub-8
1-1321 Sub-42 3,4-diClPh CO Single bond Sub-9
1-1322 Sub-42 3,4-diClPh CO Single bond Sub-10
1-1323 Sub-42 3,4-diClPh CO Single bond Sub-11
1-1324 Sub-42 3,4-diClPh CO Single bond Sub-12
1-1325 Sub-42 3,4-diClPh CO Single bond Sub-13
1-1326 Sub-42 3,4-diClPh CO Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1327 Sub-42 3,4-diClPh CO Single bond Sub-15
1-1328 Sub-42 3,4-diClPh CO Single bond Sub-16
1-1329 Sub-42 3,4-diClPh CO Single bond Sub-17
1-1330 Sub-42 3,4-diClPh CO Single bond Sub-18
1-1331 Sub-42 3,4-diClPh CO Single bond Sub-19
1-1332 Sub-42 3,4-diClPh CO Single bond Sub-20
1-1333 Sub-42 3,4-diClPh CO Single bond Sub-21
1-1334 Sub-42 3,4-diClPh CO Single bond Sub-22
1-1335 Sub-42 3,4-diClPh CO Single bond Sub-23
1-1336 Sub-42 3,4-diClPh CO Single bond Sub-24
1-1337 Sub-42 3,4-diClPh CO Single bond Sub-25
1-1338 Sub-42 3,4-diClPh CO Single bond Sub-26
1-1339 Sub-42 3,4-diClPh CO Single bond Sub-27
1-1340 Sub-42 3,4-diClPh CO Single bond Sub-28
1-1341 Sub-42 3,4-diClPh CO Single bond Sub-29
1-1342 Sub-42 3,4-diClPh CO Single bond Sub-30
1-1343 Sub-42 3,4-diClPh CO Single bond Sub-31
1-1344 Sub-42 3,4-diClPh CO Single bond Sub-32
1-1345 Sub-43 3,4-diClPh CO Single bond Sub-1
1-1346 Sub-43 3,4-diClPh CO Single bond Sub-2
1-1347 Sub-43 3,4-diClPh CO Single bond Sub-3
1-1348 Sub-43 3,4-diClPh CO Single bond Sub-4
1-1349 Sub-43 3,4-diClPh CO Single bond Sub-5
1-1350 Sub-43 3,4-diClPh CO Single bond Sub-6
1-1351 Sub-43 3,4-diClPh CO Single bond Sub-7
1-1352 Sub-43 3,4-diClPh CO Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1353 Sub-43 3,4-diClPh CO Single bond Sub-9
1-1354 Sub-43 3,4-diClPh CO Single bond Sub-10
1-1355 Sub-43 3,4-diClPh CO Single bond Sub-11
1-1356 Sub-43 3,4-diClPh CO Single bond Sub-12
1-1357 Sub-43 3,4-diClPh CO Single bond Sub-13
1-1358 Sub-43 3,4-diClPh CO Single bond Sub-14
1-1359 Sub-43 3,4-diClPh CO Single bond Sub-15
1-1360 Sub-43 3,4-diClPh CO Single bond Sub-16
1-1361 Sub-43 3,4-diClPh CO Single bond Sub-17
1-1362 Sub-43 3,4-diClPh CO Single bond Sub-18
1-1363 Sub-43 3,4-diClPh CO Single bond Sub-19
1-1364 Sub-43 3,4-diClPh CO Single bond Sub-20
1-1365 Sub-43 3,4-diClPh CO Single bond Sub-21
1-1366 Sub-43 3,4-diClPh CO Single bond Sub-22
1-1367 Sub-43 3,4-diClPh CO Single bond Sub-23
1-1368 Sub-43 3,4-diClPh CO Single bond Sub-24
1-1369 Sub-43 3,4-diClPh CO Single bond Sub-25
1-1370 Sub-43 3,4-diClPh CO Single bond Sub-26
1-1371 Sub-43 3,4-diClPh CO Single bond Sub-27
1-1372 Sub-43 3,4-diClPh CO Single bond Sub-28
1-1373 Sub-43 3,4-diClPh CO Single bond Sub-29
1-1374 Sub-43 3,4-diClPh CO Single bond Sub-30
1-1375 Sub-43 3,4-diClPh CO Single bond Sub-31
1-1376 Sub-43 3,4-diClPh CO Single bond Sub-32
1-1377 Sub-44 3,4-diClPh CO Single bond Sub-1
1-1378 Sub-44 3,4-diClPh CO Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1379 Sub-44 3,4-diClPh CO Single bond Sub-3
1-1380 Sub-44 3,4-diClPh CO Single bond Sub-4
1-1381 Sub-44 3,4-diClPh CO Single bond Sub-5
1-1382 Sub-44 3,4-diClPh CO Single bond Sub-6
1-1383 Sub-44 3,4-diClPh CO Single bond Sub-7
1-1384 Sub-44 3,4-diClPh CO Single bond Sub-8
1-1385 Sub-44 3,4-diClPh CO Single bond Sub-9
1-1386 Sub-44 3,4-diClPh CO Single bond Sub-10
1-1387 Sub-44 3,4-diClPh CO Single bond Sub-11
1-1388 Sub-44 3,4-diClPh CO Single bond Sub-12
1-1389 Sub-44 3,4-diClPh CO Single bond Sub-13
1-1390 Sub-44 3,4-diClPh CO Single bond Sub-14
1-1391 Sub-44 3,4-diClPh CO Single bond Sub-15
1-1392 Sub-44 3,4-diClPh CO Single bond Sub-16
1-1393 Sub-44 3,4-diClPh CO Single bond Sub-17
1-1394 Sub-44 3,4-diClPh CO Single bond Sub-18
1-1395 Sub-44 3,4-diClPh CO Single bond Sub-19
1-1396 Sub-44 3,4-diClPh CO Single bond Sub-20
1-1397 Sub-44 3,4-diClPh CO Single bond Sub-21
1-1398 Sub-44 3,4-diClPh CO Single bond Sub-22
1-1399 Sub-44 3,4-diClPh CO Single bond Sub-23
1-1400 Sub-44 3,4-diClPh CO Single bond Sub-24
1-1401 Sub-44 3,4-diClPh CO Single bond Sub-25
1-1402 Sub-44 3,4-diClPh CO Single bond Sub-26
1-1403 Sub-44 3,4-diClPh CO Single bond Sub-27
1-1404 Sub-44 3,4-diClPh CO Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1405 Sub-44 3,4-diClPh CO Single bond Sub-29
1-1406 Sub-44 3,4-diClPh CO Single bond Sub-30
1-1407 Sub-44 3,4-diClPh CO Single bond Sub-31
1-1408 Sub-44 3,4-diClPh CO Single bond Sub-32
1-1409 Sub-45 3,4-diClPh CO Single bond Sub-1
1-1410 Sub-45 3,4-diClPh CO Single bond Sub-2
1-1411 Sub-45 3,4-diClPh CO Single bond Sub-3
1-1412 Sub-45 3,4-diClPh CO Single bond Sub-4
1-1413 Sub-45 3,4-diClPh CO Single bond Sub-5
1-1414 Sub-45 3,4-diClPh CO Single bond Sub-6
1-1415 Sub-45 3,4-diClPh CO Single bond Sub-7
1-1416 Sub-45 3,4-diClPh CO Single bond Sub-8
1-1417 Sub-45 3,4-diClPh CO Single bond Sub-9
1-1418 Sub-45 3,4-diClPh CO Single bond Sub-10
1-1419 Sub-45 3,4-diClPh CO Single bond Sub-11
1-1420 Sub-45 3,4-diClPh CO Single bond Sub-12
1-1421 Sub-45 3,4-diClPh CO Single bond Sub-13
1-1422 Sub-45 3,4-diClPh CO Single bond Sub-14
1-1423 Sub-45 3,4-diClPh CO Single bond Sub-15
1-1424 Sub-45 3,4-diClPh CO Single bond Sub-16
1-1425 Sub-45 3,4-diClPh CO Single bond Sub-17
1-1426 Sub-45 3,4-diClPh CO Single bond Sub-18
1-1427 Sub-45 3,4-diClPh CO Single bond Sub-19
1-1428 Sub-45 3,4-diClPh CO Single bond Sub-20
1-1429 Sub-45 3,4-diClPh CO Single bond Sub-21
1-1430 Sub-45 3,4-diClPh CO Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1431 Sub-45 3,4-diClPh CO Single bond Sub-23
1-1432 Sub-45 3,4-diClPh CO Single bond Sub-24
1-1433 Sub-45 3,4-diClPh CO Single bond Sub-25
1-1434 Sub-45 3,4-diClPh CO Single bond Sub-26
1-1435 Sub-45 3,4-diClPh CO Single bond Sub-27
1-1436 Sub-45 3,4-diClPh CO Single bond Sub-28
1-1437 Sub-45 3,4-diClPh CO Single bond Sub-29
1-1438 Sub-45 3,4-diClPh CO Single bond Sub-30
1-1439 Sub-45 3,4-diClPh CO Single bond Sub-31
1-1440 Sub-45 3,4-diClPh CO Single bond Sub-32
1-1441 Sub-46 3,4-diClPh CO Single bond Sub-1
1-1442 Sub-46 3,4-diClPh CO Single bond Sub-2
1-1443 Sub-46 3,4-diClPh CO Single bond Sub-3
1-1444 Sub-46 3,4-diClPh CO Single bond Sub-4
1-1445 Sub-46 3,4-diClPh CO Single bond Sub-5
1-1446 Sub-46 3,4-diClPh CO Single bond Sub-6
1-1447 Sub-46 3,4-diClPh CO Single bond Sub-7
1-1448 Sub-46 3,4-diClPh CO Single bond Sub-8
1-1449 Sub-46 3,4-diClPh CO Single bond Sub-9
1-1450 Sub-46 3,4-diClPh CO Single bond Sub-10
1-1451 Sub-46 3,4-diClPh CO Single bond Sub-11
1-1452 Sub-46 3,4-diClPh CO Single bond Sub-12
1-1453 Sub-46 3,4-diClPh CO Single bond Sub-13
1-1454 Sub-46 3,4-diClPh CO Single bond Sub-14
1-1455 Sub-46 3,4-diClPh CO Single bond Sub-15
1-1456 Sub-46 3,4-diClPh CO Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1457 Sub-46 3,4-diClPh CO Single bond Sub-17
1-1458 Sub-46 3,4-diClPh CO Single bond Sub-18
1-1459 Sub-46 3,4-diClPh CO Single bond Sub-19
1-1460 Sub-46 3,4-diClPh CO Single bond Sub-20
1-1461 Sub-46 3,4-diClPh CO Single bond Sub-21
1-1462 Sub-46 3,4-diClPh CO Single bond Sub-22
1-1463 Sub-46 3,4-diClPh CO Single bond Sub-23
1-1464 Sub-46 3,4-diClPh CO Single bond Sub-24
1-1465 Sub-46 3,4-diClPh CO Single bond Sub-25
1-1466 Sub-46 3,4-diClPh CO Single bond Sub-26
1-1467 Sub-46 3,4-diClPh CO Single bond Sub-27
1-1468 Sub-46 3,4-diClPh CO Single bond Sub-28
1-1469 Sub-46 3,4-diClPh CO Single bond Sub-29
1-1470 Sub-46 3,4-diClPh CO Single bond Sub-30
1-1471 Sub-46 3,4-diClPh CO Single bond Sub-31
1-1472 Sub-46 3,4-diClPh CO Single bond Sub-32
1-1473 Sub-47 3,4-diClPh CO Single bond Sub-1
1-1474 Sub-47 3,4-diClPh CO Single bond Sub-2
1-1475 Sub-47 3,4-diClPh CO Single bond Sub-3
1-1476 Sub-47 3,4-diClPh CO Single bond Sub-4
1-1477 Sub-47 3,4-diClPh CO Single bond Sub-5
1-1478 Sub-47 3,4-diClPh CO Single bond Sub-6
1-1479 Sub-47 3,4-diClPh CO Single bond Sub-7
1-1480 Sub-47 3,4-diClPh CO Single bond Sub-8
1-1481 Sub-47 3,4-diClPh CO Single bond Sub-9
1-1482 Sub-47 3,4-diClPh CO Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1483 Sub-47 3,4-diClPh CO Single bond Sub-11
1-1484 Sub-47 3,4-diClPh CO Single bond Sub-12
1-1485 Sub-47 3,4-diClPh CO Single bond Sub-13
1-1486 Sub-47 3,4-diClPh CO Single bond Sub-14
1-1487 Sub-47 3,4-diClPh CO Single bond Sub-15
1-1488 Sub-47 3,4-diClPh CO Single bond Sub-16
1-1489 Sub-47 3,4-diClPh CO Single bond Sub-17
1-1490 Sub-47 3,4-diClPh CO Single bond Sub-18
1-1491 Sub-47 3,4-diClPh CO Single bond Sub-19
1-1492 Sub-47 3,4-diClPh CO Single bond Sub-20
1-1493 Sub-47 3,4-diClPh CO Single bond Sub-21
1-1494 Sub-47 3,4-diClPh CO Single bond Sub-22
1-1495 Sub-47 3,4-diClPh CO Single bond Sub-23
1-1496 Sub-47 3,4-diClPh CO Single bond Sub-24
1-1497 Sub-47 3,4-diClPh CO Single bond Sub-25
1-1498 Sub-47 3,4-diClPh CO Single bond Sub-26
1-1499 Sub-47 3,4-diClPh CO Single bond Sub-27
1-1500 Sub-47 3,4-diClPh CO Single bond Sub-28
1-1501 Sub-47 3,4-diClPh CO Single bond Sub-29
1-1502 Sub-47 3,4-diClPh CO Single bond Sub-30
1-1503 Sub-47 3,4-diClPh CO Single bond Sub-31
1-1504 Sub-47 3,4-diClPh CO Single bond Sub-32
1-1505 Sub-48 3,4-diClPh CO Single bond Sub-1
1-1506 Sub-48 3,4-diClPh CO Single bond Sub-2
1-1507 Sub-48 3,4-diClPh CO Single bond Sub-3
1-1508 Sub-48 3,4-diClPh CO Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1509 Sub-48 3,4-diClPh CO Single bond Sub-5
1-1510 Sub-48 3,4-diClPh CO Single bond Sub-6
1-1511 Sub-48 3,4-diClPh CO Single bond Sub-7
1-1512 Sub-48 3,4-diClPh CO Single bond Sub-8
1-1513 Sub-48 3,4-diClPh CO Single bond Sub-9
1-1514 Sub-48 3,4-diClPh CO Single bond Sub-10
1-1515 Sub-48 3,4-diClPh CO Single bond Sub-11
1-1516 Sub-48 3,4-diClPh CO Single bond Sub-12
1-1517 Sub-48 3,4-diClPh CO Single bond Sub-13
1-1518 Sub-48 3,4-diClPh CO Single bond Sub-14
1-1519 Sub-48 3,4-diClPh CO Single bond Sub-15
1-1520 Sub-48 3,4-diClPh CO Single bond Sub-16
1-1521 Sub-48 3,4-diClPh CO Single bond Sub-17
1-1522 Sub-48 3,4-diClPh CO Single bond Sub-18
1-1523 Sub-48 3,4-diClPh CO Single bond Sub-19
1-1524 Sub-48 3,4-diClPh CO Single bond Sub-20
1-1525 Sub-48 3,4-diClPh CO Single bond Sub-21
1-1526 Sub-48 3,4-diClPh CO Single bond Sub-22
1-1527 Sub-48 3,4-diClPh CO Single bond Sub-23
1-1528 Sub-48 3,4-diClPh CO Single bond Sub-24
1-1529 Sub-48 3,4-diClPh CO Single bond Sub-25
1-1530 Sub-48 3,4-diClPh CO Single bond Sub-26
1-1531 Sub-48 3,4-diClPh CO Single bond Sub-27
1-1532 Sub-48 3,4-diClPh CO Single bond Sub-28
1-1533 Sub-48 3,4-diClPh CO Single bond Sub-29
1-1534 Sub-48 3,4-diClPh CO Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1535 Sub-48 3,4-diClPh CO Single bond Sub-31
1-1536 Sub-48 3,4-diClPh CO Single bond Sub-32
1-1537 Sub-49 3,4-diClPh CO Single bond Sub-1
1-1538 Sub-49 3,4-diClPh CO Single bond Sub-2
1-1539 Sub-49 3,4-diClPh CO Single bond Sub-3
1-1540 Sub-49 3,4-diClPh CO Single bond Sub-4
1-1541 Sub-49 3,4-diClPh CO Single bond Sub-5
1-1542 Sub-49 3,4-diClPh CO Single bond Sub-6
1-1543 Sub-49 3,4-diClPh CO Single bond Sub-7
1-1544 Sub-49 3,4-diClPh CO Single bond Sub-8
1-1545 Sub-49 3,4-diClPh CO Single bond Sub-9
1-1546 Sub-49 3,4-diClPh CO Single bond Sub-10
1-1547 Sub-49 3,4-diClPh CO Single bond Sub-11
1-1548 Sub-49 3,4-diClPh CO Single bond Sub-12
1-1549 Sub-49 3,4-diClPh CO Single bond Sub-13
1-1550 Sub-49 3,4-diClPh CO Single bond Sub-14
1-1551 Sub-49 3,4-diClPh CO Single bond Sub-15
1-1552 Sub-49 3,4-diClPh CO Single bond Sub-16
1-1553 Sub-49 3,4-diClPh CO Single bond Sub-17
1-1554 Sub-49 3,4-diClPh CO Single bond Sub-18
1-1555 Sub-49 3,4-diClPh CO Single bond Sub-19
1-1556 Sub-49 3,4-diClPh CO Single bond Sub-20
1-1557 Sub-49 3,4-diClPh CO Single bond Sub-21
1-1558 Sub-49 3,4-diClPh CO Single bond Sub-22
1-1559 Sub-49 3,4-diClPh CO Single bond Sub-23
1-1560 Sub-49 3,4-diClPh CO Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1561 Sub-49 3,4-diClPh CO Single bond Sub-25
1-1562 Sub-49 3,4-diClPh CO Single bond Sub-26
1-1563 Sub-49 3,4-diClPh CO Single bond Sub-27
1-1564 Sub-49 3,4-diClPh CO Single bond Sub-28
1-1565 Sub-49 3,4-diClPh CO Single bond Sub-29
1-1566 Sub-49 3,4-diClPh CO Single bond Sub-30
1-1567 Sub-49 3,4-diClPh CO Single bond Sub-31
1-1568 Sub-49 3,4-diClPh CO Single bond Sub-32
1-1569 Sub-50 3,4-diClPh CO Single bond Sub-1
1-1570 Sub-50 3,4-diClPh CO Single bond Sub-2
1-1571 Sub-50 3,4-diClPh CO Single bond Sub-3
1-1572 Sub-50 3,4-diClPh CO Single bond Sub-4
1-1573 Sub-50 3,4-diClPh CO Single bond Sub-5
1-1574 Sub-50 3,4-diClPh CO Single bond Sub-6
1-1575 Sub-50 3,4-diClPh CO Single bond Sub-7
1-1576 Sub-50 3,4-diClPh CO Single bond Sub-8
1-1577 Sub-50 3,4-diClPh CO Single bond Sub-9
1-1578 Sub-50 3,4-diClPh CO Single bond Sub-10
1-1579 Sub-50 3,4-diClPh CO Single bond Sub-11
1-1580 Sub-50 3,4-diClPh CO Single bond Sub-12
1-1581 Sub-50 3,4-diClPh CO Single bond Sub-13
1-1582 Sub-50 3,4-diClPh CO Single bond Sub-14
1-1583 Sub-50 3,4-diClPh CO Single bond Sub-15
1-1584 Sub-50 3,4-diClPh CO Single bond Sub-16
1-1585 Sub-50 3,4-diClPh CO Single bond Sub-17
1-1586 Sub-50 3,4-diClPh CO Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1587 Sub-50 3,4-diClPh CO Single bond Sub-19
1-1588 Sub-50 3,4-diClPh CO Single bond Sub-20
1-1589 Sub-50 3,4-diClPh CO Single bond Sub-21
1-1590 Sub-50 3,4-diClPh CO Single bond Sub-22
1-1591 Sub-50 3,4-diClPh CO Single bond Sub-23
1-1592 Sub-50 3,4-diClPh CO Single bond Sub-24
1-1593 Sub-50 3,4-diClPh CO Single bond Sub-25
1-1594 Sub-50 3,4-diClPh CO Single bond Sub-26
1-1595 Sub-50 3,4-diClPh CO Single bond Sub-27
1-1596 Sub-50 3,4-diClPh CO Single bond Sub-28
1-1597 Sub-50 3,4-diClPh CO Single bond Sub-29
1-1598 Sub-50 3,4-diClPh CO Single bond Sub-30
1-1599 Sub-50 3,4-diClPh CO Single bond Sub-31
1-1600 Sub-50 3,4-diClPh CO Single bond Sub-32
1-1601 Sub-51 3,4-diClPh CO Single bond Sub-1
1-1602 Sub-51 3,4-diClPh CO Single bond Sub-2
1-1603 Sub-51 3,4-diClPh CO Single bond Sub-3
1-1604 Sub-51 3,4-diClPh CO Single bond Sub-4
1-1605 Sub-51 3,4-diClPh CO Single bond Sub-5
1-1606 Sub-51 3,4-diClPh CO Single bond Sub-6
1-1607 Sub-51 3,4-diClPh CO Single bond Sub-7
1-1608 Sub-51 3,4-diClPh CO Single bond Sub-8
1-1609 Sub-51 3,4-diClPh CO Single bond Sub-9
1-1610 Sub-51 3,4-diClPh CO Single bond Sub-10
1-1611 Sub-51 3,4-diClPh CO Single bond Sub-11
1-1612 Sub-51 3,4-diClPh CO Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1613 Sub-51 3,4-diClPh CO Single bond Sub-13
1-1614 Sub-51 3,4-diClPh CO Single bond Sub-14
1-1615 Sub-51 3,4-diClPh CO Single bond Sub-15
1-1616 Sub-51 3,4-diClPh CO Single bond Sub-16
1-1617 Sub-51 3,4-diClPh CO Single bond Sub-17
1-1618 Sub-51 3,4-diClPh CO Single bond Sub-18
1-1619 Sub-51 3,4-diClPh CO Single bond Sub-19
1-1620 Sub-51 3,4-diClPh CO Single bond Sub-20
1-1621 Sub-51 3,4-diClPh CO Single bond Sub-21
1-1622 Sub-51 3,4-diClPh CO Single bond Sub-22
1-1623 Sub-51 3,4-diClPh CO Single bond Sub-23
1-1624 Sub-51 3,4-diClPh CO Single bond Sub-24
1-1625 Sub-51 3,4-diClPh CO Single bond Sub-25
1-1626 Sub-51 3,4-diClPh CO Single bond Sub-26
1-1627 Sub-51 3,4-diClPh CO Single bond Sub-27
1-1628 Sub-51 3,4-diClPh CO Single bond Sub-28
1-1629 Sub-51 3,4-diClPh CO Single bond Sub-29
1-1630 Sub-51 3,4-diClPh CO Single bond Sub-30
1-1631 Sub-51 3,4-diClPh CO Single bond Sub-31
1-1632 Sub-51 3,4-diClPh CO Single bond Sub-32
1-1633 Sub-52 3,4-diClPh CO Single bond Sub-1
1-1634 Sub-52 3,4-diClPh CO Single bond Sub-2
1-1635 Sub-52 3,4-diClPh CO Single bond Sub-3
1-1636 Sub-52 3,4-diClPh CO Single bond Sub-4
1-1637 Sub-52 3,4-diClPh CO Single bond Sub-5
1-1638 Sub-52 3,4-diClPh CO Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1639 Sub-52 3,4-diClPh CO Single bond Sub-7
1-1640 Sub-52 3,4-diClPh CO Single bond Sub-8
1-1641 Sub-52 3,4-diClPh CO Single bond Sub-9
1-1642 Sub-52 3,4-diClPh CO Single bond Sub-10
1-1643 Sub-52 3,4-diClPh CO Single bond Sub-11
1-1644 Sub-52 3,4-diClPh CO Single bond Sub-12
1-1645 Sub-52 3,4-diClPh CO Single bond Sub-13
1-1646 Sub-52 3,4-diClPh CO Single bond Sub-14
1-1647 Sub-52 3,4-diClPh CO Single bond Sub-15
1-1648 Sub-52 3,4-diClPh CO Single bond Sub-16
1-1649 Sub-52 3,4-diClPh CO Single bond Sub-17
1-1650 Sub-52 3,4-diClPh CO Single bond Sub-18
1-1651 Sub-52 3,4-diClPh CO Single bond Sub-19
1-1652 Sub-52 3,4-diClPh CO Single bond Sub-20
1-1653 Sub-52 3,4-diClPh CO Single bond Sub-21
1-1654 Sub-52 3,4-diClPh CO Single bond Sub-22
1-1655 Sub-52 3,4-diClPh CO Single bond Sub-23
1-1656 Sub-52 3,4-diClPh CO Single bond Sub-24
1-1657 Sub-52 3,4-diClPh CO Single bond Sub-25
1-1658 Sub-52 3,4-diClPh CO Single bond Sub-26
1-1659 Sub-52 3,4-diClPh CO Single bond Sub-27
1-1660 Sub-52 3,4-diClPh CO Single bond Sub-28
1-1661 Sub-52 3,4-diClPh CO Single bond Sub-29
1-1662 Sub-52 3,4-diClPh CO Single bond Sub-30
1-1663 Sub-52 3,4-diClPh CO Single bond Sub-31
1-1664 Sub-52 3,4-diClPh CO Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1665 Sub-53 3,4-diClPh CO Single bond Sub-1
1-1666 Sub-53 3,4-diClPh CO Single bond Sub-2
1-1667 Sub-53 3,4-diClPh CO Single bond Sub-3
1-1668 Sub-53 3,4-diClPh CO Single bond Sub-4
1-1669 Sub-53 3,4-diClPh CO Single bond Sub-5
1-1670 Sub-53 3,4-diClPh CO Single bond Sub-6
1-1671 Sub-53 3,4-diClPh CO Single bond Sub-7
1-1672 Sub-53 3,4-diClPh CO Single bond Sub-8
1-1673 Sub-53 3,4-diClPh CO Single bond Sub-9
1-1674 Sub-53 3,4-diClPh CO Single bond Sub-10
1-1675 Sub-53 3,4-diClPh CO Single bond Sub-11
1-1676 Sub-53 3,4-diClPh CO Single bond Sub-12
1-1677 Sub-53 3,4-diClPh CO Single bond Sub-13
1-1678 Sub-53 3,4-diClPh CO Single bond Sub-14
1-1679 Sub-53 3,4-diClPh CO Single bond Sub-15
1-1680 Sub-53 3,4-diClPh CO Single bond Sub-16
1-1681 Sub-53 3,4-diClPh CO Single bond Sub-17
1-1682 Sub-53 3,4-diClPh CO Single bond Sub-18
1-1683 Sub-53 3,4-diClPh CO Single bond Sub-19
1-1684 Sub-53 3,4-diClPh CO Single bond Sub-20
1-1685 Sub-53 3,4-diClPh CO Single bond Sub-21
1-1686 Sub-53 3,4-diClPh CO Single bond Sub-22
1-1687 Sub-53 3,4-diClPh CO Single bond Sub-23
1-1688 Sub-53 3,4-diClPh CO Single bond Sub-24
1-1689 Sub-53 3,4-diClPh CO Single bond Sub-25
1-1690 Sub-53 3,4-diClPh CO Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1691 Sub-53 3,4-diClPh CO Single bond Sub-27
1-1692 Sub-53 3,4-diClPh CO Single bond Sub-28
1-1693 Sub-53 3,4-diClPh CO Single bond Sub-29
1-1694 Sub-53 3,4-diClPh CO Single bond Sub-30
1-1695 Sub-53 3,4-diClPh CO Single bond Sub-31
1-1696 Sub-53 3,4-diClPh CO Single bond Sub-32
1-1697 Sub-54 3,4-diClPh CO Single bond Sub-1
1-1698 Sub-54 3,4-diClPh CO Single bond Sub-2
1-1699 Sub-54 3,4-diClPh CO Single bond Sub-3
1-1700 Sub-54 3,4-diClPh CO Single bond Sub-4
1-1701 Sub-54 3,4-diClPh CO Single bond Sub-5
1-1702 Sub-54 3,4-diClPh CO Single bond Sub-6
1-1703 Sub-54 3,4-diClPh CO Single bond Sub-7
1-1704 Sub-54 3,4-diClPh CO Single bond Sub-8
1-1705 Sub-54 3,4-diClPh CO Single bond Sub-9
1-1706 Sub-54 3,4-diClPh CO Single bond Sub-10
1-1707 Sub-54 3,4-diClPh CO Single bond Sub-11
1-1708 Sub-54 3,4-diClPh CO Single bond Sub-12
1-1709 Sub-54 3,4-diClPh CO Single bond Sub-13
1-1710 Sub-54 3,4-diClPh CO Single bond Sub-14
1-1711 Sub-54 3,4-diClPh CO Single bond Sub-15
1-1712 Sub-54 3,4-diClPh CO Single bond Sub-16
1-1713 Sub-54 3,4-diClPh CO Single bond Sub-17
1-1714 Sub-54 3,4-diClPh CO Single bond Sub-18
1-1715 Sub-54 3,4-diClPh CO Single bond Sub-19
1-1716 Sub-54 3,4-diClPh CO Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1717 Sub-54 3,4-diClPh CO Single bond Sub-21
1-1718 Sub-54 3,4-diClPh CO Single bond Sub-22
1-1719 Sub-54 3,4-diClPh CO Single bond Sub-23
1-1720 Sub-54 3,4-diClPh CO Single bond Sub-24
1-1721 Sub-54 3,4-diClPh CO Single bond Sub-25
1-1722 Sub-54 3,4-diClPh CO Single bond Sub-26
1-1723 Sub-54 3,4-diClPh CO Single bond Sub-27
1-1724 Sub-54 3,4-diClPh CO Single bond Sub-28
1-1725 Sub-54 3,4-diClPh CO Single bond Sub-29
1-1726 Sub-54 3,4-diClPh CO Single bond Sub-30
1-1727 Sub-54 3,4-diClPh CO Single bond Sub-31
1-1728 Sub-54 3,4-diClPh CO Single bond Sub-32
1-1729 Sub-55 3,4-diClPh CO Single bond Sub-1
1-1730 Sub-55 3,4-diClPh CO Single bond Sub-2
1-1731 Sub-55 3,4-diClPh CO Single bond Sub-3
1-1732 Sub-55 3,4-diClPh CO Single bond Sub-4
1-1733 Sub-55 3,4-diClPh CO Single bond Sub-5
1-1734 Sub-55 3,4-diClPh CO Single bond Sub-6
1-1735 Sub-55 3,4-diClPh CO Single bond Sub-7
1-1736 Sub-55 3,4-diClPh CO Single bond Sub-8
1-1737 Sub-55 3,4-diClPh CO Single bond Sub-9
1-1738 Sub-55 3,4-diClPh CO Single bond Sub-10
1-1739 Sub-55 3,4-diClPh CO Single bond Sub-11
1-1740 Sub-55 3,4-diClPh CO Single bond Sub-12
1-1741 Sub-55 3,4-diClPh CO Single bond Sub-13
1-1742 Sub-55 3,4-diClPh CO Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1743 Sub-55 3,4-diClPh CO Single bond Sub-15
1-1744 Sub-55 3,4-diClPh CO Single bond Sub-16
1-1745 Sub-55 3,4-diClPh CO Single bond Sub-17
1-1746 Sub-55 3,4-diClPh CO Single bond Sub-18
1-1747 Sub-55 3,4-diClPh CO Single bond Sub-19
1-1748 Sub-55 3,4-diClPh CO Single bond Sub-20
1-1749 Sub-55 3,4-diClPh CO Single bond Sub-21
1-1750 Sub-55 3,4-diClPh CO Single bond Sub-22
1-1751 Sub-55 3,4-diClPh CO Single bond Sub-23
1-1752 Sub-55 3,4-diClPh CO Single bond Sub-24
1-1753 Sub-55 3,4-diClPh CO Single bond Sub-25
1-1754 Sub-55 3,4-diClPh CO Single bond Sub-26
1-1755 Sub-55 3,4-diClPh CO Single bond Sub-27
1-1756 Sub-55 3,4-diClPh CO Single bond Sub-28
1-1757 Sub-55 3,4-diClPh CO Single bond Sub-29
1-1758 Sub-55 3,4-diClPh CO Single bond Sub-30
1-1759 Sub-55 3,4-diClPh CO Single bond Sub-31
1-1760 Sub-55 3,4-diClPh CO Single bond Sub-32
1-1761 Sub-56 3,4-diClPh CO Single bond Sub-1
1-1762 Sub-56 3,4-diClPh CO Single bond Sub-2
1-1763 Sub-56 3,4-diClPh CO Single bond Sub-3
1-1764 Sub-56 3,4-diClPh CO Single bond Sub-4
1-1765 Sub-56 3,4-diClPh CO Single bond Sub-5
1-1766 Sub-56 3,4-diClPh CO Single bond Sub-6
1-1767 Sub-56 3,4-diClPh CO Single bond Sub-7
1-1768 Sub-56 3,4-diClPh CO Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1769 Sub-56 3,4-diClPh CO Single bond Sub-9
1-1770 Sub-56 3,4-diClPh CO Single bond Sub-10
1-1771 Sub-56 3,4-diClPh CO Single bond Sub-11
1-1772 Sub-56 3,4-diClPh CO Single bond Sub-12
1-1773 Sub-56 3,4-diClPh CO Single bond Sub-13
1-1774 Sub-56 3,4-diClPh CO Single bond Sub-14
1-1775 Sub-56 3,4-diClPh CO Single bond Sub-15
1-1776 Sub-56 3,4-diClPh CO Single bond Sub-16
1-1777 Sub-56 3,4-diClPh CO Single bond Sub-17
1-1778 Sub-56 3,4-diClPh CO Single bond Sub-18
1-1779 Sub-56 3,4-diClPh CO Single bond Sub-19
1-1780 Sub-56 3,4-diClPh CO Single bond Sub-20
1-1781 Sub-56 3,4-diClPh CO Single bond Sub-21
1-1782 Sub-56 3,4-diClPh CO Single bond Sub-22
1-1783 Sub-56 3,4-diClPh CO Single bond Sub-23
1-1784 Sub-56 3,4-diClPh CO Single bond Sub-24
1-1785 Sub-56 3,4-diClPh CO Single bond Sub-25
1-1786 Sub-56 3,4-diClPh CO Single bond Sub-26
1-1787 Sub-56 3,4-diClPh CO Single bond Sub-27
1-1788 Sub-56 3,4-diClPh CO Single bond Sub-28
1-1789 Sub-56 3,4-diClPh CO Single bond Sub-29
1-1790 Sub-56 3,4-diClPh CO Single bond Sub-30
1-1791 Sub-56 3,4-diClPh CO Single bond Sub-31
1-1792 Sub-56 3,4-diClPh CO Single bond Sub-32
1-1793 Sub-57 3,4-diClPh CO Single bond Sub-1
1-1794 Sub-57 3,4-diClPh CO Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1795 Sub-57 3,4-diClPh CO Single bond Sub-3
1-1796 Sub-57 3,4-diClPh CO Single bond Sub-4
1-1797 Sub-57 3,4-diClPh CO Single bond Sub-5
1-1798 Sub-57 3,4-diClPh CO Single bond Sub-6
1-1799 Sub-57 3,4-diClPh CO Single bond Sub-7
1-1800 Sub-57 3,4-diClPh CO Single bond Sub-8
1-1801 Sub-57 3,4-diClPh CO Single bond Sub-9
1-1802 Sub-57 3,4-diClPh CO Single bond Sub-10
1-1803 Sub-57 3,4-diClPh CO Single bond Sub-11
1-1804 Sub-57 3,4-diClPh CO Single bond Sub-12
1-1805 Sub-57 3,4-diClPh CO Single bond Sub-13
1-1806 Sub-57 3,4-diClPh CO Single bond Sub-14
1-1807 Sub-57 3,4-diClPh CO Single bond Sub-15
1-1808 Sub-57 3,4-diClPh CO Single bond Sub-16
1-1809 Sub-57 3,4-diClPh CO Single bond Sub-17
1-1810 Sub-57 3,4-diClPh CO Single bond Sub-18
1-1811 Sub-57 3,4-diClPh CO Single bond Sub-19
1-1812 Sub-57 3,4-diClPh CO Single bond Sub-20
1-1813 Sub-57 3,4-diClPh CO Single bond Sub-21
1-1814 Sub-57 3,4-diClPh CO Single bond Sub-22
1-1815 Sub-57 3,4-diClPh CO Single bond Sub-23
1-1816 Sub-57 3,4-diClPh CO Single bond Sub-24
1-1817 Sub-57 3,4-diClPh CO Single bond Sub-25
1-1818 Sub-57 3,4-diClPh CO Single bond Sub-26
1-1819 Sub-57 3,4-diClPh CO Single bond Sub-27
1-1820 Sub-57 3,4-diClPh CO Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1821 Sub-57 3,4-diClPh CO Single bond Sub-29
1-1822 Sub-57 3,4-diClPh CO Single bond Sub-30
1-1 823 Sub-57 3,4-diClPh CO Single bond Sub-31
1-1824 Sub-57 3,4-diClPh CO Single bond Sub-32
1-1825 Sub-58 3,4-diClPh CO Single bond Sub-1
1-1826 Sub-58 3,4-diClPh CO Single bond Sub-2
1-1827 Sub-58 3,4-diClPh CO Single bond Sub-3
1-1828 Sub-58 3,4-diClPh CO Single bond Sub-4
1-1829 Sub-58 3,4-diClPh CO Single bond Sub-5
1-1830 Sub-58 3,4-diClPh CO Single bond Sub-6
1-1831 Sub-58 3,4-diClPh CO Single bond Sub-7
1-1832 Sub-58 3,4-diClPh CO Single bond Sub-8
1-1833 Sub-58 3,4-diClPh CO Single bond Sub-9
1-1834 Sub-58 3,4-diClPh CO Single bond Sub-10
1-1835 Sub-58 3,4-diClPh CO Single bond Sub-11
1-1836 Sub-58 3,4-diClPh CO Single bond Sub-12
1-1837 Sub-58 3,4-diClPh CO Single bond Sub-13
1-1838 Sub-58 3,4-diClPh CO Single bond Sub-14
1-1839 Sub-58 3,4-diClPh CO Single bond Sub-15
1-1840 Sub-58 3,4-diClPh CO Single bond Sub-16
1-1841 Sub-58 3,4-diClPh CO Single bond Sub-17
1-1842 Sub-58 3,4-diClPh CO Single bond Sub-18
1-1843 Sub-58 3,4-diClPh CO Single bond Sub-19
1-1844 Sub-58 3,4-diClPh CO Single bond Sub-20
1-1845 Sub-58 3,4-diClPh CO Single bond Sub-21
1-1846 Sub-58 3,4-diClPh CO Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1847 Sub-58 3,4-diClPh CO Single bond Sub-23
1-1848 Sub-58 3,4-diClPh CO Single bond Sub-24
1-1849 Sub-58 3,4-diClPh CO Single bond Sub-25
1-1850 Sub-58 3,4-diClPh CO Single bond Sub-26
1-1851 Sub-58 3,4-diClPh CO Single bond Sub-27
1-1852 Sub-58 3,4-diClPh CO Single bond Sub-28
1-1853 Sub-58 3,4-diClPh CO Single bond Sub-29
1-1854 Sub-58 3,4-diClPh CO Single bond Sub-30
1-1855 Sub-58 3,4-diClPh CO Single bond Sub-31
1-1856 Sub-58 3,4-diClPh CO Single bond Sub-32
1-1857 Sub-59 3,4-diClPh CO Single bond Sub-1
1-1858 Sub-59 3,4-diClPh CO Single bond Sub-2
1-1859 Sub-59 3,4-diClPh CO Single bond Sub-3
1-1860 Sub-59 3,4-diClPh CO Single bond Sub-4
1-1861 Sub-59 3,4-diClPh CO Single bond Sub-5
1-1862 Sub-59 3,4-diClPh CO Single bond Sub-6
1-1863 Sub-59 3,4-diClPh CO Single bond Sub-7
1-1864 Sub-59 3,4-diClPh CO Single bond Sub-8
1-1865 Sub-59 3,4-diClPh CO Single bond Sub-9
1-1866 Sub-59 3,4-diClPh CO Single bond Sub-10
1-1867 Sub-59 3,4-diClPh CO Single bond Sub-11
1-1868 Sub-59 3,4-diClPh CO Single bond Sub-12
1-1869 Sub-59 3,4-diClPh CO Single bond Sub-13
1-1870 Sub-59 3,4-diClPh CO Single bond Sub-14
1-1871 Sub-59 3,4-diClPh CO Single bond Sub-15
1-1872 Sub-59 3,4-diClPh CO Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1873 Sub-59 3,4-diClPh CO Single bond Sub-17
1-1874 Sub-59 3,4-diClPh CO Single bond Sub-18
1-1875 Sub-59 3,4-diClPh CO Single bond Sub-19
1-1876 Sub-59 3,4-diClPh CO Single bond Sub-20
1-1877 Sub-59 3,4-diClPh CO Single bond Sub-21
1-1878 Sub-59 3,4-diClPh CO Single bond Sub-22
1-1879 Sub-59 3,4-diClPh CO Single bond Sub-23
1-1880 Sub-59 3,4-diClPh CO Single bond Sub-24
1-1881 Sub-59 3,4-diClPh CO Single bond Sub-25
1-1882 Sub-59 3,4-diClPh CO Single bond Sub-26
1-1883 Sub-59 3,4-diClPh CO Single bond Sub-27
1-1884 Sub-59 3,4-diClPh CO Single bond Sub-28
1-1885 Sub-59 3,4-diClPh CO Single bond Sub-29
1-1886 Sub-59 3,4-diClPh CO Single bond Sub-30
1-1887 Sub-59 3,4-diClPh CO Single bond Sub-31
1-1888 Sub-59 3,4-diClPh CO Single bond Sub-32
1-1889 Sub-60 3,4-diClPh CO Single bond Sub-1
1-1890 Sub-60 3,4-diClPh CO Single bond Sub-2
1-1891 Sub-60 3,4-diClPh CO Single bond Sub-3
1-1892 Sub-60 3,4-diClPh CO Single bond Sub-4
1-1893 Sub-60 3,4-diClPh CO Single bond Sub-5
1-1894 Sub-60 3,4-diClPh CO Single bond Sub-6
1-1895 Sub-60 3,4-diClPh CO Single bond Sub-7
1-1896 Sub-60 3,4-diClPh CO Single bond Sub-8
1-1897 Sub-60 3,4-diClPh CO Single bond Sub-9
1-1898 Sub-60 3,4-diClPh CO Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1899 Sub-60 3,4-diClPh CO Single bond Sub-11
1-1900 Sub-60 3,4-diClPh CO Single bond Sub-12
1-1901 Sub-60 3,4-diClPh CO Single bond Sub-13
1-1902 Sub-60 3,4-diClPh CO Single bond Sub-14
1-1903 Sub-60 3,4-diClPh CO Single bond Sub-15
1-1904 Sub-60 3,4-diClPh CO Single bond Sub-16
1-1905 Sub-60 3,4-diClPh CO Single bond Sub-17
1-1906 Sub-60 3,4-diClPh CO Single bond Sub-18
1-1907 Sub-60 3,4-diClPh CO Single bond Sub-19
1-1908 Sub-60 3,4-diClPh CO Single bond Sub-20
1-1909 Sub-60 3,4-diClPh CO Single bond Sub-21
1-1910 Sub-60 3,4-diClPh CO Single bond Sub-22
1-1911 Sub-60 3,4-diClPh CO Single bond Sub-23
1-1912 Sub-60 3,4-diClPh CO Single bond Sub-24
1-1913 Sub-60 3,4-diClPh CO Single bond Sub-25
1-1914 Sub-60 3,4-diClPh CO Single bond Sub-26
1-1915 Sub-60 3,4-diClPh CO Single bond Sub-27
1-1916 Sub-60 3,4-diClPh CO Single bond Sub-28
1-1917 Sub-60 3,4-diClPh CO Single bond Sub-29
1-1918 Sub-60 3,4-diClPh CO Single bond Sub-30
1-1919 Sub-60 3,4-diClPh CO Single bond Sub-31
1-1920 Sub-60 3,4-dtClPh CO Single bond Sub-32
1-1921 Sub-61 3,4-diClPh CO Single bond Sub-1
1-1922 Sub-61 3,4-diClPh CO Single bond Sub-2
1-1923 Sub-61 3,4-diClPh CO Single bond Sub-3
1-1924 Sub-61 3,4-diClPh CO Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1925 Sub-61 3,4-diClPh CO Single bond Sub-5
1-1926 Sub-61 3,4-diClPh CO Single bond Sub-6
1-1927 Sub-61 3,4-diClPh CO Single bond Sub-7
1-1928 Sub-61 3,4-diClPh CO Single bond Sub-8
1-1929 Sub-61 3,4-diClPh CO Single bond Sub-9
1-1930 Sub-61 3,4-diClPh CO Single bond Sub-10
1-1931 Sub-61 3,4-diClPh CO Single bond Sub-11
1-1932 Sub-61 3,4-diClPh CO Single bond Sub-12
1-1933 Sub-61 3,4-diClPh CO Single bond Sub-13
1-1934 Sub-61 3,4-diClPh CO Single bond Sub-14
1-1935 Sub-61 3,4-diClPh CO Single bond Sub-15
1-1936 Sub-61 3,4-diClPh CO Single bond Sub-16
1-1937 Sub-61 3,4-diClPh CO Single bond Sub-17
1-1938 Sub-61 3,4-diClPh CO Single bond Sub-18
1-1939 Sub-61 3,4-diClPh CO Single bond Sub-19
1-1940 Sub-61 3,4-diClPh CO Single bond Sub-20
1-1941 Sub-61 3,4-diClPh CO Single bond Sub-21
1-1942 Sub-61 3,4-diClPh CO Single bond Sub-22
1-1943 Sub-61 3,4-diClPh CO Single bond Sub-23
1-1944 Sub-61 3,4-diClPh CO Single bond Sub-24
1-1945 Sub-61 3,4-diClPh CO Single bond Sub-25
1-1946 Sub-61 3,4-diClPh CO Single bond Sub-26
1-1947 Sub-61 3,4-diClPh CO Single bond Sub-27
1-1948 Sub-61 3,4-diClPh CO Single bond Sub-28
1-1949 Sub-61 3,4-diClPh CO Single bond Sub-29
1-1950 Sub-61 3,4-diClPh CO Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1951 Sub-61 3,4-diClPh CO Single bond Sub-31
1-1952 Sub-61 3,4-diClPh CO Single bond Sub-32
1-1953 Sub-62 3,4-diClPh CO Single bond Sub-1
1-1954 Sub-62 3,4-diClPh CO Single bond Sub-2
1-1955 Sub-62 3,4-diClPh CO Single bond Sub-3
1-1956 Sub-62 3,4-diClPh CO Single bond Sub-4
1-1957 Sub-62 3,4-diClPh CO Single bond Sub-5
1-1958 Sub-62 3,4-diClPh CO Single bond Sub-6
1-1959 Sub-62 3,4-diClPh CO Single bond Sub-7
1-1960 Sub-62 3,4-diClPh CO Single bond Sub-8
1-1961 Sub-62 3,4-diClPh CO Single bond Sub-9
1-1962 Sub-62 3,4-diClPh CO Single bond Sub-10
1-1963 Sub-62 3,4-diClPh CO Single bond Sub-11
1-1964 Sub-62 3,4-diClPh CO Single bond Sub-12
1-1965 Sub-62 3,4-diClPh CO Single bond Sub-13
1-1966 Sub-62 3,4-diClPh CO Single bond Sub-14
1-1967 Sub-62 3,4-diClPh CO Single bond Sub-15
1-1968 Sub-62 3,4-diClPh CO Single bond Sub-16
1-1969 Sub-62 3,4-diClPh CO Single bond Sub-17
1-1970 Sub-62 3,4-diClPh CO Single bond Sub-18
1-1971 Sub-62 3,4-diClPh CO Single bond Sub-19
1-1972 Sub-62 3,4-diClPh CO Single bond Sub-20
1-1973 Sub-62 3,4-diClPh CO Single bond Sub-21
1-1974 Sub-62 3,4-diClPh CO Single bond Sub-22
1-1975 Sub-62 3,4-diClPh CO Single bond Sub-23
1-1976 Sub-62 3,4-diClPh CO Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-1977 Sub-62 3,4-diClPh CO Single bond Sub-25
1-1978 Sub-62 3,4-diClPh CO Single bond Sub-26
1-1979 Sub-62 3,4-diClPh CO Single bond Sub-27
1-1980 Sub-62 3,4-diClPh CO Single bond Sub-28
1-1981 Sub-62 3,4-diClPh CO Single bond Sub-29
1-1982 Sub-62 3,4-diClPh CO Single bond Sub-30
1-1983 Sub-62 3,4-diClPh CO Single bond Sub-31
1-1984 Sub-62 3,4-diClPh CO Single bond Sub-32
1-1985 Sub-63 3,4-diClPh CO Single bond Sub-1
1-1986 Sub-63 3,4-diClPh CO Single bond Sub-2
1-1987 Sub-63 3,4-diClPh CO Single bond Sub-3
1-1988 Sub-63 3,4-diClPh CO Single bond Sub-4
1-1989 Sub-63 3,4-diClPh CO Single bond Sub-5
1-1990 Sub-63 3,4-diClPh CO Single bond Sub-6
1-1991 Sub-63 3,4-diClPh CO Single bond Sub-7
1-1992 Sub-63 3,4-diClPh CO Single bond Sub-8
1-1993 Sub-63 3,4-diClPh CO Single bond Sub-9
1-1994 Sub-63 3,4-diClPh CO Single bond Sub-10
1-1995 Sub-63 3,4-diClPh CO Single bond Sub-11
1-1996 Sub-63 3,4-diclPh CO Single bond Sub-12
1-1997 Sub-63 3,4-diClPh CO Single bond Sub-13
1-1998 Sub-63 3,4-diClPh CO Single bond Sub-14
1-1999 Sub-63 3,4-diClPh CO Single bond Sub-15
1-2000 Sub-63 3,4-diClPh CO Single bond Sub-16
1-2001 Sub-63 3,4-diClPh CO Single bond Sub-17
1-2002 Sub-63 3,4-diClPh CO Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2003 Sub-63 3,4-diClPh CO Single bond Sub-19
1-2004 Sub-63 3,4-diClPh CO Single bond Sub-20
1-2005 Sub-63 3,4-diClPh CO Single bond Sub-21
1-2006 Sub-63 3,4-diClPh CO Single bond Sub-22
1-2007 Sub-63 3,4-diClPh CO Single bond Sub-23
1-2008 Sub-63 3,4-diClPh CO Single bond Sub-24
1-2009 Sub-63 3,4-diClPh CO Single bond Sub-25
1-2010 Sub-63 3,4-diClPh CO Single bond Sub-26
1-2011 Sub-63 3,4-diClPh CO Single bond Sub-27
1-2012 Sub-63 3,4-diClPh CO Single bond Sub-28
1-2013 Sub-63 3,4-diClPh CO Single bond Sub-29
1-2014 Sub-63 3,4-diClPh CO Single bond Sub-30
1-2015 Sub-63 3,4-diClPh CO Single bond Sub-31
1-2016 Sub-63 3,4-diClPh CO Single bond Sub-32
1-2017 Sub-64 3,4-diClPh CO Single bond Sub-1
1-2018 Sub-64 3,4-diClPh CO Single bond Sub-2
1-2019 Sub-64 3,4-diClPh CO Single bond Sub-3
1-2020 Sub-64 3,4-diClPh CO Single bond Sub-4
1-2021 Sub-64 3,4-diClPh CO Single bond Sub-5
1-2022 Sub-64 3,4-diClPh CO Single bond Sub-6
1-2023 Sub-64 3,4-diClPh CO Single bond Sub-7
1-2024 Sub-64 3,4-diClPh CO Single bond Sub-8
1-2025 Sub-64 3,4-diClPh CO Single bond Sub-9
1-2026 Sub-64 3,4-diClPh CO Single bond Sub-10
1-2027 Sub-64 3,4-diClPh CO Single bond Sub-11
1-2028 Sub-64 3,4-diClPh CO Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2029 Sub-64 3,4-diClPh CO Single bond Sub-13
1-2030 Sub-64 3,4-diClPh CO Single bond Sub-14
1-2031 Sub-64 3,4-diClPh CO Single bond Sub-15
1-2032 Sub-64 3,4-diClPh CO Single bond Sub-16
1-2033 Sub-64 3,4-diClPh CO Single bond Sub-17
1-2034 Sub-64 3,4-diClPh CO Single bond Sub-18
1-2035 Sub-64 3,4-diClPh CO Single bond Sub-19
1-2036 Sub-64 3,4-diClPh CO Single bond Sub-20
1-2037 Sub-64 3,4-diClPh CO Single bond Sub-21
1-2038 Sub-64 3,4-diClPh CO Single bond Sub-22
1-2039 Sub-64 3,4-diClPh CO Single bond Sub-23
1-2040 Sub-64 3,4-diClPh CO Single bond Sub-24
1-2041 Sub-64 3,4-diClPh CO Single bond Sub-25
1-2042 Sub-64 3,4-diClPh CO Single bond Sub-26
1-2043 Sub-64 3,4-diClPh CO Single bond Sub-27
1-2044 Sub-64 3,4-diClPh CO Single bond Sub-28
1-2045 Sub-64 3,4-diClPh CO Single bond Sub-29
1-2046 Sub-64 3,4-diClPh CO Single bond Sub-30
1-2047 Sub-64 3,4-diClPh CO Single bond Sub-31
1-2048 Sub-64 3,4-diClPh CO Single bond Sub-32
1-2049 Sub-33 3,4-diClPh SO2 Single bond Sub-1
1-2050 Sub-33 3,4-diClPh SO2 Single bond Sub-2
1-2051 Sub-33 3,4-diClPh SO2 Single bond Sub-3
1-2052 Sub-33 3,4-diClPh SO2 Single bond Sub-4
1-2053 Sub-33 3,4-diClPh SO2 Single bond Sub-5
1-2054 Sub-33 3,4-diClPh SO2 Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2055 Sub-33 3,4-diClPh SO2 Single bond Sub-7
1-2056 Sub-33 3,4-diClPh SO2 Single bond Sub-8
1-2057 Sub-33 3,4-diClPh SO2 Single bond Sub-9
1-2058 Sub-33 3,4-diClPh SO2 Single bond Sub-10
1-2059 Sub-33 3,4-diClPh SO2 Single bond Sub-11
1-2060 Sub-33 3,4-diClPh SO2 Single bond Sub-12
1-2061 Sub-33 3,4-diClPh SO2 Single bond Sub-13
1-2062 Sub-33 3,4-diClPh SO2 Single bond Sub-14
1-2063 Sub-33 3,4-diClPh SO2 Single bond Sub-15
1-2064 Sub-33 3,4-diClPh SO2 Single bond Sub-16
1-2065 Sub-33 3,4-diClPh S02 Single bond Sub-17
1-2066 Sub-33 3,4-diClPh SO2 Single bond Sub-18
1-2067 Sub-33 3,4-diClPh SO2 Single bond Sub-19
1-2068 Sub-33 3,4-diClPh SO2 Single bond Sub-20
1-2069 Sub-33 3,4-diClPh SO2 Single bond Sub-21
1-2070 Sub-33 3,4-diClPh SO2 Single bond Sub-22
1-2071 Sub-33 3,4-diClPh SO2 Single bond Sub-23
1-2072 Sub-33 3,4-diClPh SO2 Single bond Sub-24
1-2073 Sub-33 3,4-diClPh SO2 Single bond Sub-25
1-2074 Sub-33 3,4-diClPh SO2 Single bond Sub-26
1-2075 Sub-33 3,4-diClPh SO2 Single bond Sub-27
1-2076 Sub-33 3,4-diClPh SO2 Single bond Sub-28
1-2077 Sub-33 3,4-diClPh SO2 Single bond Sub-29
1-2078 Sub-33 3,4-diClPh SO2 Single bond Sub-30
1-2079 Sub-33 3,4-diClPh SO2 Single bond Sub-31
1-2080 Sub-33 3,4-diClPh SO2 Single bond Sub-32
Table 1(cont.)
Number of Compounds R1 R2 A B Z
1-2081 Sub-34 3,4-diClPh SO2 Single bond Sub-1
1-2082 Sub-34 3,4-diClPh SO2 Single bond Sub-2
1-2083 Sub-34 3,4-diClPh SO2 Single bond Sub-3
1-2084 Sub-34 3,4-diClPh SO2 Single bond Sub-4
1-2085 Sub-34 3,4-diClPh SO2 Single bond Sub-5
1-2086 Sub-34 3,4-diClPh SO2 Single bond Sub-6
1-2087 Sub-34 3,4-diClPh SO2 Single bond Sub-7
1-2088 Sub-34 3,4-diClPh SO2 Single bond Sub-8
1-2089 Sub-34 3,4-diClPh SO2 Single bond Sub-9
1-2090 Sub-34 3,4-diClPh SO2 Single bond Sub-10
1-2091 Sub-34 3,4-diClPh SO2 Single bond Sub-11
1-2092 Sub-34 3,4-diClPh SO2 Single bond Sub-12
1-2093 Sub-34 3,4-diClPh SO2 Single bond Sub-13
1-2094 Sub-34 3,4-diClPh SO2 Single bond Sub-14
1-2095 Sub-34 3,4-diClPh SO2 Single bond Sub-15
1-2096 Sub-34 3,4-diClPh SO2 Single bond Sub-16
1-2097 Sub-34 3,4-diClPh SO2 Single bond Sub-17
1-2098 Sub-34 3,4-diClPh SO2 Single bond Sub-18
1-2099 Sub-34 3,4-diClPh SO2 Single bond Sub-19
1-2100 Sub-34 3,4-diClPh SO2 Single bond Sub-20
1-2101 Sub-34 3,4-diClPh SO2 Single bond Sub-21
1-2102 Sub-34 3,4-diClPh SO2 Single bond Sub-22
1-2103 Sub-34 3,4-diClPh SO2 Single bond Sub-23
1-2104 Sub-34 3,4-diClPh SO2 Single bond Sub-24
1-2105 Sub-34 3,4-diClPh SO2 Single bond Sub-25
1-2106 Sub-34 3,4-diClPh SO2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2107 Sub-34 3,4-diClPh SO2 Single bond Sub-27
1-2108 Sub-34 3,4-diClPh SO2 Single bond Sub-28
1-2109 Sub-34 3,4-diClPh SO2 Single bond Sub-29
1-2110 Sub-34 3,4-diClPh SO2 Single bond Sub-30
1-2111 Sub-34 3,4-diClPh SO2 Single bond Sub-31
1-2112 Sub-34 3,4-diClPh SO2 Single bond Sub-32
1-2113 Sub-35 3,4-diClPh SO2 Single bond Sub-1
1-2114 Sub-35 3,4-diClPh SO2 Single bond Sub-2
1-2115 Sub-35 3,4-diClPh SO2 Single bond Sub-3
1-2116 Sub-35 3,4-diClPh SO2 Single bond Sub-4
1-2117 Sub-35 3,4-diClPh SO2 Single bond Sub-5
1-2118 Sub-35 3,4-diClPh SO2 Single bond Sub-6
1-2119 Sub-35 3,4-diClPh SO2 Single bond Sub-7
1-2120 Sub-35 3,4-diClPh SO2 Single bond Sub-8
1-2121 Sub-35 3,4-diClPh SO2 Single bond Sub-9
1-2122 Sub-35 3,4-diClPh SO2 Single bond Sub-10
1-2123 Sub-35 3,4-diClPh SO2 Single bond Sub-11
1-2124 Sub-35 3,4-diClPh SO2 Single bond Sub-12
1-2125 Sub-35 3,4-diClPh SO2 Single bond Sub-13
1-2126 Sub-35 3,4-diClPh SO2 Single bond Sub-14
1-2127 Sub-35 3,4-diClPh SO2 Single bond Sub-15
1-2128 Sub-35 3,4-diClPh SO2 Single bond Sub-16
1-2129 Sub-35 3,4-diClPh SO2 Single bond Sub-17
1-2130 Sub-35 3,4-diClPh SO2 Single bond Sub-18
1-2131 Sub-35 3,4-diClPh SO2 Single bond Sub-19
1-2132 Sub-35 3,4-diClPh SO2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2133 Sub-35 3,4-diClPh SO2 Single bond Sub-21
1-2134 Sub-35 3,4-diClPh SO2 Single bond Sub-22
1-2135 Sub-35 3,4-diClPh SO2 Single bond Sub-23
1-2136 Sub-35 3,4-diClPh SO2 Single bond Sub-24
1-2137 Sub-35 3,4-diClPh SO2 Single bond Sub-25
1-2138 Sub-35 3,4-diClPh SO2 Single bond Sub-26
1-2139 Sub-35 3,4-diClPh SO2 Single bond Sub-27
1-2140 Sub-35 3,4-diClPh SO2 Single bond Sub-28
1-2141 Sub-35 3,4-diClPh SO2 Single bond Sub-29
1-2142 Sub-35 3,4-diClPh SO2 Single bond Sub-30
1-2143 Sub-35 3,4-diClPh SO2 Single bond Sub-31
1-2144 Sub-35 3,4-diClPh SO2 Single bond Sub-32
1-2145 Sub-36 3,4-diClPh SO2 Single bond Sub-1
1-2146 Sub-36 3,4-diClPh SO2 Single bond Sub-2
1-2147 Sub-36 3,4-diClPh SO2 Single bond Sub-3
1-2148 Sub-36 3,4-diClPh SO2 Single bond Sub-4
1-2149 Sub-36 3,4-diClPh SO2 Single bond Sub-5
1-2150 Sub-36 3,4-diClPh SO2 Single bond Sub-6
1-2151 Sub-36 3,4-diClPh SO2 Single bond Sub-7
1-2152 Sub-36 3,4-diClPh SO2 Single bond Sub-8
1-2153 Sub-36 3,4-diClPh SO2 Single bond Sub-9
1-2154 Sub-36 3,4-diClPh SO2 Single bond Sub-10
1-2155 Sub-36 3,4-diClPh SO2 Single bond Sub-11
1-2156 Sub-36 3,4-diClPh SO2 Single bond Sub-12
1-2157 Sub-36 3,4-diClPh SO2 Single bond Sub-13
1-2158 Sub-36 3,4-diClPh SO2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2159 Sub-36 3,4-diClPh SO2 Single bond Sub-15
1-2160 Sub-36 3,4-diClPh SO2 Single bond Sub-16
1-2161 Sub-36 3,4-diClPh SO2 Single bond Sub-17
1-2162 Sub-36 3,4-diClPh SO2 Single bond Sub-18
1-2163 Sub-36 3,4-diClPh SO2 Single bond Sub-19
1-2164 Sub-36 3,4-diClPh SO2 Single bond Sub-20
1-2165 Sub-36 3,4-diClPh SO2 Single bond Sub-21
1-2166 Sub-36 3,4-diClPh SO2 Single bond Sub-22
1-2167 Sub-36 3,4-diClPh SO2 Single bond Sub-23
1-2168 Sub-36 3,4-diClPh SO2 Single bond Sub-24
1-2169 Sub-36 3,4-diClPh SO2 Single bond Sub-25
1-2170 Sub-36 3,4-diClPh SO2 Single bond Sub-26
1-2171 Sub-36 3,4-diClPh SO2 Single bond Sub-27
1-2172 Sub-36 3,4-diClPh SO2 Single bond Sub-28
1-2173 Sub-36 3,4-diClPh SO2 Single bond Sub-29
1-2174 Sub-36 3,4-diClPh SO2 Single bond Sub-30
1-2175 Sub-36 3,4-diClPh SO2 Single bond Sub-31
1-2176 Sub-36 3,4-diClPh SO2 Single bond Sub-32
1-2177 Sub-37 3,4-diClPh SO2 Single bond Sub-1
1-2178 Sub-37 3,4-diClPh SO2 Single bond Sub-2
1-2179 Sub-37 3,4-diClPh SO2 Single bond Sub-3
1-2180 Sub-37 3,4-diClPh SO2 Single bond Sub-4
1-2181 Sub-37 3,4-diClPh SO2 Single bond Sub-5
1-2182 Sub-37 3,4-diClPh SO2 Single bond Sub-6
1-2183 Sub-37 3,4-diClPh SO2 Single bond Sub-7
1-2184 Sub-37 3,4-diClPh SO2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2185 Sub-37 3,4-diClPh SO2 Single bond Sub-9
1-2186 Sub-37 3,4-diClPh SO2 Single bond Sub-10
1-2187 Sub-37 3,4-diClPh SO2 Single bond Sub-11
1-2188 Sub-37 3,4-diClPh SO2 Single bond Sub-12
1-2189 Sub-37 3,4-diClPh SO2 Single bond Sub-13
1-2190 Sub-37 3,4-diClPh SO2 Single bond Sub-14
1-2191 Sub-37 3,4-diClPh SO2 Single bond Sub-15
1-2192 Sub-37 3,4-diClPh SO2 Single bond Sub-16
1-2193 Sub-37 3,4-diClPh SO2 Single bond Sub-17
1-2194 Sub-37 3,4-diClPh SO2 Single bond Sub-18
1-2195 Sub-37 3,4-diClPh SO2 Single bond Sub-19
1-2196 Sub-37 3,4-diClPh SO2 Single bond Sub-20
1-2197 Sub-37 3,4-diClPh SO2 Single bond Sub-21
1-2198 Sub-37 3,4-diClPh SO2 Single bond Sub-22
1-2199 Sub-37 3,4-diClPh SO2 Single bond Sub-23
1-2200 Sub-37 3,4-diClPh SO2 Single bond Sub-24
1-2201 Sub-37 3,4-diClPh SO2 Single bond Sub-25
1-2202 Sub-37 3,4-diClPh SO2 Single bond Sub-26
1-2203 Sub-37 3,4-diClPh SO2 Single bond Sub-27
1-2204 Sub-37 3,4-diClPh SO2 Single bond Sub-28
1-2205 Sub-37 3,4-diClPh SO2 Single bond Sub-29
1-2206 Sub-37 3,4-diClPh SO2 Single bond Sub-30
1-2207 Sub-37 3,4-diClPh SO2 Single bond Sub-31
1-2208 Sub-37 3,4-diClPh SO2 Single bond Sub-32
1-2209 Sub-38 3,4-diClPh SO2 Single bond Sub-1
1-2210 Sub-38 3,4-diClPh SO2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2211 Sub-38 3,4-diClPh SO2 Single bond Sub-3
1-2212 Sub-38 3,4-diClPh SO2 Single bond Sub-4
1-2213 Sub-38 3,4-diClPh SO2 Single bond Sub-5
1-2214 Sub-38 3,4-diClPh SO2 Single bond Sub-6
1-2215 Sub-38 3,4-diClPh SO2 Single bond Sub-7
1-2216 Sub-38 3,4-diClPh SO2 Single bond Sub-8
1-2217 Sub-38 3,4-diClPh SO2 Single bond Sub-9
1-2218 Sub-38 3,4-diClPh SO2 Single bond Sub-10
1-2219 Sub-38 3,4-diClPh SO2 Single bond Sub-11
1-2220 Sub-38 3,4-diClPh SO2 Single bond Sub-12
1-2221 Sub-38 3,4-diClPh SO2 Single bond Sub-13
1-2222 Sub-38 3,4-diClPh SO2 Single bond Sub-14
1-2223 Sub-38 3,4-diClPh SO2 Single bond Sub-15
1-2224 Sub-38 3,4-diClPh SO2 Single bond Sub-16
1-2225 Sub-38 3,4-diClPh SO2 Single bond Sub-17
1-2226 Sub-38 3,4-diClPh SO2 Single bond Sub-18
1-2227 Sub-38 3,4-diClPh SO2 Single bond Sub-19
1-2228 Sub-38 3,4-diClPh SO2 Single bond Sub-20
1-2229 Sub-38 3,4-diClPh SO2 Single bond Sub-21
1-2230 Sub-38 3,4-diClPh SO2 Single bond Sub-22
1-2231 Sub-38 3,4-diClPh SO2 Single bond Sub-23
1-2232 Sub-38 3,4-diClPh SO2 Single bond Sub-24
1-2233 Sub-38 3,4-diClPh SO2 Single bond Sub-25
1-2234 Sub-38 3,4-diClPh SO2 Single bond Sub-26
1-2235 Sub-38 3,4-diClPh SO2 Single bond Sub-27
1-2236 Sub-38 3,4-diClPh SO2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2237 Sub-38 3,4-diClPh SO2 Single bond Sub-29
1-2238 Sub-38 3,4-diClPh SO2 Single bond Sub-30
1-2239 Sub-38 3,4-diClPh S02 Single bond Sub-31
1-2240 Sub-38 3,4-diClPh SO2 Single bond Sub-32
1-2241 Sub-39 3,4-diClPh SO2 Single bond Sub-1
1-2242 Sub-39 3,4-diClPh SO2 Single bond Sub-2
1-2243 Sub-39 3,4-diClPh SO2 Single bond Sub-3
1-2244 Sub-39 3,4-diClPh SO2 Single bond Sub-4
1-2245 Sub-39 3,4-diClPh SO2 Single bond Sub-5
1-2246 Sub-39 3,4-diClPh SO2 Single bond Sub-6
1-2247 Sub-39 3,4-diClPh SO2 Single bond Sub-7
1-2248 Sub-39 3,4-diClPh SO2 Single bond Sub-8
1-2249 Sub-39 3,4-diClPh SO2 Single bond Sub-9
1-2250 Sub-39 3,4-diClPh SO2 Single bond Sub-10
1-2251 Sub-39 3,4-diClPh SO2 Single bond Sub-11
1-2252 Sub-39 3,4-diClPh SO2 Single bond Sub-12
1-2253 Sub-39 3,4-diClPh SO2 Single bond Sub-13
1-2254 Sub-39 3,4-diClPh SO2 Single bond Sub-14
1-2255 Sub-39 3,4-diClPh SO2 Single bond Sub-15
1-2256 Sub-39 3,4-diClPh SO2 Single bond Sub-16
1-2257 Sub-39 3,4-diClPh SO2 Single bond Sub-17
1-2258 Sub-39 3,4-diClPh SO2 Single bond Sub-18
1-2259 Sub-39 3,4-diClPh SO2 Single bond Sub-19
1-2260 Sub-39 3,4-diClPh SO2 Single bond Sub-20
1-2261 Sub-39 3,4-diClPh SO2 Single bond Sub-21
1-2262 Sub-39 3,4-diClPh SO2 Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2263 Sub-39 3,4-diClPh SO2 Single bond Sub-23
1-2264 Sub-39 3,4-diClPh SO2 Single bond Sub-24
1-2265 Sub-39 3,4-diClPh SO2 Single bond Sub-25
1-2266 Sub-39 3,4-diClPh SO2 Single bond Sub-26
1-2267 Sub-39 3,4-diClPh SO2 Single bond Sub-27
1-2268 Sub-39 3,4-diClPh SO2 Single bond Sub-28
1-2269 Sub-39 3,4-diClPh SO2 Single bond Sub-29
1-2270 Sub-39 3,4-diClPh SO2 Single bond Sub-30
1-2271 Sub-39 3,4-diClPh SO2 Single bond Sub-31
1-2272 Sub-39 3,4-diClPh SO2 Single bond Sub-32
1-2273 Sub-40 3,4-diClPh SO2 Single bond Sub-1
1-2274 Sub-40 3,4-diClPh SO2 Single bond Sub-2
1-2275 Sub-40 3,4-diClPh SO2 Single bond Sub-3
1-2276 Sub-40 3,4-diClPh SO2 Single bond Sub-4
1-2277 Sub-40 3,4-diClPh SO2 Single bond Sub-5
1-2278 Sub-40 3,4-diClPh SO2 Single bond Sub-6
1-2279 Sub-40 3,4-diClPh SO2 Single bond Sub-7
1-2280 Sub-40 3,4-diClPh SO2 Single bond Sub-8
1-2281 Sub-40 3,4-diClPh SO2 Single bond Sub-9
1-2282 Sub-40 3,4-diClPh SO2 Single bond Sub-10
1-2283 Sub-40 3,4-diClPh SO2 Single bond Sub-11
1-2284 Sub-40 3,4-diClPh SO2 Single bond Sub-12
1-2285 Sub-40 3,4-diClPh SO2 Single bond Sub-13
1-2286 Sub-40 3,4-diClPh SO2 Single bond Sub-14
1-2287 Sub-40 3,4-diClPh SO2 Single bond Sub-15
1-2288 Sub-40 3,4-diClPh SO2 Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2289 Sub-40 3,4-diClPh SO2 Single bond Sub-17
1-2290 Sub-40 3,4-diClPh SO2 Single bond Sub-18
1-2291 Sub-40 3,4-diClPh SO2 Single bond Sub-19
1-2292 Sub-40 3,4-diClPh SO2 Single bond Sub-20
1-2293 Sub-40 3,4-diClPh SO2 Single bond Sub-21
1-2294 Sub-40 3,4-diClPh SO2 Single bond Sub-22
1-2295 Sub-40 3,4-diClPh SO2 Single bond Sub-23
1-2296 Sub-40 3,4-diClPh SO2 Single bond Sub-24
1-2297 Sub-40 3,4-diClPh SO2 Single bond Sub-25
1-2298 Sub-40 3,4-diClPh SO2 Single bond Sub-26
1-2299 Sub-40 3,4-diClPh SO2 Single bond Sub-27
1-2300 Sub-40 3,4-diClPh SO2 Single bond Sub-28
1-2301 Sub-40 3,4-diClPh SO2 Single bond Sub-29
1-2302 Sub-40 3,4-diClPh SO2 Single bond Sub-30
1-2303 Sub-40 3,4-diClPh SO2 Single bond Sub-31
1-2304 Sub-40 3,4-diClPh SO2 Single bond Sub-32
1-2305 Sub-41 3,4-diClPh SO2 Single bond Sub-1
1-2306 Sub-41 3,4-diClPh SO2 Single bond Sub-2
1-2307 Sub-41 3,4-diClPh SO2 Single bond Sub-3
1-2308 Sub-41 3,4-diClPh SO2 Single bond Sub-4
1-2309 Sub-41 3,4-diClPh SO2 Single bond Sub-5
1-2310 Sub-41 3,4-diClPh SO2 Single bond Sub-6
1-2311 Sub-41 3,4-diClPh SO2 Single bond Sub-7
1-2312 Sub-41 3,4-diClPh SO2 Single bond Sub-8
1-2313 Sub-41 3,4-diClPh SO2 Single bond Sub-9
1-2314 Sub-41 3,4-diClPh SO2 Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2315 Sub-41 3,4-diClPh SO2 Single bond Sub-11
1-2316 Sub-41 3,4-diClPh SO2 Single bond Sub-12
1-2317 Sub-41 3,4-diClPh SO2 Single bond Sub-13
1-2318 Sub-41 3,4-diClPh SO2 Single bond Sub-14
1-2319 Sub-41 3,4-diClPh SO2 Single bond Sub-15
1-2320 Sub-41 3,4-diClPh SO2 Single bond Sub-16
1-2321 Sub-41 3,4-diClPh SO2 Single bond Sub-17
1-2322 Sub-41 3,4-diClPh SO2 Single bond Sub-18
1-2323 Sub-41 3,4-diClPh SO2 Single bond Sub-19
1-2324 Sub-41 3,4-diClPh SO2 Single bond Sub-20
1-2325 Sub-41 3,4-diClPh SO2 Single bond Sub-21
1-2326 Sub-41 3,4-diClPh SO2 Single bond Sub-22
1-2327 Sub-41 3,4-diClPh SO2 Single bond Sub-23
1-2328 Sub-41 3,4-diClPh SO2 Single bond Sub-24
1-2329 Sub-41 3,4-diClPh SO2 Single bond Sub-25
1-2330 Sub-41 3,4-diClPh SO2 Single bond Sub-26
1-2331 Sub-41 3,4-diClPh SO2 Single bond Sub-27
1-2332 Sub-41 3,4-diClPh SO2 Single bond Sub-28
1-2333 Sub-41 3,4-diClPh SO2 Single bond Sub-29
1-2334 Sub-41 3,4-diClPh SO2 Single bond Sub-30
1-2335 Sub-41 3,4-diClPh SO2 Single bond Sub-31
1-2336 Sub-41 3,4-diClPh SO2 Single bond Sub-32
1-2337 Sub-42 3,4-diClPh SO2 Single bond Sub-1
1-2338 Sub-42 3,4-diClPh SO2 Single bond Sub-2
1-2339 Sub-42 3,4-diClPh SO2 Single bond Sub-3
1-2340 Sub-42 3,4-diClPh SO2 Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2341 Sub-42 3,4-diClPh SO2 Single bond Sub-5
1-2342 Sub-42 3,4-diClPh SO2 Single bond Sub-6
1-2343 Sub-42 3,4-diClPh SO2 Single bond Sub-7
1-2344 Sub-42 3,4-diClPh SO2 Single bond Sub-8
1-2345 Sub-42 3,4-diClPh SO2 Single bond Sub-9
1-2346 Sub-42 3,4-diClPh SO2 Single bond Sub-10
1-2347 Sub-42 3,4-diClPh SO2 Single bond Sub-11
1-2348 Sub-42 3,4-diClPh SO2 Single bond Sub-12
1-2349 Sub-42 3,4-diClPh SO2 Single bond Sub-13
1-2350 Sub-42 3,4-diClPh SO2 Single bond Sub-14
1-2351 Sub-42 3,4-diClPh SO2 Single bond Sub-15
1-2352 Sub-42 3,4-diClPh SO2 Single bond Sub-16
1-2353 Sub-42 3,4-diClPh SO2 Single bond Sub-17
1-2354 Sub-42 3,4-diClPh SO2 Single bond Sub-18
1-2355 Sub-42 3,4-diClPh SO2 Single bond Sub-19
1-2356 Sub-42 3,4-diClPh SO2 Single bond Sub-20
1-2357 Sub-42 3,4-diClPh SO2 Single bond Sub-21
1-2358 Sub-42 3,4-diClPh SO2 Single bond Sub-22
1-2359 Sub-42 3,4-diClPh SO2 Single bond Sub-23
1-2360 Sub-42 3,4-diClPh SO2 Single bond Sub-24
1-2361 Sub-42 3,4-diClPh SO2 Single bond Sub-25
1-2362 Sub-42 3,4-diClPh SO2 Single bond Sub-26
1-2363 Sub-42 3,4-diClPh SO2 Single bond Sub-27
1-2364 Sub-42 3,4-diClPh SO2 Single bond Sub-28
1-2365 Sub-42 3,4-diClPh SO2 Single bond Sub-29
1-2366 Sub-42 3,4-diClPh SO2 Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2367 Sub-42 3,4-diClPh SO2 Single bond Sub-31
1-2368 Sub-42 3,4-diClPh SO2 Single bond Sub-32
1-2369 Sub-43 3,4-diClPh SO2 Single bond Sub-1
1-2370 Sub-43 3,4-diClPh SO2 Single bond Sub-2
1-2371 Sub-43 3,4-diClPh SO2 Single bond Sub-3
1-2372 Sub-43 3,4-diClPh SO2 Single bond Sub-4
1-2373 Sub-43 3,4-diClPh SO2 Single bond Sub-5
1-2374 Sub-43 3,4-diClPh SO2 Single bond Sub-6
1-2375 Sub-43 3,4-diClPh SO2 Single bond Sub-7
1-2376 Sub-43 3,4-diClPh SO2 Single bond Sub-8
1-2377 Sub-43 3,4-diClPh SO2 Single bond Sub-9
1-2378 Sub-43 3,4-diClPh SO2 Single bond Sub-10
1-2379 Sub-43 3,4-diClPh SO2 Single bond Sub-11
1-2380 Sub-43 3,4-diClPh SO2 Single bond Sub-12
1-2381 Sub-43 3,4-diClPh SO2 Single bond Sub-13
1-2382 Sub-43 3,4-diClPh SO2 Single bond Sub-14
1-2383 Sub-43 3,4-diClPh SO2 Single bond Sub-15
1-2384 Sub-43 3,4-diClPh SO2 Single bond Sub-16
1-2385 Sub-43 3,4-diClPh SO2 Single bond Sub-17
1-2386 Sub-43 3,4-diClPh SO2 Single bond Sub-18
1-2387 Sub-43 3,4-diClPh SO2 Single bond Sub-19
1-2388 Sub-43 3,4-diClPh SO2 Single bond Sub-20
1-2389 Sub-43 3,4-diClPh SO2 Single bond Sub-21
1-2390 Sub-43 3,4-diClPh SO2 Single bond Sub-22
1-2391 Sub-43 3,4-diClPh SO2 Single bond Sub-23
1-2392 Sub-43 3,4-diClPh SO2 Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2393 Sub-43 3,4-diClPh SO2 Single bond Sub-25
1-2394 Sub-43 3,4-diClPh SO2 Single bond Sub-26
1-2395 Sub-43 3,4-diClPh SO2 Single bond Sub-27
1-2396 Sub-43 3,4-diClPh SO2 Single bond Sub-28
1-2397 Sub-43 3,4-diClPh SO2 Single bond Sub-29
1-2398 Sub-43 3,4-diClPh SO2 Single bond Sub-30
1-2399 Sub-43 3,4-diClPh SO2 Single bond Sub-31
1-2400 Sub-43 3,4-diClPh SO2 Single bond Sub-32
1-2401 Sub-44 3,4-diClPh SO2 Single bond Sub-1
1-2402 Sub-44 3,4-diClPh SO2 Single bond Sub-2
1-2403 Sub-44 3,4-diClPh SO2 Single bond Sub-3
1-2404 Sub-44 3,4-diClPh SO2 Single bond Sub-4
1-2405 Sub-44 3,4-diClPh SO2 Single bond Sub-5
1-2406 Sub-44 3,4-diClPh SO2 Single bond Sub-6
1-2407 Sub-44 3,4-diClPh SO2 Single bond Sub-7
1-2408 Sub-44 3,4-diClPh SO2 Single bond Sub-8
1-2409 Sub-44 3,4-diClPh SO2 SheetKey with a key body Sub-9
1-2410 Sub-44 3,4-diClPh SO2 Single bond Sub-10
1-2411 Sub-44 3,4-diClPh SO2 Single bond Sub-11
1-2412 Sub-44 3,4-diClPh SO2 Single bond Sub-12
1-2413 Sub-44 3,4-diClPh SO2 Single bond Sub-13
1-2414 Sub-44 3,4-diClPh SO2 Single bond Sub-14
1-2415 Sub-44 3,4-diClPh SO2 Single bond Sub-15
1-2416 Sub-44 3,4-diClPh SO2 Single bond Sub-16
1-2417 Sub-44 3,4-diClPh SO2 Single bond Sub-17
1-2418 Sub-44 3,4-diClPh SO2 Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2419 Sub-44 3,4-diClPh SO2 Single bond Sub-19
1-2420 Sub-44 3,4-diClPh SO2 Single bond Sub-20
1-2421 Sub-44 3,4-diClPh SO2 Single bond Sub-21
1-2422 Sub-44 3,4-diClPh SO2 Single bond Sub-22
1-2423 Sub-44 3,4-diClPh SO2 Single bond Sub-23
1-2424 Sub-44 3,4-diClPh SO2 Single bond Sub-24
1-2425 Sub-44 3,4-diClPh SO2 Single bond Sub-25
1-2426 Sub-44 3,4-diClPh SO2 Single bond Sub-26
1-2427 Sub-44 3,4-diClPh SO2 Single bond Sub-27
1-2428 Sub-44 3,4-diClPh SO2 Single bond Sub-28
1-2429 Sub-44 3,4-diClPh SO2 Single bond Sub-29
1-2430 Sub-44 3,4-diClPh SO2 Single bond Sub-30
1-2431 Sub-44 3,4-diClPh SO2 Single bond Sub-31
1-2432 Sub-44 3,4-diClPh SO2 Single bond Sub-32
1-2433 Sub-45 3,4-diClPh SO2 Single bond Sub-1
1-2434 Sub-45 3,4-diClPh SO2 Single bond Sub-2
1-2435 Sub-45 3,4-diClPh SO2 Single bond Sub-3
1-2436 Sub-45 3,4-diClPh SO2 Single bond Sub-4
1-2437 Sub-45 3,4-diClPh SO2 Single bond Sub-5
1-2438 Sub-45 3,4-diClPh SO2 Single bond Sub-6
1-2439 Sub-45 3,4-diClPh SO2 Single bond Sub-7
1-2440 Sub-45 3,4-diClPh SO2 Single bond Sub-8
1-2441 Sub-45 3,4-diClPh SO2 Single bond Sub-9
1-2442 Sub-45 3,4-diClPh SO2 Single bond Sub-10
1-2443 Sub-45 3,4-diClPh SO2 Single bond Sub-11
1-2444 Sub-45 3,4-diClPh SO2 Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2445 Sub-45 3,4-diClPh SO2 Single bond Sub-13
1-2446 Sub-45 3,4-diClPh SO2 Single bond Sub-14
1-2447 Sub-45 3,4-diClPh SO2 Single bond Sub-15
1-2448 Sub-45 3,4-diClPh SO2 Single bond Sub-16
1-2449 Sub-45 3,4-diClPh SO2 Single bond Sub-17
1-2450 Sub-45 3,4-diClPh SO2 Single bond Sub-18
1-2451 Sub-45 3,4-diClPh SO2 Single bond Sub-19
1-2452 Sub-45 3,4-diClPh SO2 Single bond Sub-20
1-2453 Sub-45 3,4-diClPh SO2 Single bond Sub-21
1-2454 Sub-45 3,4-diClPh SO2 Single bond Sub-22
1-2455 Sub-45 3,4-diClPh SO2 Single bond Sub-23
1-2456 Sub-45 3,4-diClPh SO2 Single bond Sub-24
1-2457 Sub-45 3,4-diClPh SO2 Single bond Sub-25
1-2458 Sub-45 3,4-diClPh SO2 Single bond Sub-26
1-2459 Sub-45 3,4-diClPh SO2 Single bond Sub-27
1-2460 Sub-45 3,4-diClPh SO2 Single bond Sub-28
1-2461 Sub-45 3,4-diClPh SO2 Single bond Sub-29
1-2462 Sub-45 3,4-diClPh SO2 Single bond Sub-30
1-2463 Sub-45 3,4-diClPh SO2 Single bond Sub-31
1-2464 Sub-45 3,4-diClPh SO2 Single bond Sub-32
1-2465 Sub-46 3,4-diClPh SO2 Single bond Sub-1
1-2466 Sub-46 3,4-diClPh SO2 Single bond Sub-2
1-2467 Sub-46 3,4-diClPh SO2 Single bond Sub-3
1-2468 Sub-46 3,4-diClPh SO2 Single bond Sub-4
1-2469 Sub-46 3,4-diClPh SO2 Single bond Sub-5
1-2470 Sub-46 3,4-diClPh SO2 Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2471 Sub-46 3,4-diClPh SO2 Single bond Sub-7
1-2472 Sub-46 3,4-diClPh SO2 Single bond Sub-8
1-2473 Sub-46 3,4-diClPh SO2 Single bond Sub-9
1-2474 Sub-46 3,4-diClPh SO2 Single bond Sub-10
1-2475 Sub-46 3,4-diClPh SO2 Single bond Sub-11
1-2476 Sub-46 3,4-diClPh SO2 Single bond Sub-12
1-2477 Sub-46 3,4-diClPh SO2 Single bond Sub-13
1-2478 Sub-46 3,4-diClPh SO2 Single bond Sub-14
1-2479 Sub-46 3,4-diClPh SO2 Single bond Sub-15
1-2480 Sub-46 3,4-diClPh SO2 Single bond Sub-16
1-2481 Sub-46 3,4-diClPh SO2 Single bond Sub-17
1-2482 Sub-46 3,4-diClPh SO2 Single bond Sub-18
1-2483 Sub-46 3,4-diClPh SO2 Single bond Sub-19
1-2484 Sub-46 3,4-diClPh SO2 Single bond Sub-20
1-2485 Sub-46 3,4-diClPh SO2 Single bond Sub-21
1-2486 Sub-46 3,4-diClPh SO2 Single bond Sub-22
1-2487 Sub-46 3,4-diClPh SO2 Single bond Sub-23
1-2488 Sub-46 3,4-diClPh SO2 Single bond Sub-24
1-2489 Sub-46 3,4-diClPh SO2 Single bond Sub-25
1-2490 Sub-46 3,4-diClPh SO2 Single bond Sub-26
1-2491 Sub-46 3,4-diClPh SO2 Single bond Sub-27
1-2492 Sub-46 3,4-diClPh SO2 Single bond Sub-28
1-2493 Sub-46 3,4-diClPh SO2 Single bond Sub-29
1-2494 Sub-46 3,4-diClPh SO2 Single bond Sub-30
1-2495 Sub-46 3,4-diClPh SO2 Single bond Sub-31
1-2496 Sub-46 3,4-diClPh SO2 Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2497 Sub-47 3,4-diClPh SO2 Single bond Sub-1
1-2498 Sub-47 3,4-diClPh SO2 Single bond Sub-2
1-2499 Sub-47 3,4-diClPh SO2 Single bond Sub-3
1-2500 Sub-47 3,4-diClPh SO2 Single bond Sub-4
1-2501 Sub-47 3,4-diClPh SO2 Single bond Sub-5
1-2502 Sub-47 3,4-diClPh SO2 Single bond Sub-6
1-2503 Sub47 3,4-diClPh SO2 Single bond Sub-7
1-2504 Sub-47 3,4-diClPh SO2 Single bond Sub-8
1-2505 Sub-47 3,4-diClPh SO2 Single bond Sub-9
1-2506 Sub-47 3,4-diClPh SO2 Single bond Sub-10
1-2507 Sub-47 3,4-diClPh SO2 Single bond Sub-11
1-2508 Sub-47 3,4-diClPh SO2 Single bond Sub-12
1-2509 Sub-47 3,4-diClPh SO2 Single bond Sub-13
1-2510 Sub-47 3,4-diClPh SO2 Single bond Sub-14
1-2511 Sub-47 3,4-diClPh SO2 Single bond Sub-15
1-2512 Sub-47 3,4-diClPh SO2 Single bond Sub-16
1-2513 Sub-47 3,4-diClPh SO2 Single bond Sub-17
1-2514 Sub-47 3,4-diClPh SO2 Single bond Sub-18
1-2515 Sub-47 3,4-diClPh SO2 Single bond Sub-19
1-2516 Sub-47 3,4-diClPh SO2 Single bond Sub-20
1-2517 Sub-47 3,4-diClPh SO2 Single bond Sub-21
1-2518 Sub-47 3,4-diClPh SO2 Single bond Sub-22
1-2519 Sub-47 3,4-diClPh SO2 Single bond Sub-23
1-2520 Sub-47 3,4-diClPh SO2 Single bond Sub-24
1-2521 Sub-47 3,4-diClPh SO2 Single bond Sub-25
1-2522 Sub-47 3,4-diClPh SO2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2523 Sub-47 3,4-diClPh SO2 Single bond Sub-27
1-2524 Sub-47 3,4-diClPh SO2 Single bond Sub-28
1-2525 Sub-47 3,4-diClPh SO2 Single bond Sub-29
1-2526 Sub-47 3,4-diClPh SO2 Single bond Sub-30
1-2527 Sub-47 3,4-diClPh SO2 Single bond Sub-31
1-2528 Sub-47 3,4-diClPh SO2 Single bond Sub-32
1-2529 Sub-48 3,4-diClPh SO2 Single bond Sub-1
1-2530 Sub-48 3,4-diClPh SO2 Single bond Sub-2
1-2531 Sub-48 3,4-diClPh SO2 Single bond Sub-3
1-2532 Sub-48 3,4-diClPh SO2 Single bond Sub-4
1-2533 Sub-48 3,4-diClPh SO2 Single bond Sub-5
1-2534 Sub-48 3,4-diClPh SO2 Single bond Sub-6
1-2535 Sub-48 3,4-diClPh SO2 Single bond Sub-7
1-2536 Sub-48 3,4-diClPh SO2 Single bond Sub-8
1-2537 Sub-48 3,4-diClPh SO2 Single bond Sub-9
1-2538 Sub-48 3,4-diClPh SO2 Single bond Sub-10
1-2539 Sub-48 3,4-diClPh SO2 Single bond Sub-11
1-2540 Sub-48 3,4-diClPh SO2 Single bond Sub-12
1-2541 Sub-48 3,4-diClPh SO2 Single bond Sub-13
1-2542 Sub-48 3,4-diClPh SO2 Single bond Sub-14
1-2543 Sub-48 3,4-diClPh SO2 Single bond Sub-15
1-2544 Sub-48 3,4-diClPh SO2 Single bond Sub-16
1-2545 Sub-48 3,4-diClPh SO2 Single bond Sub-17
1-2546 Sub-48 3,4-diClPh SO2 Single bond Sub-18
1-2547 Sub-48 3,4-diClPh SO2 Single bond Sub-19
1-2548 Sub-48 3,4-diClPh SO2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2549 Sub-48 3,4-diClPh SO2 Single bond Sub-21
1-2550 Sub-48 3,4-diClPh SO2 Single bond Sub-22
1-2551 Sub-48 3,4-diClPh SO2 Single bond Sub-23
1-2552 Sub-48 3,4-diClPh SO2 Single bond Sub-24
1-2553 Sub-48 3,4-diClPh SO2 Single bond Sub-25
1-2554 Sub-48 3,4-diClPh SO2 Single bond Sub-26
1-2555 Sub-48 3,4-diClPh SO2 Single bond Sub-27
1-2556 Sub-48 3,4-diClPh SO2 Single bond Sub-28
1-2557 Sub-48 3,4-diClPh SO2 Single bond Sub-29
1-2558 Sub-48 3,4-diClPh SO2 Single bond Sub-30
1-2559 Sub-48 3,4-diClPh SO2 Single bond Sub-31
1-2560 Sub-48 3,4-diClPh SO2 Single bond Sub-32
1-2561 Sub-49 3,4-diClPh SO2 Single bond Sub-1
1-2562 Sub-49 3,4-diClPh SO2 Single bond Sub-2
1-2563 Sub-49 3,4-diClPh SO2 Single bond Sub-3
1-2564 Sub-49 3,4-diClPh SO2 Single bond Sub-4
1-2565 Sub-49 3,4-diClPh SO2 Single bond Sub-5
1-2566 Sub-49 3,4-diClPh SO2 Single bond Sub-6
1-2567 Sub-49 3,4-diClPh SO2 Single bond Sub-7
1-2568 Sub-49 3,4-diClPh SO2 Single bond Sub-8
1-2569 Sub-49 3,4-diClPh SO2 Single bond Sub-9
1-2570 Sub-49 3,4-diClPh SO2 Single bond Sub-10
1-2571 Sub-49 3,4-diClPh SO2 Single bond Sub-11
1-2572 Sub-49 3,4-diClPh SO2 Single bond Sub-12
1-2573 Sub-49 3,4-diClPh SO2 Single bond Sub-13
1-2574 Sub-49 3,4-diClPh SO2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2575 Sub-49 3,4-diClPh SO2 Single bond Sub-15
1-2576 Sub-49 3,4-diClPh SO2 Single bond Sub-16
1-2577 Sub-49 3,4-diClPh SO2 Single bond Sub-17
1-2578 Sub-49 3,4-diClPh SO2 Single bond Sub-18
1-2579 Sub-49 3,4-diClPh SO2 Single bond Sub-19
1-2580 Sub-49 3,4-diClPh SO2 Single bond Sub-20
1-2581 Sub-49 3,4-diClPh SO2 Single bond Sub-21
1-2582 Sub-49 3,4-diClPh SO2 Single bond Sub-22
1-2583 Sub-49 3,4-diClPh SO2 Single bond Sub-23
1-2584 Sub-49 3,4-diClPh SO2 Single bond Sub-24
1-2585 Sub-49 3,4-diClPh SO2 Single bond Sub-25
1-2586 Sub-49 3,4-diClPh SO2 Single bond Sub-26
1-2587 Sub-49 3,4-diClPh SO2 Single bond Sub-27
1-2588 Sub-49 3,4-diClPh SO2 Single bond Sub-28
1-2589 Sub-49 3,4-diClPh SO2 Single bond Sub-29
1-2590 Sub-49 3,4-diClPh SO2 Single bond Sub-30
1-2591 Sub-49 3,4-diClPh SO2 Single bond Sub-31
1-2592 Sub-49 3,4-diClPh SO2 Single bond Sub-32
1-2593 Sub-50 3,4-diClPh SO2 Single bond Sub-1
1-2594 Sub-50 3,4-diClPh SO2 Single bond Sub-2
1-2595 Sub-50 3,4-diClPh SO2 Single bond Sub-3
1-2596 Sub-50 3,4-diClPh SO2 Single bond Sub-4
1-2597 Sub-50 3,4-diClPh SO2 Single bond Sub-5
1-2598 Sub-50 3,4-diClPh SO2 Single bond Sub-6
1-2599 Sub-50 3,4-diClPh SO2 Single bond Sub-7
1-2600 Sub-50 3,4-diClPh SO2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2601 Sub-50 3,4-diClPh SO2 Single bond Sub-9
1-2602 Sub-50 3,4-diClPh SO2 Single bond Sub-10
1-2603 Sub-50 3,4-diClPh SO2 Single bond Sub-11
1-2604 Sub-50 3,4-diClPh SO2 Single bond Sub-12
1-2605 Sub-50 3,4-diClPh SO2 Single bond Sub-13
1-2606 Sub-50 3,4-diClPh SO2 Single bond Sub-14
1-2607 Sub-50 3,4-diClPh SO2 Single bond Sub-15
1-2608 Sub-50 3,4-diClPh SO2 Single bond Sub-16
1-2609 Sub-50 3,4-diClPh SO2 Single bond Sub-17
1-2610 Sub-50 3,4-diClPh SO2 Single bond Sub-18
1-2611 Sub-50 3,4-diClPh SO2 Single bond Sub-19
1-2612 Sub-50 3,4-diClPh SO2 Single bond Sub-20
1-2613 Sub-50 3,4-diClPh SO2 Single bond Sub-21
1-2614 Sub-50 3,4-diClPh SO2 Single bond Sub-22
1-2615 Sub-50 3,4-diClPh SO2 Single bond Sub-23
1-2616 Sub-50 3,4-diClPh SO2 Single bond Sub-24
1-2617 Sub-50 3,4-diClPh SO2 Single bond Sub-25
1-2618 Sub-50 3,4-diClPh SO2 Single bond Sub-26
1-2619 Sub-50 3,4-diClPh SO2 Single bond Sub-27
1-2620 Sub-50 3,4-diClPh SO2 Single bond Sub-28
1-2621 Sub-50 3,4-diClPh SO2 Single bond Sub-29
1-2622 Sub-50 3,4-diClPh SO2 Single bond Sub-30
1-2623 Sub-50 3,4-diClPh SO2 Single bond Sub-31
1-2624 Sub-50 3,4-diClPh SO2 Single bond Sub-32
1-2625 Sub-51 3,4-diClPh SO2 Single bond Sub-1
1-2626 Sub-51 3,4-diClPh SO2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2627 Sub-51 3,4-diClPh SO2 Single bond Sub-3
1-2628 Sub-51 3,4-diClPh SO2 Single bond Sub-4
1-2629 Sub-51 3,4-diClPh SO2 Single bond Sub-5
1-2630 Sub-51 3,4-diClPh SO2 Single bond Sub-6
1-2631 Sub-51 3,4-diClPh SO2 Single bond Sub-7
1-2632 Sub-51 3,4-diClPh SO2 Single bond Sub-8
1-2633 Sub-51 3,4-diClPh SO2 Single bond Sub-9
1-2634 Sub-51 3,4-diClPh SO2 Single bond Sub-10
1-2635 Sub-51 3,4-diClPh SO2 Single bond Sub-11
1-2636 Sub-51 3,4-diClPh SO2 Single bond Sub-12
1-2637 Sub-51 3,4-diClPh SO2 Single bond Sub-13
1-2638 Sub-51 3,4-diClPh SO2 Single bond Sub-14
1-2639 Sub-51 3,4-diClPh SO2 Single bond Sub-15
1-2640 Sub-51 3,4-diClPh SO2 Single bond Sub-16
1-2641 Sub-51 3,4-diClPh SO2 Single bond Sub-17
1-2642 Sub-51 3,4-diClPh SO2 Single bond Sub-18
1-2643 Sub-51 3,4-diClPh SO2 Single bond Sub-19
1-2644 Sub-51 3,4-diClPh SO2 Single bond Sub-20
1-2645 Sub-51 3,4-diClPh SO2 Single bond Sub-21
1-2646 Sub-51 3,4-diClPh SO2 Single bond Sub-22
1-2647 Sub-51 3,4-diClPh SO2 Single bond Sub-23
1-2648 Sub-51 3,4-diClPh SO2 Single bond Sub-24
1-2649 Sub-51 3,4-diClPh SO2 Single bond Sub-25
1-2650 Sub-51 3,4-diClPh SO2 Single bond Sub-26
1-2651 Sub-51 3,4-diClPh SO2 Single bond Sub-27
1-2652 Sub-51 3,4-diClPh SO2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2653 Sub-51 3,4-diClPh SO2 Single bond Sub-29
1-2654 Sub-51 3,4-diClPh SO2 Single bond Sub-30
1-2655 Sub-51 3,4-diClPh SO2 Single bond Sub-31
1-2656 Sub-51 3,4-diClPh SO2 Single bond Sub-32
1-2657 Sub-52 3,4-diClPh SO2 Single bond Sub-1
1-2658 Sub-52 3,4-diClPh SO2 Single bond Sub-2
1-2659 Sub-52 3,4-diClPh SO2 Single bond Sub-3
1-2660 Sub-52 3,4-diClPh SO2 Single bond Sub-4
1-2661 Sub-52 3,4-diClPh SO2 Single bond Sub-5
1-2662 Sub-52 3,4-diClPh SO2 Single bond Sub-6
1-2663 Sub-52 3,4-diClPh SO2 Single bond Sub-7
1-2664 Sub-52 3,4-diClPh SO2 Single bond Sub-8
1-2665 Sub-52 3,4-diClPh SO2 Single bond Sub-9
1-2666 Sub-52 3,4-diClPh SO2 Single bond Sub-10
1-2667 Sub-52 3,4-diClPh SO2 Single bond Sub-11
1-2668 Sub-52 3,4-diClPh SO2 Single bond Sub-12
1-2669 Sub-52 3,4-diClPh SO2 Single bond Sub-13
1-2670 Sub-52 3,4-diClPh SO2 Single bond Sub-14
1-2671 Sub-52 3,4-diClPh SO2 Single bond Sub-15
1-2672 Sub-52 3,4-diClPh SO2 Single bond Sub-16
1-2673 Sub-52 3,4-diClPh SO2 Single bond Sub-17
1-2674 Sub-52 3,4-diClPh SO2 Single bond Sub-18
1-2675 Sub-52 3,4-diClPh SO2 Single bond Sub-19
1-2676 Sub-52 3,4-diClPh SO2 Single bond Sub-20
1-2677 Sub-52 3,4-diClPh SO2 Single bond Sub-21
1-2678 Sub-52 3,4-diClPh SO2 Single bond Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2679 Sub-52 3,4-diClPh SO2 Single bond Sub-23
1-2680 Sub-52 3,4-diClPh SO2 Single bond Sub-24
1-2681 Sub-52 3,4-diClPh SO2 Single bond Sub-25
1-2682 Sub-52 3,4-diClPh SO2 Single bond Sub-26
1-2683 Sub-52 3,4-diClPh SO2 Single bond Sub-27
1-2684 Sub-52 3,4-diClPh SO2 Single bond Sub-28
1-2685 Sub-52 3,4-diClPh SO2 Single bond Sub-29
1-2686 Sub-52 3,4-diClPh SO2 Single bond Sub-30
1-2687 Sub-52 3,4-diClPh SO2 Single bond Sub-31
1-2688 Sub-52 3,4-diClPh SO2 Single bond Sub-32
1-2689 Sub-53 3,4-diClPh SO2 Single bond Sub-1
1-2690 Sub-53 3,4-diClPh SO2 Single bond Sub-2
1-2691 Sub-53 3,4-diClPh SO2 Single bond Sub-3
1-2692 Sub-53 3,4-diClPh SO2 Single bond Sub-4
1-2693 Sub-53 3,4-diClPh SO2 Single bond Sub-5
1-2694 Sub-53 3,4-diClPh SO2 Single bond Sub-6
1-2695 Sub-53 3,4-diClPh SO2 Single bond Sub-7
1-2696 Sub-53 3,4-diClPh SO2 Single bond Sub-8
1-2697 Sub-53 3,4-diClPh SO2 Single bond Sub-9
1-2698 Sub-53 3,4-diClPh SO2 Single bond Sub-10
1-2699 Sub-53 3,4-diClPh SO2 Single bond Sub-11
1-2700 Sub-53 3,4-diClPh SO2 Single bond Sub-12
1-2701 Sub-53 3,4-diClPh SO2 Single bond Sub-13
1-2702 Sub-53 3,4-diClPh SO2 Single bond Sub-14
1-2703 Sub-53 3,4-diClPh SO2 Single bond Sub-15
1-2704 Sub-53 3,4-diClPh SO2 Single bond Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2705 Sub-53 3,4-diClPh SO2 Single bond Sub-17
1-2706 Sub-53 3,4-diClPh SO2 Single bond Sub-18
1-2707 Sub-53 3,4-diClPh SO2 Single bond Sub-19
1-2708 Sub-53 3,4-diClPh SO2 Single bond Sub-20
1-2709 Sub-53 3,4-diClPh SO2 Single bond Sub-21
1-2710 Sub-53 3,4-diClPh SO2 Single bond Sub-22
1-2711 Sub-53 3,4-diClPh SO2 Single bond Sub-23
1-2712 Sub-53 3,4-diClPh SO2 Single bond Sub-24
1-2713 Sub-53 3,4-diClPh SO2 Single bond Sub-25
1-2714 Sub-53 3,4-diClPh SO2 Single bond Sub-26
1-2715 Sub-53 3,4-diClPh SO2 Single bond Sub-27
1-2716 Sub-53 3,4-diClPh SO2 Single bond Sub-28
1-2717 Sub-53 3,4-diClPh SO2 Single bond Sub-29
1-2718 Sub-53 3,4-diClPh SO2 Single bond Sub-30
1-2719 Sub-53 3,4-diClPh SO2 Single bond Sub-31
1-2720 Sub-53 3,4-diClPh SO2 Single bond Sub-32
1-2721 Sub-54 3,4-diClPh SO2 Single bond Sub-1
1-2722 Sub-54 3,4-diClPh SO2 Single bond Sub-2
1-2723 Sub-54 3,4-diClPh SO2 Single bond Sub-3
1-2724 Sub-54 3,4-diClPh SO2 Single bond Sub-4
1-2725 Sub-54 3,4-diClPh SO2 Single bond Sub-5
1-2726 Sub-54 3,4-diClPh SO2 Single bond Sub-6
1-2727 Sub-54 3,4-diClPh SO2 Single bond Sub-7
1-2728 Sub-54 3,4-diClPh SO2 Single bond Sub-8
1-2729 Sub-54 3,4-diClPh SO2 Single bond Sub-9
1-2730 Sub-54 3,4-diClPh SO2 Single bond Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2731 Sub-54 3,4-diClPh SO2 Single bond Sub-11
1-2732 Sub-54 3,4-diClPh SO2 Single bond Sub-12
1-2733 Sub-54 3,4-diClPh SO2 Single bond Sub-13
1-2734 Sub-54 3,4-diClPh SO2 Single bond Sub-14
1-2735 Sub-54 3,4-diClPh SO2 Single bond Sub-15
1-2736 Sub-54 3,4-diClPh SO2 Single bond Sub-16
1-2737 Sub-54 3,4-diClPh SO2 Single bond Sub-17
1-2738 Sub-54 3,4-diClPh SO2 Single bond Sub-18
1-2739 Sub-54 3,4-diClPh SO2 Single bond Sub-19
1-2740 Sub-54 3,4-diClPh SO2 Single bond Sub-20
1-2741 Sub-54 3,4-diClPh SO2 Single bond Sub-21
1-2742 Sub-54 3,4-diClPh SO2 Single bond Sub-22
1-2743 Sub-54 3,4-diClPh SO2 Single bond Sub-23
1-2744 Sub-54 3,4-diClPh SO2 Single bond Sub-24
1-2745 Sub-54 3,4-diClPh SO2 Single bond Sub-25
1-2746 Sub-54 3,4-diClPh SO2 Single bond Sub-26
1-2747 Sub-54 3,4-diClPh SO2 Single bond Sub-27
1-2748 Sub-54 3,4-diClPh SO2 Single bond Sub-28
1-2749 Sub-54 3,4-diClPh SO2 Single bond Sub-29
1-2750 Sub-54 3,4-diClPh SO2 Single bond Sub-30
1-2751 Sub-54 3,4-diClPh SO2 Single bond Sub-31
1-2752 Sub-54 3,4-diClPh SO2 Single bond Sub-32
1-2753 Sub-55 3,4-diClPh SO2 Single bond Sub-1
1-2754 Sub-55 3,4-diClPh SO2 Single bond Sub-2
1-2755 Sub-55 3,4-diClPh SO2 Single bond Sub-3
1-2756 Sub-55 3,4-diClPh SO2 Single bond Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2757 Sub-55 3,4-diClPh SO2 Single bond Sub-5
1-2758 Sub-55 3,4-diClPh SO2 Single bond Sub-6
1-2759 Sub-55 3,4-diClPh SO2 Single bond Sub-7
1-2760 Sub-55 3,4-diClPh SO2 Single bond Sub-8
1-2761 Sub-55 3,4-diClPh SO2 Single bond Sub-9
1-2762 Sub-55 3,4-diClPh SO2 Single bond Sub-10
1-2763 Sub-55 3,4-diClPh SO2 Single bond Sub-11
1-2764 Sub-55 3,4-diClPh SO2 Single bond Sub-12
1-2765 Sub-55 3,4-diClPh SO2 Single bond Sub-13
1-2766 Sub-55 3,4-diClPh SO2 Single bond Sub-14
1-2767 Sub-55 3,4-diClPh SO2 Single bond Sub-15
1-2768 Sub-55 3,4-diC1Ph SO2 Single bond Sub-16
1-2769 Sub-55 3,4-diClPh SO2 Single bond Sub-17
1-2770 Sub-55 3,4-diClPh SO2 Single bond Sub-18
1-2771 Sub-55 3,4-diClPh SO2 Single bond Sub-19
1-2772 Sub-55 3,4-diClPh SO2 Single bond Sub-20
1-2773 Sub-55 3,4-diClPh SO2 Single bond Sub-21
l-2774 Sub-55 3,4-diClPh SO2 Single bond Sub-22
1-2775 Sub-55 3,4-diClPh SO2 Single bond Sub-23
1-2776 Sub-55 3,4-diClPh SO2 Single bond Sub-24
1-2777 Sub-55 3,4-diClPh SO2 Single bond Sub-25
1-2778 Sub-55 3,4-diClPh SO2 Single bond Sub-26
1-2779 Sub-55 3,4-diClPh SO2 Single bond Sub-27
1-2780 Sub-55 3,4-diClPh SO2 Single bond Sub-28
1-2781 Sub-55 3,4-diClPh SO2 Single bond Sub-29
1-2782 Sub-55 3,4-diClPh SO2 Single bond Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2783 Sub-55 3,4-diClPh SO2 Single bond Sub-31
1-2784 Sub-55 3,4-diClPh SO2 Single bond Sub-32
1-2785 Sub-56 3,4-diClPh SO2 Single bond Sub-1
1-2786 Sub-56 3,4-diClPh SO2 Single bond Sub-2
1-2787 Sub-56 3,4-diClPh SO2 Single bond Sub-3
1-2788 Sub-56 3,4-diClPh SO2 Single bond Sub-4
1-2789 Sub-56 3,4-diClPh SO2 Single bond Sub-5
1-2790 Sub-56 3,4-diClPh SO2 Single bond Sub-6
1-2791 Sub-56 3,4-diClPh SO2 Single bond Sub-7
1-2792 Sub-56 3,4-diClPh SO2 Single bond Sub-8
1-2793 Sub-56 3,4-diClPh SO2 Single bond Sub-9
1-2794 Sub-56 3,4-diClPh SO2 Single bond Sub-10
1-2795 Sub-56 3,4-diClPh SO2 Single bond Sub-11
1-2796 Sub-56 3,4-diClPh SO2 Single bond Sub-12
1-2797 Sub-56 3,4-diClPh SO2 Single bond Sub-13
1-2798 Sub-56 3,4-diClPh SO2 Single bond Sub-14
1-2799 Sub-56 3,4-diClPh SO2 Single bond Sub-15
1-2800 Sub-56 3,4-diClPh SO2 Single bond Sub-16
1-2801 Sub-56 3,4-diClPh SO2 Single bond Sub-17
1-2802 Sub-56 3,4-diClPh SO2 Single bond Sub-18
1-2803 Sub-56 3,4-diClPh SO2 Single bond Sub-19
1-2804 Sub-56 3,4-diClPh SO2 Single bond Sub-20
1-2805 Sub-56 3,4-diClPh SO2 Single bond Sub-21
1-2806 Sub-56 3,4-diClPh SO2 Single bond Sub-22
1-2807 Sub-56 3,4-diClPh SO2 Single bond Sub-23
1-2808 Sub-56 3,4-diClPh SO2 Single bond Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2809 Sub-56 3,4-diClPh SO2 Single bond Sub-25
1-2810 Sub-56 3,4-diClPh SO2 Single bond Sub-26
1-2811 Sub-56 3,4-diClPh SO2 Single bond Sub-27
1-2812 Sub-56 3,4-diClPh SO2 Single bond Sub-28
1-2813 Sub-56 3,4-diClPh SO2 Single bond Sub-29
1-2814 Sub-56 3,4-diClPh SO2 Single bond Sub-30
1-2815 Sub-56 3,4-diClPh SO2 Single bond Sub-31
1-2816 Sub-56 3,4-diClPh SO2 Single bond Sub-32
1-2817 Sub-57 3,4-diClPh SO2 Single bond Sub-1
1-2818 Sub-57 3,4-diClPh SO2 Single bond Sub-2
1-2819 Sub-57 3,4-diClPh SO2 Single bond Sub-3
1-2820 Sub-57 3,4-diClPh SO2 Single bond Sub-4
1-2821 Sub-57 3,4-diClPh SO2 Single bond Sub-5
1-2822 Sub-57 3,4-diClPh SO2 Single bond Sub-6
1-2823 Sub-57 3,4-diClPh SO2 Single bond Sub-7
1-2824 Sub-57 3,4-diClPh SO2 Single bond Sub-8
1-2825 Sub-57 3,4-diClPh SO2 Single bond Sub-9
1-2826 Sub-57 3,4-diClPh SO2 Single bond Sub-10
1-2827 Sub-57 3,4-diClPh SO2 Single bond Sub-11
1-2828 Sub-57 3,4-diClPh SO2 Single bond Sub-12
1-2829 Sub-57 3,4-diClPh SO2 Single bond Sub-13
1-2830 Sub-57 3,4-diClPh SO2 Single bond Sub-14
1-2831 Sub-57 3,4-diClPh SO2 Single bond Sub-15
1-2832 Sub-57 3,4-diClPh SO2 Single bond Sub-16
1-2833 Sub-57 3,4-diClPh SO2 Single bond Sub-17
1-2834 Sub-57 3,4-diClPh SO2 Single bond Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2835 Sub-57 3,4-diClPh SO2 Single bond Sub-19
1-2836 Sub-57 3,4-diClPh SO2 Single bond Sub-20
1-2837 Sub-57 3,4-diClPh SO2 Single bond Sub-21
1-2838 Sub-57 3,4-diClPh SO2 Single bond Sub-22
1-2839 Sub-57 3,4-diClPh SO2 Single bond Sub-23
1-2840 Sub-57 3,4-diClPh SO2 Single bond Sub-24
1-2841 Sub-57 3,4-diClPh SO2 Single bond Sub-25
1-2842 Sub-57 3,4-diClPh SO2 Single bond Sub-26
1-2843 Sub-57 3,4-diClPh SO2 Single bond Sub-27
1-2844 Sub-57 3,4-diClPh SO2 Single bond Sub-28
1-2845 Sub-57 3,4-diClPh SO2 Single bond Sub-29
1-2846 Sub-57 3,4-diClPh SO2 Single bond Sub-30
1-2847 Sub-57 3,4-diClPh SO2 Single bond Sub-31
1-2848 Sub-57 3,4-diClPh SO2 Single bond Sub-32
1-2849 Sub-58 3,4-diClPh SO2 Single bond Sub-1
1-2850 Sub-58 3,4-diClPh SO2 Single bond Sub-2
1-2851 Sub-58 3,4-diClPh SO2 Single bond Sub-3
1-2852 Sub-58 3,4-diClPh SO2 Single bond Sub-4
1-2853 Sub-58 3,4-diClPh SO2 Single bond Sub-5
1-2854 Sub-58 3,4-diClPh SO2 Single bond Sub-6
1-2855 Sub-58 3,4-diClPh SO2 Single bond Sub-7
1-2856 Sub-58 3,4-diClPh SO2 Single bond Sub-8
1-2857 Sub-58 3,4-diClPh SO2 Single bond Sub-9
1-2858 Sub-58 3,4-diClPh SO2 Single bond Sub-10
1-2859 Sub-58 3,4-diClPh SO2 Single bond Sub-11
1-2860 Sub-58 3,4-diClPh SO2 Single bond Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2861 Sub-58 3,4-diClPh SO2 Single bond Sub-13
1-2862 Sub-58 3,4-diClPh SO2 Single bond Sub-14
1-2863 Sub-58 3,4-diClPh SO2 Single bond Sub-15
1-2864 Sub-58 3,4-diClPh SO2 Single bond Sub-16
1-2865 Sub-58 3,4-diClPh SO2 Single bond Sub-17
1-2866 Sub-58 3,4-diClPh SO2 Single bond Sub-18
1-2867 Sub-58 3,4-diClPh SO2 Single bond Sub-19
1-2868 Sub-58 3,4-diClPh SO2 Single bond Sub-20
1-2869 Sub-58 3,4-diClPh SO2 Single bond Sub-21
1-2870 Sub-58 3,4-diClPh SO2 Single bond Sub-22
1-2871 Sub-58 3,4-diClPh SO2 Single bond Sub-23
1-2872 Sub-58 3,4-diClPh SO2 Single bond Sub-24
1-2873 Sub-58 3,4-diClPh SO2 Single bond Sub-25
1-2874 Sub-58 3,4-diClPh SO2 Single bond Sub-26
1-2875 Sub-58 3,4-diClPh SO2 Single bond Sub-27
1-2876 Sub-58 3,4-diClPh SO2 Single bond Sub-28
1-2877 Sub-58 3,4-diClPh SO2 Single bond Sub-29
1-2878 Sub-58 3,4-diClPh SO2 Single bond Sub-30
1-2879 Sub-58 3,4-diClPh SO2 Single bond Sub-31
1-2880 Sub-58 3,4-diClPh SO2 Single bond Sub-32
1-2881 Sub-59 3,4-diClPh SO2 Single bond Sub-1
1-2882 Sub-59 3,4-diClPh SO2 Single bond Sub-2
1-2883 Sub-59 3,4-diClPh SO2 Single bond Sub-3
1-2884 Sub-59 3,4-diClPh SO2 Single bond Sub-4
1-2885 Sub-59 3,4-diClPh SO2 Single bond Sub-5
1-2886 Sub-59 3,4-diClPh SO2 Single bond Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2887 Sub-59 3,4-diClPh SO2 Single bond Sub-7
1-2888 Sub-59 3,4-diClPh SO2 Single bond Sub-8
1-2889 Sub-59 3,4-diClPh SO2 Single bond Sub-9
1-2890 Sub-59 3,4-diClPh SO2 Single bond Sub-10
1-2891 Sub-59 3,4-diClPh SO2 Single bond Sub-11
1-2892 Sub-59 3,4-diClPh SO2 Single bond Sub-12
1-2893 Sub-59 3,4-diClPh SO2 Single bond Sub-13
1-2894 Sub-59 3,4-diClPh SO2 Single bond Sub-14
1-2895 Sub-59 3,4-diClPh SO2 Single bond Sub-15
1-2896 Sub-59 3,4-diClPh SO2 Single bond Sub-16
1-2897 Sub-59 3,4-diClPh SO2 Single bond Sub-17
1-2898 Sub-59 3,4-diClPh SO2 Single bond Sub-18
1-2899 Sub-59 3,4-diClPh SO2 Single bond Sub-19
1-2900 Sub-59 3,4-diClPh SO2 Single bond Sub-20
1-2901 Sub-59 3,4-diClPh SO2 Single bond Sub-21
1-2902 Sub-59 3,4-diClPh SO2 Single bond Sub-22
1-2903 Sub-59 3,4-diClPh SO2 Single bond Sub-23
1-2904 Sub-59 3,4-diClPh SO2 Single bond Sub-24
1-2905 Sub-59 3,4-diClPh SO2 Single bond Sub-25
1-2906 Sub-59 3,4-diClPh SO2 Single bond Sub-26
1-2907 Sub-59 3,4-diClPh SO2 Single bond Sub-27
1-2908 Sub-59 3,4-diClPh SO2 Single bond Sub-28
1-2909 Sub-59 3,4-diClPh SO2 Single bond Sub-29
1-2910 Sub-59 3,4-diClPh SO2 Single bond Sub-30
1-2911 Sub-59 3,4-diClPh SO2 Single bond Sub-31
1-2912 Sub-59 3,4-diClPh SO2 Single bond Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2913 Sub-60 3,4-diClPh SO2 Single bond Sub-1
1-2914 Sub-60 3,4-diClPh SO2 Single bond Sub-2
1-2915 Sub-60 3,4-diClPh SO2 Single bond Sub-3
1-2916 Sub-60 3,4-diClPh SO2 Single bond Sub-4
1-2917 Sub-60 3,4-diClPh SO2 Single bond Sub-5
1-2918 Sub-60 3,4-diClPh SO2 Single bond Sub-6
1-2919 Sub-60 3,4-diClPh SO2 Single bond Sub-7
1-2920 Sub-60 3,4-diClPh SO2 Single bond Sub-8
1-2921 Sub-60 3,4-diClPh SO2 Single bond Sub-9
1-2922 Sub-60 3,4-diClPh SO2 Single bond Sub-10
1-2923 Sub-60 3,4-diClPh SO2 Single bond Sub-11
1-2924 Sub-60 3,4-diClPh SO2 Single bond Sub-12
1-2925 Sub-60 3,4-diClPh SO2 Single bond Sub-13
1-2926 Sub-60 3,4-diClPh SO2 Single bond Sub-14
1-2927 Sub-60 3,4-diClPh SO2 Single bond Sub-15
1-2928 Sub-60 3,4-diClPh SO2 Single bond Sub-16
1-2929 Sub-60 3,4-diClPh SO2 Single bond Sub-17
1-2930 Sub-60 3,4-diClPh SO2 Single bond Sub-18
1-2931 Sub-60 3,4-diClPh SO2 Single bond Sub-19
1-2932 Sub-60 3,4-diClPh SO2 Single bond Sub-20
1-2933 Sub-60 3,4-diClPh SO2 Single bond Sub-21
1-2934 Sub-60 3,4-diClPh SO2 Single bond Sub-22
1-2935 Sub-60 3,4-diClPh SO2 Single bond Sub-23
1-2936 Sub-60 3,4-diClPh SO2 Single bond Sub-24
1-2937 Sub-60 3,4-diClPh SO2 Single bond Sub-25
1-2938 Sub-60 3,4-diClPh SO2 Single bond Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2939 Sub-60 3,4-diClPh SO2 Single bond Sub-27
1-2940 Sub-60 3,4-diClPh SO2 Single bond Sub-28
1-2941 Sub-60 3,4-diClPh SO2 Single bond Sub-29
1-2942 Sub-60 3,4-diClPh SO2 Single bond Sub-30
1-2943 Sub-60 3,4-diClPh SO2 Single bond Sub-31
1-2944 Sub-60 3,4-diClPh SO2 Single bond Sub-32
1-2945 Sub-61 3,4-diClPh SO2 Single bond Sub-1
1-2946 Sub-61 3,4-diClPh SO2 Single bond Sub-2
1-2947 Sub-61 3,4-diClPh SO2 Single bond Sub-3
1-2948 Sub-61 3,4-diClPh SO2 Single bond Sub-4
1-2949 Sub-61 3,4-diClPh SO2 Single bond Sub-5
1-2950 Sub-61 3,4-diClPh SO2 Single bond Sub-6
1-2951 Sub-61 3,4-diClPh SO2 Single bond Sub-7
1-2952 Sub-61 3,4-diClPh SO2 Single bond Sub-8
1-2953 Sub-61 3,4-diClPh SO2 Single bond Sub-9
1-2954 Sub-61 3,4-diClPh SO2 Single bond Sub-10
1-2955 Sub-61 3,4-diClPh SO2 Single bond Sub-11
1-2956 Sub-61 3,4-diClPh SO2 Single bond Sub-12
1-2957 Sub-61 3,4-diClPh SO2 Single bond Sub-13
1-2958 Sub-61 3,4-diClPh SO2 Single bond Sub-14
1-2959 Sub-61 3,4-diClPh SO2 Single bond Sub-15
1-2960 Sub-61 3,4-diClPh SO2 Single bond Sub-16
1-2961 Sub-61 3,4-diClPh SO2 Single bond Sub-17
1-2962 Sub-61 3,4-diClPh SO2 Single bond Sub-18
1-2963 Sub-61 3,4-diClPh SO2 Single bond Sub-19
1-2964 Sub-61 3,4-diClPh SO2 Single bond Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2965 Sub-61 3,4-diClPh SO2 Single bond Sub-21
1-2966 Sub-61 3,4-diClPh SO2 Single bond Sub-22
1-2967 Sub-61 3,4-diClPh SO2 Single bond Sub-23
1-2968 Sub-61 3,4-diClPh SO2 Single bond Sub-24
1-2969 Sub-61 3,4-diClPh SO2 Single bond Sub-25
1-2970 Sub-61 3,4-diClPh SO2 Single bond Sub-26
1-2971 Sub-61 3,4-diClPh SO2 Single bond Sub-27
1-2972 Sub-61 3,4-diClPh SO2 Single bond Sub-28
1-2973 Sub-61 3,4-diClPh SO2 Single bond Sub-29
1-2974 Sub-61 3,4-diClPh SO2 Single bond Sub-30
1-2975 Sub-61 3,4-diClPh SO2 Single bond Sub-31
1-2976 Sub-61 3,4-diClPh SO2 Single bond Sub-32
1-2977 Sub-62 3,4-diClPh SO2 Single bond Sub-1
1-2978 Sub-62 3,4-diClPh SO2 Single bond Sub-2
1-2979 Sub-62 3,4-diClPh SO2 Single bond Sub-3
1-2980 Sub-62 3,4-diClPh SO2 Single bond Sub-4
1-2981 Sub-62 3,4-diClPh SO2 Single bond Sub-5
1-2982 Sub-62 3,4-diClPh SO2 Single bond Sub-6
1-2983 Sub-62 3,4-diClPh SO2 Single bond Sub-7
1-2984 Sub-62 3,4-diClPh SO2 Single bond Sub-8
1-2985 Sub-62 3,4-diClPh SO2 Single bond Sub-9
1-2986 Sub-62 3,4-diClPh SO2 Single bond Sub-10
1-2987 Sub-62 3,4-diClPh SO2 Single bond Sub-11
1-2988 Sub-62 3,4-diClPh SO2 Single bond Sub-12
1-2989 Sub-62 3,4-diClPh SO2 Single bond Sub-13
1-2990 Sub-62 3,4-diClPh SO2 Single bond Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-2991 Sub-62 3,4-diClPh SO2 Single bond Sub-15
1-2992 Sub-62 3,4-diClPh SO2 Single bond Sub-16
1-2993 Sub-62 3,4-diClPh SO2 Single bond Sub-17
1-2994 Sub-62 3,4-diClPh SO2 Single bond Sub-18
1-2995 Sub-62 3,4-diClPh SO2 Single bond Sub-19
1-2996 Sub-62 3,4-diClPh SO2 Single bond Sub-20
1-2997 Sub-62 3,4-diClPh SO2 Single bond Sub-21
1-2998 Sub-62 3,4-diClPh SO2 Single bond Sub-22
1-2999 Sub-62 3,4-diClPh SO2 Single bond Sub-23
1-3000 Sub-62 3,4-diClPh SO2 Single bond Sub-24
1-3001 Sub-62 3,4-diClPh SO2 Single bond Sub-25
1-3002 Sub-62 3,4-diClPh SO2 Single bond Sub-26
1-3003 Sub-62 3,4-diClPh SO2 Single bond Sub-27
1-3004 Sub-62 3,4-diClPh SO2 Single bond Sub-28
1-3005 Sub-62 3,4-diClPh SO2 Single bond Sub-29
1-3006 Sub-62 3,4-diClPh SO2 Single bond Sub-30
1-3007 Sub-62 3,4-diClPh SO2 Single bond Sub-31
1-3008 Sub-62 3,4-diClPh SO2 Single bond Sub-32
1-3009 Sub-63 3,4-diClPh SO2 Single bond Sub-1
1-3010 Sub-63 3,4-diClPh SO2 Single bond Sub-2
1-3011 Sub-63 3,4-diClPh SO2 Single bond Sub-3
1-3012 Sub-63 3,4-diClPh SO2 Single bond Sub-4
1-3013 Sub-63 3,4-diClPh SO2 Single bond Sub-5
1-3014 Sub-63 3,4-diClPh SO2 Single bond Sub-6
1-3015 Sub-63 3,4-diClPh SO2 Single bond Sub-7
1-3016 Sub-63 3,4-diClPh SO2 Single bond Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3017 Sub-63 3,4-diClPh SO2 Single bond Sub-9
1-3018 Sub-63 3,4-diClPh SO2 Single bond Sub-10
1-3019 Sub-63 3,4-diClPh SO2 Single bond Sub-11
1-3020 Sub-63 3,4-diClPh SO2 Single bond Sub-12
1-3021 Sub-63 3,4-diClPh SO2 Single bond Sub-13
1-3022 Sub-63 3,4-diClPh SO2 Single bond Sub-14
1-3023 Sub-63 3,4-diClPh SO2 Single bond Sub-15
1-3024 Sub-63 3,4-diClPh SO2 Single bond Sub-16
1-3025 Sub-63 3,4-diClPh SO2 Single bond Sub-17
1-3026 Sub-63 3,4-diClPh SO2 Single bond Sub-18
1-3027 Sub-63 3,4-diClPh SO2 Single bond Sub-19
1-3028 Sub-63 3,4-diClPh SO2 Single bond Sub-20
1-3029 Sub-63 3,4-diClPh SO2 Single bond Sub-21
1-3030 Sub-63 3,4-diClPh SO2 Single bond Sub-22
1-3031 Sub-63 3,4-diClPh SO2 Single bond Sub-23
1-3032 Sub-63 3,4-diClPh SO2 Single bond Sub-24
1-3033 Sub-63 3,4-diClPh SO2 Single bond Sub-25
1-3034 Sub-63 3,4-diClPh SO2 Single bond Sub-26
1-3035 Sub-63 3,4-diClPh SO2 Single bond Sub-27
1-3036 Sub-63 3,4-diClPh SO2 Single bond Sub-28
1-3037 Sub-63 3,4-diClPh SO2 Single bond Sub-29
1-3038 Sub-63 3,4-diClPh SO2 Single bond Sub-30
1-3039 Sub-63 3,4-diClPh SO2 Single bond Sub-31
1-3040 Sub-63 3,4-diClPh SO2 Single bond Sub-32
1-3041 Sub-64 3,4-diClPh SO2 Single bond Sub-1
1-3042 Sub-64 3,4-diClPh SO2 Single bond Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3043 Sub-64 3,4-diClPh SO2 Single bond Sub-3
1-3044 Sub-64 3,4-diClPh SO2 Single bond Sub-4
1-3045 Sub-64 3,4-diClPh SO2 Single bond Sub-5
1-3046 Sub-64 3,4-diClPh SO2 Single bond Sub-6
1-3047 Sub-64 3,4-diClPh SO2 Single bond Sub-7
1-3048 Sub-64 3,4-diClPh SO2 Single bond Sub-8
1-3049 Sub-64 3,4-diClPh SO2 Single bond Sub-9
1-3050 Sub-64 3,4-diClPh SO2 Single bond Sub-10
1-3051 Sub-64 3,4-diClPh SO2 Single bond Sub-11
1-3052 Sub-64 3,4-diClPh SO2 Single bond Sub-12
1-3053 Sub-64 3,4-diClPh SO2 Single bond Sub-13
1-3054 Sub-64 3,4-diClPh SO2 Single bond Sub-14
1-3055 Sub-64 3,4-diClPh SO2 Single bond Sub-15
1-3056 Sub-64 3,4-diClPh SO2 Single bond Sub-16
1-3057 Sub-64 3,4-diClPh SO2 Single bond Sub-17
1-3058 Sub-64 3,4-diClPh SO2 Single bond Sub-18
1-3059 Sub-64 3,4-diClPh SO2 Single bond Sub-19
1-3060 Sub-64 3,4-diClPh SO2 Single bond Sub-20
1-3061 Sub-64 3,4-diClPh SO2 Single bond Sub-21
1-3062 Sub-64 3,4-diClPh SO2 Single bond Sub-22
1-3063 Sub-64 3,4-diClPh SO2 Single bond Sub-23
1-3064 Sub-64 3,4-diClPh SO2 Single bond Sub-24
1-3065 Sub-64 3,4-diClPh SO2 Single bond Sub-25
1-3066 Sub-64 3,4-diClPh SO2 Single bond Sub-26
1-3067 Sub-64 3,4-diClPh SO2 Single bond Sub-27
1-3068 Sub-64 3,4-diClPh SO2 Single bond Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3069 Sub-64 3,4-diClPh SO2 Single bond Sub-29
1-3070 Sub-64 3,4-diClPh SO2 Single bond Sub-30
1-3071 Sub-64 3,4-diClPh SO2 Single bond Sub-31
1-3072 Sub-64 3,4-diClPh SO2 Single bond Sub-32
1-3073 Sub-33 3,4-diClPh CO CH2 Sub-1
1-3074 Sub-33 3,4-diClPh CO CH2 Sub-2
1-3075 Sub-33 3,4-diClPh CO CH2 Sub-3
1-3076 Sub-33 3,4-diClPh CO CH2 Sub-4
1-3077 Sub-33 3,4-diClPh CO CH2 Sub-5
1-3078 Sub-33 3,4-diClPh CO CH2 Sub-6
1-3079 Sub-33 3,4-diClPh CO CH2 Sub-7
1-3080 Sub-33 3,4-diClPh CO CH2 Sub-8
1-3081 Sub-33 3,4-diClPh CO CH2 Sub-9
1-3082 Sub-33 3,4-diClPh CO CH2 Sub-10
1-3083 Sub-33 3,4-diClPh CO CH2 Sub-11
1-3084 Sub-33 3,4-diClPh CO CH2 Sub-12
1-3085 Sub-33 3,4-diClPh CO CH2 Sub-13
1-3086 Sub-33 3,4-diClPh CO CH2 Sub-14
1-3087 Sub-33 3,4-diClPh CO CH2 Sub-15
1-3088 Sub-33 3,4-diClPh CO CH2 Sub-16
1-3089 Sub-33 3,4-diClPh CO CH2 Sub-17
1-3090 Sub-33 3,4-diClPh CO CH2 Sub-18
1-3091 Sub-33 3,4-diClPh CO CH2 Sub-19
1-3092 Sub-33 3,4-diClPh CO CH2 Sub-20
1-3093 Sub-33 3,4-diClPh CO CH2 Sub-21
1-3094 Sub-33 3,4-diClPh CO CH2 Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3095 Sub-33 3,4-diClPh CO CH2 Sub-23
1-3096 Sub-33 3,4-diClPh CO CH2 Sub-24
1-3097 Sub-33 3,4-diClPh CO CH2 Sub-25
1-3098 Sub-33 3,4-diClPh CO CH2 Sub-26
1-3099 Sub-33 3,4-diClPh CO CH2 Sub-27
1-3100 Sub-33 3,4-diClPh CO CH2 Sub-28
1-3101 Sub-33 3,4-diClPh CO CH2 Sub-29
1-3102 Sub-33 3,4-diClPh CO CH2 Sub-30
1-3103 Sub-33 3,4-diClPh CO CH2 Sub-31
1-3104 Sub-33 3,4-diClPh CO CH2 Sub-32
1-3105 Sub-34 3,4-diClPh CO CH2 Sub-1
1-3106 Sub-34 3,4-diClPh CO CH2 Sub-2
1-3107 Sub-34 3,4-diClPh CO CH2 Sub-3
1-3108 Sub-34 3,4-diClPh CO CH2 Sub-4
1-3109 Sub-34 3,4-diClPh CO CH2 Sub-5
1-3110 Sub-34 3,4-diClPh CO CH2 Sub-6
1-3111 Sub-34 3,4-diClPh CO CH2 Sub-7
1-3112 Sub-34 3,4-diClPh CO CH2 Sub-8
1-3113 Sub-34 3,4-diClPh CO CH2 Sub-9
1-3114 Sub-34 3,4-diClPh CO CH2 Sub-10
1-3115 Sub-34 3,4-diClPh CO CH2 Sub-11
1-3116 Sub-34 3,4-diClPh CO CH2 Sub-12
1-3117 Sub-34 3,4-diClPh CO CH2 Sub-13
1-3118 Sub-34 3,4-diClPh CO CH2 Sub-14
1-3119 Sub-34 3,4-diClPh CO CH2 Sub-15
1-3120 Sub-34 3,4-diClPh CO CH2 Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3121 Sub-34 3,4-diClPh CO CH2 Sub-17
1-3122 Sub-34 3,4-diClPh CO CH2 Sub-18
1-3123 Sub-34 3,4-diClPh CO CH2 Sub-19
1-3124 Sub-34 3,4-diClPh CO CH2 Sub-20
1-3125 Sub-34 3,4-diClPh CO CH2 Sub-21
1-3126 Sub-34 3,4-diClPh CO CH2 Sub-22
1-3127 Sub-34 3,4-diClPh CO CH2 Sub-23
1-3128 Sub-34 3,4-diClPh CO CH2 Sub-24
1-3129 Sub-34 3,4-diClPh CO CH2 Sub-25
1-3130 Sub-34 3,4-diClPh CO CH2 Sub-26
1-3131 Sub-34 3,4-diClPh CO CH2 Sub-27
1-3132 Sub-34 3,4-diClPh CO CH2 Sub-28
1-3133 Sub-34 3,4-diClPh CO CH2 Sub-29
1-3134 Sub-34 3,4-diClPh CO CH2 Sub-30
1-3135 Sub-34 3,4-diClPh CO CH2 Sub-31
1-3136 Sub-34 3,4-diClPh CO CH2 Sub-32
1-3137 Sub-35 3,4-diClPh CO CH2 Sub-1
1-3138 Sub-35 3,4-diClPh CO CH2 Sub-2
1-3139 Sub-35 3,4-diClPh CO CH2 Sub-3
1-3140 Sub-35 3,4-diClPh CO CH2 Sub-4
1-3141 Sub-35 3,4-diClPh CO CH2 Sub-5
1-3142 Sub-35 3,4-diClPh CO CH2 Sub-6
1-3143 Sub-35 3,4-diClPh CO CH2 Sub-7
1-3144 Sub-35 3,4-diClPh CO CH2 Sub-8
1-3145 Sub-35 3,4-diClPh CO CH2 Sub-9
1-3146 Sub-35 3,4-diClPh CO CH2 Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3147 Sub-35 3,4-diClPh CO CH2 Sub-11
1-3148 Sub-35 3,4-diClPh CO CH2 Sub-12
1-3149 Sub-35 3,4-diClPh CO CH2 Sub-13
1-3150 Sub-35 3,4-diClPh CO CH2 Sub-14
1-3151 Sub-35 3,4-diClPh CO CH2 Sub-15
1-3152 Sub-35 3,4-diClPh CO CH2 Sub-16
1-3153 Sub-35 3,4-diClPh CO CH2 Sub-17
1-3154 Sub-35 3,4-diClPh CO CH2 Sub-18
1-3155 Sub-35 3,4-diClPh CO CH2 Sub-19
1-3156 Sub-35 3,4-diClPh CO CH2 Sub-20
1-3157 Sub-35 3,4-diClPh CO CH2 Sub-21
1-3158 Sub-35 3,4-diClPh CO CH2 Sub-22
1-3159 Sub-35 3,4-diClPh CO CH2 Sub-23
1-3160 Sub-35 3,4-diClPh CO CH2 Sub-24
1-3161 Sub-35 3,4-diClPh CO CH2 Sub-25
1-3162 Sub-35 3,4-diClPh CO CH2 Sub-26
1-3163 Sub-35 3,4-diClPh CO CH2 Sub-27
1-3164 Sub-35 3,4-diClPh CO CH2 Sub-28
1-3165 Sub-35 3,4-diClPh CO CH2 Sub-29
1-3166 Sub-35 3,4-diClPh CO CH2 Sub-30
1-3167 Sub-35 3,4-diClPh CO CH2 Sub-31
1-3168 Sub-35 3,4-diClPh CO CH2 Sub-32
1-3169 Sub-36 3,4-diClPh CO CH2 Sub-1
1-3170 Sub-36 3,4-diClPh CO CH2 Sub-2
1-3171 Sub-36 3,4-diClPh CO CH2 Sub-3
1-3172 Sub-36 3,4-diClPh CO CH2 Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3173 Sub-36 3,4-diClPh CO CH2 Sub-5
1-3174 Sub-36 3,4-diClPh CO CH2 Sub-6
1-3175 Sub-36 3,4-diClPh CO CH2 Sub-7
1-3176 Sub-36 3,4-diClPh CO CH2 Sub-8
1-3177 Sub-36 3,4-diClPh CO CH2 Sub-9
1-3178 Sub-36 3,4-diClPh CO CH2 Sub-10
1-3179 Sub-36 3,4-diClPh CO CH2 Sub-11
1-3180 Sub-36 3,4-diClPh CO CH2 Sub-12
1-3181 Sub-36 3,4-diClPh CO CH2 Sub-13
1-3182 Sub-36 3,4-diClPh CO CH2 Sub-14
1-3183 Sub-36 3,4-diClPh CO CH2 Sub-15
1-3184 Sub-36 3,4-diClPh CO CH2 Sub-16
1-3185 Sub-36 3,4-diClPh CO CH2 Sub-17
1-3186 Sub-36 3,4-diClPh CO CH2 Sub-18
1-3187 Sub-36 3,4-diClPh CO CH2 Sub-19
1-3188 Sub-36 3,4-diClPh CO CH2 Sub-20
1-3189 Sub-36 3,4-diClPh CO CH2 Sub-21
1-3190 Sub-36 3,4-diClPh CO CH2 Sub-22
1-3191 Sub-36 3,4-diClPh CO CH2 Sub-23
1-3192 Sub-36 3,4-diClPh CO CH2 Sub-24
1-3193 Sub-36 3,4-diClPh CO CH2 Sub-25
1-3194 Sub-36 3,4-diClPh CO CH2 Sub-26
1-3195 Sub-36 3,4-diClPh CO CH2 Sub-27
1-3196 Sub-36 3,4-diClPh CO CH2 Sub-28
1-3197 Sub-36 3,4-diClPh CO CH2 Sub-29
1-3198 Sub-36 3,4-diClPh CO CH2 Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3199 Sub-36 3,4-diClPh CO CH2 Sub-31
1-3200 Sub-36 3,4-diClPh CO CH2 Sub-32
1-3201 Sub-37 3,4-diClPh CO CH2 Sub-1
1-3202 Sub-37 3,4-diClPh CO CH2 Sub-2
1-3203 Sub-37 3,4-diClPh CO CH2 Sub-3
1-3204 Sub-37 3,4-diClPh CO CH2 Sub-4
1-3205 Sub-37 3,4-diClPh CO CH2 Sub-5
1-3206 Sub-37 3,4-diClPh CO CH2 Sub-6
1-3207 Sub-37 3,4-diClPh CO CH2 Sub-7
1-3208 Sub-37 3,4-diClPh CO CH2 Sub-8
1-3209 Sub-37 3,4-diClPh CO CH2 Sub-9
1-3210 Sub-37 3,4-diClPh CO CH2 Sub-10
1-3211 Sub-37 3,4-diClPh CO CH2 Sub-11
1-3212 Sub-37 3,4-diClPh CO CH2 Sub-12
1-3213 Sub-37 3,4-diClPh CO CH2 Sub-13
1-3214 Sub-37 3,4-diClPh CO CH2 Sub-14
1-3215 Sub-37 3,4-diClPh CO CH2 Sub-15
1-3216 Sub-37 3,4-diClPh CO CH2 Sub-16
1-3217 Sub-37 3,4-diClPh CO CH2 Sub-17
1-3218 Sub-37 3,4-diClPh CO CH2 Sub-18
1-3219 Sub-37 3,4-diClPh CO CH2 Sub-19
1-3220 Sub-37 3,4-diClPh CO CH2 Sub-20
1-3221 Sub-37 3,4-diClPh CO CH2 Sub-21
1-3222 Sub-37 3,4-diClPh CO CH2 Sub-22
1-3223 Sub-37 3,4-diClPh CO CH2 Sub-23
1-3224 Sub-37 3,4-diClPh CO CH2 Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3225 Sub-37 3,4-diClPh CO CH2 Sub-25
1-3226 Sub-37 3,4-diClPh CO CH2 Sub-26
1-3227 Sub-37 3,4-diClPh CO CH2 Sub-27
1-3228 Sub-37 3,4-diClPh CO CH2 Sub-28
1-3229 Sub-37 3,4-diClPh CO CH2 Sub-29
1-3230 Sub-37 3,4-diClPh CO CH2 Sub-30
1-3231 Sub-37 3,4-diClPh CO CH2 Sub-31
1-3232 Sub-37 3,4-diClPh CO CH2 Sub-32
1-3233 Sub-38 3,4-diClPh CO CH2 Sub-1
1-3234 Sub-38 3,4-diClPh CO CH2 Sub-2
1-3235 Sub-38 3,4-diClPh CO CH2 Sub-3
1-3236 Sub-38 3,4-diClPh CO CH2 Sub-4
1-3237 Sub-38 3,4-diClPh CO CH2 Sub-5
1-3238 Sub-38 3,4-diClPh CO CH2 Sub-6
1-3239 Sub-38 3,4-diClPh CO CH2 Sub-7
1-3240 Sub-38 3,4-diClPh CO CH2 Sub-8
1-3241 Sub-38 3,4-diClPh CO CH2 Sub-9
1-3242 Sub-38 3,4-diClPh CO CH2 Sub-10
1-3243 Sub-38 3,4-diClPh CO CH2 Sub-11
1-3244 Sub-38 3,4-diClPh CO CH2 Sub-12
1-3245 Sub-38 3,4-diClPh CO CH2 Sub-13
1-3246 Sub-38 3,4-diClPh CO CH2 Sub-14
1-3247 Sub-38 3,4-diClPh CO CH2 Sub-15
1-3248 Sub-38 3,4-diClPh CO CH2 Sub-16
1-3249 Sub-38 3,4-diClPh CO CH2 Sub-17
1-3250 Sub-38 3,4-diClPh CO CH2 Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3251 Sub-38 3,4-diClPh CO CH2 Sub-19
1-3252 Sub-38 3,4-diClPh CO CH2 Sub-20
1-3253 Sub-38 3,4-diClPh CO CH2 Sub-21
1-3254 Sub-38 3,4-diClPh CO CH2 Sub-22
1-3255 Sub-38 3,4-diClPh CO CH2 Sub-23
1-3256 Sub-38 3,4-diClPh CO CH2 Sub-24
1-3257 Sub-38 3,4-diClPh CO CH2 Sub-25
1-3258 Sub-38 3,4-diClPh CO CH2 Sub-26
1-3259 Sub-38 3,4-diClPh CO CH2 Sub-27
1-3260 Sub-38 3,4-diClPh CO CH2 Sub-28
1-3261 Sub-38 3,4-diClPh CO CH2 Sub-29
1-3262 Sub-38 3,4-diClPh CO CH2 Sub-30
1-3263 Sub-38 3,4-diClPh CO CH2 Sub-31
1-3264 Sub-38 3,4-diClPh CO CH2 Sub-32
1-3265 Sub-39 3,4-diClPh CO CH2 Sub-1
1-3266 Sub-39 3,4-diClPh CO CH2 Sub-2
1-3267 Sub-39 3,4-diClPh CO CH2 Sub-3
1-3268 Sub-39 3,4-diClPh CO CH2 Sub-4
1-3269 Sub-39 3,4-diClPh CO CH2 Sub-5
1-3270 Sub-39 3,4-diClPh CO CH2 Sub-6
1-3271 Sub-39 3,4-diClPh CO CH2 Sub-7
1-3272 Sub-39 3,4-diClPh CO CH2 Sub-8
1-3273 Sub-39 3,4-diClPh CO CH2 Sub-9
1-3274 Sub-39 3,4-diClPh CO CH2 Sub-10
1-3275 Sub-39 3,4-diClPh CO CH2 Sub-11
1-3276 Sub-39 3,4-diClPh CO CH2 Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3277 Sub-39 3,4-diClPh CO CH2 Sub-13
1-3278 Sub-39 3,4-diClPh CO CH2 Sub-14
1-3279 Sub-39 3,4-diClPh CO CH2 Sub-15
1-3280 Sub-39 3,4-diClPh CO CH2 Sub-16
1-3281 Sub-39 3,4-diClPh CO CH2 Sub-17
1-3282 Sub-39 3,4-diClPh CO CH2 Sub-18
1-3283 Sub-39 3,4-diClPh CO CH2 Sub-19
1-3284 Sub-39 3,4-diClPh CO CH2 Sub-20
1-3285 Sub-39 3,4-diClPh CO CH2 Sub-21
1-3286 Sub-39 3,4-diClPh CO CH2 Sub-22
1-3287 Sub-39 3,4-diClPh CO CH2 Sub-23
1-3288 Sub-39 3,4-diClPh CO CH2 Sub-24
1-3289 Sub-39 3,4-diClPh CO CH2 Sub-25
1-3290 Sub-39 3,4-diClPh CO CH2 Sub-26
1-3291 Sub-39 3,4-diClPh CO CH2 Sub-27
1-3292 Sub-39 3,4-diClPh CO CH2 Sub-28
1-3293 Sub-39 3,4-diClPh CO CH2 Sub-29
1-3294 Sub-39 3,4-diClPh CO CH2 Sub-30
1-3295 Sub-39 3,4-diClPh CO CH2 Sub-31
1-3296 Sub-39 3,4-diClPh CO CH2 Sub-32
1-3297 Sub-40 3,4-diClPh CO CH2 Sub-1
1-3298 Sub-40 3,4-diClPh CO CH2 Sub-2
1-3299 Sub-40 3,4-diClPh CO CH2 Sub-3
1-3300 Sub-40 3,4-diClPh CO CH2 Sub-4
1-3301 Sub-40 3,4-diClPh CO CH2 Sub-5
1-3302 Sub-40 3,4-diClPh CO CH2 Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3303 Sub-40 3,4-diClPh CO CH2 Sub-7
1-3304 Sub-40 3,4-diClPh CO CH2 Sub-8
1-3305 Sub-40 3,4-diClPh CO CH2 Sub-9
1-3306 Sub-40 3,4-diClPh CO CH2 Sub-10
1-3307 Sub-40 3,4-diClPh CO CH2 Sub-11
1-3308 Sub-40 3,4-diClPh CO CH2 Sub-12
1-3309 Sub-40 3,4-diClPh CO CH2 Sub-13
1-3310 Sub-40 3,4-diClPh CO CH2 Sub-14
1-3311 Sub-40 3,4-diClPh CO CH2 Sub-15
1-3312 Sub-40 3,4-diClPh CO CH2 Sub-16
1-3313 Sub-40 3,4-diClPh CO CH2 Sub-17
1-3314 Sub-40 3,4-diClPh CO CH2 Sub-18
1-3315 Sub-40 3,4-diClPh CO CH2 Sub-19
1-3316 Sub-40 3,4-diClPh CO CH2 Sub-20
1-3317 Sub-40 3,4-diClPh CO CH2 Sub-21
1-3318 Sub-40 3,4-diClPh CO CH2 Sub-22
1-3319 Sub-40 3,4-diClPh CO CH2 Sub-23
1-3320 Sub-40 3,4-diClPh CO CH2 Sub-24
1-3321 Sub-40 3,4-diClPh CO CH2 Sub-25
l-3322 Sub-40 3,4-diClPh CO CH2 Sub-26
1-3323 Sub-40 3,4-diClPh CO CH2 Sub-27
1-3324 Sub-40 3,4-diClPh CO CH2 Sub-28
1-3325 Sub-40 3,4-diClPh CO CH2 Sub-29
1-3326 Sub-40 3,4-diClPh CO CH2 Sub-30
1-3327 Sub-40 3,4-diClPh CO CH2 Sub-31
1-3328 Sub-40 3,4-diClPh CO CH2 Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3329 Sub-41 3,4-diClPh CO CH2 Sub-1
1-3330 Sub-41 3,4-diClPh CO CH2 Sub-2
1-3331 Sub-41 3,4-diClPh CO CH2 Sub-3
1-3332 Sub-41 3,4-diClPh CO CH2 Sub-4
1-3333 Sub-41 3,4-diClPh CO CH2 Sub-5
1-3334 Sub-41 3,4-diClPh CO CH2 Sub-6
1-3335 Sub-41 3,4-diClPh CO CH2 Sub-7
1-3336 Sub-41 3,4-diClPh CO CH2 Sub-8
1-3337 Sub-41 3,4-diClPh CO CH2 Sub-9
1-3338 Sub-41 3,4-diClPh CO CH2 Sub-10
1-3339 Sub-41 3,4-diClPh CO CH2 Sub-11
1-3340 Sub-41 3,4-diClPh CO CH2 Sub-12
1-3341 Sub-41 3,4-diClPh CO CH2 Sub-13
1-3342 Sub-41 3,4-diClPh CO CH2 Sub-14
1-3343 Sub-41 3,4-diClPh CO CH2 Sub-15
1-3344 Sub-41 3,4-diClPh CO CH2 Sub-16
1-3345 Sub-41 3,4-diClPh CO CH2 Sub-17
1-3346 Sub-41 3,4-diClPh CO CH2 Sub-18
1-3347 Sub-41 3,4-diClPh CO CH2 Sub-19
1-3348 Sub-41 3,4-diClPh CO CH2 Sub-20
1-3349 Sub-41 3,4-diClPh CO CH2 Sub-21
1-3350 Sub-41 3,4-diClPh CO CH2 Sub-22
1-3351 Sub-41 3,4-diClPh CO CH2 Sub-23
1-3352 Sub-41 3,4-diClPh CO CH2 Sub-24
1-3353 Sub-41 3,4-diClPh CO CH2 Sub-25
1-3354 Sub-41 3,4-diClPh CO CH2 Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3355 Sub-41 3,4-diClPh CO CH2 Sub-27
1-3356 Sub-41 3,4-diClPh CO CH2 Sub-28
1-3357 Sub-41 3,4-diClPh CO CH2 Sub-29
1-3358 Sub-41 3,4-diClPh CO CH2 Sub-30
1-3359 Sub-41 3,4-diClPh CO CH2 Sub-31
1-3360 Sub-41 3,4-diClPh CO CH2 Sub-32
1-3361 Sub-42 3,4-diClPh CO CH2 Sub-1
1-3362 Sub-42 3,4-diClPh CO CH2 Sub-2
1-3363 Sub-42 3,4-diClPh CO CH2 Sub-3
1-3364 Sub-42 3,4-diClPh CO CH2 Sub-4
1-3365 Sub-42 3,4-diClPh CO CH2 Sub-5
1-3366 Sub-42 3,4-diClPh CO CH2 Sub-6
1-3367 Sub-42 3,4-diClPh CO CH2 Sub-7
1-3368 Sub-42 3,4-diClPh CO CH2 Sub-8
1-3369 Sub-42 3,4-diClPh CO CH2 Sub-9
1-3370 Sub-42 3,4-diClPh CO CH2 Sub-10
1-3371 Sub-42 3,4-diClPh CO CH2 Sub-11
1-3372 Sub-42 3,4-diClPh CO CH2 Sub-12
1-3373 Sub-42 3,4-diClPh CO CH2 Sub-13
1-3374 Sub-42 3,4-diClPh CO CH2 Sub-14
1-3375 Sub-42 3,4-diClPh CO CH2 Sub-15
1-3376 Sub-42 3,4-diClPh CO CH2 Sub-16
1-3377 Sub-42 3,4-diClPh CO CH2 Sub-17
1-3378 Sub-42 3,4-diClPh CO CH2 Sub-18
1-3379 Sub-42 3,4-diClPh CO CH2 Sub-19
1-3380 Sub-42 3,4-diClPh CO CH2 Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3381 Sub-42 3,4-diClPh CO CH2 Sub-21
1-3382 Sub-42 3,4-diClPh CO CH2 Sub-22
1-3383 Sub-42 3,4-diClPh CO CH2 Sub-23
1-3384 Sub-42 3,4-diClPh CO CH2 Sub-24
1-3385 Sub-42 3,4-diClPh CO CH2 Sub-25
1-3386 Sub-42 3,4-diClPh CO CH2 Sub-26
1-3387 Sub-42 3,4-diClPh CO CH2 Sub-27
1-3388 Sub-42 3,4-diClPh CO CH2 Sub-28
1-3389 Sub-42 3,4-diClPh CO CH2 Sub-29
1-3390 Sub-42 3,4-diClPh CO CH2 Sub-30
1-3391 Sub-42 3,4-diClPh CO CH2 Sub-31
1-3392 Sub-42 3,4-diClPh CO CH2 Sub-32
1-3393 Sub-43 3,4-diClPh CO CH2 Sub-1
1-3394 Sub-43 3,4-diClPh CO CH2 Sub-2
1-3395 Sub-43 3,4-diClPh CO CH2 Sub-3
1-3396 Sub-43 3,4-diClPh CO CH2 Sub-4
1-3397 Sub-43 3,4-diClPh CO CH2 Sub-5
1-3398 Sub-43 3,4-diClPh CO CH2 Sub-6
1-3399 Sub-43 3,4-diClPh CO CH2 Sub-7
1-3400 Sub-43 3,4-diClPh CO CH2 Sub-8
1-3401 Sub-43 3,4-diClPh CO CH2 Sub-9
1-3402 Sub-43 3,4-diClPh CO CH2 Sub-10
1-3403 Sub-43 3,4-diClPh CO CH2 Sub-11
1-3404 Sub-43 3,4-diClPh CO CH2 Sub-12
1-3405 Sub-43 3,4-diClPh CO CH2 Sub-13
1-3406 Sub-43 3,4-diClPh CO CH2 Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3407 Sub-43 3,4-diClPh CO CH2 Sub-15
1-3408 Sub-43 3,4-diClPh CO CH2 Sub-16
1-3409 Sub-43 3,4-diClPh CO CH2 Sub-17
1-3410 Sub-43 3,4-diClPh CO CH2 Sub-18
1-3411 Sub-43 3,4-diClPh CO CH2 Sub-19
1-3412 Sub-43 3,4-diClPh CO CH2 Sub-20
1-3413 Sub-43 3,4-diClPh CO CH2 Sub-21
1-3414 Sub-43 3,4-diClPh CO CH2 Sub-22
1-3415 Sub-43 3,4-diClPh CO CH2 Sub-23
1-3416 Sub-43 3,4-diClPh CO CH2 Sub-24
1-3417 Sub-43 3,4-diClPh CO CH2 Sub-25
1-3418 Sub-43 3,4-diClPh CO CH2 Sub-26
1-3419 Sub-43 3,4-diClPh CO CH2 Sub-27
1-3420 Sub-43 3,4-diClPh CO CH2 Sub-28
1-3421 Sub-43 3,4-diClPh CO CH2 Sub-29
1-3422 Sub-43 3,4-diClPh CO CH2 Sub-30
1-3423 Sub-43 3,4-diClPh CO CH2 Sub-31
1-3424 Sub-43 3,4-diClPb CO CH2 Sub-32
1-3425 Sub-44 3,4-diClPh CO CH2 Sub-1
1-3426 Sub-44 3,4-diClPh CO CH2 Sub-2
1-3427 Sub-44 3,4-diClPh CO CH2 Sub-3
1-3428 Sub-44 3,4-diClPh CO CH2 Sub-4
1-3429 Sub-44 3,4-diClPh CO CH2 Sub-5
1-3430 Sub-44 3,4-diClPh CO CH2 Sub-6
1-3431 Sub-44 3,4-diClPh CO CH2 Sub-7
1-3432 Sub-44 3,4-diClPh CO CH2 Sub-8
Table1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3433 Sub-44 3,4-diClPh CO CH2 Sub-9
1-3434 Sub-44 3,4-diClPh CO CH2 Sub-10
1-3435 Sub-44 3,4-diClPh CO CH2 Sub-11
1-3436 Sub-44 3,4-diClPh CO CH2 Sub-12
1-3437 Sub-44 3,4-diClPh CO CH2 Sub-13
1-3438 Sub-44 3,4-diClPh CO CH2 Sub-14
1-3439 Sub-44 3,4-diClPh CO CH2 Sub-15
1-3440 Sub-44 3,4-diClPh CO CH2 Sub-16
1-3441 Sub-44 3,4-diClPh CO CH2 Sub-17
1-3442 Sub-44 3,4-diClPh CO CH2 Sub-18
1-3443 Sub-44 3,4-diClPh CO CH2 Sub-19
1-3444 Sub-44 3,4-diC1Ph CO CH2 Sub-20
1-3445 Sub-44 3,4-diClPh CO CH2 Sub-21
1-3446 Sub-44 3,4-diClPh CO CH2 Sub-22
1-3447 Sub-44 3,4-diClPh CO CH2 Sub-23
1-3448 Sub-44 3,4-diClPh CO CH2 Sub-24
1-3449 Sub-44 3,4-diClPh CO CH2 Sub-25
1-3450 Sub-44 3,4-diClPh CO CH2 Sub-26
1-3451 Sub-44 3,4-diClPh CO CH2 Sub-27
1-3452 Sub-44 3,4-diClPh CO CH2 Sub-28
1-3453 Sub-44 3,4-diClPh CO CH2 Sub-29
1-3454 Sub-44 3,4-diClPh CO CH2 Sub-30
1-3455 Sub-44 3,4-diClPh CO CH2 Sub-31
1-3456 Sub-44 3,4-diClPh CO CH2 Sub-32
1-3457 Sub-45 3,4-diClPh CO CH2 Sub-1
1-3458 Sub-45 3,4-diClPh CO CH2 Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3459 Sub-45 3,4-diClPh CO CH2 Sub-3
1-3460 Sub-45 3,4-diClPh CO CH2 Sub-4
1-3461 Sub-45 3,4-diClPh CO CH2 Sub-5
1-3462 Sub-45 3,4-diClPh CO CH2 Sub-6
1-3463 Sub-45 3,4-diClPh CO CH2 Sub-7
1-3464 Sub-45 3,4-diClPh CO CH2 Sub-8
1-3465 Sub-45 3,4-diClPh CO CH2 Sub-9
1-3466 Sub-45 3,4-diClPh CO CH2 Sub-10
1-3467 Sub-45 3,4-diClPh CO CH2 Sub-11
1-3468 Sub-45 3,4-diClPh CO CH2 Sub-12
1-3469 Sub-45 3,4-diClPh CO CH2 Sub-13
1-3470 Sub-45 3,4-diClPh CO CH2 Sub-14
1-3471 Sub-45 3,4-diClPh CO CH2 Sub-15
1-3472 Sub-45 3,4-diClPh CO CH2 Sub-16
1-3473 Sub-45 3,4-diClPh CO CH2 Sub-17
1-3474 Sub-45 3,4-diClPh CO CH2 Sub-18
1-3475 Sub-45 3,4-diClPh CO CH2 Sub-19
1-3476 Sub-45 3,4-diClPh CO CH2 Sub-20
1-3477 Sub-45 3,4-diClPh CO CH2 Sub-21
1-3478 Sub-45 3,4-diClPh CO CH2 Sub-22
1-3479 Sub-45 3,4-diClPh CO CH2 Sub-23
1-3480 Sub-45 3,4-diClPh CO CH2 Sub-24
1-3481 Sub-45 3,4-diClPh CO CH2 Sub-25
1-3482 Sub-45 3,4-diClPh CO CH2 Sub-26
1-3483 Sub-45 3,4-diClPh CO CH2 Sub-27
1-3484 Sub-45 3,4-diClPh CO CH2 Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3485 Sub-45 3,4-diClPh CO CH2 Sub-29
1-3486 Sub-45 3,4-diClPh CO CH2 Sub-30
1-3487 Sub-45 3,4-diClPh CO CH2 Sub-31
1-3488 Sub-45 3,4-diClPh CO CH2 Sub-32
1-3489 Sub-46 3,4-diClPh CO CH2 Sub-1
1-3490 Sub-46 3,4-diClPh CO CH2 Sub-2
1-3491 Sub-46 3,4-diClPh CO CH2 Sub-3
1-3492 Sub-46 3,4-diClPh CO CH2 Sub-4
1-3493 Sub-46 3,4-diClPh CO CH2 Sub-5
1-3494 Sub-46 3,4-diClPh CO CH2 Sub-6
1-3495 Sub-46 3,4-diClPh CO CH2 Sub-7
1-3496 Sub-46 3,4-diClPh CO CH2 Sub-8
1-3497 Sub-46 3,4-diClPh CO CH2 Sub-9
1-3498 Sub-46 3,4-diClPh CO CH2 Sub-10
1-3499 Sub-46 3,4-diClPh CO CH2 Sub-11
1-3500 Sub-46 3,4-diClPh CO CH2 Sub-12
1-3501 Sub-46 3,4-diClPh CO CH2 Sub-13
1-3502 Sub-46 3,4-diClPh CO CH2 Sub-14
1-3503 Sub-46 3,4-diClPh CO CH2 Sub-15
1-3504 Sub-46 3,4-diClPh CO CH2 Sub-16
1-3505 Sub-46 3,4-diClPh CO CH2 Sub-17
1-3506 Sub-46 3,4-diClPh CO CH2 Sub-18
1-3507 Sub-46 3,4-diClPh CO CH2 Sub-19
1-3508 Sub-46 3,4-diClPh CO CH2 Sub-20
1-3509 Sub-46 3,4-diClPh CO CH2 Sub-21
1-3510 Sub-46 3,4-diClPh CO CH2 Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3511 Sub-46 3,4-diClPh CO CH2 Sub-23
1-3512 Sub-46 3,4-diClPh CO CH2 Sub-24
1-3513 Sub-46 3,4-diClPh CO CH2 Sub-25
1-3514 Sub-46 3,4-diClPh CO CH2 Sub-26
1-3515 Sub-46 3,4-diClPh CO CH2 Sub-27
1-3516 Sub-46 3,4-diClPh CO CH2 Sub-28
1-3517 Sub-46 3,4-diClPh CO CH2 Sub-29
1-3518 Sub-46 3,4-diClPh CO CH2 Sub-30
1-3519 Sub-46 3,4-diClPh CO CH2 Sub-31
1-3520 Sub-46 3,4-diClPh CO CH2 Sub-32
1-352l Sub-47 3,4-diClPh CO CH2 Sub-1
1-3522 Sub-47 3,4-diClPh CO CH2 Sub-2
l-3523 Sub-47 3,4-diClPh CO CH2 Sub-3
1-3524 Sub-47 3,4-diClPh CO CH2 Sub-4
1-3525 Sub-47 3,4-diClPh CO CH2 Sub-5
1-3526 Sub-47 3,4-diClPh CO CH2 Sub-6
1-3527 Sub-47 3,4-diClPh CO CH2 Sub-7
1-3528 Sub-47 3,4-diClPh CO CH2 Sub-8
1-3529 Sub-47 3,4-diClPh CO CH2 Sub-9
1-3530 Sub-47 3,4-diClPh CO CH2 Sub-10
1-3531 Sub-47 3,4-diClPh CO CH2 Sub-11
1-3532 Sub-47 3,4-diClPh CO CH2 Sub-12
1-3533 Sub-47 3,4-diClPh CO CH2 Sub-13
1-3534 Sub-47 3,4-diClPh CO CH2 Sub-14
1-3535 Sub-47 3,4-diClPh CO CH2 Sub-15
1-3536 Sub-47 3,4-diClPh CO CH2 Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3537 Sub-47 3,4-diClPh CO CH2 Sub-17
1-3538 Sub-47 3,4-diClPh CO CH2 Sub-18
1-3539 Sub-47 3,4-diClPh CO CH2 Sub-19
1-3540 Sub-47 3,4-diClPh CO CH2 Sub-20
1-3541 Sub-47 3,4-diClPh CO CH2 Sub-21
1-3542 Sub-47 3,4-diClPh CO CH2 Sub-22
1-3543 Sub-47 3,4-diClPh CO CH2 Sub-23
1-3544 Sub-47 3,4-diClPh CO CH2 Sub-24
1-3545 Sub-47 3,4-diClPh CO CH2 Sub-25
1-3546 Sub-47 3,4-diClPh CO CH2 Sub-26
1-3547 Sub-47 3,4-diClPh CO CH2 Sub-27
1-3548 Sub-47 3,4-diClPh CO CH2 Sub-28
1-3549 Sub-47 3,4-diClPh CO CH2 Sub-29
1-3550 Sub-47 3,4-diClPh CO CH2 Sub-30
1-3551 Sub-47 3,4-diClPh CO CH2 Sub-31
1-3552 Sub-47 3,4-diClPh CO CH2 Sub-32
1-3553 Sub-48 3,4-diClPh CO CH2 Sub-1
1-3554 Sub-48 3,4-diClPh CO CH2 Sub-2
1-3555 Sub-48 3,4-diClPh CO CH2 Sub-3
1-3556 Sub-48 3,4-diClPh CO CH2 Sub-4
1-3557 Sub-48 3,4-diClPh CO CH2 Sub-5
1-3558 Sub-48 3,4-diClPh CO CH2 Sub-6
1-3559 Sub-48 3,4-diClPh CO CH2 Sub-7
1-3560 Sub-48 3,4-diClPh CO CH2 Sub-8
1-3561 Sub-48 3,4-diClPh CO CH2 Sub-9
1-3562 Sub-48 3,4-diClPh CO CH2 Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3563 Sub-48 3,4-diClPh CO CH2 Sub-11
1-3564 Sub-48 3,4-diClPh CO CH2 Sub-12
1-3565 Sub-48 3,4-diClPh CO CH2 Sub-13
1-3566 Sub-48 3,4-diClPh CO CH2 Sub-14
1-3567 Sub-48 3,4-diClPh CO CH2 Sub-15
1-3568 Sub-48 3,4-diClPh CO CH2 Sub-16
1-3569 Sub-48 3,4-diClPh CO CH2 Sub-17
1-3570 Sub-48 3,4-diClPh CO CH2 Sub-18
1-3571 Sub-48 3,4-diClPh CO CH2 Sub-19
1-3572 Sub-48 3,4-diClPh CO CH2 Sub-20
1-3573 Sub-48 3,4-diClPh CO CH2 Sub-21
1-3574 Sub-48 3,4-diClPh CO CH2 Sub-22
1-3575 Sub-48 3,4-diClPh CO CH2 Sub-23
1-3576 Sub-48 3,4-diClPh CO CH2 Sub-24
1-3577 Sub-48 3,4-diClPh CO CH2 Sub-25
1-3578 Sub-48 3,4-diClPh CO CH2 Sub-26
1-3579 Sub-48 3,4-diClPh CO CH2 Sub-27
1-3580 Sub-48 3,4-diClPh CO CH2 Sub-28
1-3581 Sub-48 3,4-diClPh CO CH2 Sub-29
1-3582 Sub-48 3,4-diClPh CO CH2 Sub-30
1-3583 Sub-48 3,4-diClPh CO CH2 Sub-31
1-3584 Sub-48 3,4-diClPh CO CH2 Sub-32
1-3585 Sub-49 3,4-diClPh CO CH2 Sub-1
1-3586 Sub-49 3,4-diClPh CO CH2 Sub-2
1-3587 Sub-49 3,4-diClPh CO CH2 Sub-3
1-3588 Sub-49 3,4-diClPh CO CH2 Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3589 Sub-49 3,4-diClPh CO CH2 Sub-5
1-3590 Sub-49 3,4-diClPh CO CH2 Sub-6
1-3591 Sub-49 3,4-diClPh CO CH2 Sub-7
1-3592 Sub-49 3,4-diClPh CO CH2 Sub-8
1-3593 Sub-49 3,4-diClPh CO CH2 Sub-9
1-3594 Sub-49 3,4-diClPh CO CH2 Sub-10
1-3595 Sub-49 3,4-diClPh CO CH2 Sub-11
1-3596 Sub-49 3,4-diClPh CO CH2 Sub-12
1-3597 Sub-49 3,4-diClPh CO CH2 Sub-13
1-3598 Sub-49 3,4-diClPh CO CH2 Sub-14
1-3599 Sub-49 3,4-diClPh CO CH2 Sub-15
1-3600 Sub-49 3,4-diClPh CO CH2 Sub-16
1-3601 Sub-49 3,4-diClPh CO CH2 Sub-17
1-3602 Sub-49 3,4-diClPh CO CH2 Sub-18
1-3603 Sub-49 3,4-diClPh CO CH2 Sub-19
1-3604 Sub-49 3,4-diClPh CO CH2 Sub-20
1-3605 Sub-49 3,4-diClPh CO CH2 Sub-21
1-3606 Sub-49 3,4-diClPh CO CH2 Sub-22
1-3607 Sub-49 3,4-diClPh CO CH2 Sub-23
1-3608 Sub-49 3,4-diClPh CO CH2 Sub-24
1-3609 Sub-49 3,4-diClPh CO CH2 Sub-25
1-3610 Sub-49 3,4-diClPh CO CH2 Sub-26
1-3611 Sub-49 3,4-diC1Ph CO CH2 Sub-27
1-3612 Sub-49 3,4-diClPh CO CH2 Sub-28
1-3613 Sub-49 3,4-diClPh CO CH2 Sub-29
1-3614 Sub-49 3,4-diClPh CO CH2 Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3615 Sub-49 3,4-diClPh CO CH2 Sub-31
1-3616 Sub-49 3,4-diClPh CO CH2 Sub-32
1-3617 Sub-50 3,4-diClPh CO CH2 Sub-1
1-3618 Sub-50 3,4-diClPh CO CH2 Sub-2
1-3619 Sub-50 3,4-diClPh CO CH2 Sub-3
1-3620 Sub-50 3,4-diClPh CO CH2 Sub-4
1-3621 Sub-50 3,4-diClPh CO CH2 Sub-5
1-3622 Sub-50 3,4-diClPh CO CH2 Sub-6
1-3623 Sub-50 3,4-diClPh CO CH2 Sub-7
1-3624 Sub-50 3,4-diClPh CO CH2 Sub-8
1-3625 Sub-50 3,4-diClPh CO CH2 Sub-9
1-3626 Sub-50 3,4-diClPh CO CH2 Sub-10
1-3627 Sub-50 3,4-diClPh CO CH2 Sub-11
1-3628 Sub-50 3,4-diClPh CO CH2 Sub-12
1-3629 Sub-50 3,4-diClPh CO CH2 Sub-13
1-3630 Sub-50 3,4-diClPh CO CH2 Sub-14
1-3631 Sub-50 3,4-diClPh CO CH2 Sub-15
1-3632 Sub-50 3,4-diClPh CO CH2 Sub-16
1-3633 Sub-50 3,4-diClPh CO CH2 Sub-17
1-3634 Sub-50 3,4-diClPh CO CH2 Sub-18
1-3635 Sub-50 3,4-diClPh CO CH2 Sub-19
1-3636 Sub-50 3,4-diClPh CO CH2 Sub-20
1-3637 Sub-50 3,4-diClPh CO CH2 Sub-21
1-3638 Sub-50 3,4-diClPh CO CH2 Sub-22
1-3639 Sub-50 3,4-diClPh CO CH2 Sub-23
1-3640 Sub-50 3,4-diClPh CO CH2 Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3641 Sub-50 3,4-diClPh CO CH2 Sub-25
1-3642 Sub-50 3,4-diClPh CO CH2 Sub-26
1-3643 Sub-50 3,4-diClPh CO CH2 Sub-27
1-3644 Sub-50 3,4-diClPh CO CH2 Sub-28
1-3645 Sub-50 3,4-diClPh CO CH2 Sub-29
1-3646 Sub-50 3,4-diClPh CO CH2 Sub-30
1-3647 Sub-50 3,4-diClPh CO CH2 Sub-31
1-3648 Sub-50 3,4-diClPh CO CH2 Sub-32
1-3649 Sub-51 3,4-diClPh CO CH2 Sub-1
1-3650 Sub-51 3,4-diClPh CO CH2 Sub-2
1-3651 Sub-51 3,4-diClPh CO CH2 Sub-3
1-3652 Sub-51 3,4-diClPh CO CH2 Sub-4
1-3653 Sub-51 3,4-diClPh CO CH2 Sub-5
1-3654 Sub-51 3,4-diClPh CO CH2 Sub-6
1-3655 Sub-51 3,4-diClPh CO CH2 Sub-7
1-3656 Sub-51 3,4-diClPh CO CH2 Sub-8
1-3657 Sub-51 3,4-diClPh CO CH2 Sub-9
1-3658 Sub-51 3,4-diClPh CO CH2 Sub-10
1-3659 Sub-51 3,4-diClPh CO CH2 Sub-11
1-3660 Sub-51 3,4-diClPh CO CH2 Sub-12
1-3661 Sub-51 3,4-diClPh CO CH2 Sub-13
1-3662 Sub-51 3,4-diClPh CO CH2 Sub-14
1-3663 Sub-51 3,4-diClPh CO CH2 Sub-15
1-3664 Sub-51 3,4-diClPh CO CH2 Sub-16
1-3665 Sub-51 3,4-diClPh CO CH2 Sub-17
1-3666 Sub-51 3,4-diClPh CO CH2 Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3667 Sub-51 3,4-diClPh CO CH2 Sub-19
1-3668 Sub-51 3,4-diClPh CO CH2 Sub-20
1-3669 Sub-51 3,4-diClPh CO CH2 Sub-21
1-3670 Sub-51 3,4-diClPh CO CH2 Sub-22
1-3671 Sub-51 3,4-diClPh CO CH2 Sub-23
1-3672 Sub-51 3,4-diClPh CO CH2 Sub-24
1-3673 Sub-51 3,4-diClPh CO CH2 Sub-25
1-3674 Sub-51 3,4-diClPh CO CH2 Sub-26
1-3675 Sub-51 3,4-diClPh CO CH2 Sub-27
1-3676 Sub-51 3,4-diClPh CO CH2 Sub-28
1-3677 Sub-51 3,4-diClPh CO CH2 Sub-29
1-3678 Sub-51 3,4-diClPh CO CH2 Sub-30
1-3679 Sub-51 3,4-diClPh CO CH2 Sub-31
1-3680 Sub-51 3,4-diClPh CO CH2 Sub-32
1-3681 Sub-52 3,4-diClPh CO CH2 Sub-1
1-3682 Sub-52 3,4-diClPh CO CH2 Sub-2
1-3683 Sub-52 3,4-diClPh CO CH2 Sub-3
1-3684 Sub-52 3,4-diClPh CO CH2 Sub-4
1-3685 Sub-52 3,4-diClPh CO CH2 Sub-5
1-3686 Sub-52 3,4-diClPh CO CH2 Sub-6
1-3687 Sub-52 3,4-diClPh CO CH2 Sub-7
1-3688 Sub-52 3,4-diClPh CO CH2 Sub-8
1-3689 Sub-52 3,4-diClPh CO CH2 Sub-9
1-3690 Sub-52 3,4-diC1Ph CO CH2 Sub-10
1-3691 Sub-52 3,4-diClPh CO CH2 Sub-11
1-3692 Sub-52 3,4-diClPh CO CH2 Sub-12
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3693 Sub-52 3,4-diClPh CO CH2 Sub-13
1-3694 Sub-52 3,4-diClPh CO CH2 Sub-14
1-3695 Sub-52 3,4-diClPh CO CH2 Sub-15
1-3696 Sub-52 3,4-diClPh CO CH2 Sub-16
1-3697 Sub-52 3,4-diClPh CO CH2 Sub-17
1-3698 Sub-52 3,4-diClPh CO CH2 Sub-18
1-3699 Sub-52 3,4-diClPh CO CH2 Sub-19
1-3700 Sub-52 3,4-diClPh CO CH2 Sub-20
1-3701 Sub-52 3,4-diClPh CO CH2 Sub-21
1-3702 Sub-52 3,4-diClPh CO CH2 Sub-22
1-3703 Sub-52 3,4-diClPh CO CH2 Sub-23
1-3704 Sub-52 3,4-diClPh CO CH2 Sub-24
1-3705 Sub-52 3,4-diClPh CO CH2 Sub-25
1-3706 Sub-52 3,4-diClPh CO CH2 Sub-26
1-3707 Sub-52 3,4-diClPh CO CH2 Sub-27
1-3708 Sub-52 3,4-diClPh CO CH2 Sub-28
1-3709 Sub-52 3,4-diClPh CO CH2 Sub-29
1-3710 Sub-52 3,4-diClPh CO CH2 Sub-30
1-3711 Sub-52 3,4-diClPh CO CH2 Sub-31
1-3712 Sub-52 3,4-diClPh CO CH2 Sub-32
1-3713 Sub-53 3,4-diClPh CO CH2 Sub-1
1-3714 Sub-53 3,4-diClPh CO CH2 Sub-2
1-3715 Sub-53 3,4-diClPh CO CH2 Sub-3
1-3716 Sub-53 3,4-diClPh CO CH2 Sub-4
1-3717 Sub-53 3,4-diClPh CO CH2 Sub-5
1-3718 Sub-53 3,4-diClPh CO CH2 Sub-6
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3719 Sub-53 3,4-diClPh CO CH2 Sub-7
1-3720 Sub-53 3,4-diClPh CO CH2 Sub-8
1-3721 Sub-53 3,4-diClPh CO CH2 Sub-9
1-3722 Sub-53 3,4-diClPh CO CH2 Sub-10
1-3723 Sub-53 3,4-diClPh CO CH2 Sub-11
1-3724 Sub-53 3,4-diClPh CO CH2 Sub-12
1-3725 Sub-53 3,4-diClPh CO CH2 Sub-13
1-3726 Sub-53 3,4-diClPh CO CH2 Sub-14
1-3727 Sub-53 3,4-diClPh CO CH2 Sub-15
1-3728 Sub-53 3,4-diClPh CO CH2 Sub-16
1-3729 Sub-53 3,4-diClPh CO CH2 Sub-17
1-3730 Sub-53 3,4-diClPh CO CH2 Sub-18
1-3731 Sub-53 3,4-diClPh CO CH2 Sub-19
1-3732 Sub-53 3,4-diClPh CO CH2 Sub-20
1-3733 Sub-53 3,4-diClPh CO CH2 Sub-21
1-3734 Sub-53 3,4-diClPh CO CH2 Sub-22
1-3735 Sub-53 3,4-diClPh CO CH2 Sub-23
1-3736 Sub-53 3,4-diClPh CO CH2 Sub-24
1-3737 Sub-53 3,4-diClPh CO CH2 Sub-25
1-3738 Sub-53 3,4-diClPh CO CH2 Sub-26
1-3739 Sub-53 3,4-diClPh CO CH2 Sub-27
1-3740 Sub-53 3,4-diClPh CO CH2 Sub-28
1-3741 Sub-53 3,4-diClPh CO CH2 Sub-29
1-3742 Sub-53 3,4-diClPh CO CH2 Sub-30
1-3743 Sub-53 3,4-diClPh CO CH2 Sub-31
1-3744 Sub-53 3,4-diClPh CO CH2 Sub-32
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3745 Sub-54 3,4-diClPh CO CH2 Sub-1
1-3746 Sub-54 3,4-diClPh CO CH2 Sub-2
1-3747 Sub-54 3,4-diClPh CO CH2 Sub-3
1-3748 Sub-54 3,4-diClPh CO CH2 Sub-4
1-3749 Sub-54 3,4-diClPh CO CH2 Sub-5
1-3750 Sub-54 3,4-diClPh CO CH2 Sub-6
1-3751 Sub-54 3,4-diClPh CO CH2 Sub-7
1-3752 Sub-54 3,4-diClPh CO CH2 Sub-8
1-3753 Sub-54 3,4-diClPh CO CH2 Sub-9
1-3754 Sub-54 3,4-diClPh CO CH2 Sub-10
1-3755 Sub-54 3,4-diClPh CO CH2 Sub-11
1-3756 Sub-54 3,4-diClPh CO CH2 Sub-12
1-3757 Sub-54 3,4-diClPh CO CH2 Sub-13
1-3758 Sub-54 3,4-diClPh CO CH2 Sub-14
1-3759 Sub-54 3,4-diClPh CO CH2 Sub-15
1-3760 Sub-54 3,4-diClPh CO CH2 Sub-16
1-3761 Sub-54 3,4-diClPh CO CH2 Sub-17
1-3762 Sub-54 3,4-diClPh CO CH2 Sub-18
1-3763 Sub-54 3,4-diClPh CO CH2 Sub-19
1-3764 Sub-54 3,4-diClPh CO CH2 Sub-20
1-3765 Sub-54 3,4-diClPh CO CH2 Sub-21
1-3766 Sub-54 3,4-diClPh CO CH2 Sub-22
1-3767 Sub-54 3,4-diClPh CO CH2 Sub-23
1-3768 Sub-54 3,4-diClPh CO CH2 Sub-24
1-3769 Sub-54 3,4-diClPh CO CH2 Sub-25
1-3770 Sub-54 3,4-diClPh CO CH2 Sub-26
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3771 Sub-54 3,4-diClPh CO CH2 Sub-27
1-3772 Sub-54 3,4-diClPh CO CH2 Sub-28
1-3773 Sub-54 3,4-diClPh CO CH2 Sub-29
1-3774 Sub-54 3,4-diClPh CO CH2 Sub-30
1-3775 Sub-54 3,4-diClPh CO CH2 Sub-31
1-3776 Sub-54 3,4-diClPh CO CH2 Sub-32
1-3777 Sub-55 3,4-diClPh CO CH2 Sub-1
1-3778 Sub-55 3,4-diClPh CO CH2 Sub-2
1-3779 Sub-55 3,4-diClPh CO CH2 Sub-3
1-3780 Sub-55 3,4-diClPh CO CH2 Sub-4
1-3781 Sub-55 3,4-diClPh CO CH2 Sub-5
1-3782 Sub-55 3,4-diClPh CO CH2 Sub-6
1-3783 Sub-55 3,4-diClPh CO CH2 Sub-7
1-3784 Sub-55 3,4-diClPh CO CH2 Sub-8
1-3785 Sub-55 3,4-diClPh CO CH2 Sub-9
1-3786 Sub-55 3,4-diClPh CO CH2 Sub-10
1-3787 Sub-55 3,4-diClPh CO CH2 Sub-11
1-3788 Sub-55 3,4-diClPh CO CH2 Sub-12
1-3789 Sub-55 3,4-diClPh CO CH2 Sub-13
1-3790 Sub-55 3,4-diClPh CO CH2 Sub-14
1-3791 Sub-55 3,4-diClPh CO CH2 Sub-15
1-3792 Sub-55 3,4-diClPh CO CH2 Sub-16
1-3793 Sub-55 3,4-diClPh CO CH2 Sub-17
1-3794 Sub-55 3,4-diClPh CO CH2 Sub-18
1-3795 Sub-55 3,4-diClPh CO CH2 Sub-19
1-3796 Sub-55 3,4-diClPh CO CH2 Sub-20
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3797 Sub-55 3,4-diClPh CO CH2 Sub-21
1-3798 Sub-55 3,4-diClPh CO CH2 Sub-22
1-3799 Sub-55 3,4-diClPh CO CH2 Sub-23
1-3800 Sub-55 3,4-diClPh CO CH2 Sub-24
1-3801 Sub-55 3,4-diClPh CO CH2 Sub-25
1-3802 Sub-55 3,4-diClPh CO CH2 Sub-26
1-3803 Sub-55 3,4-diClPh CO CH2 Sub-27
1-3804 Sub-55 3,4-diClPh CO CH2 Sub-28
1-3805 Sub-55 3,4-diClPh CO CH2 Sub-29
1-3806 Sub-55 3,4-diClPh CO CH2 Sub-30
1-3807 Sub-55 3,4-diClPh CO CH2 Sub-31
1-3808 Sub-55 3,4-diClPh CO CH2 Sub-32
1-3809 Sub-56 3,4-diClPh CO CH2 Sub-1
1-3810 Sub-56 3,4-diClPh CO CH2 Sub-2
1-3811 Sub-56 3,4-diClPh CO CH2 Sub-3
1-3812 Sub-56 3,4-diClPh CO CH2 Sub-4
1-3813 Sub-56 3,4-diClPh CO CH2 Sub-5
1-3814 Sub-56 3,4-diClPh CO CH2 Sub-6
1-3815 Sub-56 3,4-diClPh CO CH2 Sub-7
1-3816 Sub-56 3,4-diClPh CO CH2 Sub-8
1-3817 Sub-56 3,4-diClPh CO CH2 Sub-9
1-3818 Sub-56 3,4-diClPh CO CH2 Sub-10
1-3819 Sub-56 3,4-diClPh CO CH2 Sub-11
1-3820 Sub-56 3,4-diClPh CO CH2 Sub-12
1-3821 Sub-56 3,4-diClPh CO CH2 Sub-13
1-3822 Sub-56 3,4-diClPh CO CH2 Sub-14
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3823 Sub-56 3,4-diClPh CO CH2 Sub-15
1-3824 Sub-56 3,4-diClPh CO CH2 Sub-16
1-3825 Sub-56 3,4-diClPh CO CH2 Sub-17
1-3826 Sub-56 3,4-diClPh CO CH2 Sub-18
1-3827 Sub-56 3,4-diClPh CO CH2 Sub-19
1-3828 Sub-56 3,4-diClPh CO CH2 Sub-20
1-3829 Sub-56 3,4-diClPh CO CH2 Sub-21
1-3830 Sub-56 3,4-diClPh CO CH2 Sub-22
1-3831 Sub-56 3,4-diClPh CO CH2 Sub-23
1-3832 Sub-56 3,4-diClPh CO CH2 Sub-24
1-3833 Sub-56 3,4-diClPh CO CH2 Sub-25
1-3834 Sub-56 3,4-diClPh CO CH2 Sub-26
1-3835 Sub-56 3,4-diClPh CO CH2 Sub-27
1-3836 Sub-56 3,4-diClPh CO CH2 Sub-28
1-3837 Sub-56 3,4-diClPh CO CH2 Sub-29
1-3838 Sub-56 3,4-diClPh CO CH2 Sub-30
1-3839 Sub-56 3,4-diClPh CO CH2 Sub-31
1-3840 Sub-56 3,4-diClPh CO CH2 Sub-32
1-3841 Sub-57 3,4-diClPh CO CH2 Sub-1
1-3842 Sub-57 3,4-diCldh CO CH2 Sub-2
1-3843 Sub-57 3,4-diClPh CO CH2 Sub-3
1-3844 Sub-57 3,4-diClPh CO CH2 Sub-4
1-3845 Sub-57 3,4-diClPh CO CH2 Sub-5
1-3846 Sub-57 3,4-diClPh CO CH2 Sub-6
1-3847 Sub-57 3,4-diClPh CO CH2 Sub-7
1-3848 Sub-57 3,4-diClPh CO CH2 Sub-8
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3849 Sub-57 3,4-diClPh CO CH2 Sub-9
1-3850 Sub-57 3,4-diClPh CO CH2 Sub-10
1-3851 Sub-57 3,4-diClPh CO CH2 Sub-11
1-3852 Sub-57 3,4-diClPh CO CH2 Sub-12
1-3853 Sub-57 3,4-diClPh CO CH2 Sub-13
1-3854 Sub-57 3,4-diClPh CO CH2 Sub-14
1-3855 Sub-57 3,4-diClPh CO CH2 Sub-15
1-3856 Sub-57 3,4-diClPh CO CH2 Sub-16
1-3857 Sub-57 3,4-diClPh CO CH2 Sub-17
1-3858 Sub-57 3,4-diClPh CO CH2 Sub-18
1-3859 Sub-57 3,4-diClPh CO CH2 Sub-19
1-3860 Sub-57 3,4-diClPh CO CH2 Sub-20
1-3861 Sub-57 3,4-diClPh CO CH2 Sub-21
1-3862 Sub-57 3,4-diClPh CO CH2 Sub-22
1-3863 Sub-57 3,4-diClPh CO CH2 Sub-23
1-3864 Sub-57 3,4-diClPh CO CH2 Sub-24
1-3865 Sub-57 3,4-diClPh CO CH2 Sub-25
1-3866 Sub-57 3,4-diClPh CO CH2 Sub-26
1-3867 Sub-57 3,4-diClPh CO CH2 Sub-27
1-3868 Sub-57 3,4-diClPh CO CH2 Sub-28
1-3869 Sub-57 3,4-diClPh CO CH2 Sub-29
1-3870 Sub-57 3,4-diClPh CO CH2 Sub-30
1-3871 Sub-57 3,4-diClPh CO CH2 Sub-31
1-3872 Sub-57 3,4-diClPh CO CH2 Sub-32
1-3873 Sub-58 3,4-diClPh CO CH2 Sub-1
1-3874 Sub-58 3,4-diClPh CO CH2 Sub-2
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3875 Sub-58 3,4-diClPh CO CH2 Sub-3
1-3876 Sub-58 3,4-diClPh CO CH2 Sub-4
1-3877 Sub-58 3,4-diClPh CO CH2 Sub-5
1-3878 Sub-58 3,4-diClPh CO CH2 Sub-6
1-3879 Sub-58 3,4-diClPh CO CH2 Sub-7
1-3880 Sub-58 3,4-diClPh CO CH2 Sub-8
1-3881 Sub-58 3,4-diClPh CO CH2 Sub-9
1-3882 Sub-58 3,4-diClPh CO CH2 Sub-10
1-3883 Sub-58 3,4-diClPh CO CH2 Sub-11
1-3884 Sub-58 3,4-diClPh CO CH2 Sub-12
1-3885 Sub-58 3,4-diClPh CO CH2 Sub-13
1-3886 Sub-58 3,4-diClPh CO CH2 Sub-14
1-3887 Sub-58 3,4-diClPh CO CH2 Sub-15
1-3888 Sub-58 3,4-diClPh CO CH2 Sub-16
1-3889 Sub-58 3,4-diClPh CO CH2 Sub-17
1-3890 Sub-58 3,4-diClPh CO CH2 Sub-18
1-3891 Sub-58 3,4-diClPh CO CH2 Sub-19
1-3892 Sub-58 3,4-diClPh CO CH2 Sub-20
1-3893 Sub-58 3,4-diClPh CO CH2 Sub-21
1-3894 Sub-58 3,4-diClPh CO CH2 Sub-22
1-3895 Sub-58 3,4-diClPh CO CH2 Sub-23
1-3896 Sub-58 3,4-diClPh CO CH2 Sub-24
1-3897 Sub-58 3,4-diClPh CO CH2 Sub-25
1-3898 Sub-58 3,4-diClPh CO CH2 Sub-26
1-3899 Sub-58 3,4-diClPh CO CH2 Sub-27
1-3900 Sub-58 3,4-diClPh CO CH2 Sub-28
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3901 Sub-58 3,4-diClPh CO CH2 Sub-29
1-3902 Sub-58 3,4-diClPh CO CH2 Sub-30
1-3903 Sub-58 3,4-diClPh CO CH2 Sub-31
1-3904 Sub-58 3,4-diClPh CO CH2 Sub-32
1-3905 Sub-59 3,4-diClPh CO CH2 Sub-1
1-3906 Sub-59 3,4-diClPh CO CH2 Sub-2
1-3907 Sub-59 3,4-diClPh CO CH2 Sub-3
1-3908 Sub-59 3,4-diClPh CO CH2 Sub-4
1-3909 Sub-59 3,4-diClPh CO CH2 Sub-5
1-3910 Sub-59 3,4-diClPh CO CH2 Sub-6
1-3911 Sub-59 3,4-diClPh CO CH2 Sub-7
1-3912 Sub-59 3,4-diClPh CO CH2 Sub-8
1-3913 Sub-59 3,4-diClPh CO CH2 Sub-9
1-3914 Sub-59 3,4-diClPh CO CH2 Sub-10
1-3915 Sub-59 3,4-diClPh CO CH2 Sub-11
1-3916 Sub-59 3,4-diClPh CO CH2 Sub-12
1-3917 Sub-59 3,4-diClPh CO CH2 Sub-13
1-3918 Sub-59 3,4-diClPh CO CH2 Sub-14
1-3919 Sub-59 3,4-diClPh CO CH2 Sub-15
1-3920 Sub-59 3,4-diClPh CO CH2 Sub-16
1-3921 Sub-59 3,4-diClPh CO CH2 Sub-17
1-3922 Sub-59 3,4-diClPh CO CH2 Sub-18
1-3923 Sub-59 3,4-diClPh CO CH2 Sub-19
1-3924 Sub-59 3,4-diClPh CO CH2 Sub-20
1-3925 Sub-59 3,4-diClPh CO CH2 Sub-21
1-3926 Sub-59 3,4-diClPh CO CH2 Sub-22
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3927 Sub-59 3,4-diClPh CO CH2 Sub-23
1-3928 Sub-59 3,4-diClPh CO CH2 Sub-24
1-3929 Sub-59 3,4-diClPh CO CH2 Sub-25
1-3930 Sub-59 3,4-diClPh CO CH2 Sub-26
1-3931 Sub-59 3,4-diClPh CO CH2 Sub-27
1-3932 Sub-59 3,4-diClPh CO CH2 Sub-28
1-3933 Sub-59 3,4-diClPh CO CH2 Sub-29
1-3934 Sub-59 3,4-diClPh CO CH2 Sub-30
1-3935 Sub-59 3,4-diClPh CO CH2 Sub-31
1-3936 Sub-59 3,4-diClPh CO CH2 Sub-32
1-3937 Sub-60 3,4-diClPh CO CH2 Sub-1
1-3938 Sub-60 3,4-diClPh CO CH2 Sub-2
1-3939 Sub-60 3,4-diClPh CO CH2 Sub-3
1-3940 Sub-60 3,4-diClPh CO CH2 Sub-4
1-3941 Sub-60 3,4-diClPh CO CH2 Sub-5
1-3942 Sub-60 3,4-diClPh CO CH2 Sub-6
1-3943 Sub-60 3,4-diClPh CO CH2 Sub-7
1-3944 Sub-60 3,4-diClPh CO CH2 Sub-8
1-3945 Sub-60 3,4-diClPh CO CH2 Sub-9
1-3946 Sub-60 3,4-diClPh CO CH2 Sub-10
1-3947 Sub-60 3,4-diClPh CO CH2 Sub-11
1-3948 Sub-60 3,4-diClPh CO CH2 Sub-12
1-3949 Sub-60 3,4-diClPh CO CH2 Sub-13
1-3950 Sub-60 3,4-diClPh CO CH2 Sub-14
1-3951 Sub-60 3,4-diClPh CO CH2 Sub-15
1-3952 Sub-60 3,4-diClPh CO CH2 Sub-16
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3953 Sub-59 3,4-diClPh CO CH2 Sub-17
1-3954 Sub-59 3,4-diClPh CO CH2 Sub-18
1-3955 Sub-59 3,4-diClPh CO CH2 Sub-19
1-3956 Sub-59 3,4-diClPh CO CH2 Sub-20
1-3957 Sub-59 3,4-diClPh CO CH2 Sub-21
1-3958 Sub-59 3,4-diClPh CO CH2 Sub-22
1-3959 Sub-59 3,4-diClPh CO CH2 Sub-23
1-3960 Sub-59 3,4-diClPh CO CH2 Sub-24
1-3961 Sub-59 3,4-diClPh CO CH2 Sub-25
1-3962 Sub-59 3,4-diClPh CO CH2 Sub-26
1-3963 Sub-60 3,4-diClPh CO CH2 Sub-27
1-3964 Sub-60 3,4-diClPh CO CH2 Sub-28
1-3965 Sub-60 3,4-diClPh CO CH2 Sub-29
1-3966 Sub-60 3,4-diClPh CO CH2 Sub-30
1-3967 Sub-60 3,4-diClPh CO CH2 Sub-31
1-3968 Sub-60 3,4-diClPh CO CH2 Sub-32
1-3969 Sub-61 3,4-diClPh CO CH2 Sub-1
1-3970 Sub-61 3,4-diClPh CO CH2 Sub-2
1-3971 Sub-61 3,4-diClPh CO CH2 Sub-3
1-3972 Sub-61 3,4-diClPh CO CH2 Sub-4
1-3973 Sub-61 3,4-diClPh CO CH2 Sub-5
1-3974 Sub-61 3,4-diClPh CO CH2 Sub-6
1-3975 Sub-61 3,4-diClPh CO CH2 Sub-7
1-3976 Sub-61 3,4-diClPh CO CH2 Sub-8
1-3977 Sub-61 3,4-diClPh CO CH2 Sub-9
1-3978 Sub-61 3,4-diClPh CO CH2 Sub-10
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-3979 Sub-61 3,4-diClPh CO CH2 Sub-11
1-3980 Sub-61 3,4-diClPh CO CH2 Sub-12
1-3981 Sub-61 3,4-diClPh CO CH2 Sub-13
1-3982 Sub-61 3,4-diClPh CO CH2 Sub-14
1-3983 Sub-61 3,4-diClPh CO CH2 Sub-15
1-3984 Sub-61 3,4-diClPh CO CH2 Sub-16
1-3985 Sub-61 3,4-diClPh CO CH2 Sub-17
1-3986 Sub-61 3,4-diClPh CO CH2 Sub-18
1-3987 Sub-61 3,4-diClPh CO CH2 Sub-19
1-3988 Sub-61 3,4-diClPh CO CH2 Sub-20
1-3989 Sub-61 3,4-diClPh CO CH2 Sub-21
1-3990 Sub-61 3,4-diClPh CO CH2 Sub-22
1-3991 Sub-61 3,4-diClPh CO CH2 Sub-23
1-3992 Sub-61 3,4-diClPh CO CH2 Sub-24
1-3993 Sub-61 3,4-diClPh CO CH2 Sub-25
1-3994 Sub-61 3,4-diClPh CO CH2 Sub-26
1-3995 Sub-61 3,4-diClPh CO CH2 Sub-27
1-3996 Sub-61 3,4-diClPh CO CH2 Sub-28
1-3997 Sub-61 3,4-diClPh CO CH2 Sub-29
1-3998 Sub-61 3,4-diClPh CO CH2 Sub-30
1-3999 Sub-61 3,4-diClPh CO CH2 Sub-31
1-4000 Sub-61 3,4-diClPh CO CH2 Sub-32
1-4001 Sub-62 3,4-diClPh CO CH2 Sub-1
1-4002 Sub-62 3,4-diClPh CO CH2 Sub-2
1-4003 Sub-62 3,4-diClPh CO CH2 Sub-3
1-4004 Sub-62 3,4-diClPh CO CH2 Sub-4
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-4005 Sub-62 3,4-diClPh CO CH2 Sub-5
1-4006 Sub-62 3,4-diClPh CO CH2 Sub-6
1-4007 Sub-62 3,4-diClPh CO CH2 Sub-7
1-4008 Sub-62 3,4-diClPh CO CH2 Sub-8
1-4009 Sub-62 3,4-diClPh CO CH2 Sub-9
1-4010 Sub-62 3,4-diClPh CO CH2 Sub-10
1-4011 Sub-62 3,4-diClPh CO CH2 Sub-11
1-4012 Sub-62 3,4-diClPh CO CH2 Sub-12
1-4013 Sub-62 3,4-diClPh CO CH2 Sub-13
1-4014 Sub-62 3,4-diClPh CO CH2 Sub-14
1-4015 Sub-62 3,4-diClPh CO CH2 Sub-15
1-4016 Sub-62 3,4-diClPh CO CH2 Sub-16
1-4017 Sub-62 3,4-diClPh CO CH2 Sub-17
1-4018 Sub-62 3,4-diClPh CO CH2 Sub-18
1-4019 Sub-62 3,4-diClPh CO CH2 Sub-19
1-4020 Sub-62 3,4-diClPh CO CH2 Sub-20
1-4021 Sub-62 3,4-diClPh CO CH2 Sub-21
1-4022 Sub-62 3,4-diClPh CO CH2 Sub-22
1-4023 Sub-62 3,4-diClPh CO CH2 Sub-23
1-4024 Sub-62 3,4-diClPh CO CH2 Sub-24
1-4025 Sub-62 3,4-diClPh CO CH2 Sub-25
1-4026 Sub-62 3,4-diClPh CO CH2 Sub-26
1-4027 Sub-62 3,4-diClPh CO CH2 SHb-27
1-4028 Sub-62 3,4-diClPh CO CH2 Sub-28
1-4029 Sub-62 3,4-diClPh CO CH2 Sub-29
1-4030 Sub-62 3,4-diClPh CO CH2 Sub-30
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-4031 Sub-62 3,4-diClPh CO CH2 Sub-31
1-4032 Sub-62 3,4-diClPh CO CH2 Sub-32
1-4033 Sub-63 3,4-diClPh CO CH2 Sub-1
1-4034 Sub-63 3,4-diClPh CO CH2 Sub-2
1-4035 Sub-63 3,4-diClPh CO CH2 Sub-3
1-4036 Sub-63 3,4-diClPh CO CH2 Sub-4
1-4037 Sub-63 3,4-diClPh CO CH2 Sub-5
1-4038 Sub-63 3,4-diClPh CO CH2 Sub-6
1-4039 Sub-63 3,4-diCiPh CO CH2 Sub-7
1-4040 Sub-63 3,4-diClPh CO CH2 Sub-8
1-4041 Sub-63 3,4-diClPh CO CH2 Sub-9
1-4042 Sub-63 3,4-diClPh CO CH2 Sub-10
1-4043 Sub-63 3,4-diClPh CO CH2 Sub-11
1-4044 Sub-63 3,4-diClPh CO CH2 Sub-12
1-4045 Sub-63 3,4-diClPh CO CH2 Sub-13
1-4046 Sub-63 3,4-diClPh CO CH2 Sub-14
1-4047 Sub-63 3,4-diClPh CO CH2 Sub-15
1-4048 Sub-63 3,4-diClPh CO CH2 Sub-16
1-4049 Sub-63 3,4-diClPh CO CH2 Sub-17
1-4050 Sub-63 3,4-diClPh CO CH2 Sub-18
1-4051 Sub-63 3,4-diClPh CO CH2 Sub-19
1-4052 Sub-63 3,4-diClPh CO CH2 Sub-20
1-4053 Sub-63 3,4-diClPh CO CH2 Sub-21
1-4054 Sub-63 3,4-diClPh CO CH2 Sub-22
1-4055 Sub-63 3,4-diClPh CO CH2 Sub-23
1-4056 Sub-63 3,4-diClPh CO CH2 Sub-24
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-4057 Sub-63 3,4-diClPh CO CH2 Sub-25
1-4058 Sub-63 3,4-diClPh CO CH2 Sub-26
1-4059 Sub-63 3,4-diClPh CO CH2 Sub-27
1-4060 Sub-63 3,4-diClPh CO CH2 Sub-28
1-4061 Sub-63 3,4-diClPh CO CH2 Sub-29
1-4062 Sub-63 3,4-diClPh CO CH2 Sub-30
1-4063 Sub-63 3,4-diClPh CO CH2 Sub-31
1-4064 Sub-63 3,4-diClPh CO CH2 Sub-32
1-4065 Sub-64 3,4-diClPh CO CH2 Sub-1
1-4066 Sub-64 3,4-diClPh CO CH2 Sub-2
1-4067 Sub-64 3,4-diClPh CO CH2 Sub-3
1-4068 Sub-64 3,4-diClPh CO CH2 Sub-4
1-4069 Sub-64 3,4-diClPh CO CH2 Sub-5
1-4070 Sub-64 3,4-diClPh CO CH2 Sub-6
1-4071 Sub-64 3,4-diClPh CO CH2 Sub-7
1-4072 Sub-64 3,4-diClPh CO CH2 Sub-8
1-4073 Sub-64 3,4-diClPh CO CH2 Sub-9
1-4074 Sub-64 3,4-diClPh CO CH2 Sub-10
1-4075 Sub-64 3,4-diClPh CO CH2 Sub-11
1-4076 Sub-64 3,4-diClPh CO CH2 Sub-12
1-4077 0ub-64 3,4-diClPh CO CH2 Sub-13
1-4078 Sub-64 3,4-diClPh CO CH2 Sub-14
1-4079 Sub-64 3,4-diClPh CO CH2 Sub-15
1-4080 Sub-64 3,4-diClPh CO CH2 Sub-16
1-4081 Sub-64 3,4-diClPh CO CH2 Sub-17
1-4082 Sub-64 3,4-diClPh CO CH2 Sub-18
Table 1(cont.)
Compound (I) Serial number R1 R2 A B Z
1-4083 Sub-64 3,4-diClPh CO CH2 Sub-19
1-4084 Sub-64 3,4-diClPh CO CH2 Sub-20
1-4085 Sub-64 3,4-diClPh CO CH2 Sub-21
1-4086 Sub-64 3,4-diClPh CO CH2 Sub-22
1-4087 Sub-64 3,4-diClPh CO CH2 Sub-23
1-4088 Sub-64 3,4-diClPh CO CH2 Sub-24
1-4089 Sub-64 3,4-diClPh CO CH2 Sub-25
1-4090 Sub-64 3,4-diClPh CO CH2 Sub-26
1-4091 Sub-64 3,4-diClPh CO CH2 Sub-27
1-4092 Sub-64 3,4-diClPh CO CH2 Sub-28
1-4093 Sub-64 3,4-diClPh CO CH2 Sub-29
1-4094 Sub-64 3,4-diClPh CO CH2 Sub-30
1-4095 Sub-64 3,4-diClPh CO CH2 Sub-31
1-4096 Sub-64 3,4-diClPh CO CH2 Sub-32
TABLE 2
Compound (I) Serial number R1 R2 A B Z
2-1 Sub-33 3,4-diClPh CH2 Single bond Sub-1
2-2 Sub-33 3,4-diClPh CH2 Single bond Sub-2
2-3 Sub-33 3,4-diClPh CH2 Single bond Sub-3
2-4 Sub-33 3,4-diClPh CH2 Single bond Sub-4
2-5 Sub-33 3,4-diClPh CH2 Single bond Sub-5
2-6 Sub-33 3,4-diClPh CH2 Single bond Sub-6
2-7 Sub-33 3,4-diClPh CH2 Single bond Sub-7
2-8 Sub-33 3,4-diClPh CH2 Single bond Sub-8
2-9 Sub-33 3,4-diClPh CH2 Single bond Sub-9
2-10 Sub-33 3,4-diClPh CH2 Single bond Sub-10
2-11 Sub-33 3,4-diClPh CH2 Single bond Sub-11
2-12 Sub-33 3,4-diClPh CH2 Single bond Sub-12
2-13 Sub-33 3,4-diClPh CH2 Single bond Sub-13
2-14 Sub-33 3,4-diClPh CH2 Single bond Sub-14
2-15 Sub-33 3,4-diClPh CH2 Single bond Sub-15
2-16 Sub-33 3,4-diClPh CH2 Single bond Sub-16
2-17 Sub-33 3,4-diClPh CH2 Single bond Sub-17
2-18 Sub-33 3,4-diClPh CH2 Single bond Sub-18
2-19 Sub-33 3,4-diClPh CH2 Single bond Sub-19
2-20 Sub-33 3,4-diClPh CH2 Single bond Sub-20
2-21 Sub-33 3,4-diClPh CH2 Single bond Sub-21
2-22 Sub-33 3,4-diClPh CH2 Single bond Sub-22
2-23 Sub-33 3,4-diClPh CH2 Single bond Sub-23
2-24 Sub-33 3,4-diClPh CH2 Single bond Sub-24
2-25 Sub-33 3,4-diClPh CH2 Single bond Sub-25
2-26 Sub-33 3,4-diClPh CH2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-27 Sub-33 3,4-diClPh CH2 Single bond Sub-27
2-28 Sub-33 3,4-diClPh CH2 Single bond Sub-28
2-29 Sub-33 3,4-diClPh CH2 Single bond Sub-29
2-30 Sub-33 3,4-diClPh CH2 Single bond Sub-30
2-31 Sub-33 3,4-diClPh CH2 Single bond Sub-31
2-32 Sub-33 3,4-diClPh CH2 Single bond Sub-32
2-33 Sub-33 3,4-diClPh CH2 Single bond Sub-65
2-34 Sub-33 3,4-diClPh CH2 Single bond Sub-66
2-35 Sub-33 3,4-diClPh CH2 Single bond Sub-67
2-36 Sub-33 3,4-diClPh CH2 Single bond Sub-68
2-37 Sub-33 3,4-diClPh CH2 Single bond Sub-69
2-38 Sub-33 3,4-diClPh CH2 Single bond Sub-70
2-39 Sub-33 3,4-diClPh CH2 Single bond Sub-71
2-40 Sub-33 3,4-diClPh CH2 Single bond Sub-72
2-41 Sub-33 3,4-diClPh CH2 Single bond Sub-73
2-42 Sub-33 3,4-diClPh CH2 Single bond Sub-74
2-43 Sub-33 3,4-diClPh CH2 Single bond Sub-75
2-44 Sub-33 3,4-diClPh CH2 Single bond Sub-76
2-45 Sub-33 3,4-diClPh CH2 Single bond Sub-77
2-46 Sub-33 3,4-diClPh CH2 Single bond Sub-78
2-47 Sub-33 3,4-diClPh CH2 Single bond Sub-79
2-48 Sub-33 3,4-diClPh CH2 Single bond Sub-80
2-49 Sub-34 3,4-diClPh CH2 Single bond Sub-1
2-50 Sub-34 3,4-diClPh CH2 Single bond Sub-2
2-51 Sub-34 3,4-diClPh CH2 Single bond Sub-3
2-52 Sub-34 3,4-diClPh CH2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-53 Sub-34 3,4-diClPh CH2 Single bond Sub-5
2-54 Sub-34 3,4-diClPh CH2 Single bond Sub-6
2-55 Sub-34 3,4-diClPh CH2 Single bond Sub-7
2-56 Sub-34 3,4-diClPh CH2 Single bond Sub-8
2-57 Sub-34 3,4-diClPh CH2 Single bond Sub-9
2-58 Sub-34 3,4-diClPh CH2 Single bond Sub-10
2-59 Sub-34 3,4-diClPh CH2 Single bond Sub-11
2-60 Sub-34 3,4-diClPh CH2 Single bond Sub-12
2-61 Sub-34 3,4-diClPh CH2 Single bond Sub-13
2-62 Sub-34 3,4-diClPh CH2 Single bond Sub-14
2-63 Sub-34 3,4-diClPh CH2 Single bond Sub-15
2-64 Sub-34 3,4-diClPh CH2 Single bond Sub-16
2-65 Sub-34 3,4-diClPh CH2 Single bond Sub-17
2-66 Sub-34 3,4-diClPh CH2 Single bond Sub-18
2-67 Sub-34 3,4-diClPh CH2 Single bond Sub-19
2-68 Sub-34 3,4-diClPh CH2 Single bond Sub-20
2-69 Sub-34 3,4-diClPh CH2 Single bond Sub-21
2-70 Sub-34 3,4-diClPh CH2 Single bond Sub-22
2-71 Sub-34 3,4-diClPh CH2 Single bond Sub-23
2-72 Sub-34 3,4-diClPh CH2 Single bond Sub-24
2-73 Sub-34 3,4-diClPh CH2 Single bond Sub-25
2-74 Sub-34 3,4-diClPh CH2 Single bond Sub-26
2-75 Sub-34 3,4-diClPh CH2 Single bond Sub-27
2-76 Sub-34 3,4-diClPh CH2 Single bond Sub-28
2-77 Sub-34 3,4-diClPh CH2 Single bond Sub-29
2-78 Sub-34 3,4-diClPh CH2 Single bond Sub-30
Table 2(cont.)
The compound sequence Number (C) R1 R2 A B Z
2-79 Sub-34 3,4-diClPh CH2 Single bond Sub-31
2-80 Sub-34 3,4-diClPh CH2 Single bond Sub-32
2-81 Sub-34 3,4-diClPh CH2 Single bond Sub-65
2-82 Sub-34 3,4-diClPh CH2 Single bond Sub-66
2-83 Sub-34 3,4-diClPh CH2 Single bond Sub-67
2-84 Sub-34 3,4-diClPh CH2 Single bond Sub-68
2-85 Sub-34 3,4-diClPh CH2 Single bond Sub-69
2-86 Sub-34 3,4-diClPh CH2 Single bond Sub-70
2-87 Sub-34 3,4-diClPh CH2 Single bond Sub-71
2-88 Sub-34 3,4-diClPh CH2 Single bond Sub-72
2-89 Sub-34 3,4-diClPh CH2 Single bond Sub-73
2-90 Sub-34 3,4-diClPh CH2 Single bond Sub-74
2-91 Sub-34 3,4-diClPh CH2 Single bond Sub-75
2-92 Sub-34 3,4-diClPh CH2 Single bond Sub-76
2-93 Sub-34 3,4-diClPh CH2 Single bond Sub-77
2-94 Sub-34 3,4-diClPh CH2 Single bond Sub-78
2-95 Sub-34 3,4-diClPh CH2 Single bond Sub-79
2-96 Sub-34 3,4-diClPh CH2 Single bond Sub-80
2-97 Sub-35 3,4-diClPh CH2 Single bond Sub-1
2-98 Sub-35 3,4-diClPh CH2 Single bond Sub-2
2-99 Sub-35 3,4-diClPh CH2 Single bond Sub-3
2-100 Sub-35 3,4-diClPh CH2 Single bond Sub-4
2-101 Sub-35 3,4-diClPh CH2 Single bond Sub-5
2-102 Sub-35 3,4-diClPh CH2 Single bond Sub-6
2-103 Sub-35 3,4-diClPh CH2 Single bond Sub-7
2-104 Sub-35 3,4-diClPh CH2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-105 Sub-35 3,4-diClPh CH2 Single bond Sub-9
2-106 Sub-35 3,4-diClPh CH2 Single bond Sub-10
2-107 Sub-35 3,4-diClPh CH2 Single bond Sub-11
2-108 Sub-35 3,4-diClPh CH2 Single bond Sub-12
2-109 Sub-35 3,4-diClPh CH2 Single bond Sub-13
2-110 Sub-35 3,4-diClPh CH2 Single bond Sub-14
2-111 Sub-35 3,4-diClPh CH2 Single bond Sub-15
2-112 Sub-35 3,4-diClPh CH2 Single bond Sub-16
2-113 Sub-35 3,4-diClPh CH2 Single bond Sub-17
2-114 Sub-35 3,4-diClPh CH2 Single bond Sub-18
2-115 Sub-35 3,4-diClPh CH2 Single bond Sub-19
2-116 Sub-35 3,4-diClPH CH2 Single bond Sub-20
2-117 Sub-35 3,4-diClPh CH2 Single bond Sub-21
2-118 Sub-35 3,4-diClPh CH2 Single bond Sub-22
2-119 Sub-35 3,4-diClPh CH2 Single bond Sub-23
2-120 Sub-35 3,4-diClPh CH2 Single bond Sub-24
2-121 Sub-35 3,4-diClPh CH2 Single bond Sub-25
2-122 Sub-35 3,4-diClPh CH2 Single bond Sub-26
2-123 Sub-35 3,4-diClPh CH2 Single bond Sub-27
2-124 Sub-35 3,4-diClPh CH2 Single bond Sub-28
2-125 Sub-35 3,4-diClPh CH2 Single bond Sub-29
2-126 Sub-35 3,4-diClPh CH2 Single bond Sub-30
2-127 Sub-35 3,4-diClPh CH2 Single bond Sub-31
2-128 Sub-35 3,4-diClPh CH2 Single bond Sub-32
2-129 Sub-35 3,4-diClPh CH2 Single bond Sub-65
2-130 Sub-35 3,4-diClPh CH2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-131 Sub-35 3,4-diClPh CH2 Single bond Sub-67
2-132 Sub-35 3,4-diClPh CH2 Single bond Sub-68
2-133 Sub-35 3,4-diClPh CH2 Single bond Sub-69
2-134 Sub-35 3,4-diClPh CH2 Single bond Sub-70
2-135 Sub-35 3,4-diClPh CH2 Single bond Sub-71
2-136 Sub-35 3,4-diClPh CH2 Single bond Sub-72
2-137 Sub-35 3,4-diClPh CH2 Single bond Sub-73
2-138 Sub-35 3,4-diClPh CH2 Single bond Sub-74
2-139 Sub-35 3,4-diClPh CH2 Single bond Sub-75
2-140 Sub-35 3,4-diClPh CH2 Single bond Sub-76
2-141 Sub-35 3,4-diClPh CH2 Single bond Sub-77
2-142 Sub-35 3,4-diClPh CH2 Single bond Sub-78
2-143 Sub-35 3,4-diClPh CH2 Single bond Sub-79
2-144 Sub-35 3,4-diClPh CH2 Single bond Sub-80
2-145 Sub-36 3,4-diClPh CH2 Single bond Sub-1
2-146 Sub-36 3,4-diClPh CH2 Single bond Sub-2
2-147 Sub-36 3,4-diClPh CH2 Single bond Sub-3
2-148 Sub-36 3,4-diClPh CH2 Single bond Sub-4
2-149 Sub-36 3,4-diClPh CH2 Single bond Sub-5
2-150 Sub-36 3,4-diClPh CH2 Single bond Sub-6
2-151 Sub-36 3,4-diClPh CH2 Single bond Sub-7
2-152 Sub-36 3,4-diClPh CH2 Single bond Sub-8
2-153 Sub-36 3,4-diClPh CH2 Single bond Sub-9
2-154 Sub-36 3,4-diClPh CH2 Single bond Sub-10
2-155 Sub-36 3,4-diClPh CH2 Single bond Sub-11
2-156 Sub-36 3,4-diClPh CH2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-157 Sub-36 3,4-diClPh CH2 Single bond Sub-13
2-158 Sub-36 3,4-diClPh CH2 Single bond Sub-14
2-159 Sub-36 3,4-diClPh CH2 Single bond Sub-15
2-160 Sub-36 3,4-diClPh CH2 Single bond Sub-16
2-161 Sub-36 3,4-diClPh CH2 Single bond Sub-17
2-162 Sub-36 3,4-diClPh CH2 Single bond Sub-18
2-163 Sub-36 3,4-diClPh CH2 Single bond Sub-19
2-164 Sub-36 3,4-diClPh CH2 Single bond Sub-20
2-165 Sub-36 3,4-diClPh CH2 Single bond Sub-21
2-166 Sub-36 3,4-diClPh CH2 Single bond Sub-22
2-167 Sub-36 3,4-diClPh CH2 Single bond Sub-23
2-168 Sub-36 3,4-diClPh CH2 Single bond Sub-24
2-169 Sub-36 3,4-diClPh CH2 Single bond Sub-25
2-170 Sub-36 3,4-diClPh CH2 Single bond Sub-26
2-171 Sub-36 3,4-diClPh CH2 Single bond Sub-27
2-172 Sub-36 3,4-diClPh CH2 Single bond Sub-28
2-173 Sub-36 3,4-diClPh CH2 Single bond Sub-29
2-174 Sub-36 3,4-diClPh CH2 Single bond Sub-30
2-175 Sub-36 3,4-diClPh CH2 Single bond Sub-31
2-176 Sub-36 3,4-diClPh CH2 Single bond Sub-32
2-177 Sub-36 3,4-diClPh CH2 Single bond Sub-65
2-178 Sub-36 3,4-diClPh CH2 Single bond Sub-66
2-179 Sub-36 3,4-diClPh CH2 Single bond Sub-67
2-180 Sub-36 3,4-diClPh CH2 Single bond Sub-68
2-181 Sub-36 3,4-diClPh CH2 Single bond Sub-69
2-182 Sub-36 3,4-diClPh CH2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-183 Sub-36 3,4-diClPh CH2 Single bond Sub-71
2-184 Sub-36 3,4-diClPh CH2 Single bond Sub-72
2-185 Sub-36 3,4-diClPh CH2 Single bond Sub-73
2-186 Sub-36 3,4-diClPh CH2 Single bond Sub-74
2-187 Sub-36 3,4-diClPh CH2 Single bond Sub-75
2-188 Sub-36 3,4-diClPh CH2 Single bond Sub-76
2-189 Sub-36 3,4-diClPh CH2 Single bond Sub-77
2-190 Sub-36 3,4-diClPh CH2 Single bond Sub-78
2-191 Sub-36 3,4-diClPh CH2 Single bond Sub-79
2-192 Sub-36 3,4-diClPh CH2 Single bond Sub-80
2-193 Sub-37 3,4-diClPh CH2 Single bond Sub-1
2-194 Sub-37 3,4-diClPh CH2 Single bond Sub-2
2-195 Sub-37 3,4-diClPh CH2 Single bond Sub-3
2-196 Sub-37 3,4-diClPh CH2 Single bond Sub-4
2-197 Sub-37 3,4-diClPh CH2 Single bond Sub-5
2-198 Sub-37 3,4-diClPh CH2 Single bond Sub-6
2-199 Sub-37 3,4-diClPh CH2 Single bond Sub-7
2-200 Sub-37 3,4-diClPh CH2 Single bond Sub-8
2-201 Sub-37 3,4-diClPh CH2 Single bond Sub-9
2-202 Sub-37 3,4-diClPh CH2 Single bond Sub-10
2-203 Sub-37 3,4-diClPh CH2 Single bond Sub-11
2-204 Sub-37 3,4-diClPh CH2 Single bond Sub-12
2-205 Sub-37 3,4-diClPh CH2 Single bond Sub-13
2-206 Sub-37 3,4-diClPh CH2 Single bond Sub-14
2-207 Sub-37 3,4-diClPh CH2 Single bond Sub-15
2-208 Sub-37 3,4-diClPh CH2 Single bond Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-209 Sub-37 3,4-diClPh CH2 Single bond Sub-17
2-210 Sub-37 3,4-diClPh CH2 Single bond Sub-18
2-211 Sub-37 3,4-diClPh CH2 Single bond Sub-19
2-212 Sub-37 3,4-diClPh CH2 Single bond Sub-20
2-213 Sub-37 3,4-diClPh CH2 Single bond Sub-21
2-214 Sub-37 3,4-diClPh CH2 Single bond Sub-22
2-215 Sub-37 3,4-diClPh CH2 Single bond Sub-23
2-216 Sub-37 3,4-diClPh CH2 Single bond Sub-24
2-217 Sub-37 3,4-diClPh CH2 Single bond Sub-25
2-218 Sub-37 3,4-diClPh CH2 Single bond Sub-26
2-219 Sub-37 3,4-diClPh CH2 Single bond Sub-27
2-220 Sub-37 3,4-diClPh CH2 Single bond Sub-28
2-221 Sub-37 3,4-diClPh CH2 Single bond Sub-29
2-222 Sub-37 3,4-diClPh CH2 Single bond Sub-30
2-223 Sub-37 3,4-diClPh CH2 Single bond Sub-31
2-224 Sub-37 3,4-diClPh CH2 Single bond Sub-32
2-225 Sub-37 3,4-diClPh CH2 Single bond Sub-65
2-226 Sub-37 3,4-diClPh CH2 Single bond Sub-66
2-227 Sub-37 3,4-diClPh CH2 Single bond Sub-67
2-228 Sub-37 3,4-diClPh CH2 Single bond Sub-68
2-229 Sub-37 3,4-diClPh CH2 Single bond Sub-69
2-230 Sub-37 3,4-diClPh CH2 Single bond Sub-70
2-231 Sub-37 3,4-diClPh CH2 Single bond Sub-71
2-232 Sub-37 3,4-diClPh CH2 Single bond Sub-72
2-233 Sub-37 3,4-diClPh CH2 Single bond Sub-73
2-234 Sub-37 3,4-diClPh CH2 Single bond Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-235 Sub-37 3,4-diClPh CH2 Single bond Sub-75
2-236 Sub-37 3,4-diClPh CH2 Single bond Sub-76
2-237 Sub-37 3,4-diClPh CH2 Single bond Sub-77
2-238 Sub-37 3,4-diClPh CH2 Single bond Sub-78
2-239 Sub-37 3,4-diClPh CH2 Single bond Sub-79
2-240 Sub-37 3,4-diClPh CH2 Single bond Sub-80
2-241 Sub-38 3,4-diClPh CH2 Single bond Sub-1
2-242 Sub-38 3,4-diClPh CH2 Single bond Sub-2
2-243 Sub-38 3,4-diClPh CH2 Single bond Sub-3
2-244 Sub-38 3,4-diClPh CH2 Single bond Sub-4
2-245 Sub-38 3,4-diClPh CH2 Single bond Sub-5
2-246 Sub-38 3,4-diClPh CH2 Single bond Sub-6
2-247 Sub-38 3,4-diClPh CH2 Single bond Sub-7
2-248 Sub-38 3,4-diClPh CH2 Single bond Sub-8
2-249 Sub-38 3,4-diClPh CH2 Single bond Sub-9
2-250 Sub-38 3,4-diClPh CH2 Single bond Sub-10
2-251 Sub-38 3,4-diClPh CH2 Single bond Sub-11
2-252 Sub-38 3,4-diClPh CH2 Single bond Sub-12
2-253 Sub-38 3,4-diClPh CH2 Single bond Sub-13
2-254 Sub-38 3,4-diClPh CH2 Single bond Sub-14
2-255 Sub-38 3,4-diClPh CH2 Single bond Sub-15
2-256 Sub-38 3,4-diClPh CH2 Single bond Sub-16
2-257 Sub-38 3,4-diClPh CH2 Single bond Sub-17
2-258 Sub-38 3,4-diClPh CH2 Single bond Sub-18
2-259 Sub-38 3,4-diClPh CH2 Single bond Sub-19
2-260 Sub-38 3,4-diClPh CH2 Single bond Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-261 Sub-38 3,4-diClPh CH2 Single bond Sub-21
2-262 Sub-38 3,4-diClPh CH2 Single bond Sub-22
2-263 Sub-38 3,4-diClPh CH2 Single bond Sub-23
2-264 Sub-38 3,4-diClPh CH2 Single bond Sub-24
2-265 Sub-38 3,4-diClPh CH2 Single bond Sub-25
2-266 Sub-38 3,4-diClPh CH2 Single bond Sub-26
2-267 Sub-38 3,4-diClPh CH2 Single bond Sub-27
2-268 Sub-38 3,4-diClPh CH2 Single bond Sub-28
2-269 Sub-38 3,4-diClPh CH2 Single bond Sub-29
2-270 Sub-38 3,4-diClPh CH2 Single bond Sub-30
2-271 Sub-38 3,4-diClPh CH2 Single bond Sub-31
2-272 Sub-38 3,4-diClPh CH2 Single bond Sub-32
2-273 Sub-38 3,4-diClPh CH2 Single bond Sub-65
2-274 Sub-38 3,4-diClPh CH2 Single bond Sub-66
2-275 Sub-38 3,4-diClPh CH2 Single bond Sub-67
2-276 Sub-38 3,4-diClPh CH2 Single bond Sub-68
2-277 Sub-38 3,4-diClPh CH2 Single bond Sub-69
2-278 Sub-38 3,4-diClPh CH2 Single bond Sub-70
2-279 Sub-38 3,4-diClPh CH2 Single bond Sub-71
2-280 Sub-38 3,4-diClPh CH2 Single bond Sub-72
2-281 Sub-38 3,4-diClPh CH2 Single bond Sub-73
2-282 Sub-38 3,4-diClPh CH2 Single bond Sub-74
2-283 Sub-38 3,4-diClPh CH2 Single bond Sub-75
2-284 Sub-38 3,4-diClPh CH2 Single bond Sub-76
2-285 Sub-38 3,4-diClPh CH2 Single bond Sub-77
2-286 Sub-38 3,4-diClPh CH2 Single bond Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-287 Sub-38 3,4-diClPh CH2 Single bond Sub-79
2-288 Sub-38 3,4-diClPh CH2 Single bond Sub-80
2-289 Sub-39 3,4-diClPh CH2 Single bond Sub-1
2-290 Sub-39 3,4-diClPh CH2 Single bond Sub-2
2-291 Sub-39 3,4-diClPh CH2 Single bond Sub-3
2-292 Sub-39 3,4-diClPh CH2 Single bond Sub-4
2-293 Sub-39 3,4-diClPh CH2 Single bond Sub-5
2-294 Sub-39 3,4-diClPh CH2 Single bond Sub-6
2-295 Sub-39 3,4-diClPh CH2 Single bond Sub-7
2-296 Sub-39 3,4-diClPh CH2 Single bond Sub-8
2-297 Sub-39 3,4-diClPh CH2 Single bond Sub-9
2-298 Sub-39 3,4-diClPh CH2 Single bond Sub-10
2-299 Sub-39 3,4-diClPh CH2 Single bond Sub-11
2-300 Sub-39 3,4-diClPh CH2 Single bond Sub-12
2-301 Sub-39 3,4-diClPh CH2 Single bond Sub-13
2-302 Sub-39 3,4-diClPh CH2 Single bond Sub-14
2-303 Sub-39 3,4-diClPh CH2 Single bond Sub-15
2-304 Sub-39 3,4-diClPh CH2 Single bond Sub-16
2-305 Sub-39 3,4-diClPh CH2 Single bond Sub-17
2-306 Sub-39 3,4-diClPh CH2 Single bond Sub-18
2-307 Sub-39 3,4-diClPh CH2 Single bond Sub-19
2-308 Sub-39 3,4-diClPh CH2 Single bond Sub-20
2-309 Sub-39 3,4-diClPh CH2 Single bond Sub-21
2-310 Sub-39 3,4-diClPh CH2 Single bond Sub-22
2-311 Sub-39 3,4-diClPh CH2 Single bond Sub-23
2-312 Sub-39 3,4-diClPh CH2 Single bond Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-313 Sub-39 3,4-diClPh CH2 Single bond Sub-25
2-314 Sub-39 3,4-diClPh CH2 Single bond Sub-26
2-315 Sub-39 3,4-diClPh CH2 Single bond Sub-27
2-316 Sub-39 3,4-diClPh CH2 Single bond Sub-28
2-317 Sub-39 3,4-diClPh CH2 Single bond Sub-29
2-318 Sub-39 3,4-diClPh CH2 Single bond Sub-30
2-319 Sub-39 3,4-diClPh CH2 Single bond Sub-31
2-320 Sub-39 3,4-diClPh CH2 Single bond Sub-32
2-321 Sub-39 3,4-diClPh CH2 Single bond Sub-65
2-322 Sub-39 3,4-diClPh CH2 Single bond Sub-66
2-323 Sub-39 3,4-diClPh CH2 Single bond Sub-67
2-324 Sub-39 3,4-diClPh CH2 Single bond Sub-68
2-325 Sub-39 3,4-diClPh CH2 Single bond Sub-69
2-326 Sub-39 3,4-diClPh CH2 Single bond Sub-70
2-327 Sub-39 3,4-diClPh CH2 Single bond Sub-71
2-328 Sub-39 3,4-diClPh CH2 Single bond Sub-72
2-329 Sub-39 3,4-diClPh CH2 Single bond Sub-73
2-330 Sub-39 3,4-diClPh CH2 Single bond Sub-74
2-331 Sub-39 3,4-diClPh CH2 Single bond Sub-75
2-332 Sub-39 3,4-diClPh CH2 Single bond Sub-76
2-333 Sub-39 3,4-diClPh CH2 Single bond Sub-77
2-334 Sub-39 3,4-diClPh CH2 Single bond Sub-78
2-335 Sub-39 3,4-diClPh CH2 Single bond Sub-79
2-336 Sub-39 3,4-diClPh CH2 Single bond Sub-80
2-337 Sub-40 3,4-diClPh CH2 Single bond Sub-1
2-338 Sub-40 3,4-diClPh CH2 Single bond Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-339 Sub-40 3,4-diClPh CH2 Single bond Sub-3
2-340 Sub-40 3,4-diClPh CH2 Single bond Sub-4
2-341 Sub-40 3,4-diClPh CH2 Single bond Sub-5
2-342 Sub-40 3,4-diClPh CH2 Single bond Sub-6
2-343 Sub-40 3,4-diClPh CH2 Single bond Sub-7
2-344 Sub-40 3,4-diClPh CH2 Single bond Sub-8
2-345 Sub-40 3,4-diClPh CH2 Single bond Sub-9
2-346 Sub-40 3,4-diClPh CH2 Single bond Sub-10
2-347 Sub-40 3,4-diClPh CH2 Single bond Sub-11
2-348 Sub-40 3,4-diClPh CH2 Single bond Sub-12
2-349 Sub-40 3,4-diClPh CH2 Single bond Sub-13
2-350 Sub-40 3,4-diClPh CH2 Single bond Sub-14
2-351 Sub-40 3,4-diClPh CH2 Single bond Sub-15
2-352 Sub-40 3,4-diClPh CH2 Single bond Sub-16
2-353 Sub-40 3,4-diClPh CH2 Single bond Sub-17
2-354 Sub-40 3,4-diClPh CH2 Single bond Sub-18
2-355 Sub-40 3,4-diClPh CH2 Single bond Sub-19
2-356 Sub-40 3,4-diClPh CH2 Single bond Sub-20
2-357 Sub-40 3,4-diClPh CH2 Single bond Sub-21
2-358 Sub-40 3,4-diClPh CH2 Single bond Sub-22
2-359 Sub-40 3,4-diClPh CH2 Single bond Sub-23
2-360 Sub-40 3,4-diClPh CH2 Single bond Sub-24
2-361 Sub-40 3,4-diClPh CH2 Single bond Sub-25
2-362 Sub-40 3,4-diClPh CH2 Single bond Sub-26
2-363 Sub-40 3,4-diClPh CH2 Single bond Sub-27
2-364 Sub-40 3,4-diClPh CH2 Single bond Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-365 Sub-40 3,4-diClPh CH2 Single bond Sub-29
2-366 Sub-40 3,4-diClPh CH2 Single bond Sub-30
2-367 Sub-40 3,4-diClPh CH2 Single bond Sub-31
2-368 Sub-40 3,4-diClPh CH2 Single bond Sub-32
2-369 Sub-40 3,4-diClPh CH2 Single bond Sub-65
2-370 Sub-40 3,4-diClPh CH2 Single bond Sub-66
2-371 Sub-40 3,4-diClPh CH2 Single bond Sub-67
2-372 Sub-40 3,4-diClPh CH2 Single bond Sub-68
2-373 Sub-40 3,4-diClPh CH2 Single bond Sub-69
2-374 Sub-40 3,4-diClPh CH2 Single bond Sub-70
2-375 Sub-40 3,4-diClPh CH2 Single bond Sub-71
2-376 Sub-40 3,4-diClPh CH2 Single bond Sub-72
2-377 Sub-40 3,4-diClPh CH2 Single bond Sub-73
2-378 Sub-40 3,4-diClPh CH2 Single bond Sub-74
2-379 Sub-40 3,4-diClPh CH2 Single bond Sub-75
2-380 Sub-40 3,4-diClPh CH2 Single bond Sub-76
2-381 Sub-40 3,4-diClPh CH2 Single bond Sub-77
2-382 Sub-40 3,4-diClPh CH2 Single bond Sub-78
2-383 Sub-40 3,4-diClPh CH2 Single bond Sub-79
2-384 Sub-40 3,4-diClPh CH2 Single bond Sub-80
2-385 Sub-41 3,4-diClPh CH2 Single bond Sub-1
2-386 Sub-41 3,4-diClPh CH2 Single bond Sub-2
2-387 Sub-41 3,4-diClPh CH2 Single bond Sub-3
2-388 Sub-41 3,4-diClPh CH2 Single bond Sub-4
2-389 Sub-41 3,4-diClPh CH2 Single bond Sub-5
2-390 Sub-41 3,4-diClPh CH2 Single bond Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-391 Sub-41 3,4-diClPh CH2 Single bond Sub-7
2-392 Sub-41 3,4-diClPh CH2 Single bond Sub-8
2-393 Sub-41 3,4-diClPh CH2 Single bond Sub-9
2-394 Sub-41 3,4-diClPh CH2 Single bond Sub-10
2-395 Sub-41 3,4-diClPh CH2 Single bond Sub-11
2-396 Sub-41 3,4-diClPh CH2 Single bond Sub-12
2-397 Sub-41 3,4-diClPh CH2 Single bond Sub-13
2-398 Sub-41 3,4-diClPh CH2 Single bond Sub-14
2-399 Sub-41 3,4-diClPh CH2 Single bond Sub-15
2-400 Sub-41 3,4-diClPh CH2 Single bond Sub-16
2-401 Sub-41 3,4-diClPh CH2 Single bond Sub-17
2-402 Sub-41 3,4-diClPh CH2 Single bond Sub-18
2-403 Sub-41 3,4-diClPh CH2 Single bond Sub-19
2-404 Sub-41 3,4-diClPh CH2 Single bond Sub-20
2-405 Sub-41 3,4-diClPh CH2 Single bond Sub-21
2-406 Sub-41 3,4-diClPh CH2 Single bond Sub-22
2-407 Sub-41 3,4-diClPh CH2 Single bond Sub-23
2-408 Sub-41 3,4-diClPh CH2 Single bond Sub-24
2-409 Sub-41 3,4-diClPh CH2 Single bond Sub-25
2-410 Sub-41 3,4-diClPh CH2 Single bond Sub-26
2-411 Sub-41 3,4-diClPh CH2 Single bond Sub-27
2-412 Sub-41 3,4-diClPh CH2 Single bond Sub-28
2-413 Sub-41 3,4-diClPh CH2 Single bond Sub-29
2-414 Sub-41 3,4-diClPh CH2 Single bond Sub-30
2-415 Sub-41 3,4-diClPh CH2 Single bond Sub-31
2-416 Sub-41 3,4-diClPh CH2 Single bond Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-417 Sub-41 3,4-diClPh CH2 Single bond Sub-65
2-418 Sub-41 3,4-diClPh CH2 Single bond Sub-66
2-419 Sub-41 3,4-diClPh CH2 Single bond Sub-67
2-420 Sub-41 3,4-diClPh CH2 Single bond Sub-68
2-421 Sub-41 3,4-diClPh CH2 Single bond Sub-69
2-422 Sub-41 3,4-diClPh CH2 Single bond Sub-70
2-423 Sub-41 3,4-diClPh CH2 Single bond Sub-71
2-424 Sub-41 3,4-diClPh CH2 Single bond Sub-72
2-425 Sub-41 3,4-diClPh CH2 Single bond Sub-73
2-426 Sub-41 3,4-diClPh CH2 Single bond Sub-74
2-427 Sub-41 3,4-diClPh CH2 Single bond Sub-75
2-428 Sub-41 3,4-diClPh CH2 Single bond Sub-76
2-429 Sub-41 3,4-diClPh CH2 Single bond Sub-77
2-430 Sub-41 3,4-diClPh CH2 Single bond Sub-78
2-431 Sub-41 3,4-diClPh CH2 Single bond Sub-79
2-432 Sub-41 3,4-diClPh CH2 Single bond Sub-80
2-433 Sub-42 3,4-diClPh CH2 Single bond Sub-1
2-434 Sub-42 3,4-diClPh CH2 Single bond Sub-2
2-435 Sub-42 3,4-diClPh CH2 Single bond Sub-3
2-436 Sub-42 3,4-diClPh CH2 Single bond Sub-4
2-437 Sub-42 3,4-diClPh CH2 Single bond Sub-5
2-438 Sub-42 3,4-diClPh CH2 Single bond Sub-6
2-439 Sub-42 3,4-diClPh CH2 Single bond Sub-7
2-440 Sub-42 3,4-diClPh CH2 Single bond Sub-8
2-441 Sub-42 3,4-diClPh CH2 Single bond Sub-9
2-442 Sub-42 3,4-diClPh CH2 Single bond Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-443 Sub-42 3,4-diClPh CH2 Single bond Sub-11
2-444 Sub-42 3,4-diClPh CH2 Single bond Sub-12
2-445 Sub-42 3,4-diClPh CH2 Single bond Sub-13
2-446 Sub-42 3,4-diClPh CH2 Single bond Sub-14
2-447 Sub-42 3,4-diClPh CH2 Single bond Sub-15
2-448 Sub-42 3,4-diClPh CH2 Single bond Sub-16
2-449 Sub-42 3,4-diClPh CH2 Single bond Sub-17
2-450 Sub-42 3,4-diClPh CH2 Single bond Sub-18
2-451 Sub-42 3,4-diClPh CH2 Single bond Sub-19
2-452 Sub-42 3,4-diClPh CH2 Single bond Sub-20
2-453 Sub-42 3,4-diClPh CH2 Single bond Sub-21
2-454 Sub-42 3,4-diClPh CH2 Single bond Sub-22
2-455 Sub-42 3,4-diClPh CH2 Single bond Sub-23
2-456 Sub-42 3,4-diClPh CH2 Single bond Sub-24
2-457 Sub-42 3,4-diClPh CH2 Single bond Sub-25
2-458 Sub-42 3,4-diClPh CH2 Single bond Sub-26
2-459 Sub-42 3,4-diClPh CH2 Single bond Sub-27
2-460 Sub-42 3,4-diClPh CH2 Single bond Sub-28
2-461 Sub-42 3,4-diClPh CH2 Single bond Sub-29
2-462 Sub-42 3,4-diClPh CH2 Single bond Sub-30
2-463 Sub-42 3,4-diClPh CH2 Single bond Sub-31
2-464 Sub-42 3,4-diClPh CH2 Single bond Sub-32
2-465 Sub-42 3,4-diClPh CH2 Single bond Sub-65
2-466 Sub-42 3,4-diClPh CH2 Single bond Sub-66
2-467 Sub-42 3,4-diClPh CH2 Single bond Sub-67
2-468 Sub-42 3,4-diClPh CH2 Single bond Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-469 Sub-42 3,4-diClPh CH2 Single bond Sub-69
2-470 Sub-42 3,4-diClPh CH2 Single bond Sub-70
2-471 Sub-42 3,4-diClPh CH2 Single bond Sub-71
2-472 Sub-42 3,4-diClPh CH2 Single bond Sub-72
2-473 Sub-42 3,4-diClPh CH2 Single bond Sub-73
2-474 Sub-42 3,4-diClPh CH2 Single bond Sub-74
2-475 Sub-42 3,4-diClPh CH2 Single bond Sub-75
2-476 Sub-42 3,4-diClPh CH2 Single bond Sub-76
2-477 Sub-42 3,4-diClPh CH2 Single bond Sub-77
2-478 Sub-42 3,4-diClPh CH2 Single bond Sub-78
2-479 Sub-42 3,4-diClPh CH2 Single bond Sub-79
2-480 Sub-42 3,4-diClPh CH2 Single bond Sub-80
2-481 Sub-43 3,4-diClPh CH2 Single bond Sub-1
2-482 Sub-43 3,4-diClPh CH2 Single bond Sub-2
2-483 Sub-43 3,4-diClPh CH2 Single bond Sub-3
2-484 Sub-43 3,4-diClPh CH2 Single bond Sub-4
2-485 Sub-43 3,4-diClPh CH2 Single bond Sub-5
2-486 Sub-43 3,4-diClPh CH2 Single bond Sub-6
2-487 Sub-43 3,4-diClPh CH2 Single bond Sub-7
2-488 Sub-43 3,4-diClPh CH2 Single bond Sub-8
2-489 Sub-43 3,4-diClPh CH2 Single bond Sub-9
2-490 Sub-43 3,4-diClPh CH2 Single bond Sub-10
2-491 Sub-43 3,4-diClPh CH2 Single bond Sub-11
2-492 Sub-43 3,4-diClPh CH2 Single bond Sub-12
2-493 Sub-43 3,4-diClPh CH2 Single bond Sub-13
2-494 Sub-43 3,4-diClPh CH2 Single bond Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-495 Sub-43 3,4-diClPh CH2 Single bond Sub-15
2-496 Sub-43 3,4-diClPh CH2 Single bond Sub-16
2-497 Sub-43 3,4-diClPh CH2 Single bond Sub-17
2-498 Sub-43 3,4-diClPh CH2 Single bond Sub-18
2-499 Sub-43 3,4-diClPh CH2 Single bond Sub-19
2-500 Sub-43 3,4-diClPh CH2 Single bond Sub-20
2-501 Sub-43 3,4-diClPh CH2 Single bond Sub-21
2-502 Sub-43 3,4-diClPh CH2 Single bond Sub-22
2-503 Sub-43 3,4-diClPh CH2 Single bond Sub-23
2-504 Sub-43 3,4-diClPh CH2 Single bond Sub-24
2-505 Sub-43 3,4-diClPh CH2 Single bond Sub-25
2-506 Sub-43 3,4-diClPh CH2 Single bond Sub-26
2-507 Sub-43 3,4-diClPh CH2 Single bond Sub-27
2-508 Sub-43 3,4-diClPh CH2 Single bond Sub-28
2-509 Sub-43 3,4-diClPh CH2 Single bond Sub-29
2-510 Sub-43 3,4-diClPh CH2 Single bond Sub-30
2-511 Sub-43 3,4-diClPh CH2 Single bond Sub-31
2-512 Sub-43 3,4-diClPh CH2 Single bond Sub-32
2-513 Sub-43 3,4-diClPh CH2 Single bond Sub-65
2-514 Sub-43 3,4-diClPh CH2 Single bond Sub-66
2-515 Sub-43 3,4-diClPh CH2 Single bond Sub-67
2-516 Sub-43 3,4-diClPh CH2 Single bond Sub-68
2-517 Sub-43 3,4-diClPh CH2 Single bond Sub-69
2-518 Sub-43 3,4-diClPh CH2 Single bond Sub-70
2-519 Sub-43 3,4-diClPh CH2 Single bond Sub-71
2-520 Sub-43 3,4-diClPh CH2 Single bond Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-521 Sub-43 3,4-diClPh CH2 Single bond Sub-73
2-522 Sub-43 3,4-diClPh CH2 Single bond Sub-74
2-523 Sub-43 3,4-diClPh CH2 Single bond Sub-75
2-524 Sub-43 3,4-diClPh CH2 Single bond Sub-76
2-525 Sub-43 3,4-diClPh CH2 Single bond Sub-77
2-526 Sub-43 3,4-diClPh CH2 Single bond Sub-78
2-527 Sub-43 3,4-diClPh CH2 Single bond Sub-79
2-528 Sub-43 3,4-diClPh CH2 Single bond Sub-80
2-529 Sub-44 3,4-diClPh CH2 Single bond Sub-1
2-530 Sub-44 3,4-diClPh CH2 Single bond Sub-2
2-531 Sub-44 3,4-diClPh CH2 Single bond Sub-3
2-532 Sub-44 3,4-diClPh CH2 Single bond Sub-4
2-533 Sub-44 3,4-diClPh CH2 Single bond Sub-5
2-534 Sub-44 3,4-diClPh CH2 Single bond Sub-6
2-535 Sub-44 3,4-diClPh CH2 Single bond Sub-7
2-536 Sub-44 3,4-diClPh CH2 Single bond Sub-8
2-537 Sub-44 3,4-diClPh CH2 Single bond Sub-9
2-538 Sub-44 3,4-diClPh CH2 Single bond Sub-10
2-539 Sub-44 3,4-diClPh CH2 Single bond Sub-11
2-540 Sub-44 3,4-diClPh CH2 Single bond Sub-12
2-541 Sub-44 3,4-diClPh CH2 Single bond Sub-13
2-542 Sub-44 3,4-diClPh CH2 Single bond Sub-14
2-543 Sub-44 3,4-diClPh CH2 Single bond Sub-15
2-544 Sub-44 3,4-diClPh CH2 Single bond Sub-16
2-545 Sub-44 3,4-diClPh CH2 Single bond Sub-17
2-546 Sub-44 3,4-diClPh CH2 Single bond Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-547 Sub-44 3,4-diClPh CH2 Single bond Sub-19
2-548 Sub-44 3,4-diClPh CH2 Single bond Sub-20
2-549 Sub-44 3,4-diClPh CH2 Single bond Sub-21
2-550 Sub-44 3,4-diClPh CH2 Single bond Sub-22
2-551 Sub-44 3,4-diClPh CH2 Single bond Sub-23
2-552 Sub-44 3,4-diClPh CH2 Single bond Sub-24
2-553 Sub-44 3,4-diClPh CH2 Single bond Sub-25
2-554 Sub-44 3,4-diClPh CH2 Single bond Sub-26
2-555 Sub-44 3,4-diClPh CH2 Single bond Sub-27
2-556 Sub-44 3,4-diClPh CH2 Single bond Sub-28
2-557 Sub-44 3,4-diClPh CH2 Single bond Sub-29
2-558 Sub-44 3,4-diClPh CH2 Single bond Sub-30
2-559 Sub-44 3,4-diClPh CH2 Single bond Sub-31
2-560 Sub-44 3,4-diClPh CH2 Single bond Sub-32
2-561 Sub-44 3,4-diClPh CH2 Single bond Sub-65
2-562 Sub-44 3,4-diClPh CH2 Single bond Sub-66
2-563 Sub-44 3,4-diClPh CH2 Single bond Sub-67
2-564 Sub-44 3,4-diClPh CH2 Single bond Sub-68
2-565 Sub-44 3,4-diClPh CH2 Single bond Sub-69
2-566 Sub-44 3,4-diClPh CH2 Single bond Sub-70
2-567 Sub-44 3,4-diClPh CH2 Single bond Sub-71
2-568 Sub-44 3,4-diClPh CH2 Single bond Sub-72
2-569 Sub-44 3,4-diClPh CH2 Single bond Sub-73
2-570 Sub-44 3,4-diClPh CH2 Single bond Sub-74
2-571 Sub-44 3,4-diClPh CH2 Single bond Sub-75
2-572 Sub-44 3,4-diClPh CH2 Single bond Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-573 Sub-44 3,4-diClPh CH2 Single bond Sub-77
2-574 Sub-44 3,4-diClPh CH2 Single bond Sub-78
2-575 Sub-44 3,4-diClPh CH2 Single bond Sub-79
2-576 Sub-44 3,4-diClPh CH2 Single bond Sub-80
2-577 Sub-45 3,4-diClPh CH2 Single bond Sub-1
2-578 Sub-45 3,4-diClPh CH2 Single bond Sub-2
2-579 Sub-45 3,4-diClPh CH2 Single bond Sub-3
2-580 Sub-45 3,4-diClPh CH2 Single bond Sub-4
2-581 Sub-45 3,4-diClPh CH2 Single bond Sub-5
2-582 Sub-45 3,4-diClPh CH2 Single bond Sub-6
2-583 Sub-45 3,4-diClPh CH2 Single bond Sub-7
2-584 Sub-45 3,4-diClPh CH2 Single bond Sub-8
2-585 Sub-45 3,4-diClPh CH2 Single bond Sub-9
2-586 Sub-45 3,4-diClPh CH2 Single bond Sub-10
2-587 Sub-45 3,4-diClPh CH2 Single bond Sub-11
2-588 Sub-45 3,4-diClPh CH2 Single bond Sub-12
2-589 Sub-45 3,4-diClPh CH2 Single bond Sub-13
2-590 Sub-45 3,4-diClPh CH2 Single bond Sub-14
2-591 Sub-45 3,4-diClPh CH2 Single bond Sub-15
2-592 Sub-45 3,4-diClPh CH2 Single bond Sub-16
2-593 Sub-45 3,4-diClPh CH2 Single bond Sub-17
2-594 Sub-45 3,4-diClPh CH2 Single bond Sub-18
2-595 Sub-45 3,4-diClPh CH2 Single bond Sub-19
2-596 Sub-45 3,4-diClPh CH2 Single bond Sub-20
2-597 Sub-45 3,4-diClPh CH2 Single bond Sub-21
2-598 Sub-45 3,4-diClPh CH2 Single bond Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-599 Sub-45 3,4-diClPh CH2 Single bond Sub-23
2-600 Sub-45 3,4-diClPh CH2 Single bond Sub-24
2-601 Sub-45 3,4-diClPh CH2 Single bond Sub-25
2-602 Sub-45 3,4-diClPh CH2 Single bond Sub-26
2-603 Sub-45 3,4-diClPh CH2 Single bond Sub-27
2-604 Sub-45 3,4-diClPh CH2 Single bond Sub-28
2-605 Sub-45 3,4-diClPh CH2 Single bond Sub-29
2-606 Sub-45 3,4-diClPh CH2 Single bond Sub-30
2-607 Sub-45 3,4-diClPh CH2 Single bond Sub-31
2-608 Sub-45 3,4-diClPh CH2 Single bond Sub-32
2-609 Sub-45 3,4-diClPh CH2 Single bond Sub-65
2-610 Sub-45 3,4-diClPh CH2 Single bond Sub-66
2-611 Sub-45 3,4-diClPh CH2 Single bond Sub-67
2-612 Sub-45 3,4-diClPh CH2 Single bond Sub-68
2-613 Sub-45 3,4-diClPh CH2 Single bond Sub-69
2-614 Sub-45 3,4-diClPh CH2 Single bond Sub-70
2-615 Sub-45 3,4-diClPh CH2 Single bond Sub-71
2-616 Sub-45 3,4-diClPh CH2 Single bond Sub-72
2-617 Sub-45 3,4-diClPh CH2 Single bond Sub-73
2-618 Sub-45 3,4-diClPh CH2 Single bond Sub-74
2-619 Sub-45 3,4-diClPh CH2 Single bond Sub-75
2-620 Sub-45 3,4-diClPh CH2 Single bond Sub-76
2-621 Sub-45 3,4-diClPh CH2 Single bond Sub-77
2-622 Sub-45 3,4-diClPh CH2 Single bond Sub-78
2-623 Sub-45 3,4-diClPh CH2 Single bond Sub-79
2-624 Sub-45 3,4-diClPh CH2 Single bond Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-625 Sub-46 3,4-diClPh CH2 Single bond Sub-1
2-626 Sub-46 3,4-diClPh CH2 Single bond Sub-2
2-627 Sub-46 3,4-diClPh CH2 Single bond Sub-3
2-628 Sub-46 3,4-diClPh CH2 Single bond Sub-4
2-629 Sub-46 3,4-diClPh CH2 Single bond Sub-5
2-630 Sub-46 3,4-diClPh CH2 Single bond Sub-6
2-631 Sub-46 3,4-diClPh CH2 Single bond Sub-7
2-632 Sub-46 3,4-diClPh CH2 Single bond Sub-8
2-633 Sub-46 3,4-diClPh CH2 Single bond Sub-9
2-634 Sub-46 3,4-diClPh CH2 Single bond Sub-10
2-635 Sub-46 3,4-diClPh CH2 Single bond Sub-11
2-636 Sub-46 3,4-diClPh CH2 Single bond Sub-12
2-637 Sub-46 3,4-diClPh CH2 Single bond Sub-13
2-638 Sub-46 3,4-diClPh CH2 Single bond Sub-14
2-639 Sub-46 3,4-diClPh CH2 Single bond Sub-15
2-640 Sub-46 3,4-diClPh CH2 Single bond Sub-16
2-641 Sub-46 3,4-diClPh CH2 Single bond Sub-17
2-642 Sub-46 3,4-diClPh CH2 Single bond Sub-18
2-643 Sub-46 3,4-diClPh CH2 Single bond Sub-19
2-644 Sub-46 3,4-diClPh CH2 Single bond Sub-20
2-645 Sub-46 3,4-diClPh CH2 Single bond Sub-21
2-646 Sub-46 3,4-diClPh CH2 Single bond Sub-22
2-647 Sub-46 3,4-diClPh CH2 Single bond Sub-23
2-648 Sub-46 3,4-diClPh CH2 Single bond Sub-24
2-649 Sub-46 3,4-diClPh CH2 Single bond Sub-25
2-650 Sub-46 3,4-diClPh CH2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-651 Sub-46 3,4-diClPh CH2 Single bond Sub-27
2-652 Sub-46 3,4-diClPh CH2 Single bond Sub-28
2-653 Sub-46 3,4-diClPh CH2 Single bond Sub-29
2-654 Sub-46 3,4-diClPh CH2 Single bond Sub-30
2-655 Sub-46 3,4-diClPh CH2 Single bond Sub-31
2-656 Sub-46 3,4-diClPh CH2 Single bond Sub-32
2-657 Sub-46 3,4-diClPh CH2 Single bond Sub-65
2-658 Sub-46 3,4-diClPh CH2 Single bond Sub-66
2-659 Sub-46 3,4-diClPh CH2 Single bond Sub-67
2-660 Sub-46 3,4-diClPh CH2 Single bond Sub-68
2-661 Sub-46 3,4-diClPh CH2 Single bond Sub-69
2-662 Sub-46 3,4-diClPh CH2 Single bond Sub-70
2-663 Sub-46 3,4-diClPh CH2 Single bond Sub-71
2-664 Sub-46 3,4-diClPh CH2 Single bond Sub-72
2-665 Sub-46 3,4-diClPh CH2 Single bond Sub-73
2-666 Sub-46 3,4-diClPh CH2 Single bond Sub-74
2-667 Sub-46 3,4-diClPh CH2 Single bond Sub-75
2-668 Sub-46 3,4-diClPh CH2 Single bond Sub-76
2-669 Sub-46 3,4-diClPh CH2 Single bond Sub-77
2-670 Sub-46 3,4-diClPh CH2 Single bond Sub-78
2-671 Sub-46 3,4-diClPh CH2 Single bond Sub-79
2-672 Sub-46 3,4-diClPh CH2 Single bond Sub-80
2-673 Sub-47 3,4-diClPh CH2 Single bond Sub-1
2-674 Sub-47 3,4-diClPh CH2 Single bond Sub-2
2-675 Sub-47 3,4-diClPh CH2 Single bond Sub-3
2-676 Sub-47 3,4-diClPh CH2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-677 Sub-47 3,4-diClPh CH2 Single bond Sub-5
2-678 Sub-47 3,4-diClPh CH2 Single bond Sub-6
2-679 Sub-47 3,4-diClPh CH2 Single bond Sub-7
2-680 Sub-47 3,4-diClPh CH2 Single bond Sub-8
2-681 Sub-47 3,4-diClPh CH2 Single bond Sub-9
2-682 Sub-47 3,4-diClPh CH2 Single bond Sub-10
2-683 Sub-47 3,4-diClPh CH2 Single bond Sub-11
2-684 Sub-47 3,4-diClPh CH2 SheetKey with a key body Sub-12
2-685 Sub-47 3,4-diClPh CH2 Single bond Sub-13
2-686 Sub-47 3,4-diClPh CH2 Single bond Sub-14
2-687 Sub-47 3,4-diClPh CH2 Single bond Sub-15
2-688 Sub-47 3,4-diClPh CH2 Single bond Sub-16
2-689 Sub-47 3,4-diClPh CH2 Single bond Sub-17
2-690 Sub-47 3,4-diClPh CH2 Single bond Sub-18
2-691 Sub-47 3,4-diClPh CH2 Single bond Sub-19
2-692 Sub-47 3,4-diClPh CH2 Single bond Sub-20
2-693 Sub-47 3,4-diClPh CH2 Single bond Sub-21
2-694 Sub-47 3,4-diClPh CH2 Single bond Sub-22
2-695 Sub-47 3,4-diClPh CH2 Single bond Sub-23
2-696 Sub-47 3,4-diClPh CH2 Single bond Sub-24
2-697 Sub-47 3,4-diClPh CH2 Single bond Sub-25
2-698 Sub-47 3,4-diClPh CH2 Single bond Sub-26
2-699 Sub-47 3,4-diClPh CH2 Single bond Sub-27
2-700 Sub-47 3,4-diClPh CH2 Single bond Sub-28
2-701 Sub-47 3,4-diClPh CH2 Single bond Sub-29
2-702 Sub-47 3,4-diClPh CH2 Single bond Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-703 Sub-47 3,4-diClPh CH2 Single bond Sub-31
2-704 Sub-47 3,4-diClPh CH2 Single bond Sub-32
2-705 Sub-47 3,4-diClPh CH2 Single bond Sub-65
2-706 Sub-47 3,4-diClPh CH2 Single bond Sub-66
2-707 Sub-47 3,4-diClPh CH2 Single bond Sub-67
2-708 Sub-47 3,4-diClPh CH2 Single bond Sub-68
2-709 Sub-47 3,4-diClPh CH2 Single bond Sub-69
2-710 Sub-47 3,4-diClPh CH2 Single bond Sub-70
2-711 Sub-47 3,4-diClPh CH2 Single bond Sub-71
2-712 Sub-47 3,4-diClPh CH2 Single bond Sub-72
2-713 Sub-47 3,4-diClPh CH2 Single bond Sub-73
2-714 Sub-47 3,4-diClPh CH2 Single bond Sub-74
2-715 Sub-47 3,4-diClPh CH2 Single bond Sub-75
2-716 Sub-47 3,4-diClPh CH2 Single bond Sub-76
2-717 Sub-47 3,4-diClPh CH2 Single bond Sub-77
2-718 Sub-47 3,4-diClPh CH2 Single bond Sub-78
2-719 Sub-47 3,4-diClPh CH2 Single bond Sub-79
2-720 Sub-47 3,4-diClPh CH2 Single bond Sub-80
2-721 Sub-81 3,4-diClPh CH2 Single bond Sub-1
2-722 Sub-81 3,4-diClPh CH2 Single bond Sub-2
2-723 Sub-81 3,4-diClPh CH2 Single bond Sub-3
2-724 Sub-81 3,4-diClPh CH2 Single bond Sub-4
2-725 Sub-81 3,4-diClPh CH2 Single bond Sub-5
2-726 Sub-81 3,4-diClPh CH2 Single bond Sub-6
2-727 Sub-81 3,4-diClPh CH2 Single bond Sub-7
2-728 Sub-81 3,4-diClPh CH2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-729 Sub-81 3,4-diClPh CH2 Single bond Sub-9
2-730 Sub-81 3,4-diClPh CH2 Single bond Sub-10
2-731 Sub-81 3,4-diClPh CH2 Single bond Sub-11
2-732 Sub-81 3,4-diClPh CH2 Single bond Sub-12
2-733 Sub-81 3,4-diClPh CH2 Single bond Sub-13
2-734 Sub-81 3,4-diClPh CH2 Single bond Sub-14
2-735 Sub-81 3,4-diClPh CH2 Single bond Sub-15
2-736 Sub-81 3,4-diClPh CH2 Single bond Sub-16
2-737 Sub-81 3,4-diClPh CH2 Single bond Sub-17
2-738 Sub-81 3,4-diClPh CH2 Single bond Sub-18
2-739 Sub-81 3,4-diClPh CH2 Single bond Sub-19
2-740 Sub-81 3,4-diClPh CH2 Single bond Sub-20
2-741 Sub-81 3,4-diClPh CH2 Single bond Sub-21
2-742 Sub-81 3,4-diClPh CH2 Single bond Sub-22
2-743 Sub-81 3,4-diClPh CH2 Single bond Sub-23
2-744 Sub-81 3,4-diClPh CH2 Single bond Sub-24
2-745 Sub-81 3,4-diClPh CH2 Single bond Sub-25
2-746 Sub-81 3,4-diClPh CH2 Single bond Sub-26
2-747 Sub-81 3,4-diClPh CH2 Single bond Sub-27
2-748 Sub-81 3,4-diClPh CH2 Single bond Sub-28
2-749 Sub-81 3,4-diClPh CH2 Single bond Sub-29
2-750 Sub-81 3,4-diClPh CH2 Single bond Sub-30
2-751 Sub-81 3,4-diClPh CH2 Single bond Sub-31
2-752 Sub-81 3,4-diClPh CH2 Single bond Sub-32
2-753 Sub-81 3,4-diClPh CH2 Single bond Sub-65
2-754 Sub-81 3,4-diClPh CH2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-755 Sub-81 3,4-diClPh CH2 Single bond Sub-67
2-756 Sub-81 3,4-diClPh CH2 Single bond Sub-68
2-757 Sub-81 3,4-diClPh CH2 Single bond Sub-69
2-758 Sub-81 3,4-diClPh CH2 Single bond Sub-70
2-759 Sub-81 3,4-diClPh CH2 Single bond Sub-71
2-760 Sub-81 3,4-diClPh CH2 Single bond Sub-72
2-761 Sub-81 3,4-diClPh CH2 Single bond Sub-73
2-762 Sub-81 3,4-diClPh CH2 Single bond Sub-74
2-763 Sub-81 3,4-diClPh CH2 Single bond Sub-75
2-764 Sub-81 3,4-diClPh CH2 Single bond Sub-76
2-765 Sub-81 3,4-diClPh CH2 Single bond Sub-77
2-766 Sub-81 3,4-diClPh CH2 Single bond Sub-78
2-767 Sub-81 3,4-diClPh CH2 Single bond Sub-79
2-768 Sub-81 3,4-diClPh CH2 Single bond Sub-80
2-769 Sub-48 3,4-diClPh CH2 Single bond Sub-1
2-770 Sub-48 3,4-diClPh CH2 Single bond Sub-2
2-771 Sub-48 3,4-diClPh CH2 Single bond Sub-3
2-772 Sub-48 3,4-diClPh CH2 Single bond Sub-4
2-773 Sub-48 3,4-diClPh CH2 Single bond Sub-5
2-774 Sub-48 3,4-diClPh CH2 Single bond Sub-6
2-775 Sub-48 3,4-diClPh CH2 Single bond Sub-7
2-776 Sub-48 3,4-diClPh CH2 Single bond Sub-8
2-777 Sub-48 3,4-diClPh CH2 Single bond Sub-9
2-778 Sub-48 3,4-diClPh CH2 Single bond Sub-10
2-779 Sub-48 3,4-diClPh CH2 Single bond Sub-11
2-780 Sub-48 3,4-diClPh CH2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-781 Sub-48 3,4-diClPh CH2 Single bond Sub-13
2-782 Sub-48 3,4-diClPh CH2 Single bond Sub-14
2-783 Sub-48 3,4-diClPh CH2 Single bond Sub-15
2-784 Sub-48 3,4-diClPh CH2 Single bond Sub-16
2-785 Sub-48 3,4-diClPh CH2 Single bond Sub-17
2-786 Sub-48 3,4-diClPh CH2 Single bond Sub-18
2-787 Sub-48 3,4-diClPh CH2 Single bond Sub-19
2-788 Sub-48 3,4-diClPh CH2 Single bond Sub-20
2-789 Sub-48 3,4-diClPh CH2 Single bond Sub-21
2-790 Sub-48 3,4-diClPh CH2 Single bond Sub-22
2-791 Sub-48 3,4-diClPh CH2 Single bond Sub-23
2-792 Sub-48 3,4-diClPh CH2 Single bond Sub-24
2-793 Sub-48 3,4-diClPh CH2 Single bond Sub-25
2-794 Sub-48 3,4-diClPh CH2 Single bond Sub-26
2-795 Sub-48 3,4-diClPh CH2 Single bond Sub-27
2-796 Sub-48 3,4-diClPh CH2 Single bond Sub-28
2-797 Sub-48 3,4-diClPh CH2 Single bond Sub-29
2-798 Sub-48 3,4-diClPh CH2 Single bond Sub-30
2-799 Sub-48 3,4-diClPh CH2 Single bond Sub-31
2-800 Sub-48 3,4-diClPh CH2 Single bond Sub-32
2-801 Sub-48 3,4-diClPh CH2 Single bond Sub-65
2-802 Sub-48 3,4-diClPh CH2 Single bond Sub-66
2-803 Sub-48 3,4-diClPh CH2 Single bond Sub-67
2-804 Sub-48 3,4-diClPh CH2 Single bond Sub-68
2-805 Sub-48 3,4-diClPh CH2 Single bond Sub-69
2-806 Sub-48 3,4-diClPh CH2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-807 Sub-48 3,4-diClPh CH2 Single bond Sub-71
2-808 Sub-48 3,4-diClPh CH2 Single bond Sub-72
2-809 Sub-48 3,4-diClPh CH2 Single bond Sub-73
2-810 Sub-48 3,4-diClPh CH2 Single bond Sub-74
2-811 Sub-48 3,4-diClPh CH2 Single bond Sub-75
2-812 Sub-48 3,4-diClPh CH2 Single bond Sub-76
2-813 Sub-48 3,4-diClPh CH2 Single bond Sub-77
2-814 Sub-48 3,4-diClPh CH2 Single bond Sub-78
2-815 Sub-48 3,4-diClPh CH2 Single bond Sub-79
2-816 Sub-48 3,4-diClPh CH2 Single bond Sub-80
2-817 Sub-49 3,4-diClPh CH2 Single bond Sub-1
2-818 Sub-49 3,4-diClPh CH2 Single bond Sub-2
2-819 Sub-49 3,4-diClPh CH2 Single bond Sub-3
2-820 Sub-49 3,4-diClPh CH2 Single bond Sub-4
2-821 Sub-49 3,4-diClPh CH2 Single bond Sub-5
2-822 Sub-49 3,4-diClPh CH2 Single bond Sub-6
2-823 Sub-49 3,4-diClPh CH2 Single bond Sub-7
2-824 Sub-49 3,4-diClPh CH2 Single bond Sub-8
2-825 Sub-49 3,4-diClPh CH2 Single bond Sub-9
2-826 Sub-49 3,4-diClPh CH2 Single bond Sub-10
2-827 Sub-49 3,4-diClPh CH2 Single bond Sub-11
2-828 Sub-49 3,4-diClPh CH2 Single bond Sub-12
2-829 Sub-49 3,4-diClPh CH2 Single bond Sub-13
2-830 Sub-49 3,4-diClPh CH2 Single bond Sub-14
2-831 Sub-49 3,4-diClPh CH2 Single bond Sub-15
2-832 Sub-49 3,4-diClPh CH2 Single bond Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-833 Sub-49 3,4-diClPh CH2 Single bond Sub-17
2-834 Sub-49 3,4-diClPh CH2 Single bond Sub-18
2-835 Sub-49 3,4-diClPh CH2 Single bond Sub-19
2-836 Sub-49 3,4-diClPh CH2 Single bond Sub-20
2-837 Sub-49 3,4-diClPh CH2 Single bond Sub-21
2-838 Sub-49 3,4-diClPh CH2 Single bond Sub-22
2-839 Sub-49 3,4-diClPh CH2 Single bond Sub-23
2-840 Sub-49 3,4-diClPh CH2 Single bond Sub-24
2-841 Sub-49 3,4-diClPh CH2 Single bond Sub-25
2-842 Sub-49 3,4-diClPh CH2 Single bond Sub-26
2-843 Sub-49 3,4-diClPh CH2 Single bond Sub-27
2-844 Sub-49 3,4-diClPh CH2 Single bond Sub-28
2-845 Sub-49 3,4-diClPh CH2 Single bond Sub-29
2-846 Sub-49 3,4-diClPh CH2 Single bond Sub-30
2-847 Sub-49 3,4-diClPh CH2 Single bond Sub-31
2-848 Sub-49 3,4-diClPh CH2 Single bond Sub-32
2-849 Sub-49 3,4-diClPh CH2 Single bond Sub-65
2-850 Sub-49 3,4-diClPh CH2 Single bond Sub-66
2-851 Sub-49 3,4-diClPh CH2 Single bond Sub-67
2-852 Sub-49 3,4-diClPh CH2 Single bond Sub-68
2-853 Sub-49 3,4-diClPh CH2 Single bond Sub-69
2-854 Sub-49 3,4-diClPh CH2 Single bond Sub-70
2-855 Sub-49 3,4-diClPh CH2 Single bond Sub-71
2-856 Sub-49 3,4-diClPh CH2 Single bond Sub-72
2-857 Sub-49 3,4-diClPh CH2 Single bond Sub-73
2-858 Sub-49 3,4-diClPh CH2 Single bond Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-859 Sub-49 3,4-diClPh CH2 Single bond Sub-75
2-860 Sub-49 3,4-diClPh CH2 Single bond Sub-76
2-861 Sub-49 3,4-diClPh CH2 Single bond Sub-77
2-862 Sub-49 3,4-diClPh CH2 Single bond Sub-78
2-863 Sub-49 3,4-diClPh CH2 Single bond Sub-79
2-864 Sub-49 3,4-diClPh CH2 Single bond Sub-80
2-865 Sub-50 3,4-diClPh CH2 Single bond Sub-1
2-866 Sub-50 3,4-diClPh CH2 Single bond Sub-2
2-867 Sub-50 3,4-diClPh CH2 Single bond Sub-3
2-868 Sub-50 3,4-diClPh CH2 Single bond Sub-4
2-869 Sub-50 3,4-diClPh CH2 Single bond Sub-5
2-870 Sub-50 3,4-diClPh CH2 Single bond Sub-6
2-871 Sub-50 3,4-diClPh CH2 Single bond Sub-7
2-872 Sub-50 3,4-diClPh CH2 Single bond Sub-8
2-873 Sub-50 3,4-diClPh CH2 Single bond Sub-9
2-874 Sub-50 3,4-diClPh CH2 Single bond Sub-10
2-875 Sub-50 3,4-diClPh CH2 Single bond Sub-11
2-876 Sub-50 3,4-diClPh CH2 Single bond Sub-12
2-877 Sub-50 3,4-diClPh CH2 Single bond Sub-13
2-878 Sub-50 3,4-diClPh CH2 Single bond Sub-14
2-879 Sub-50 3,4-diClPh CH2 Single bond Sub-15
2-880 Sub-50 3,4-diClPh CH2 Single bond Sub-16
2-881 Sub-50 3,4-diClPh CH2 Single bond Sub-17
2-882 Sub-50 3,4-diClPh CH2 Single bond Sub-18
2-883 Sub-50 3,4-diClPh CH2 Single bond Sub-19
2-884 Sub-50 3,4-diClPh CH2 Single bond Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-885 Sub-50 3,4-diClPh CH2 Single bond Sub-21
2-886 Sub-50 3,4-diClPh CH2 Single bond Sub-22
2-887 Sub-50 3,4-diClPh CH2 Single bond Sub-23
2-888 Sub-50 3,4-diClPh CH2 Single bond Sub-24
2-889 Sub-50 3,4-diClPh CH2 Single bond Sub-25
2-890 Sub-50 3,4-diClPh CH2 Single bond Sub-26
2-891 Sub-50 3,4-diClPh CH2 Single bond Sub-27
2-892 Sub-50 3,4-diClPh CH2 Single bond Sub-28
2-893 Sub-50 3,4-diClPh CH2 Single bond Sub-29
2-894 Sub-50 3,4-diClPh CH2 Single bond Sub-30
2-895 Sub-50 3,4-diClPh CH2 Single bond Sub-31
2-896 Sub-50 3,4-diClPh CH2 Single bond Sub-32
2-897 Sub-50 3,4-diClPh CH2 Single bond Sub-65
2-898 Sub-50 3,4-diClPh CH2 Single bond Sub-66
2-899 Sub-50 3,4-diClPh CH2 Single bond Sub-67
2-900 Sub-50 3,4-diClPh CH2 Single bond Sub-68
2-901 Sub-50 3,4-diClPh CH2 Single bond Sub-69
2-902 Sub-50 3,4-diClPh CH2 Single bond Sub-70
2-903 Sub-50 3,4-diClPh CH2 Single bond Sub-71
2-904 Sub-50 3,4-diClPh CH2 Single bond Sub-72
2-905 Sub-50 3,4-diClPh CH2 Single bond Sub-73
2-906 Sub-50 3,4-diClPh CH2 Single bond Sub-74
2-907 Sub-50 3,4-diClPh CH2 Single bond Sub-75
2-908 Sub-50 3,4-diClPh CH2 Single bond Sub-76
2-909 Sub-50 3,4-diClPh CH2 Single bond Sub-77
2-910 Sub-50 3,4-diClPh CH2 Single bond Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-911 Sub-50 3,4-diClPh CH2 Single bond Sub-79
2-912 Sub-50 3,4-diClPh CH2 Single bond Sub-80
2-913 Sub-51 3,4-diClPh CH2 Single bond Sub-1
2-914 Sub-51 3,4-diClPh CH2 Single bond Sub-2
2-915 Sub-51 3,4-diClPh CH2 Single bond Sub-3
2-916 Sub-51 3,4-diClPh CH2 Single bond Sub-4
2-917 Sub-51 3,4-diClPh CH2 Single bond Sub-5
2-918 Sub-51 3,4-diClPh CH2 Single bond Sub-6
2-919 Sub-51 3,4-diClPh CH2 Single bond Sub-7
2-920 Sub-51 3,4-diClPh CH2 Single bond Sub-8
2-921 Sub-51 3,4-diClPh CH2 Single bond Sub-9
2-922 Sub-51 3,4-diClPh CH2 Single bond Sub-10
2-923 Sub-51 3,4-diClPh CH2 Single bond Sub-11
2-924 Sub-51 3,4-diClPh CH2 Single bond Sub-12
2-925 Sub-51 3,4-diClPh CH2 Single bond Sub-13
2-926 Sub-51 3,4-diClPh CH2 Single bond Sub-14
2-927 Sub-51 3,4-diClPh CH2 Single bond Sub-15
2-928 Sub-51 3,4-diClPh CH2 Single bond Sub-16
2-929 Sub-51 3,4-diClPh CH2 Single bond Sub-17
2-930 Sub-51 3,4-diClPh CH2 Single bond Sub-18
2-931 Sub-51 3,4-diClPh CH2 Single bond Sub-19
2-932 Sub-51 3,4-diClPh CH2 Single bond Sub-20
2-933 Sub-51 3,4-diClPh CH2 Single bond Sub-21
2-934 Sub-51 3,4-diClPh CH2 Single bond Sub-22
2-935 Sub-51 3,4-diClPh CH2 Single bond Sub-23
2-936 Sub-51 3,4-diClPh CH2 Single bond Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-937 Sub-51 3,4-diClPh CH2 Single bond Sub-25
2-938 Sub-51 3,4-diClPh CH2 Single bond Sub-26
2-939 Sub-51 3,4-diClPh CH2 Single bond Sub-27
2-940 Sub-51 3,4-diClPh CH2 Single bond Sub-28
2-941 Sub-51 3,4-diClPh CH2 Single bond Sub-29
2-942 Sub-51 3,4-diClPh CH2 Single bond Sub-30
2-943 Sub-51 3,4-diClPh CH2 Single bond Sub-31
2-944 Sub-51 3,4-diClPh CH2 Single bond Sub-32
2-945 Sub-51 3,4-diClPh CH2 Single bond Sub-65
2-946 Sub-51 3,4-diClPh CH2 Single bond Sub-66
2-947 Sub-51 3,4-diClPh CH2 Single bond Sub-67
2-948 Sub-51 3,4-diClPh CH2 Single bond Sub-68
2-949 Sub-51 3,4-diClPh CH2 Single bond Sub-69
2-950 Sub-51 3,4-diClPh CH2 Single bond Sub-70
2-951 Sub-51 3,4-diClPh CH2 Single bond Sub-71
2-952 Sub-51 3,4-diClPh CH2 Single bond Sub-72
2-953 Sub-51 3,4-diClPh CH2 Single bond Sub-73
2-954 Sub-51 3,4-diClPh CH2 Single bond Sub-74
2-955 Sub-51 3,4-diClPh CH2 Single bond Sub-75
2-956 Sub-51 3,4-diClPh CH2 Single bond Sub-76
2-957 Sub-51 3,4-diClPh CH2 Single bond Sub-77
2-958 Sub-51 3,4-diClPh CH2 Single bond Sub-78
2-959 Sub-51 3,4-diClPh CH2 Single bond Sub-79
2-960 Sub-51 3,4-diClPh CH2 Single bond Sub-80
2-961 Sub-52 3,4-diClPh CH2 Single bond Sub-1
2-962 Sub-52 3,4-diClPh CH2 Single bond Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-963 Sub-52 3,4-diClPh CH2 Single bond Sub-3
2-964 Sub-52 3,4-diClPh CH2 Single bond Sub-4
2-965 Sub-52 3,4-diClPh CH2 Single bond Sub-5
2-966 Sub-52 3,4-diClPh CH2 Single bond Sub-6
2-967 Sub-52 3,4-diClPh CH2 Single bond Sub-7
2-968 Sub-52 3,4-diClPh CH2 Single bond Sub-8
2-969 Sub-52 3,4-diClPh CH2 Single bond Sub-9
2-970 Sub-52 3,4-diClPh CH2 Single bond Sub-10
2-971 Sub-52 3,4-diClPh CH2 Single bond Sub-11
2-972 Sub-52 3,4-diClPh CH2 Single bond Sub-12
2-973 Sub-52 3,4-diClPh CH2 Single bond Sub-13
2-974 Sub-52 3,4-diClPh CH2 Single bond Sub-14
2-975 Sub-52 3,4-diClPh CH2 Single bond Sub-15
2-976 Sub-52 3,4-diClPh CH2 Single bond Sub-16
2-977 Sub-52 3,4-diClPh CH2 Single bond Sub-17
2-978 Sub-52 3,4-diClPh CH2 Single bond Sub-18
2-979 Sub-52 3,4-diClPh CH2 Single bond Sub-19
2-980 Sub-52 3,4-diClPh CH2 Single bond Sub-20
2-981 Sub-52 3,4-diClPh CH2 Single bond Sub-21
2-982 Sub-52 3,4-diClPh CH2 Single bond Sub-22
2-983 Sub-52 3,4-diClPh CH2 Single bond Sub-23
2-984 Sub-52 3,4-diClPh CH2 Single bond Sub-24
2-985 Sub-52 3,4-diClPh CH2 Single bond Sub-25
2-986 Sub-52 3,4-diClPh CH2 Single bond Sub-26
2-987 Sub-52 3,4-diClPh CH2 Single bond Sub-27
2-988 Sub-52 3,4-diClPh CH2 Single bond Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-989 Sub-52 3,4-diClPh CH2 Single bond Sub-29
2-990 Sub-52 3,4-diClPh CH2 Single bond Sub-30
2-991 Sub-52 3,4-diClPh CH2 Single bond Sub-31
2-992 Sub-52 3,4-diClPh CH2 Single bond Sub-32
2-993 Sub-52 3,4-diClPh CH2 Single bond Sub-65
2-994 Sub-52 3,4-diClPh CH2 Single bond Sub-66
2-995 Sub-52 3,4-diClPh CH2 Single bond Sub-67
2-996 Sub-52 3,4-diClPh CH2 Single bond Sub-68
2-997 Sub-52 3,4-diClPh CH2 Single bond Sub-69
2-998 Sub-52 3,4-diClPh CH2 Single bond Sub-70
2-999 Sub-52 3,4-diClPh CH2 Single bond Sub-71
2-1000 Sub-52 3,4-diClPh CH2 Single bond Sub-72
2-1001 Sub-52 3,4-diClPh CH2 Single bond Sub-73
2-1002 Sub-52 3,4-diClPh CH2 Single bond Sub-74
2-1003 Sub-52 3,4-diClPh CH2 Single bond Sub-75
2-1004 Sub-52 3,4-diClPh CH2 Single bond Sub-76
2-1005 Sub-52 3,4-diClPh CH2 Single bond Sub-77
2-1006 Sub-52 3,4-diClPh CH2 Single bond Sub-78
2-1007 Sub-52 3,4-diClPh CH2 Single bond Sub-79
2-1008 Sub-52 3,4-diClPh CH2 Single bond Sub-80
2-1009 Sub-53 3,4-diClPh CH2 Single bond Sub-1
2-1010 Sub-53 3,4-diClPh CH2 Single bond Sub-2
2-1011 Sub-53 3,4-diClPh CH2 Single bond Sub-3
2-1012 Sub-53 3,4-diClPh CH2 Single bond Sub-4
2-1013 Sub-53 3,4-diClPh CH2 Single bond Sub-5
2-1014 Sub-53 3,4-diClPh CH2 Single bond Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1015 Sub-53 3,4-diClPh CH2 Single bond Sub-7
2-1016 Sub-53 3,4-diClPh CH2 Single bond Sub-8
2-1017 Sub-53 3,4-diClPh CH2 Single bond Sub-9
2-1018 Sub-53 3,4-diClPh CH2 Single bond Sub-10
2-1019 Sub-53 3,4-diClPh CH2 Single bond Sub-11
2-1020 Sub-53 3,4-diClPh CH2 Single bond Sub-12
2-1021 Sub-53 3,4-diClPh CH2 Single bond Sub-13
2-1022 Sub-53 3,4-diClPh CH2 Single bond Sub-14
2-1023 Sub-53 3,4-diClPh CH2 Single bond Sub-15
2-1024 Sub-53 3,4-diClPh CH2 Single bond Sub-16
2-1025 Sub-53 3,4-diClPh CH2 Single bond Sub-17
2-1026 Sub-53 3,4-diClPh CH2 Single bond Sub-18
2-1027 Sub-53 3,4-diClPh CH2 Single bond Sub-19
2-1028 Sub-53 3,4-diClPh CH2 Single bond Sub-20
2-1029 Sub-53 3,4-diClPh CH2 Single bond Sub-21
2-1030 Sub-53 3,4-diClPh CH2 Single bond Sub-22
2-1031 Sub-53 3,4-diClPh CH2 Single bond Sub-23
2-1032 Sub-53 3,4-diClPh CH2 Single bond Sub-24
2-1033 Sub-53 3,4-diClPh CH2 Single bond Sub-25
2-1034 Sub-53 3,4-diClPh CH2 Single bond Sub-26
2-1035 Sub-53 3,4-diClPh CH2 Single bond Sub-27
2-1036 Sub-53 3,4-diClPh CH2 Single bond Sub-28
2-1037 Sub-53 3,4-diClPh CH2 Single bond Sub-29
2-1038 Sub-53 3,4-diClPh CH2 Single bond Sub-30
2-1039 Sub-53 3,4-diClPh CH2 Single bond Sub-31
2-1040 Sub-53 3,4-diClPh CH2 Single bond Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1041 Sub-53 3,4-diClPh CH2 Single bond Sub-65
2-1042 Sub-53 3,4-diClPh CH2 Single bond Sub-66
2-1043 Sub-53 3,4-diClPh CH2 Single bond Sub-67
2-1044 Sub-53 3,4-diClPh CH2 Single bond Sub-68
2-1045 Sub-53 3,4-diClPh CH2 Single bond Sub-69
2-1046 Sub-53 3,4-diClPh CH2 SheetKey with a key body Sub-70
2-1047 Sub-53 3,4-diClPh CH2 Single bond Sub-71
2-1048 Sub-53 3,4-diClPh CH2 Single bond Sub-72
2-1049 Sub-53 3,4-diClPh CH2 Single bond Sub-73
2-1050 Sub-53 3,4-diClPh CH2 Single bond Sub-74
2-1051 Sub-53 3,4-diClPh CH2 Single bond Sub-75
2-1052 Sub-53 3,4-diClPh CH2 Single bond Sub-76
2-1053 Sub-53 3,4-diClPh CH2 Single bond Sub-77
2-1054 Sub-53 3,4-diClPh CH2 Single bond Sub-78
2-1055 Sub-53 3,4-diClPh CH2 Single bond Sub-79
2-1056 Sub-53 3,4-diClPh CH2 Single bond Sub-80
2-1057 Sub-54 3,4-diClPh CH2 Single bond Sub-1
2-1058 Sub-54 3,4-diClPh CH2 Single bond Sub-2
2-1059 Sub-54 3,4-diClPh CH2 Single bond Sub-3
2-1060 Sub-54 3,4-diClPh CH2 Single bond Sub-4
2-1061 Sub-54 3,4-diClPh CH2 Single bond Sub-5
2-1062 Sub-54 3,4-diClPh CH2 Single bond Sub-6
2-1063 Sub-54 3,4-diClPh CH2 Single bond Sub-7
2-1064 Sub-54 3,4-diClPh CH2 Single bond Sub-8
2-1065 Sub-54 3,4-diClPh CH2 Single bond Sub-9
2-1066 Sub-54 3,4-diClPh CH2 Single bond Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1067 Sub-54 3,4-diClPh CH2 Single bond Sub-11
2-1068 Sub-54 3,4-diClPh CH2 Single bond Sub-12
2-1069 Sub-54 3,4-diClPh CH2 Single bond Sub-13
2-1070 Sub-54 3,4-diClPh CH2 Single bond Sub-14
2-1071 Sub-54 3,4-diClPh CH2 Single bond Sub-15
2-1072 Sub-54 3,4-diClPh CH2 Single bond Sub-16
2-1073 Sub-54 3,4-diClPh CH2 Single bond Sub-17
2-1074 Sub-54 3,4-diClPh CH2 Single bond Sub-18
2-1075 Sub-54 3,4-diClPh CH2 Single bond Sub-19
2-1076 Sub-54 3,4-diClPh CH2 Single bond Sub-20
2-1077 Sub-54 3,4-diClPh CH2 Single bond Sub-21
2-1078 Sub-54 3,4-diClPh CH2 Single bond Sub-22
2-1079 Sub-54 3,4-diClPh CH2 Single bond Sub-23
2-1080 Sub-54 3,4-diClPh CH2 Single bond Sub-24
2-1081 Sub-54 3,4-diClPh CH2 Single bond Sub-25
2-1082 Sub-54 3,4-diClPh CH2 Single bond Sub-26
2-1083 Sub-54 3,4-diClPh CH2 Single bond Sub-27
2-1084 Sub-54 3,4-diClPh CH2 Single bond Sub-28
2-1085 Sub-54 3,4-diClPh CH2 Single bond Sub-29
2-1086 Sub-54 3,4-diClPh CH2 Single bond Sub-30
2-1087 Sub-54 3,4-diClPh CH2 Single bond Sub-31
2-1088 Sub-54 3,4-diClPh CH2 Single bond Sub-32
2-1089 Sub-54 3,4-diClPh CH2 Single bond Sub-65
2-1090 Sub-54 3,4-diClPh CH2 Single bond Sub-66
2-1091 Sub-54 3,4-diClPh CH2 Single bond Sub-67
2-1092 Sub-54 3,4-diClPh CH2 Single bond Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1093 Sub-54 3,4-diClPh CH2 Single bond Sub-69
2-1094 Sub-54 3,4-diClPh CH2 Single bond Sub-70
2-1095 Sub-54 3,4-diClPh CH2 Single bond Sub-71
2-1096 Sub-54 3,4-diClPh CH2 Single bond Sub-72
2-1097 Sub-54 3,4-diClPh CH2 Single bond Sub-73
2-1098 Sub-54 3,4-diClPh CH2 Single bond Sub-74
2-1099 Sub-54 3,4-diClPh CH2 Single bond Sub-75
2-1100 Sub-54 3,4-diClPh CH2 Single bond Sub-76
2-1101 Sub-54 3,4-diClPh CH2 Single bond Sub-77
2-1102 Sub-54 3,4-diClPh CH2 Single bond Sub-78
2-1103 Sub-54 3,4-diClPh CH2 Single bond Sub-79
2-1104 Sub-54 3,4-diClPh CH2 Single bond Sub-80
2-1105 Sub-55 3,4-diClPh CH2 Single bond Sub-1
2-1106 Sub-55 3,4-diClPh CH2 Single bond Sub-2
2-1107 Sub-55 3,4-diClPh CH2 Single bond Sub-3
2-1108 Sub-55 3,4-diClPh CH2 Single bond Sub-4
2-1109 Sub-55 3,4-diClPh CH2 Single bond Sub-5
2-1110 Sub-55 3,4-diClPh CH2 Single bond Sub-6
2-1111 Sub-55 3,4-diClPh CH2 Single bond Sub-7
2-1112 Sub-55 3,4-diClPh CH2 Single bond Sub-8
2-1113 Sub-55 3,4-diClPh CH2 Single bond Sub-9
2-1114 Sub-55 3,4-diClPh CH2 Single bond Sub-10
2-1115 Sub-55 3,4-diClPh CH2 Single bond Sub-11
2-1116 Sub-55 3,4-diClPh CH2 Single bond Sub-12
2-1117 Sub-55 3,4-diClPh CH2 Single bond Sub-13
2-1118 Sub-55 3,4-diClPh CH2 Single bond Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1119 Sub-55 3,4-diClPh CH2 Single bond Sub-15
2-1120 Sub-55 3,4-diClPh CH2 Single bond Sub-16
2-1121 Sub-55 3,4-diClPh CH2 Single bond Sub-17
2-1122 Sub-55 3,4-diClPh CH2 Single bond Sub-18
2-1123 Sub-55 3,4-diClPh CH2 Single bond Sub-19
2-1124 Sub-55 3,4-diClPh CH2 Single bond Sub-20
2-1125 Sub-55 3,4-diClPh CH2 Single bond Sub-21
2-1126 Sub-55 3,4-diClPh CH2 Single bond Sub-22
2-1127 Sub-55 3,4-diClPh CH2 Single bond Sub-23
2-1128 Sub-55 3,4-diClPh CH2 Single bond Sub-24
2-1129 Sub-55 3,4-diClPh CH2 Single bond Sub-25
2-1130 Sub-55 3,4-diClPh CH2 Single bond Sub-26
2-1131 Sub-55 3,4-diClPh CH2 Single bond Sub-27
2-1132 Sub-55 3,4-diClPh CH2 Single bond Sub-28
2-1133 Sub-55 3,4-diClPh CH2 Single bond Sub-29
2-1134 Sub-55 3,4-diClPh CH2 Single bond Sub-30
2-1135 Sub-55 3,4-diClPh CH2 Single bond Sub-31
2-1136 Sub-55 3,4-diClPh CH2 Single bond Sub-32
2-1137 Sub-55 3,4-diClPh CH2 Single bond Sub-65
2-1138 Sub-55 3,4-diClPh CH2 Single bond Sub-66
2-1139 Sub-55 3,4-diClPh CH2 Single bond Sub-67
2-1140 Sub-55 3,4-diClPh CH2 Single bond Sub-68
2-1141 Sub-55 3,4-diClPh CH2 Single bond Sub-69
2-1142 Sub-55 3,4-diClPh CH2 Single bond Sub-70
2-1143 Sub-55 3,4-diClPh CH2 Single bond Sub-71
2-1144 Sub-55 3,4-diClPh CH2 Single bond Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1145 Sub-55 3,4-diClPh CH2 Single bond Sub-73
2-1146 Sub-55 3,4-diClPh CH2 Single bond Sub-74
2-1147 Sub-55 3,4-diClPh CH2 Single bond Sub-75
2-1148 Sub-55 3,4-diClPh CH2 Single bond Sub-76
2-1149 Sub-55 3,4-diClPh CH2 Single bond Sub-77
2-1150 Sub-55 3,4-diClPh CH2 Single bond Sub-78
2-1151 Sub-55 3,4-diClPh CH2 Single bond Sub-79
2-1152 Sub-55 3,4-diClPh CH2 Single bond Sub-80
2-1153 Sub-56 3,4-diClPh CH2 Single bond Sub-1
2-1154 Sub-56 3,4-diClPh CH2 Single bond Sub-2
2-1155 Sub-56 3,4-diClPh CH2 Single bond Sub-3
2-1156 Sub-56 3,4-diClPh CH2 Single bond Sub-4
2-1157 Sub-56 3,4-diClPh CH2 Single bond Sub-5
2-1158 Sub-56 3,4-diClPh CH2 Single bond Sub-6
2-1159 Sub-56 3,4-diClPh CH2 Single bond Sub-7
2-1160 Sub-56 3,4-diClPh CH2 Single bond Sub-8
2-1161 Sub-56 3,4-diClPh CH2 Single bond Sub-9
2-1162 Sub-56 3,4-diClPh CH2 Single bond Sub-10
2-1163 Sub-56 3,4-diClPh CH2 Single bond Sub-11
2-1164 Sub-56 3,4-diClPh CH2 Single bond Sub-12
2-1165 Sub-56 3,4-diClPh CH2 Single bond Sub-13
2-1166 Sub-56 3,4-diClPh CH2 Single bond Sub-14
2-1167 Sub-56 3,4-diClPh CH2 Single bond Sub-15
2-1168 Sub-56 3,4-diClPh CH2 Single bond Sub-16
2-1169 Sub-56 3,4-diClPh CH2 Single bond Sub-17
2-1170 Sub-56 3,4-diClPh CH2 Single bond Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1171 Sub-56 3,4-diClPh CH2 Single bond Sub-19
2-1172 Sub-56 3,4-diClPh CH2 Single bond Sub-20
2-1173 Sub-56 3,4-diClPh CH2 Single bond Sub-21
2-1174 Sub-56 3,4-diClPh CH2 Single bond Sub-22
2-1175 Sub-56 3,4-diClPh CH2 Single bond Sub-23
2-1176 Sub-56 3,4-diClPh CH2 Single bond Sub-24
2-1177 Sub-56 3,4-diClPh CH2 Single bond Sub-25
2-1178 Sub-56 3,4-diClPh CH2 Single bond Sub-26
2-1179 Sub-56 3,4-diClPh CH2 Single bond Sub-27
2-1180 Sub-56 3,4-diClPh CH2 Single bond Sub-28
2-1181 Sub-56 3,4-diClPh CH2 Single bond Sub-29
2-1182 Sub-56 3,4-diClPh CH2 Single bond Sub-30
2-1183 Sub-56 3,4-diClPh CH2 Single bond Sub-31
2-1184 Sub-56 3,4-diClPh CH2 Single bond Sub-32
2-1185 Sub-56 3,4-diClPh CH2 Single bond Sub-65
2-1186 Sub-56 3,4-diClPh CH2 Single bond Sub-66
2-1187 Sub-56 3,4-diClPh CH2 Single bond Sub-67
2-1188 Sub-56 3,4-diClPh CH2 Single bond Sub-68
2-1189 Sub-56 3,4-diClPh CH2 Single bond Sub-69
2-1190 Sub-56 3,4-diClPh CH2 Single bond Sub-70
2-1191 Sub-56 3,4-diClPh CH2 Single bond Sub-71
2-1192 Sub-56 3,4-diClPh CH2 Single bond Sub-72
2-1193 Sub-56 3,4-diClPh CH2 Single bond Sub-73
2-1194 Sub-56 3,4-diClPh CH2 Single bond Sub-74
2-1195 Sub-56 3,4-diClPh CH2 Single bond Sub-75
2-1196 Sub-56 3,4-diClPh CH2 Single bond Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1197 Sub-56 3,4-diClPh CH2 Single bond Sub-77
2-1198 Sub-56 3,4-diClPh CH2 Single bond Sub-78
2-1199 Sub-56 3,4-diClPh CH2 Single bond Sub-79
2-1200 Sub-56 3,4-diClPh CH2 Single bond Sub-80
2-1201 Sub-57 3,4-diClPh CH2 Single bond Sub-1
2-1202 Sub-57 3,4-diClPh CH2 Single bond Sub-2
2-1203 Sub-57 3,4-diClPh CH2 Single bond Sub-3
2-1204 Sub-57 3,4-diClPh CH2 Single bond Sub-4
2-1205 Sub-57 3,4-diClPh CH2 Single bond Sub-5
2-1206 Sub-57 3,4-diClPh CH2 Single bond Sub-6
2-1207 Sub-57 3,4-diClPh CH2 Single bond Sub-7
2-1208 Sub-57 3,4-diClPh CH2 Single bond Sub-8
2-1209 Sub-57 3,4-diClPh CH2 Single bond Sub-9
2-1210 Sub-57 3,4-diClPh CH2 Single bond Sub-10
2-1211 Sub-57 3,4-diClPh CH2 Single bond Sub-11
2-1212 Sub-57 3,4-diClPh CH2 Single bond Sub-12
2-1213 Sub-57 3,4-diClPh CH2 Single bond Sub-13
2-1214 Sub-57 3,4-diClPh CH2 Single bond Sub-14
2-1215 Sub-57 3,4-diClPh CH2 Single bond Sub-15
2-1216 Sub-57 3,4-diClPh CH2 Single bond Sub-16
2-1217 Sub-57 3,4-diClPh CH2 Single bond Sub-17
2-1218 Sub-57 3,4-diClPh CH2 Single bond Sub-18
2-1219 Sub-57 3,4-diClPh CH2 Single bond Sub-19
2-1220 Sub-57 3,4-diClPh CH2 Single bond Sub-20
2-1221 Sub-57 3,4-diClPh CH2 Single bond Sub-21
2-1222 Sub-57 3,4-diClPh CH2 Single bond Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1223 Sub-57 3,4-diClPh CH2 Single bond Sub-23
2-1224 Sub-57 3,4-diClPh CH2 Single bond Sub-24
2-1225 Sub-57 3,4-diClPh CH2 Single bond Sub-25
2-1226 Sub-57 3,4-diClPh CH2 Single bond Sub-26
2-1227 Sub-57 3,4-diClPh CH2 Single bond Sub-27
2-1228 Sub-57 3,4-diClPh CH2 Single bond Sub-28
2-1229 Sub-57 3,4-diClPh CH2 Single bond Sub-29
2-1230 Sub-57 3,4-diClPh CH2 Single bond Sub-30
2-1231 Sub-57 3,4-diClPh CH2 Single bond Sub-31
2-1232 Sub-57 3,4-diClPh CH2 Single bond Sub-32
2-1233 Sub-57 3,4-diClPh CH2 Single bond Sub-65
2-1234 Sub-57 3,4-diClPh CH2 Single bond Sub-66
2-1235 Sub-57 3,4-diClPh CH2 Single bond Sub-67
2-1236 Sub-57 3,4-diClPh CH2 Single bond Sub-68
2-1237 Sub-57 3,4-diClPh CH2 Single bond Sub-69
2-1238 Sub-57 3,4-diClPh CH2 Single bond Sub-70
2-1239 Sub-57 3,4-diClPh CH2 Single bond Sub-71
2-1240 Sub-57 3,4-diClPh CH2 Single bond Sub-72
2-1241 Sub-57 3,4-diClPh CH2 Single bond Sub-73
2-1242 Sub-57 3,4-diClPh CH2 Single bond Sub-74
2-1243 Sub-57 3,4-diClPh CH2 Single bond Sub-75
2-1244 Sub-57 3,4-diClPh CH2 Single bond Sub-76
2-1245 Sub-57 3,4-diClPh CH2 Single bond Sub-77
2-1246 Sub-57 3,4-diClPh CH2 Single bond Sub-78
2-1247 Sub-57 3,4-diClPh CH2 Single bond Sub-79
2-1248 Sub-57 3,4-diClPh CH2 Single bond Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1249 Sub-58 3,4-diClPh CH2 Single bond Sub-1
2-1250 Sub-58 3,4-diClPh CH2 Single bond Sub-2
2-1251 Sub-58 3,4-diClPh CH2 Single bond Sub-3
2-1252 Sub-58 3,4-diClPh CH2 Single bond Sub-4
2-1253 Sub-58 3,4-diClPh CH2 Single bond Sub-5
2-1254 Sub-58 3,4-diClPh CH2 Single bond Sub-6
2-1255 Sub-58 3,4-diClPh CH2 Single bond Sub-7
2-1256 Sub-58 3,4-diClPh CH2 Single bond Sub-8
2-1257 Sub-58 3,4-diClPh CH2 Single bond Sub-9
2-1258 Sub-58 3,4-diClPh CH2 Single bond Sub-10
2-1259 Sub-58 3,4-diClPh CH2 Single bond Sub-11
2-1260 Sub-58 3,4-diClPh CH2 Single bond Sub-12
2-1261 Sub-58 3,4-diClPh CH2 Single bond Sub-13
2-1262 Sub-58 3,4-diClPh CH2 Single bond Sub-14
2-1263 Sub-58 3,4-diClPh CH2 Single bond Sub-15
2-1264 Sub-58 3,4-diClPh CH2 Single bond Sub-16
2-1265 Sub-58 3,4-diClPh CH2 Single bond Sub-17
2-1266 Sub-58 3,4-diClPh CH2 Single bond Sub-18
2-1267 Sub-58 3,4-diClPh CH2 Single bond Sub-19
2-1268 Sub-58 3,4-diClPh CH2 Single bond Sub-20
2-1269 Sub-58 3,4-diClPh CH2 Single bond Sub-21
2-1270 Sub-58 3,4-diClPh CH2 Single bond Sub-22
2-1271 Sub-58 3,4-diClPh CH2 Single bond Sub-23
2-1272 Sub-58 3,4-diClPh CH2 Single bond Sub-24
2-1273 Sub-58 3,4-diClPh CH2 Single bond Sub-25
2-1274 Sub-58 3,4-diClPh CH2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1275 Sub-58 3,4-diClPh CH2 Single bond Sub-27
2-1276 Sub-58 3,4-diClPh CH2 Single bond Sub-28
2-1277 Sub-58 3,4-diClPh CH2 Single bond Sub-29
2-1278 Sub-58 3,4-diClPh CH2 Single bond Sub-30
2-1279 Sub-58 3,4-diClPh CH2 Single bond Sub-31
2-1280 Sub-58 3,4-diClPh CH2 Single bond Sub-32
2-1281 Sub-58 3,4-diClPh CH2 Single bond Sub-65
2-1282 Sub-58 3,4-diClPh CH2 Single bond Sub-66
2-1283 Sub-58 3,4-diClPh CH2 Single bond Sub-67
2-1284 Sub-58 3,4-diClPh CH2 Single bond Sub-68
2-1285 Sub-58 3,4-diClPh CH2 Single bond Sub-69
2-1286 Sub-58 3,4-diClPh CH2 Single bond Sub-70
2-1287 Sub-58 3,4-diClPh CH2 Single bond Sub-71
2-1288 Sub-58 3,4-diClPh CH2 Single bond Sub-72
2-1289 Sub-58 3,4-diClPh CH2 Single bond Sub-73
2-1290 Sub-58 3,4-diClPh CH2 Single bond Sub-74
2-1291 Sub-58 3,4-diClPh CH2 Single bond Sub-75
2-1292 Sub-58 3,4-diClPh CH2 Single bond Sub-76
2-1293 Sub-58 3,4-diClPh CH2 Single bond Sub-77
2-1294 Sub-58 3,4-diClPh CH2 Single bond Sub-78
2-1295 Sub-58 3,4-diClPh CH2 Single bond Sub-79
2-1296 Sub-58 3,4-diClPh CH2 Single bond Sub-80
2-1297 Sub-59 3,4-diClPh CH2 Single bond Sub-1
2-1298 Sub-59 3,4-diClPh CH2 Single bond Sub-2
2-1299 Sub-59 3,4-diClPh CH2 Single bond Sub-3
2-1300 Sub-59 3,4-diClPh CH2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1301 Sub-59 3,4-diClPh CH2 Single bond Sub-5
2-1302 Sub-59 3,4-diClPh CH2 Single bond Sub-6
2-1303 Sub-59 3,4-diClPh CH2 Single bond Sub-7
2-1304 Sub-59 3,4-diClPh CH2 Single bond Sub-8
2-1305 Sub-59 3,4-diClPh CH2 Single bond Sub-9
2-1306 Sub-59 3,4-diClPh CH2 Single bond Sub-10
2-1307 Sub-59 3,4-diClPh CH2 Single bond Sub-11
2-1308 Sub-59 3,4-diClPh CH2 Single bond Sub-12
2-1309 Sub-59 3,4-diClPh CH2 Single bond Sub-13
2-1310 Sub-59 3,4-diClPh CH2 Single bond Sub-14
2-1311 Sub-59 3,4-diClPh CH2 Single bond Sub-15
2-1312 Sub-59 3,4-diClPh CH2 Single bond Sub-16
2-1313 Sub-59 3,4-diClPh CH2 Single bond Sub-17
2-1314 Sub-59 3,4-diClPh CH2 Single bond Sub-18
2-1315 Sub-59 3,4-diClPh CH2 Single bond Sub-19
2-1316 Sub-59 3,4-diClPh CH2 Single bond Sub-20
2-1317 Sub-59 3,4-diClPh CH2 Single bond Sub-21
2-1318 Sub-59 3,4-diClPh CH2 Single bond Sub-22
2-1319 Sub-59 3,4-diClPh CH2 Single bond Sub-23
2-1320 Sub-59 3,4-diClPh CH2 Single bond Sub-24
2-1321 Sub-59 3,4-diClPh CH2 Single bond Sub-25
2-1322 Sub-59 3,4-diClPh CH2 Single bond Sub-26
2-1323 Sub-59 3,4-diClPh CH2 Single bond Sub-27
2-1324 Sub-59 3,4-diClPh CH2 Single bond Sub-28
2-1325 Sub-59 3,4-diClPh CH2 Single bond Sub-29
2-1326 Sub-59 3,4-diClPh CH2 Single bond Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1327 Sub-59 3,4-diClPh CH2 Single bond Sub-31
2-1328 Sub-59 3,4-diClPh CH2 Single bond Sub-32
2-1329 Sub-59 3,4-diClPh CH2 Single bond Sub-65
2-1330 Sub-59 3,4-diClPh CH2 Single bond Sub-66
2-1331 Sub-59 3,4-diClPh CH2 Single bond Sub-67
2-1332 Sub-59 3,4-diClPh CH2 Single bond Sub-68
2-1333 Sub-59 3,4-diClPh CH2 Single bond Sub-69
2-1334 Sub-59 3,4-diClPh CH2 Single bond Sub-70
2-1335 Sub-59 3,4-diClPh CH2 Single bond Sub-71
2-1336 Sub-59 3,4-diClPh CH2 Single bond Sub-72
2-1337 Sub-59 3,4-diClPh CH2 Single bond Sub-73
2-1338 Sub-59 3,4-diClPh CH2 Single bond Sub-74
2-1339 Sub-59 3,4-diClPh CH2 Single bond Sub-75
2-1340 Sub-59 3,4-diClPh CH2 Single bond Sub-76
2-1341 Sub-59 3,4-diClPh CH2 Single bond Sub-77
2-1342 Sub-59 3,4-diClPh CH2 Single bond Sub-78
2-1343 Sub-59 3,4-diClPh CH2 Single bond Sub-79
2-1344 Sub-59 3,4-diClPh CH2 Single bond Sub-80
2-1345 Sub-82 3,4-diClPh CH2 Single bond Sub-1
2-1346 Sub-82 3,4-diClPh CH2 Single bond Sub-2
2-1347 Sub-82 3,4-diClPh CH2 Single bond Sub-3
2-1348 Sub-82 3,4-diClPh CH2 Single bond Sub-4
2-1349 Sub-82 3,4-diClPh CH2 Single bond Sub-5
2-1350 Sub-82 3,4-diClPh CH2 Single bond Sub-6
2-1351 Sub-82 3,4-diClPh CH2 Single bond Sub-7
2-1352 Sub-82 3,4-diClPh CH2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1353 Sub-82 3,4-diClPh CH2 Single bond Sub-9
2-1354 Sub-82 3,4-diClPh CH2 Single bond Sub-10
2-1355 Sub-82 3,4-diClPh CH2 Single bond Sub-11
2-1356 Sub-82 3,4-diClPh CH2 Single bond Sub-12
2-1357 Sub-82 3,4-diClPh CH2 Single bond Sub-13
2-1358 Sub-82 3,4-diClPh CH2 Single bond Sub-14
2-1359 Sub-82 3,4-diClPh CH2 Single bond Sub-15
2-1360 Sub-82 3,4-diClPh CH2 Single bond Sub-16
2-1361 Sub-82 3,4-diClPh CH2 Single bond Sub-17
2-1362 Sub-82 3,4-diClPh CH2 Single bond Sub-18
2-1363 Sub-82 3,4-diClPh CH2 Single bond Sub-19
2-1364 Sub-82 3,4-diClPh CH2 Single bond Sub-20
2-1365 Sub-82 3,4-diClPh CH2 Single bond Sub-21
2-1366 Sub-82 3,4-diClPh CH2 Single bond Sub-22
2-1367 Sub-82 3,4-diClPh CH2 Single bond Sub-23
2-1368 Sub-82 3,4-diClPh CH2 Single bond Sub-24
2-1369 Sub-82 3,4-diClPh CH2 Single bond Sub-25
2-1370 Sub-82 3,4-diClPh CH2 Single bond Sub-26
2-1371 Sub-82 3,4-diClPh CH2 Single bond Sub-27
2-1372 Sub-82 3,4-diClPh CH2 Single bond Sub-28
2-1373 Sub-82 3,4-diClPh CH2 Single bond Sub-29
2-1374 Sub-82 3,4-diClPh CH2 Single bond Sub-30
2-1375 Sub-82 3,4-diClPh CH2 Single bond Sub-31
2-1376 Sub-82 3,4-diClPh CH2 Single bond Sub-32
2-1377 Sub-82 3,4-diClPh CH2 Single bond Sub-65
2-1378 Sub-82 3,4-diClPh CH2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1379 Sub-82 3,4-diClPh CH2 Single bond Sub-67
2-1380 Sub-82 3,4-diClPh CH2 Single bond Sub-68
2-1381 Sub-82 3,4-diClPh CH2 Single bond Sub-69
2-1382 Sub-82 3,4-diClPh CH2 Single bond Sub-70
2-1383 Sub-82 3,4-diClPh CH2 Single bond Sub-71
2-1384 Sub-82 3,4-diClPh CH2 Single bond Sub-72
2-1385 Sub-82 3,4-diClPh CH2 Single bond Sub-73
2-1386 Sub-82 3,4-diClPh CH2 Single bond Sub-74
2-1387 Sub-82 3,4-diClPh CH2 Single bond Sub-75
2-1388 Sub-82 3,4-diClPh CH2 Single bond Sub-76
2-1389 Sub-82 3,4-diClPh CH2 Single bond Sub-77
2-1390 Sub-82 3,4-diClPh CH2 Single bond Sub-78
2-1391 Sub-82 3,4-diClPh CH2 Single bond Sub-79
2-1392 Sub-82 3,4-diClPh CH2 Single bond Sub-80
2-1393 Sub-83 3,4-diClPh CH2 Single bond Sub-1
2-1394 Sub-83 3,4-diClPh CH2 Single bond Sub-2
2-1395 Sub-83 3,4-diClPh CH2 Single bond Sub-3
2-1396 Sub-83 3,4-diClPh CH2 Single bond Sub-4
2-1397 Sub-83 3,4-diClPh CH2 Single bond Sub-5
2-1398 Sub-83 3,4-diClPh CH2 Single bond Sub-6
2-1399 Sub-83 3,4-diClPh CH2 Single bond Sub-7
2-1400 Sub-83 3,4-diClPh CH2 Single bond Sub-8
2-1401 Sub-83 3,4-diClPh CH2 Single bond Sub-9
2-1402 Sub-83 3,4-diClPh CH2 Single bond Sub-10
2-1403 Sub-83 3,4-diClPh CH2 Single bond Sub-11
2-1404 Sub-83 3,4-diClPh CH2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1405 Sub-83 3,4-diClPh CH2 Single bond Sub-13
2-1406 Sub-83 3,4-diClPh CH2 Single bond Sub-14
2-1407 Sub-83 3,4-diClPh CH2 Single bond Sub-15
2-1408 Sub-83 3,4-diClPh CH2 Single bond Sub-16
2-1409 Sub-83 3,4-diClPh CH2 Single bond Sub-17
2-1410 Sub-83 3,4-diClPh CH2 Single bond Sub-18
2-1411 Sub-83 3,4-diClPh CH2 Single bond Sub-19
2-1412 Sub-83 3,4-diClPh CH2 Single bond Sub-20
2-1413 Sub-83 3,4-diClPh CH2 Single bond Sub-21
2-1414 Sub-83 3,4-diClPh CH2 Single bond Sub-22
2-1415 Sub-83 3,4-diClPh CH2 Single bond Sub-23
2-1416 Sub-83 3,4-diClPh CH2 Single bond Sub-24
2-1417 Sub-83 3,4-diClPh CH2 Single bond Sub-25
2-1418 Sub-83 3,4-diClPh CH2 Single bond Sub-26
2-1419 Sub-83 3,4-diClPh CH2 Single bond Sub-27
2-1420 Sub-83 3,4-diClPh CH2 Single bond Sub-28
2-1421 Sub-83 3,4-diClPh CH2 Single bond Sub-29
2-1422 Sub-83 3,4-diClPh CH2 Single bond Sub-30
2-1423 Sub-83 3,4-diClPh CH2 Single bond Sub-31
2-1424 Sub-83 3,4-diClPh CH2 Single bond Sub-32
2-1425 Sub-83 3,4-diClPh CH2 Single bond Sub-65
2-1426 Sub-83 3,4-diClPh CH2 Single bond Sub-66
2-1427 Sub-83 3,4-diClPh CH2 Single bond Sub-67
2-1428 Sub-83 3,4-diClPh CH2 Single bond Sub-68
2-1429 Sub-83 3,4-diClPh CH2 Single bond Sub-69
2-1430 Sub-83 3,4-diClPh CH2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1431 Sub-83 3,4-diClPh CH2 Single bond Sub-71
2-1432 Sub-83 3,4-diClPh CH2 Single bond Sub-72
2-1433 Sub-83 3,4-diClPh CH2 Single bond Sub-73
2-1434 Sub-83 3,4-diClPh CH2 Single bond Sub-74
2-1435 Sub-83 3,4-diClPh CH2 Single bond Sub-75
2-1436 Sub-83 3,4-diClPh CH2 Single bond Sub-76
2-1437 Sub-83 3,4-diClPh CH2 Single bond Sub-77
2-1438 Sub-83 3,4-diClPh CH2 Single bond Sub-78
2-1439 Sub-83 3,4-diClPh CH2 Single bond Sub-79
2-1440 Sub-83 3,4-diClPh CH2 Single bond Sub-80
2-1441 Sub-61 3,4-diClPh CH2 Single bond Sub-1
2-1442 Sub-61 3,4-diClPh CH2 Single bond Sub-2
2-1443 Sub-61 3,4-diClPh CH2 Single bond Sub-3
2-1444 Sub-61 3,4-diClPh CH2 Single bond Sub-4
2-1445 Sub-61 3,4-diClPh CH2 Single bond Sub-5
2-1446 Sub-61 3,4-diClPh CH2 Single bond Sub-6
2-1447 Sub-61 3,4-diClPh CH2 Single bond Sub-7
2-1448 Sub-61 3,4-diClPh CH2 Single bond Sub-8
2-1449 Sub-61 3,4-diClPh CH2 Single bond Sub-9
2-1450 Sub-61 3,4-diClPh CH2 Single bond Sub-10
2-1451 Sub-61 3,4-diClPh CH2 Single bond Sub-11
2-1452 Sub-61 3,4-diClPh CH2 Single bond Sub-12
2-1453 Sub-61 3,4-diClPh CH2 Single bond Sub-13
2-1454 Sub-61 3,4-diClPh CH2 Single bond Sub-14
2-1455 Sub-61 3,4-diClPh CH2 Single bond Sub-15
2-1456 Sub-61 3,4-diClPh CH2 Single bond Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1457 Sub-61 3,4-diClPh CH2 Single bond Sub-17
2-1458 Sub-61 3,4-diClPh CH2 Single bond Sub-18
2-1459 Sub-61 3,4-diClPh CH2 Single bond Sub-19
2-1460 Sub-61 3,4-diClPh CH2 Single bond Sub-20
2-1461 Sub-61 3,4-diClPh CH2 Single bond Sub-21
2-1462 Sub-61 3,4-diClPh CH2 Single bond Sub-22
2-1463 Sub-61 3,4-diClPh CH2 Single bond Sub-23
2-1464 Sub-61 3,4-diClPh CH2 Single bond Sub-24
2-1465 Sub-61 3,4-diClPh CH2 Single bond Sub-25
2-1466 Sub-61 3,4-diClPh CH2 Single bond Sub-26
2-1467 Sub-61 3,4-diClPh CH2 Single bond Sub-27
2-1468 Sub-61 3,4-diClPh CH2 Single bond Sub-28
2-1469 Sub-61 3,4-diClPh CH2 Single bond Sub-29
2-1470 Sub-61 3,4-diClPh CH2 Single bond Sub-30
2-1471 Sub-61 3,4-diClPh CH2 Single bond Sub-31
2-1472 Sub-61 3,4-diClPh CH2 Single bond Sub-32
2-1473 Sub-61 3,4-diClPh CH2 Single bond Sub-65
2-1474 Sub-61 3,4-diClPh CH2 Single bond Sub-66
2-1475 Sub-61 3,4-diClPh CH2 Single bond Sub-67
2-1476 Sub-61 3,4-diClPh CH2 Single bond Sub-68
2-1477 Sub-61 3,4-diClPh CH2 Single bond Sub-69
2-1478 Sub-61 3,4-diClPh CH2 Single bond Sub-70
2-1479 Sub-61 3,4-diClPh CH2 Single bond Sub-71
2-1480 Sub-61 3,4-diClPh CH2 Single bond Sub-72
2-1481 Sub-61 3,4-diClPh CH2 Single bond Sub-73
2-1482 Sub-61 3,4-diClPh CH2 Single bond Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1483 Sub-61 3,4-diClPh CH2 Single bond Sub-75
2-1484 Sub-61 3,4-diClPh CH2 Single bond Sub-76
2-1485 Sub-61 3,4-diClPh CH2 Single bond Sub-77
2-1486 Sub-61 3,4-diClPh CH2 Single bond Sub-78
2-1487 Sub-61 3,4-diClPh CH2 Single bond Sub-79
2-1488 Sub-61 3,4-diClPh CH2 Single bond Sub-80
2-1489 Sub-60 3,4-diClPh CH2 Single bond Sub-1
2-1490 Sub-60 3,4-diClPh CH2 Single bond Sub-2
2-1491 Sub-60 3,4-diClPh CH2 Single bond Sub-3
2-1492 Sub-60 3,4-diClPh CH2 Single bond Sub-4
2-1493 Sub-60 3,4-diClPh CH2 Single bond Sub-5
2-1494 Sub-60 3,4-diClPh CH2 Single bond Sub-6
2-1495 Sub-60 3,4-diClPh CH2 Single bond Sub-7
2-1496 Sub-60 3,4-diClPh CH2 Single bond Sub-8
2-1497 Sub-60 3,4-diClPh CH2 Single bond Sub-9
2-1498 Sub-60 3,4-diClPh CH2 Single bond Sub-10
2-1499 Sub-60 3,4-diClPh CH2 Single bond Sub-11
2-1500 Sub-60 3,4-diClPh CH2 Single bond Sub-12
2-1501 Sub-60 3,4-diClPh CH2 Single bond Sub-13
2-1502 Sub-60 3,4-diClPh CH2 Single bond Sub-14
2-1503 Sub-60 3,4-diClPh CH2 Single bond Sub-15
2-1504 Sub-60 3,4-diClPh CH2 Single bond Sub-16
2-1505 Sub-60 3,4-diClPh CH2 Single bond Sub-17
2-1506 Sub-60 3,4-diClPh CH2 Single bond Sub-18
2-1507 Sub-60 3,4-diClPh CH2 Single bond Sub-19
2-1508 Sub-60 3,4-diClPh CH2 Single bond Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1509 Sub-60 3,4-diClPh CH2 Single bond Sub-21
2-1510 Sub-60 3,4-diClPh CH2 Single bond Sub-22
2-1511 Sub-60 3,4-diClPh CH2 Single bond Sub-23
2-1512 Sub-60 3,4-diClPh CH2 Single bond Sub-24
2-1513 Sub-60 3,4-diClPh CH2 Single bond Sub-25
2-1514 Sub-60 3,4-diClPh CH2 Single bond Sub-26
2-1515 Sub-60 3,4-diClPh CH2 Single bond Sub-27
2-1516 Sub-60 3,4-diClPh CH2 Single bond Sub-28
2-1517 Sub-60 3,4-diClPh CH2 Single bond Sub-29
2-1518 Sub-60 3,4-diClPh CH2 Single bond Sub-30
2-1519 Sub-60 3,4-diClPh CH2 Single bond Sub-31
2-1520 Sub-60 3,4-diClPh CH2 Single bond Sub-32
2-1521 Sub-60 3,4-diClPh CH2 Single bond Sub-65
2-1522 Sub-60 3,4-diClPh CH2 Single bond Sub-66
2-1523 Sub-60 3,4-diClPh CH2 Single bond Sub-67
2-1524 Sub-60 3,4-diClPh CH2 Single bond Sub-68
2-1525 Sub-60 3,4-diClPh CH2 Single bond Sub-69
2-1526 Sub-60 3,4-diClPh CH2 Single bond Sub-70
2-1527 Sub-60 3,4-diClPh CH2 Single bond Sub-71
2-1528 Sub-60 3,4-diClPh CH2 Single bond Sub-72
2-1529 Sub-60 3,4-diClPh CH2 Single bond Sub-73
2-1530 Sub-60 3,4-diClPh CH2 Single bond Sub-74
2-1531 Sub-60 3,4-diClPh CH2 Single bond Sub-75
2-1532 Sub-60 3,4-diClPh CH2 Single bond Sub-76
2-1533 Sub-60 3,4-diClPh CH2 Single bond Sub-77
2-1534 Sub-60 3,4-diClPh CH2 Single bond Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1535 Sub-60 3,4-diClPh CH2 Single bond Sub-79
2-1536 Sub-60 3,4-diClPh CH2 Single bond Sub-80
2-1537 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-1
2-1538 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-2
2-1539 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-3
2-1540 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-4
2-1541 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-5
2-1542 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-6
2-1543 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-7
2-1544 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-8
2-1545 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-9
2-1546 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-10
2-1547 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-11
2-1548 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-12
2-1549 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-13
2-1550 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-14
2-1551 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-15
2-1552 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-16
2-1553 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-17
2-1554 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-18
2-1555 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-19
2-1556 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-20
2-1557 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-21
2-1558 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-22
2-1559 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-23
2-1560 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1561 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-25
2-1562 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-26
2-1563 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-27
2-1564 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-28
2-1565 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-29
2-1566 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-30
2-1567 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-31
2-1568 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-32
2-1569 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-65
2-1570 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-66
2-1571 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-67
2-1572 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-68
2-1573 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-69
2-1574 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-70
2-1575 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-71
2-1576 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-72
2-1577 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-73
2-1578 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-74
2-1579 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-75
2-1580 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-76
2-1581 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-77
2-1582 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-78
2-1583 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-79
2-1584 Sub-33 3,4-diClPh CO Single bond or CH2 Sub-80
2-1585 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-1
2-1586 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1587 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-3
2-1588 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-4
2-1589 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-5
2-1590 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-6
2-1591 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-7
2-1592 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-8
2-1593 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-9
2-1594 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-10
2-1595 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-11
2-1596 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-12
2-1597 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-13
2-1598 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-14
2-1599 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-15
2-1600 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-16
2-16O1 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-17
2-1602 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-18
2-1603 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-19
2-1604 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-20
2-1605 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-21
2-1606 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-22
2-1607 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-23
2-1608 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-24
2-1609 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-25
2-1610 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-26
2-1611 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-27
2-1612 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1613 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-29
2-1614 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-30
2-1615 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-31
2-1616 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-32
2-1617 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-65
2-1618 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-66
2-1619 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-67
2-1620 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-68
2-1621 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-69
2-1622 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-70
2-1623 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-71
2-1624 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-72
2-1625 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-73
2-1626 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-74
2-1627 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-75
2-1628 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-76
2-1629 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-77
2-1630 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-78
2-1631 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-79
2-1632 Sub-34 3,4-diClPh CO Single bond or CH2 Sub-80
2-1633 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-1
2-1634 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-2
2-1635 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-3
2-1636 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-4
2-1637 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-5
2-1638 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1639 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-7
2-1640 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-8
2-1641 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-9
2-1642 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-10
2-1643 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-11
2-1644 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-12
2-1645 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-13
2-1646 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-14
2-1647 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-15
2-1648 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-16
2-1649 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-17
2-1650 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-18
2-1651 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-19
2-1652 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-20
2-1653 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-21
2-1654 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-22
2-1655 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-23
2-1656 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-24
2-1657 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-25
2-1658 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-26
2-1659 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-27
2-1660 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-28
2-1661 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-29
2-1662 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-30
2-1663 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-31
2-1664 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1665 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-65
2-1666 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-66
2-1667 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-67
2-1668 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-68
2-1669 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-69
2-1670 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-70
2-1671 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-71
2-1672 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-72
2-1673 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-73
2-1674 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-74
2-1675 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-75
2-1676 Sub-35 3,4-diClPh CO Single bondor CH2 Sub-76
2-1677 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-77
2-1678 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-78
2-1679 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-79
2-1680 Sub-35 3,4-diClPh CO Single bond or CH2 Sub-80
2-1681 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-1
2-1682 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-2
2-1683 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-3
2-1684 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-4
2-1685 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-5
2-1686 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-6
2-1687 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-7
2-1688 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-8
2-1689 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-9
2-1690 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1691 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-11
2-1692 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-12
2-1693 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-13
2-1694 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-14
2-1695 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-15
2-1696 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-16
2-1697 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-17
2-1698 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-18
2-1699 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-19
2-1700 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-20
2-1701 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-21
2-1702 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-22
2-1703 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-23
2-1704 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-24
2-1705 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-25
2-1706 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-26
2-1707 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-27
2-1708 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-28
2-1709 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-29
2-1710 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-30
2-1711 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-31
2-1712 Sub-36 3,4-diClPh C0 Single bond or CH2 Sub-32
2-1713 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-65
2-1714 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-66
2-1715 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-67
2-1716 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1717 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-69
2-1718 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-70
2-1719 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-71
2-1720 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-72
2-1721 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-73
2-1722 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-74
2-1723 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-75
2-1724 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-76
2-1725 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-77
2-1726 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-78
2-1727 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-79
2-1728 Sub-36 3,4-diClPh CO Single bond or CH2 Sub-80
2-1729 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-1
2-1730 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-2
2-1731 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-3
2-1732 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-4
2-1733 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-5
2-1734 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-6
2-1735 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-7
2-1736 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-8
2-1737 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-9
2-1738 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-10
2-1739 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-11
2-1740 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-12
2-1741 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-13
2-1742 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1743 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-15
2-1744 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-16
2-1745 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-17
2-1746 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-18
2-1747 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-19
2-1748 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-20
2-1749 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-21
2-1750 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-22
2-1751 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-23
2-1752 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-24
2-1753 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-25
2-1754 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-26
2-1755 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-27
2-1756 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-28
2-1757 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-29
2-1758 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-30
2-1759 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-31
2-1760 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-32
2-1761 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-65
2-1762 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-66
2-1763 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-67
2-1764 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-68
2-1765 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-69
2-1766 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-70
2-1767 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-71
2-1768 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1769 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-73
2-1770 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-74
2-1771 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-75
2-1772 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-76
2-1773 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-77
2-1774 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-78
2-1775 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-79
2-1776 Sub-37 3,4-diClPh CO Single bond or CH2 Sub-80
2-1777 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-1
2-1778 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-2
2-1779 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-3
2-1780 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-4
2-1781 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-5
2-1782 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-6
2-1783 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-7
2-1784 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-8
2-1785 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-9
2-1786 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-10
2-1787 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-11
2-1788 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-12
2-1789 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-13
2-1790 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-14
2-1791 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-15
2-1792 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-16
2-1793 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-17
2-1794 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1795 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-19
2-1796 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-20
2-1797 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-21
2-1798 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-22
2-1799 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-23
2-1800 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-24
2-1801 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-25
2-1802 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-26
2-1803 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-27
2-1804 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-28
2-1805 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-29
2-1806 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-30
2-1807 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-31
2-1808 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-32
2-1809 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-65
2-1810 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-66
2-1811 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-67
2-1812 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-68
2-1813 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-69
2-1814 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-70
2-1815 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-71
2-1816 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-72
2-1817 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-73
2-1818 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-74
2-1819 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-75
2-1820 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1821 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-77
2-1822 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-78
2-1823 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-79
2-1824 Sub-38 3,4-diClPh CO Single bond or CH2 Sub-80
2-1825 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-1
2-1826 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-2
2-1827 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-3
2-1828 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-4
2-1829 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-5
2-1830 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-6
2-1831 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-7
2-1832 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-8
2-1833 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-9
2-1834 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-10
2-1835 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-11
2-1836 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-12
2-1837 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-13
2-1838 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-14
2-1839 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-15
2-1840 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-16
2-1841 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-17
2-1842 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-18
2-1843 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-19
2-1844 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-20
2-1845 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-21
2-1846 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1847 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-23
2-1848 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-24
2-1849 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-25
2-1850 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-26
2-1851 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-27
2-1852 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-28
2-1853 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-29
2-1854 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-30
2-1855 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-31
2-1856 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-32
2-1857 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-65
2-1858 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-66
2-1859 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-67
2-1860 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-68
2-1861 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-69
2-1862 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-70
2-1863 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-71
2-1864 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-72
2-1865 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-73
2-1866 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-74
2-1867 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-75
2-1868 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-76
2-1869 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-77
2-1870 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-78
2-1871 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-79
2-1872 Sub-39 3,4-diClPh CO Single bond or CH2 Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1873 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-1
2-1874 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-2
2-1875 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-3
2-1876 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-4
2-1877 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-5
2-1878 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-6
2-1879 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-7
2-1880 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-8
2-1881 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-9
2-1882 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-10
2-1883 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-11
2-1884 Sub-40 3,4-diClPh CO Single bond or CH2 Suh-12
2-1885 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-13
2-1886 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-14
2-1887 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-15
2-1888 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-16
2-1889 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-17
2-1890 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-18
2-1891 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-19
2-1892 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-20
2-1893 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-21
2-1894 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-22
2-1895 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-23
2-1896 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-24
2-1897 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-25
2-1898 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1899 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-27
2-1900 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-28
2-1901 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-29
2-1902 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-30
2-1903 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-31
2-1904 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-32
2-1905 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-65
2-1906 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-66
2-1907 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-67
2-1908 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-68
2-1909 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-69
2-1910 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-70
2-1911 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-71
2-1912 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-72
2-1913 Sub-40 3,4-diClPh C0 Single bond or CH2 Sub-73
2-1914 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-74
2-1915 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-75
2-1916 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-76
2-1917 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-77
2-1918 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-78
2-1919 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-79
2-1920 Sub-40 3,4-diClPh CO Single bond or CH2 Sub-80
2-1921 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-1
2-1922 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-2
2-1923 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-3
2-1924 Sub-41 3,4-diClPh CO SheetKey or CH2 Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1925 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-5
2-1926 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-6
2-1927 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-7
2-1928 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-8
2-1929 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-9
2-1930 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-10
2-1931 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-11
2-1932 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-12
2-1933 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-13
2-1934 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-14
2-1935 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-15
2-1936 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-16
2-1937 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-17
2-1938 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-18
2-1939 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-19
2-1940 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-20
2-1941 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-21
2-1942 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-22
2-1943 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-23
2-1944 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-24
2-1945 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-25
2-1946 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-26
2-1947 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-27
2-1948 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-28
2-1949 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-29
2-1950 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1951 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-31
2-1952 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-32
2-1953 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-65
2-1954 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-66
2-1955 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-67
2-1956 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-68
2-1957 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-69
2-1958 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-70
2-1959 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-71
2-1960 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-72
2-1961 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-73
2-1962 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-74
2-1963 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-75
2-1964 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-76
2-1965 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-77
2-1966 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-78
2-1967 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-79
2-1968 Sub-41 3,4-diClPh CO Single bond or CH2 Sub-80
2-1969 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-1
2-1970 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-2
2-1971 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-3
2-1972 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-4
2-1973 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-5
2-1974 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-6
2-1975 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-7
2-1976 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-1977 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-9
2-1978 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-10
2-1979 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-11
2-1980 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-12
2-1981 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-13
2-1982 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-14
2-1983 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-15
2-1984 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-16
2-1985 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-17
2-1986 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-18
2-1987 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-19
2-1988 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-20
2-1989 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-21
2-1990 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-22
2-1991 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-23
2-1992 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-24
2-1993 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-25
2-1994 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-26
2-1995 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-27
2-1996 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-28
2-1997 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-29
2-1998 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-30
2-1999 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-31
2-2000 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-32
2-2001 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-65
2-2002 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2003 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-67
2-2004 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-68
2-2005 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-69
2-2006 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-70
2-2007 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-71
2-2008 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-72
2-2009 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-73
2-2010 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-74
2-2011 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-75
2-2012 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-76
2-2013 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-77
2-2014 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-78
2-2015 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-79
2-2016 Sub-42 3,4-diClPh CO Single bond or CH2 Sub-80
2-2017 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-1
2-2018 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-2
2-2019 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-3
2-2020 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-4
2-2021 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-5
2-2022 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-6
2-2023 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-7
2-2024 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-8
2-2025 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-9
2-2026 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-10
2-2027 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-11
2-2028 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2029 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-13
2-2030 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-14
2-2031 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-15
2-2032 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-16
2-2033 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-17
2-2034 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-18
2-2035 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-19
2-2036 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-20
2-2037 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-21
2-2038 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-22
2-2039 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-23
2-2040 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-24
2-2041 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-25
2-2042 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-26
2-2043 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-27
2-2044 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-28
2-2045 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-29
2-2046 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-30
2-2047 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-31
2-2048 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-32
2-2049 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-65
2-2050 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-66
2-2051 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-67
2-2052 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-68
2-2053 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-69
2-2054 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2055 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-71
2-2056 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-72
2-2057 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-73
2-2058 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-74
2-2059 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-75
2-2060 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-76
2-2061 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-77
2-2062 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-78
2-2063 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-79
2-2064 Sub-43 3,4-diClPh CO Single bond or CH2 Sub-80
2-2065 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-1
2-2066 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-2
2-2067 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-3
2-2068 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-4
2-2069 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-5
2-2070 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-6
2-2071 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-7
2-2072 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-8
2-2073 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-9
2-2074 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-10
2-2075 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-11
2-2076 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-12
2-2077 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-13
2-2078 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-14
2-2079 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-15
2-2080 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2081 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-17
2-2082 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-18
2-2083 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-19
2-2084 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-20
2-2085 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-21
2-2086 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-22
2-2087 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-23
2-2088 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-24
2-2089 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-25
2-2090 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-26
2-2091 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-27
2-2092 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-28
2-2093 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-29
2-2094 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-30
2-2095 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-31
2-2096 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-32
2-2097 Sub-44 3,4-diClPh C0 Single bond or CH2 Sub-65
2-2098 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-66
2-2099 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-67
2-2100 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-68
2-2101 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-69
2-2102 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-70
2-2103 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-71
2-2104 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-72
2-2105 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-73
2-2106 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2107 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-75
2-2108 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-76
2-2109 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-77
2-2110 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-78
2-2111 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-79
2-2112 Sub-44 3,4-diClPh CO Single bond or CH2 Sub-80
2-2113 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-1
2-2114 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-2
2-2115 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-3
2-2116 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-4
2-2117 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-5
2-2118 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-6
2-2119 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-7
2-2120 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-8
2-2121 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-9
2-2122 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-1O
2-2123 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-11
2-2124 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-12
2-2125 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-13
2-2126 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-14
2-2127 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-15
2-2128 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-16
2-2129 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-17
2-2130 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-18
2-2131 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-19
2-2132 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2133 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-21
2-2134 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-22
2-2135 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-23
2-2136 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-24
2-2137 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-25
2-2138 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-26
2-2139 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-27
2-2140 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-28
2-2141 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-29
2-2142 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-30
2-2143 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-31
2-2144 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-32
2-2145 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-65
2-2146 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-66
2-2147 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-67
2-2148 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-68
2-2149 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-69
2-2150 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-70
2-2151 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-71
2-2152 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-72
2-2153 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-73
2-2154 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-74
2-2155 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-75
2-2156 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-76
2-2157 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-77
2-2158 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2159 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-79
2-2160 Sub-45 3,4-diClPh CO Single bond or CH2 Sub-80
2-2161 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-1
2-2162 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-2
2-2163 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-3
2-2164 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-4
2-2165 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-5
2-2166 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-6
2-2167 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-7
2-2168 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-8
2-2169 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-9
2-2170 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-10
2-2171 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-11
2-2172 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-12
2-2173 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-13
2-2174 Sub46 3,4-diClPh CO Single bond or CH2 Sub-14
2-2175 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-15
2-2176 Sub46 3,4-diClPh CO Single bond or CH2 Sub-16
2-2177 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-17
2-2178 Sub-46 3,4-diClPh CO Single key orCH2 Sub-18
2-2179 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-19
2-2180 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-20
2-2181 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-21
2-2182 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-22
2-2183 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-23
2-2184 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2185 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-25
2-2186 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-26
2-2187 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-27
2-2188 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-28
2-2189 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-29
2-2190 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-30
2-2191 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-31
2-2192 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-32
2-2193 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-65
2-2194 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-66
2-2195 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-67
2-2196 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-68
2-2197 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-69
2-2198 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-70
2-2199 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-71
2-2200 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-72
2-2201 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-73
2-2202 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-74
2-2203 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-75
2-2204 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-76
2-2205 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-77
2-2206 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-78
2-2207 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-79
2-2208 Sub-46 3,4-diClPh CO Single bond or CH2 Sub-80
2-2209 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-1
2-2210 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2211 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-3
2-2212 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-4
2-2213 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-5
2-2214 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-6
2-2215 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-7
2-2216 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-8
2-2217 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-9
2-2218 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-10
2-2219 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-11
2-2220 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-12
2-2221 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-13
2-2222 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-14
2-2223 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-15
2-2224 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-16
2-2225 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-17
2-2226 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-18
2-2227 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-19
2-2228 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-20
2-2229 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-21
2-2230 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-22
2-2231 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-23
2-2232 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-24
2-2233 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-25
2-2234 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-26
2-2235 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-27
2-2236 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2237 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-29
2-2238 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-30
2-2239 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-31
2-2240 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-32
2-2241 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-65
2-2242 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-66
2-2243 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-67
2-2244 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-68
2-2245 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-69
2-2246 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-70
2-2247 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-71
2-2248 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-72
2-2249 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-73
2-2250 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-74
2-2251 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-75
2-2252 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-76
2-2253 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-77
2-2254 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-78
2-2255 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-79
2-2256 Sub-47 3,4-diClPh CO Single bond or CH2 Sub-80
2-2257 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-1
2-2258 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-2
2-2259 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-3
2-2260 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-4
2-2261 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-5
2-2262 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2263 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-7
2-2264 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-8
2-2265 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-9
2-2266 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-10
2-2267 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-11
2-2268 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-12
2-2269 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-13
2-2270 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-14
2-2271 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-15
2-2272 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-16
2-2273 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-17
2-2274 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-18
2-2275 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-19
2-2276 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-20
2-2277 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-21
2-2278 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-22
2-2279 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-23
2-2280 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-24
2-2281 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-25
2-2282 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-26
2-2283 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-27
2-2284 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-28
2-2285 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-29
2-2286 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-30
2-2287 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-31
2-2288 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2289 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-65
2-2290 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-66
2-2291 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-67
2-2292 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-68
2-2293 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-69
2-2294 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-70
2-2295 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-71
2-2296 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-72
2-2297 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-73
2-2298 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-74
2-2299 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-75
2-2300 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-76
2-2301 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-77
2-2302 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-78
2-2303 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-79
2-2304 Sub-81 3,4-diClPh CO Single bond or CH2 Sub-80
2-2305 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-1
2-2306 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-2
2-2307 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-3
2-2308 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-4
2-2309 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-5
2-2310 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-6
2-2311 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-7
2-2312 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-8
2-2313 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-9
2-2314 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2315 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-11
2-2316 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-12
2-2317 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-13
2-2318 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-14
2-2319 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-15
2-232O Sub-48 3,4-diClPh CO Single bond or CH2 Sub-16
2-2321 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-17
2-2322 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-18
2-2323 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-19
2-2324 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-20
2-2325 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-21
2-2326 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-22
2-2327 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-23
2-2328 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-24
2-2329 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-25
2-2330 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-26
2-2331 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-27
2-2332 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-28
2-2333 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-29
2-2334 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-30
2-2335 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-31
2-2336 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-32
2-2337 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-65
2-2338 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-66
2-2339 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-67
2-2340 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2341 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-69
2-2342 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-70
2-2343 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-71
2-2344 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-72
2-2345 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-73
2-2346 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-74
2-2347 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-75
2-2348 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-76
2-2349 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-77
2-2350 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-78
2-2351 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-79
2-2352 Sub-48 3,4-diClPh CO Single bond or CH2 Sub-80
2-2353 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-1
2-2354 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-2
2-2355 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-3
2-2356 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-4
2-2357 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-5
2-2358 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-6
2-2359 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-7
2-2360 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-8
2-2361 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-9
2-2362 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-10
2-2363 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-11
2-2364 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-12
2-2365 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-13
2-2366 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2367 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-15
2-2368 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-16
2-2369 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-17
2-2370 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-18
2-2371 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-19
2-2372 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-20
2-2373 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-21
2-2374 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-22
2-2375 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-23
2-2376 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-24
2-2377 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-25
2-2378 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-26
2-2379 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-27
2-2380 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-28
2-2381 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-29
2-2382 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-30
2-2383 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-31
2-2384 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-32
2-2385 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-65
2-2386 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-66
2-2387 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-67
2-2388 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-68
2-2389 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-69
2-2390 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-70
2-2391 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-71
2-2392 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2393 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-73
2-2394 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-74
2-2395 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-75
2-2396 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-76
2-2397 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-77
2-2398 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-78
2-2399 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-79
2-2400 Sub-49 3,4-diClPh CO Single bond or CH2 Sub-80
2-2401 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-1
2-2402 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-2
2-2403 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-3
2-2404 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-4
2-2405 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-5
2-2406 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-6
2-2407 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-7
2-2408 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-8
2-2409 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-9
2-2410 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-10
2-2411 Sub-50 3,4-diClPh C0 Single bond or CH2 Sub-11
2-2412 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-12
2-2413 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-13
2-2414 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-14
2-2415 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-15
2-2416 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-16
2-2417 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-17
2-2418 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2419 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-19
2-2420 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-20
2-2421 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-21
2-2422 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-22
2-2423 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-23
2-2424 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-24
2-2425 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-25
2-2426 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-26
2-2427 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-27
2-2428 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-28
2-2429 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-29
2-2430 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-30
2-2431 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-31
2-2432 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-32
2-2433 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-65
2-2434 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-66
2-2435 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-67
2-2436 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-68
2-2437 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-69
2-2438 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-70
2-2439 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-71
2-2440 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-72
2-2441 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-73
2-2442 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-74
2-2443 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-75
2-2444 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2445 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-77
2-2446 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-78
2-2447 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-79
2-2448 Sub-50 3,4-diClPh CO Single bond or CH2 Sub-80
2-2449 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-1
2-2450 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-2
2-2451 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-3
2-2452 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-4
2-2453 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-5
2-2454 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-6
2-2455 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-7
2-2456 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-8
2-2457 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-9
2-2458 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-10
2-2459 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-11
2-2460 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-12
2-2461 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-13
2-2462 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-14
2-2463 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-15
2-2464 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-16
2-2465 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-17
2-2466 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-18
2-2467 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-19
2-2468 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-20
2-2469 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-21
2-2470 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2471 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-23
2-2472 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-24
2-2473 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-25
2-2474 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-26
2-2475 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-27
2-2476 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-28
2-2477 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-29
2-2478 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-30
2-2479 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-31
2-2480 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-32
2-2481 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-65
2-2482 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-66
2-2483 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-67
2-2484 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-68
2-2485 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-69
2-2486 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-70
2-2487 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-71
2-2488 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-72
2-2489 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-73
2-2490 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-74
2-2491 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-75
2-2492 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-76
2-2493 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-77
2-2494 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-78
2-2495 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-79
2-2496 Sub-51 3,4-diClPh CO Single bond or CH2 Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2497 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-1
2-2498 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-2
2-2499 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-3
2-2500 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-4
2-2501 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-5
2-2502 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-6
2-2503 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-7
2-2504 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-8
2-2505 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-9
2-2506 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-10
2-2507 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-11
2-2508 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-12
2-2509 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-13
2-2510 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-14
2-2511 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-15
2-2512 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-16
2-2513 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-17
2-2514 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-18
2-2515 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-19
2-2516 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-20
2-2517 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-21
2-2518 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-22
2-2519 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-23
2-2520 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-24
2-2521 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-25
2-2522 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2523 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-27
2-2524 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-28
2-2525 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-29
2-2526 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-30
2-2527 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-31
2-2528 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-32
2-2529 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-65
2-2530 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-66
2-2531 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-67
2-2532 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-68
2-2533 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-69
2-2534 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-70
2-2535 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-71
2-2536 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-72
2-2537 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-73
2-2538 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-74
2-2539 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-75
2-2540 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-76
2-2541 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-77
2-2542 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-78
2-2543 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-79
2-2544 Sub-52 3,4-diClPh CO Single bond or CH2 Sub-80
2-2545 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-1
2-2546 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-2
2-2547 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-3
2-2548 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2549 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-5
2-2550 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-6
2-2551 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-7
2-2552 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-8
2-2553 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-9
2-2554 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-10
2-2555 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-11
2-2556 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-12
2-2557 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-13
2-2558 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-14
2-2559 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-15
2-2560 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-16
2-2561 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-17
2-2562 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-18
2-2563 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-19
2-2564 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-20
2-2565 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-21
2-2566 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-22
2-2567 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-23
2-2568 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-24
2-2569 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-25
2-2570 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-26
2-2571 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-27
2-2572 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-28
2-2573 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-29
2-2574 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2575 Sub-53 3,4-diClPh CO SheetKey or CH2 Sub-31
2-2576 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-32
2-2577 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-65
2-2578 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-66
2-2579 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-67
2-2580 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-68
2-2581 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-69
2-2582 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-70
2-2583 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-71
2-2584 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-72
2-2585 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-73
2-2586 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-74
2-2587 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-75
2-2588 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-76
2-2589 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-77
2-2590 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-78
2-2591 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-79
2-2592 Sub-53 3,4-diClPh CO Single bond or CH2 Sub-80
2-2593 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-1
2-2594 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-2
2-2595 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-3
2-2596 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-4
2-2597 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-5
2-2598 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-6
2-2599 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-7
2-2600 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2601 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-9
2-2602 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-1O
2-2603 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-11
2-2604 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-12
2-2605 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-13
2-2606 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-14
2-2607 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-15
2-2608 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-16
2-2609 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-17
2-2610 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-18
2-2611 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-19
2-2612 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-20
2-2613 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-21
2-2614 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-22
2-2615 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-23
2-2616 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-24
2-2617 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-25
2-2618 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-26
2-2619 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-27
2-2620 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-28
2-2621 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-29
2-2622 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-30
2-2623 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-31
2-2624 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-32
2-2625 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-65
2-2626 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2627 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-67
2-2628 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-68
2-2629 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-69
2-2630 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-70
2-2631 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-71
2-2632 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-72
2-2633 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-73
2-2634 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-74
2-2635 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-75
2-2636 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-76
2-2637 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-77
2-2638 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-78
2-2639 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-79
2-2640 Sub-54 3,4-diClPh CO Single bond or CH2 Sub-80
2-2641 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-1
2-2642 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-2
2-2643 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-3
2-2644 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-4
2-2645 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-5
2-2646 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-6
2-2647 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-7
2-2648 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-8
2-2649 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-9
2-2650 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-10
2-2651 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-11
2-2652 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2653 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-13
2-2654 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-14
2-2655 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-15
2-2656 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-16
2-2657 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-17
2-2658 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-18
2-2659 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-19
2-2660 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-20
2-2661 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-21
2-2662 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-22
2-2663 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-23
2-2664 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-24
2-2665 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-25
2-2666 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-26
2-2667 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-27
2-2668 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-28
2-2669 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-29
2-2670 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-30
2-2671 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-31
2-2672 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-32
2-2673 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-65
2-2674 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-66
2-2675 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-67
2-2676 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-68
2-2677 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-69
2-2678 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2679 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-71
2-2680 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-72
2-2681 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-73
2-2682 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-74
2-2683 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-75
2-2684 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-76
2-2685 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-77
2-2686 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-78
2-2687 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-79
2-2688 Sub-55 3,4-diClPh CO Single bond or CH2 Sub-80
2-2689 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-1
2-2690 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-2
2-2691 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-3
2-2692 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-4
2-2693 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-5
2-2694 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-6
2-2695 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-7
2-2696 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-8
2-2697 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-9
2-2698 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-10
2-2699 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-11
2-2700 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-12
2-2701 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-13
2-2702 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-14
2-2703 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-15
2-2704 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2705 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-17
2-2706 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-18
2-2707 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-19
2-2708 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-20
2-2709 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-21
2-2710 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-22
2-2711 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-23
2-2712 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-24
2-2713 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-25
2-2714 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-26
2-2715 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-27
2-2716 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-28
2-2717 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-29
2-2718 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-30
2-2719 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-31
2-2720 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-32
2-2721 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-65
2-2722 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-66
2-2723 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-67
2-2724 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-68
2-2725 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-69
2-2726 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-70
2-2727 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-71
2-2728 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-72
2-2729 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-73
2-2730 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2731 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-75
2-2732 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-76
2-2733 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-77
2-2734 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-78
2-2735 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-79
2-2736 Sub-56 3,4-diClPh CO Single bond or CH2 Sub-80
2-2737 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-1
2-2738 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-2
2-2739 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-3
2-2740 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-4
2-2741 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-5
2-2742 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-6
2-2743 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-7
2-2744 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-8
2-2745 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-9
2-2746 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-10
2-2747 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-11
2-2748 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-12
2-2749 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-13
2-2750 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-14
2-2751 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-15
2-2752 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-16
2-2753 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-17
2-2754 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-18
2-2755 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-19
2-2756 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2757 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-21
2-2758 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-22
2-2759 Sub-57 3,4-diClPh CO SheetKey or CH2 Sub-23
2-2760 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-24
2-2761 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-25
2-2762 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-26
2-2763 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-27
2-2764 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-28
2-2765 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-29
2-2766 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-30
2-2767 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-31
2-2768 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-32
2-2769 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-65
2-2770 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-66
2-2771 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-67
2-2772 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-68
2-2773 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-69
2-2774 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-70
2-2775 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-71
2-2776 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-72
2-2777 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-73
2-2778 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-74
2-2779 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-75
2-2780 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-76
2-2781 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-77
2-2782 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2783 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-79
2-2784 Sub-57 3,4-diClPh CO Single bond or CH2 Sub-80
2-2785 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-1
2-2786 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-2
2-2787 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-3
2-2788 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-4
2-2789 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-5
2-2790 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-6
2-2791 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-7
2-2792 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-8
2-2793 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-9
2-2794 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-10
2-2795 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-11
2-2796 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-12
2-2797 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-13
2-2798 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-14
2-2799 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-15
2-2800 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-16
2-2801 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-17
2-2802 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-18
2-2803 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-19
2-2804 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-20
2-2805 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-21
2-2806 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-22
2-2807 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-23
2-2808 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2809 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-25
2-2810 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-26
2-2811 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-27
2-2812 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-28
2-2813 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-29
2-2814 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-30
2-2815 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-31
2-2816 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-32
2-2817 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-65
2-2818 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-66
2-2819 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-67
2-2820 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-68
2-2821 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-69
2-2822 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-70
2-2823 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-71
2-2824 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-72
2-2825 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-73
2-2826 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-74
2-2827 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-75
2-2828 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-76
2-2829 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-77
2-2830 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-78
2-2831 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-79
2-2832 Sub-58 3,4-diClPh CO Single bond or CH2 Sub-80
2-2833 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-1
2-2834 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2835 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-3
2-2836 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-4
2-2837 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-5
2-2838 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-6
2-2839 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-7
2-2840 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-8
2-2841 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-9
2-2842 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-1O
2-2843 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-11
2-2844 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-12
2-2845 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-13
2-2846 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-14
2-2847 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-15
2-2848 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-16
2-2849 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-17
2-2850 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-18
2-2851 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-19
2-2852 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-20
2-2853 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-21
2-2854 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-22
2-2855 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-23
2-2856 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-24
2-2857 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-25
2-2858 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-26
2-2859 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-27
2-2860 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2861 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-29
2-2862 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-30
2-2863 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-31
2-2864 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-32
2-2865 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-65
2-2866 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-66
2-2867 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-67
2-2868 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-68
2-2869 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-69
2-2870 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-70
2-2871 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-71
2-2872 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-72
2-2873 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-73
2-2874 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-74
2-2875 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-75
2-2876 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-76
2-2877 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-77
2-2878 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-78
2-2879 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-79
2-2880 Sub-59 3,4-diClPh CO Single bond or CH2 Sub-80
2-2881 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-1
2-2882 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-2
2-2883 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-3
2-2884 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-4
2-2885 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-5
2-2886 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2887 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-7
2-2888 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-8
2-2889 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-9
2-2890 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-10
2-2891 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-11
2-2892 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-12
2-2893 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-13
2-2894 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-14
2-2895 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-15
2-2896 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-16
2-2897 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-17
2-2898 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-18
2-2899 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-19
2-2900 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-20
2-2901 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-21
2-2902 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-22
2-2903 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-23
2-2904 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-24
2-2905 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-25
2-2906 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-26
2-2907 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-27
2-2908 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-28
2-2909 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-29
2-2910 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-30
2-2911 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-31
2-2912 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2913 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-65
2-2914 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-66
2-2915 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-67
2-2916 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-68
2-2917 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-69
2-2918 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-70
2-2919 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-71
2-2920 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-72
2-2921 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-73
2-2922 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-74
2-2923 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-75
2-2924 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-76
2-2925 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-77
2-2926 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-78
2-2927 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-79
2-2928 Sub-82 3,4-diClPh CO Single bond or CH2 Sub-80
2-2929 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-1
2-2930 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-2
2-2931 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-3
2-2932 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-4
2-2933 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-5
2-2934 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-6
2-2935 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-7
2-2936 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-8
2-2937 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-9
2-2938 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2939 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-11
2-2940 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-12
2-2941 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-13
2-2942 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-14
2-2943 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-15
2-2944 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-16
2-2945 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-17
2-2946 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-18
2-2947 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-19
2-2948 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-2O
2-2949 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-21
2-2950 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-22
2-2951 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-23
2-2952 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-24
2-2953 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-25
2-2954 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-26
2-2955 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-27
2-2956 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-28
2-2957 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-29
2-2958 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-30
2-2959 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-31
2-2960 Sub-83 3,4-diClPh C0 Single bond or CH2 Sub-32
2-2961 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-65
2-2962 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-66
2-2963 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-67
2-2964 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2965 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-69
2-2966 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-70
2-2967 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-71
2-2968 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-72
2-2969 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-73
2-2970 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-74
2-2971 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-75
2-2972 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-76
2-2973 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-77
2-2974 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-78
2-2975 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-79
2-2976 Sub-83 3,4-diClPh CO Single bond or CH2 Sub-80
2-2977 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-1
2-2978 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-2
2-2979 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-3
2-2980 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-4
2-2981 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-5
2-2982 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-6
2-2983 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-7
2-2984 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-8
2-2985 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-9
2-2986 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-10
2-2987 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-11
2-2988 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-12
2-2989 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-13
2-2990 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-2991 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-15
2-2992 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-16
2-2993 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-17
2-2994 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-18
2-2995 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-19
2-2996 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-20
2-2997 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-21
2-2998 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-22
2-2999 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-23
2-3000 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-24
2-3001 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-25
2-3002 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-26
2-3003 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-27
2-3004 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-28
2-3005 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-29
2-3006 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-30
2-3007 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-31
2-3008 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-32
2-3009 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-65
2-3010 Sub-61 3,4-diClPh CO Single bond or CH 2 Sub-66
2-3011 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-67
2-3012 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-68
2-3013 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-69
2-3014 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-70
2-3015 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-71
2-3016 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3017 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-73
2-3018 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-74
2-3019 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-75
2-3020 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-76
2-3021 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-77
2-3022 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-78
2-3023 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-79
2-3024 Sub-61 3,4-diClPh CO Single bond or CH2 Sub-80
2-3025 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-1
2-3026 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-2
2-3027 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-3
2-3028 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-4
2-3029 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-5
2-3030 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-6
2-3031 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-7
2-3032 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-8
2-3033 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-9
2-3034 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-10
2-3035 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-11
2-3036 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-12
2-3037 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-13
2-3038 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-14
2-3039 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-15
2-3040 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-16
2-3041 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-17
2-3042 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3043 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-19
2-3044 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-20
2-3045 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-21
2-3046 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-22
2-3047 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-23
2-3048 Sub-60 3,4-diCiPh CO Single bond or CH2 Sub-24
2-3049 Sub-60 3,4-diClPh C0 Single bond or CH2 Sub-25
2-3050 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-26
2-3051 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-27
2-3052 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-28
2-3053 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-29
2-3054 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-30
2-3055 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-31
2-3056 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-32
2-3057 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-65
2-3058 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-66
2-3059 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-67
2-3060 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-68
2-3061 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-69
2-3062 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-70
2-3063 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-71
2-3064 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-72
2-3065 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-73
2-3066 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-74
2-3067 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-75
2-3068 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3069 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-77
2-3070 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-78
2-3071 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-79
2-3072 Sub-60 3,4-diClPh CO Single bond or CH2 Sub-80
2-3073 Sub-33 3,4-diClPh SO2 Single bond Sub-1
2-3074 Sub-33 3,4-diClPh SO2 Single bond Sub-2
2-3075 Sub-33 3,4-diClPh SO2 Single bond Sub-3
2-3076 Sub-33 3,4-diClPh SO2 Single bond Sub-4
2-3077 Sub-33 3,4-diClPh SO2 Single bond Sub-5
2-3078 Sub-33 3,4-diClPh SO2 Single bond Sub-6
2-3079 Sub-33 3,4-diClPh SO2 Single bond Sub-7
2-3080 Sub-33 3,4-diClPh SO2 Single bond Sub-8
2-3081 Sub-33 3,4-diClPh SO2 Single bond Sub-9
2-3082 Sub-33 3,4-diClPh SO2 Single bond Sub-10
2-3083 Sub-33 3,4-diClPh SO2 Single bond Sub-11
2-3084 Sub-33 3,4-diClPh SO2 Single bond Sub-12
2-3085 Sub-33 3,4-diClPh SO2 Single bond Sub-13
2-3086 Sub-33 3,4-diClPh SO2 Single bond Sub-14
2-3087 Sub-33 3,4-diClPh SO2 Single bond Sub-15
2-3088 Sub-33 3,4-diClPh SO2 Single bond Sub-16
2-3089 Sub-33 3,4-diClPh SO2 Single bond Sub-17
2-3090 Sub-33 3,4-diClPh SO2 Single bond Sub-18
2-3091 Sub-33 3,4-diClPh SO2 Single bond Sub-19
2-3092 Sub-33 3,4-diClPh SO2 Single bond Sub-20
2-3093 Sub-33 3,4-diClPh SO2 Single bond Sub-21
2-3094 Sub-33 3,4-diClPh SO2 Single bond Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3095 Sub-33 3,4-diClPh SO2 Single bond Sub-23
2-3096 Sub-33 3,4-diClPh SO2 Single bond Sub-24
2-3097 Sub-33 3,4-diClPh SO2 Single bond Sub-25
2-3098 Sub-33 3,4-diClPh SO2 Single bond Sub-26
2-3099 Sub-33 3,4-diClPh SO2 Single bond Sub-27
2-3100 Sub-33 3,4-diClPh SO2 Single bond Sub-28
2-3101 Sub-33 3,4-diClPh SO2 Single bond Sub-29
2-3102 Sub-33 3,4-diClPh SO2 Single bond Sub-30
2-3103 Sub-33 3,4-diClPh SO2 Single bond Sub-31
2-3104 Sub-33 3,4-diClPh SO2 Single bond Sub-32
2-3105 Sub-33 3,4-diClPh SO2 Single bond Sub-65
2-3106 Sub-33 3,4-diClPh SO2 Single bond Sub-66
2-3107 Sub-33 3,4-diClPh SO2 Single bond Sub-67
2-3108 Sub-33 3,4-diClPh SO2 Single bond Sub-68
2-3109 Sub-33 3,4-diClPh SO2 Single bond Sub-69
2-3110 Sub-33 3,4-diClPh SO2 Single bond Sub-70
2-3111 Sub-33 3,4-diClPh SO2 Single bond Sub-71
2-3112 Sub-33 3,4-diClPh SO2 Single bond Sub-72
2-3113 Sub-33 3,4-diClPh SO2 Single bond Sub-73
2-3114 Sub-33 3,4-diClPh SO2 Single bond Sub-74
2-3115 Sub-33 3,4-diClPh SO2 Single bond Sub-75
2-3116 Sub-33 3,4-diClPh SO2 Single bond Sub-76
2-3117 Sub-33 3,4-diClPh SO2 Single bond Sub-77
2-3118 Sub-33 3,4-diClPh SO2 Single bond Sub-78
2-3119 Sub-33 3,4-diClPh SO2 Single bond Sub-79
2-3120 Sub-33 3,4-diClPh SO2 Single bond Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3121 Sub-34 3,4-diClPh SO2 Single bond Sub-1
2-3122 Sub-34 3,4-diClPh SO2 Single bond Sub-2
2-3123 Sub-34 3,4-diClPh SO2 Single bond Sub-3
2-3124 Sub-34 3,4-diClPh SO2 Single bond Sub-4
2-3125 Sub-34 3,4-diClPh SO2 Single bond Sub-5
2-3126 Sub-34 3,4-diClPh SO2 Single bond Sub-6
2-3127 Sub-34 3,4-diClPh SO2 Single bond Sub-7
2-3128 Sub-34 3,4-diClPh SO2 Single bond Sub-8
2-3129 Sub-34 3,4-diClPh SO2 Single bond Sub-9
2-3130 Sub-34 3,4-diClPh SO2 Single bond Sub-10
2-3131 Sub-34 3,4-diClPh SO2 Single bond Sub-11
2-3132 Sub-34 3,4-diClPh SO2 Single bond Sub-12
2-3133 Sub-34 3,4-diClPh SO2 Single bond Sub-13
2-3134 Sub-34 3,4-diClPh SO2 Single bond Sub-14
2-3135 Sub-34 3,4-diClPh SO2 Single bond Sub-15
2-3136 Sub-34 3,4-diClPh SO2 Single bond Sub-16
2-3137 Sub-34 3,4-diClPh SO2 Single bond Sub-17
2-3138 Sub-34 3,4-diClPh SO2 Single bond Sub-18
2-3139 Sub-34 3,4-diClPh SO2 Single bond Sub-19
2-3140 Sub-34 3,4-diClPh SO2 Single bond Sub-20
2-3141 Sub-34 3,4-diClPh SO2 Single bond Sub-21
2-3142 Sub-34 3,4-diClPh SO2 Single bond Sub-22
2-3143 Sub-34 3,4-diClPh SO2 Single bond Sub-23
2-3144 Sub-34 3,4-diClPh SO2 Single bond Sub-24
2-3145 Sub-34 3,4-diClPh SO2 Single bond Sub-25
2-3146 Sub-34 3,4-diClPh SO2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3147 Sub-34 3,4-diClPh SO2 Single bond Sub-27
2-3148 Sub-34 3,4-diClPh SO2 Single bond Sub-28
2-3149 Sub-34 3,4-diClPh SO2 Single bond Sub-29
2-3150 Sub-34 3,4-diClPh SO2 Single bond Sub-30
2-3151 Sub-34 3,4-diClPh SO2 Single bond Sub-31
2-3152 Sub-34 3,4-diClPh SO2 Single bond Sub-32
2-3153 Sub-34 3,4-diClPh SO2 Single bond Sub-65
2-3154 Sub-34 3,4-diClPh SO2 Single bond Sub-66
2-3155 Sub-34 3,4-diClPh SO2 Single bond Sub-67
2-3156 Sub-34 3,4-diClPh SO2 Single bond Sub-68
2-3157 Sub-34 3,4-diClPh SO2 Single bond Sub-69
2-3158 Sub-34 3,4-diClPh SO2 Single bond Sub-70
2-3159 Sub-34 3,4-diClPh SO2 Single bond Sub-71
2-3160 Sub-34 3,4-diClPh SO2 Single bond Sub-72
2-3161 Sub-34 3,4-diClPh SO2 Single bond Sub-73
2-3162 Sub-34 3,4-dClPh SO2 Single bond Sub-74
2-3163 Sub-34 3,4-diClPh SO2 Single bond Sub-75
2-3164 Sub-34 3,4-diClPh SO2 Single bond Sub-76
2-3165 Sub-34 3,4-diClPh SO2 Single bond Sub-77
2-3166 Sub-34 3,4-diClPh SO2 Single bond Sub-78
2-3167 Sub-34 3,4-diClPh SO2 Single bond Sub-79
2-3168 Sub-34 3,4-diClPh SO2 Single bond Sub-80
2-3169 Sub-35 3,4-diClPh SO2 Single bond Sub-1
2-3170 Sub-35 3,4-diClPh SO2 Single bond Sub-2
2-3171 Sub-35 3,4-diClPh SO2 Single bond Sub-3
2-3172 Sub-35 3,4-diClPh SO2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3173 Sub-35 3,4-diClPh SO2 Single bond Sub-5
2-3174 Sub-35 3,4-diClPh SO2 Single bond Sub-6
2-3175 Sub-35 3,4-diClPh SO2 Single bond Sub-7
2-3176 Sub-35 3,4-diClPh SO2 Single bond Sub-8
2-3177 Sub-35 3,4-diClPh SO2 Single bond Sub-9
2-3178 Sub-35 3,4-diClPh SO2 Single bond Sub-10
2-3179 Sub-35 3,4-diClPh SO2 Single bond Sub-11
2-3180 Sub-35 3,4-diClPh SO2 Single bond Sub-12
2-3181 Sub-35 3,4-diClPh SO2 Single bond Sub-13
2-3182 Sub-35 3,4-diClPh SO2 Single bond Sub-14
2-3183 Sub-35 3,4-diClPh SO2 Single bond Sub-15
2-3184 Sub-35 3,4-diClPh SO2 Single bond Sub-16
2-3185 Sub-35 3,4-diClPh SO2 Single bond Sub-17
2-3186 Sub-35 3,4-diClPh SO2 Single bond Sub-18
2-3187 Sub-35 3,4-diClPh SO2 Single bond Sub-19
2-3188 Sub-35 3,4-diClPh SO2 Single bond Sub-20
2-3189 Sub-35 3,4-diClPh SO2 Single bond Sub-21
2-3190 Sub-35 3,4-diClPh SO2 Single bond Sub-22
2-3191 Sub-35 3,4-diClPh SO2 Single bond Sub-23
2-3192 Sub-35 3,4-diClPh SO2 Single bond Sub-24
2-3193 Sub-35 3,4-diClPh SO2 Single bond Sub-25
2-3194 Sub-35 3,4-diClPh SO2 Single bond Sub-26
2-3195 Sub-35 3,4-diClPh SO2 Single bond Sub-27
2-3196 Sub-35 3,4-diClPh SO2 Single bond Sub-28
2-3197 Sub-35 3,4-diClPh SO2 Single bond Sub-29
2-3198 Sub-35 3,4-diClPh SO2 Single bond Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3199 Sub-35 3,4-diClPh SO2 Single bond Sub-31
2-3200 Sub-35 3,4-diClPh SO2 Single bond Sub-32
2-3201 Sub-35 3,4-diClPh SO2 Single bond Sub-65
2-3202 Sub-35 3,4-diClPh SO2 Single bond Sub-66
2-3203 Sub-35 3,4-diClPh SO2 Single bond Sub-67
2-3204 Sub-35 3,4-diClPh SO2 Single bond Sub-68
2-3205 Sub-35 3,4-diClPh SO2 Single bond Sub-69
2-3206 Sub-35 3,4-diClPh SO2 Single bond Sub-70
2-3207 Sub-35 3,4-diClPh SO2 Single bond Sub-71
2-3208 Sub-35 3,4-diClPh SO2 Single bond Sub-72
2-3209 Sub-35 3,4-diClPh SO2 Single bond Sub-73
2-3210 Sub-35 3,4-diClPh SO2 Single bond Sub-74
2-3211 Sub-35 3,4-diClPh SO2 Single bond Sub-75
2-3212 Sub-35 3,4-diClPh SO2 Single bond Sub-76
2-3213 Sub-35 3,4-diClPh SO2 Single bond Sub-77
2-3214 Sub-35 3,4-diClPh SO2 Single bond Sub-78
2-3215 Sub-35 3,4-diClPh SO2 Single bond Sub-79
2-3216 Sub-35 3,4-diClPh SO2 Single bond Sub-80
2-3217 Sub-36 3,4-diClPh SO2 Single bond Sub-1
2-3218 Sub-36 3,4-diClPh SO2 Single bond Sub-2
2-3219 Sub-36 3,4-diClPh SO2 Single bond Sub-3
2-3220 Sub-36 3,4-diClPh SO2 Single bond Sub-4
2-3221 Sub-36 3,4-diClPh SO2 Single bond Sub-5
2-3222 Sub-36 3,4-diClPh SO2 Single bond Sub-6
2-3223 Sub-36 3,4-diClPh SO2 Single bond Sub-7
2-3224 Sub-36 3,4-diClPh SO2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3225 Sub-36 3,4-diClPh SO2 Single bond Sub-9
2-3226 Sub-36 3,4-diClPh SO2 Single bond Sub-10
2-3227 Sub-36 3,4-diClPh SO2 Single bond Sub-11
2-3228 Sub-36 3,4-diClPh SO2 Single bond Sub-12
2-3229 Sub-36 3,4-diClPh SO2 Single bond Sub-13
2-3230 Sub-36 3,4-diClPh SO2 Single bond Sub-14
2-3231 Sub-36 3,4-diClPh SO2 Single bond Sub-15
2-3232 Sub-36 3,4-diClPh SO2 Single bond Sub-16
2-3233 Sub-36 3,4-diClPh SO2 Single bond Sub-17
2-3234 Sub-36 3,4-diClPh SO2 Single bond Sub-18
2-3235 Sub-36 3,4-diClPh SO2 Single bond Sub-19
2-3236 Sub-36 3,4-diClPh SO2 Single bond Sub-20
2-3237 Sub-36 3,4-diClPh SO2 Single bond Sub-21
2-3238 Sub-36 3,4-diClPh SO2 Single bond Sub-22
2-3239 Sub-36 3,4-diClPh SO2 Single bond Sub-23
2-3240 Sub-36 3,4-diClPh SO2 Single bond Sub-24
2-3241 Sub-36 3,4-diClPh SO2 Single bond Sub-25
2-3242 Sub-36 3,4-diClPh SO2 Single bond Sub-26
2-3243 Sub-36 3,4-diClPh SO2 Single bond Sub-27
2-3244 Sub-36 3,4-diClPh SO2 Single bond Sub-28
2-3245 Sub-36 3,4-diClPh SO2 Single bond Sub-29
2-3246 Sub-36 3,4-diClPh SO2 Single bond Sub-30
2-3247 Sub-36 3,4-diClPh SO2 Single bond Sub-31
2-3248 Sub-36 3,4-diClPh SO2 Single bond Sub-32
2-3249 Sub-36 3,4-diClPh SO2 Single bond Sub-65
2-3250 Sub-36 3,4-diClPh SO2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3251 Sub-36 3,4-diClPh SO2 Single bond Sub-67
2-3252 Sub-36 3,4-diClPh SO2 Single bond Sub-68
2-3253 Sub-36 3,4-diClPh SO2 Single bond Sub-69
2-3254 Sub-36 3,4-diClPh SO2 Single bond Sub-70
2-3255 Sub-36 3,4-diClPh SO2 Single bond Sub-71
2-3256 Sub-36 3,4-diClPh SO2 Single bond Sub-72
2-3257 Sub-36 3,4-diClPh SO2 Single bond Sub-73
2-3258 Sub-36 3,4-diClPh SO2 Single bond Sub-74
2-3259 Sub-36 3,4-diClPh SO2 Single bond Sub-75
2-3260 Sub-36 3,4-diClPh SO2 Single bond Sub-76
2-3261 Sub-36 3,4-diClPh SO2 Single bond Sub-77
2-3262 Sub-36 3,4-diClPh SO2 Single bond Sub-78
2-3263 Sub-36 3,4-diClPh SO2 Single bond Sub-79
2-3264 Sub-36 3,4-diClPh SO2 Single bond Sub-80
2-3265 Sub-37 3,4-diClPh SO2 Single bond Sub-1
2-3266 Sub-37 3,4-diClPh SO2 Single bond Sub-2
2-3267 Sub-37 3,4-diClPh SO2 Single bond Sub-3
2-3268 Sub-37 3,4-diClPh SO2 Single bond Sub-4
2-3269 Sub-37 3,4-diClPh SO2 Single bond Sub-5
2-3270 Sub-37 3,4-diClPh SO2 Single bond Sub-6
2-3271 Sub-37 3,4-diClPh SO2 Single bond Sub-7
2-3272 Sub-37 3,4-diClPh SO2 Single bond Sub-8
2-3273 Sub-37 3,4-diClPh SO2 Single bond Sub-9
2-3274 Sub-37 3,4-diClPh SO2 Single bond Sub-10
2-3275 Sub-37 3,4-diClPh SO2 Single bond Sub-11
2-3276 Sub-37 3,4-diClPh SO2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3277 Sub-37 3,4-diClPh SO2 Single bond Sub-13
2-3278 Sub-37 3,4-diClPh SO2 Single bond Sub-14
2-3279 Sub-37 3,4-diClPh SO2 Single bond Sub-15
2-3280 Sub-37 3,4-diClPh SO2 Single bond Sub-16
2-3281 Sub-37 3,4-diClPh SO2 Single bond Sub-17
2-3282 Sub-37 3,4-diClPh SO2 Single bond Sub-18
2-3283 Sub-37 3,4-diClPh SO2 Single bond Sub-19
2-3284 Sub-37 3,4-diClPh SO2 Single bond Sub-20
2-3285 Sub-37 3,4-diClPh SO2 Single bond Sub-21
2-3286 Sub-37 3,4-diClPh SO2 Single bond Sub-22
2-3287 Sub-37 3,4-diClPh SO2 Single bond Sub-23
2-3288 Sub-37 3,4-diClPh SO2 Single bond Sub-24
2-3289 Sub-37 3,4-diClPh SO2 Single bond Sub-25
2-3290 Sub-37 3,4-diClPh SO2 Single bond Sub-26
2-3291 Sub-37 3,4-diClPh SO2 Single bond Sub-27
2-3292 Sub-37 3,4-diClPh SO2 Single bond Sub-28
2-3293 Sub-37 3,4-diClPh SO2 Single bond Sub-29
2-3294 Sub-37 3,4-diClPh SO2 Single bond Sub-30
2-3295 Sub-37 3,4-diClPh SO2 Single bond Sub-31
2-3296 Sub-37 3,4-diClPh SO2 Single bond Sub-32
2-3297 Sub-37 3,4-diClPh SO2 Single bond Sub-65
2-3298 Sub-37 3,4-diClPh SO2 Single bond Sub-66
2-3299 Sub-37 3,4-diClPh SO2 Single bond Sub-67
2-3300 Sub-37 3,4-diClPh SO2 Single bond Sub-68
2-3301 Sub-37 3,4-diClPh SO2 Single bond Sub-69
2-3302 Sub-37 3,4-diClPh SO2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3303 Sub-37 3,4-diClPh SO2 Single bond Sub-71
2-3304 Sub-37 3,4-diClPh SO2 Single bond Sub-72
2-3305 Sub-37 3,4-diClPh SO2 Single bond Sub-73
2-3306 Sub-37 3,4-diClPh SO2 Single bond Sub-74
2-3307 Sub-37 3,4-diClPh SO2 Single bond Sub-75
2-3308 Sub-37 3,4-diClPh SO2 Single bond Sub-76
2-3309 Sub-37 3,4-diClPh SO2 Single bond Sub-77
2-3310 Sub-37 3,4-diClPh SO2 Single bond Sub-78
2-3311 Sub-37 3,4-diClPh SO2 Single bond Sub-79
2-3312 Sub-37 3,4-diClPh SO2 Single bond Sub-80
2-3313 Sub-38 3,4-diClPh SO2 Single bond Sub-1
2-3314 Sub-38 3,4-diClPh SO2 Single bond Sub-2
2-3315 Sub-38 3,4-diClPh SO2 Single bond Sub-3
2-3316 Sub-38 3,4-diClPh SO2 Single bond Sub-4
2-3317 Sub-38 3,4-diClPh SO2 Single bond Sub-5
2-3318 Sub-38 3,4-diClPh SO2 Single bond Sub-6
2-3319 Sub-38 3,4-diClPh SO2 Single bond Sub-7
2-3320 Sub-38 3,4-diClPh SO2 Single bond Sub-8
2-3321 Sub-38 3,4-diClPh SO2 Single bond Sub-9
2-3322 Sub-38 3,4-diClPh SO2 Single bond Sub-10
2-3323 Sub-38 3,4-diClPh SO2 Single bond Sub-11
2-3324 Sub-38 3,4-diClPh SO2 Single bond Sub-12
2-3325 Sub-38 3,4-diClPh SO2 Single bond Sub-13
2-3326 Sub-38 3,4-diClPh SO2 Single bond Sub-14
2-3327 Sub-38 3,4-diClPh SO2 Single bond Sub-15
2-3328 Sub-38 3,4-diClPh SO2 Single bond Sub-16
Table 2(cont.)
Chemical combinationArticle (A) Serial number R1 R2 A B Z
2-3329 Sub-38 3,4-diClPh SO2 Single bond Sub-17
2-3330 Sub-38 3,4-diClPh SO2 Single bond Sub-18
2-3331 Sub-38 3,4-diClPh SO2 Single bond Sub-19
2-3332 Sub-38 3,4-diClPh SO2 Single bond Sub-20
2-3333 Sub-38 3,4-diClPh SO2 Single bond Sub-21
2-3334 Sub-38 3,4-diClPh SO2 Single bond Sub-22
2-3335 Sub-38 3,4-diClPh SO2 Single bond Sub-23
2-3336 Sub-38 3,4-diClPh SO2 Single bond Sub-24
2-3337 Sub-38 3,4-diClPh SO2 Single bond Sub-25
2-3338 Sub-38 3,4-diClPh SO2 Single bond Sub-26
2-3339 Sub-38 3,4-diClPh SO2 Single bond Sub-27
2-3340 Sub-38 3,4-diClPh SO2 Single bond Sub-28
2-3341 Sub-38 3,4-diClPh SO2 Single bond Sub-29
2-3342 Sub-38 3,4-diClPh SO2 Single bond Sub-30
2-3343 Sub-38 3,4-diClPh SO2 Single bond Sub-31
2-3344 Sub-38 3,4-diClPh SO2 Single bond Sub-32
2-3345 Sub-38 3,4-diClPh SO2 Single bond Sub-65
2-3346 Sub-38 3,4-diClPh SO2 Single bond Sub-66
2-3347 Sub-38 3,4-diClPh SO2 Single bond Sub-67
2-3348 Sub-38 3,4-diClPh SO2 Single bond Sub-68
2-3349 Sub-38 3,4-diClPh SO2 Single bond Sub-69
2-3350 Sub-38 3,4-diClPh SO2 Single bond Sub-70
2-3351 Sub-38 3,4-diClPh SO2 Single bond Sub-71
2-3352 Sub-38 3,4-diClPh SO2 Single bond Sub-72
2-3353 Sub-38 3,4-diClPh SO2 Single bond Sub-73
2-3354 Sub-38 3,4-diClPh SO2 Single bond Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3355 Sub-38 3,4-diClPh SO2 Single bond Sub-75
2-3356 Sub-38 3,4-diClPh SO2 Single bond Sub-76
2-3357 Sub-38 3,4-diClPh SO2 Single bond Sub-77
2-3358 Sub-38 3,4-diClPh SO2 Single bond Sub-78
2-3359 Sub-38 3,4-diClPh SO2 Single bond Sub-79
2-3360 Sub-38 3,4-diClPh SO2 Single bond Sub-80
2-3361 Sub-39 3,4-diClPh SO2 Single bond Sub-1
2-3362 Sub-39 3,4-diClPh SO2 Single bond Sub-2
2-3363 Sub-39 3,4-diClPh SO2 Single bond Sub-3
2-3364 Sub-39 3,4-diClPh SO2 Single bond Sub-4
2-3365 Sub-39 3,4-diClPh SO2 Single bond Sub-5
2-3366 Sub-39 3,4-diClPh SO2 Single bond Sub-6
2-3367 Sub-39 3,4-diClPh SO2 Single bond Sub-7
2-3368 Sub-39 3,4-diClPh SO2 Single bond Sub-8
2-3369 Sub-39 3,4-diClPh SO2 Single bond Sub-9
2-3370 Sub-39 3,4-diClPh SO2 Single bond Sub-10
2-3371 Sub-39 3,4-diClPh SO2 Single bond Sub-11
2-3372 Sub-39 3,4-diClPh SO2 Single bond Sub-12
2-3373 Sub-39 3,4-diClPh SO2 Single bond Sub-13
2-3374 Sub-39 3,4-diClPh SO2 Single bond Sub-14
2-3375 Sub-39 3,4-diClPh SO2 Single bond Sub-15
2-3376 Sub-39 3,4-diClPh SO2 Single bond Sub-16
2-3377 Sub-39 3,4-diClPh SO2 Single bond Sub-17
2-3378 Sub-39 3,4-diClPh SO2 Single bond Sub-18
2-3379 Sub-39 3,4-diClPh SO2 Single bond Sub-19
2-3380 Sub-39 3,4-diClPh SO2 Single bond Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3381 Sub-39 3,4-diClPh SO2 Single bond Sub-21
2-3382 Sub-39 3,4-diClPh SO2 Single bond Sub-22
2-3383 Sub-39 3,4-diClPh SO2 Single bond Sub-23
2-3384 Sub-39 3,4-diClPh SO2 Single bond Sub-24
2-3385 Sub-39 3,4-diClPh SO2 Single bond Sub-25
2-3386 Sub-39 3,4-diClPh SO2 Single bond Sub-26
2-3387 Sub-39 3,4-diClPh SO2 Single bond Sub-27
2-3388 Sub-39 3,4-diClPh SO2 Single bond Sub-28
2-3389 Sub-39 3,4-diClPh SO2 Single bond Sub-29
2-3390 Sub-39 3,4-diClPh SO2 Single bond Sub-30
2-3391 Sub-39 3,4-diClPh SO2 Single bond Sub-31
2-3392 Sub-39 3,4-diClPh SO2 Single bond Sub-32
2-3393 Sub-39 3,4-diClPh SO2 Single bond Sub-65
2-3394 Sub-39 3,4-diClPh SO2 Single bond Sub-66
2-3395 Sub-39 3,4-diClPh SO2 Single bond Sub-67
2-3396 Sub-39 3,4-diClPh SO2 Single bond Sub-68
2-3397 Sub-39 3,4-diClPh SO2 Single bond Sub-69
2-3398 Sub-39 3,4-diClPh SO2 Single bond Sub-70
2-3399 Sub-39 3,4-diClPh SO2 Single bond Sub-71
2-3400 Sub-39 3,4-diClPh SO2 Single bond Sub-72
2-3401 Sub-39 3,4-diClPh SO2 Single bond Sub-73
2-3402 Sub-39 3,4-diClPh SO2 Single bond Sub-74
2-3403 Sub-39 3,4-diClPh SO2 Single bond Sub-75
2-3404 Sub-39 3,4-diClPh SO2 Single bond Sub-76
2-3405 Sub-39 3,4-diClPh SO2 Single bond Sub-77
2-3406 Sub-39 3,4-diClPh SO2 Single bond Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3407 Sub-39 3,4-diClPh SO2 Single bond Sub-79
2-3408 Sub-39 3,4-diClPh SO2 Single bond Sub-80
2-3409 Sub-40 3,4-diClPh SO2 Single bond Sub-1
2-3410 Sub-40 3,4-diClPh SO2 Single bond Sub-2
2-3411 Sub-40 3,4-diClPh SO2 Single bond Sub-3
2-3412 Sub-40 3,4-diClPh SO2 Single bond Sub-4
2-3413 Sub-40 3,4-diClPh SO2 Single bond Sub-5
2-3414 Sub-40 3,4-diClPh SO2 Single bond Sub-6
2-3415 Sub-40 3,4-diClPh SO2 Single bond Sub-7
2-3416 Sub-40 3,4-diClPh SO2 Single bond Sub-8
2-3417 Sub-40 3,4-diClPh SO2 Single bond Sub-9
2-3418 Sub-40 3,4-diClPh SO2 Single bond Sub-10
2-3419 Sub-40 3,4-diClPh SO2 Single bond Sub-11
2-3420 Sub-40 3,4-diClPh SO2 Single bond Sub-12
2-3421 Sub-40 3,4-diClPh SO2 Single bond Sub-13
2-3422 Sub-40 3,4-diClPh SO2 Single bond Sub-14
2-3423 Sub-40 3,4-diClPh SO2 Single bond Sub-15
2-3424 Sub-40 3,4-diClPh SO2 Single bond Sub-16
2-3425 Sub-40 3,4-diClPh SO2 Single bond Sub-17
2-3426 Sub-40 3,4-diClPh SO2 Single bond Sub-18
2-3427 Sub-40 3,4-diClPh SO2 Single bond Sub-19
2-3428 Sub-40 3,4-diClPh SO2 Single bond Sub-20
2-3429 Sub-40 3,4-diClPh SO2 Single bond Sub-21
2-3430 Sub-40 3,4-diClPh SO2 Single bond Sub-22
2-3431 Sub-40 3,4-diClPh SO2 Single bond Sub-23
2-3432 Sub-40 3,4-diClPh SO2 Single bond Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3433 Sub-40 3,4-diClPh SO2 Single bond Sub-25
2-3434 Sub-40 3,4-diClPh SO2 Single bond Sub-26
2-3435 Sub-40 3,4-diClPh SO2 Single bond Sub-27
2-3436 Sub-40 3,4-diClPh SO2 Single bond Sub-28
2-3437 Sub-40 3,4-diClPh SO2 Sin le bond Sub-29
2-3438 Sub-40 3,4-diClPh SO2 Single bond Sub-30
2-3439 Sub-40 3,4-diClPh SO2 Single bond Sub-31
2-3440 Sub-40 3,4-diClPh SO2 Single bond Sub-32
2-3441 Sub-40 3,4-diClPh SO2 Single bond Sub-65
2-3442 Sub-40 3,4-diClPh SO2 Single bond Sub-66
2-3443 Sub-40 3,4-diClPh SO2 Single bond Sub-67
2-3444 Sub-40 3,4-diClPh SO2 Single bond Sub-68
2-3445 Sub-40 3,4-diClPh SO2 Single bond Sub-69
2-3446 Sub-40 3,4-diClPh SO2 Single bond Sub-70
2-3447 Sub-40 3,4-diClPh SO2 Single bond Sub-71
2-3448 Sub-40 3,4-diClPh SO2 Single bond Sub-72
2-3449 Sub-40 3,4-diClPh SO2 Single bond Sub-73
2-3450 Sub-40 3,4-diClPh SO2 Single bond Sub-74
2-3451 Sub-40 3,4-diClPh SO2 Single bond Sub-75
2-3452 Sub-40 3,4-diClPh SO2 Single bond Sub-76
2-3453 Sub-40 3,4-diClPh SO2 Single bond Sub-77
2-3454 Sub-40 3,4-diClPh SO2 Single bond Sub-78
2-3455 Sub-40 3,4-diClPh SO2 Single bond Sub-79
2-3456 Sub-40 3,4-diClPh SO2 Single bond Sub-80
2-3457 Sub-41 3,4-diClPh SO2 Single bond Sub-1
2-3458 Sub-41 3,4-diClPh SO2 Single bond Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3459 Sub-41 3,4-diClPh SO2 Single bond Sub-3
2-3460 Sub-41 3,4-diClPh SO2 Single bond Sub-4
2-3461 Sub-41 3,4-diClPh SO2 Single bond Sub-5
2-3462 Sub-41 3,4-diClPh SO2 Single bond Sub-6
2-3463 Sub-41 3,4-diClPh SO2 Single bond Sub-7
2-3464 Sub-41 3,4-diClPh SO2 Single bond Sub-8
2-3465 Sub-41 3,4-diClPh SO2 Single bond Sub-9
2-3466 Sub-41 3,4-diClPh SO2 Single bond Sub-10
2-3467 Sub-41 3,4-diClPh SO2 Single bond Sub-11
2-3468 Sub-41 3,4-diClPh SO2 Single bond Sub-12
2-3469 Sub-41 3,4-diClPh SO2 Single bond Sub-13
2-3470 Sub-41 3,4-diClPh SO2 Single bond Sub-14
2-3471 Sub-41 3,4-diClPh SO2 Single bond Sub-15
2-3472 Sub-41 3,4-diClPh SO2 Single bond Sub-16
2-3473 Sub-41 3,4-diClPh SO2 Single bond Sub-17
2-3474 Sub-41 3,4-diClPh SO2 Single bond Sub-18
2-3475 Sub-41 3,4-diClPh SO2 Single bond Sub-19
2-3476 Sub-41 3,4-diClPh SO2 Single bond Sub-20
2-3477 Sub-41 3,4-diClPh SO2 Single bond Sub-21
2-3478 Sub-41 3,4-diClPh SO2 Single bond Sub-22
2-3479 Sub-41 3,4-diClPh SO2 Single bond Sub-23
2-3480 Sub-41 3,4-diClPh SO2 Single bond Sub-24
2-3481 Sub-41 3,4-diClPh SO2 Single bond Sub-25
2-3482 Sub-41 3,4-diClPh SO2 Single bond Sub-26
2-3483 Sub-41 3,4-diClPh SO2 Single bond Sub-27
2-3484 Sub-41 3,4-diClPh SO2 Single bond Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3485 Sub-41 3,4-diClPh SO2 Single bond Sub-29
2-3486 Sub-41 3,4-diClPh SO2 Single bond Sub-30
2-3487 Sub-41 3,4-diClPh SO2 Single bond Sub-31
2-3488 Sub-41 3,4-diClPh SO2 Single bond Sub-32
2-3489 Sub-41 3,4-diClPh SO2 Single bond Sub-65
2-3490 Sub-41 3,4-diClPh SO2 Single bond Sub-66
2-3491 Sub-41 3,4-diClPh SO2 Single bond Sub-67
2-3492 Sub-41 3,4-diClPh SO2 Single bond Sub-68
2-3493 Sub-41 3,4-diClPh SO2 Single bond Sub-69
2-3494 Sub-41 3,4-diClPh SO2 Single bond Sub-70
2-3495 Sub-41 3,4-diClPh SO2 Single bond Sub-71
2-3496 Sub-41 3,4-diClPh SO2 Single bond Sub-72
2-3497 Sub-41 3,4-diClPh SO2 Single bond Sub-73
2-3498 Sub-41 3,4-diClPh SO2 Single bond Sub-74
2-3499 Sub-41 3,4-diClPh SO2 Single bond Sub-75
2-3500 Sub-41 3,4-diClPh SO2 Single bond Sub-76
2-3501 Sub-41 3,4-diClPh SO2 Single bond Sub-77
2-3502 Sub-41 3,4-diClPh SO2 Single bond Sub-78
2-3503 Sub-41 3,4-diClPh SO2 Single bond Sub-79
2-3504 Sub-41 3,4-diClPh SO2 Single bond Sub-80
2-3505 Sub-42 3,4-diClPh SO2 Single bond Sub-1
2-3506 Sub-42 3,4-diClPh SO2 Single bond Sub-2
2-3507 Sub-42 3,4-diClPh SO2 Single bond Sub-3
2-3508 Sub-42 3,4-diClPh SO2 Single bond Sub-4
2-3509 Sub-42 3,4-diClPh SO2 Single bond Sub-5
2-3510 Sub-42 3,4-diClPh SO2 Single bond Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3511 Sub-42 3,4-diClPh SO2 Single bond Sub-7
2-3512 Sub-42 3,4-diClPh SO2 Single bond Sub-8
2-3513 Sub-42 3,4-diClPh SO2 Single bond Sub-9
2-3514 Sub-42 3,4-diClPh SO2 Single bond Sub-10
2-3515 Sub-42 3,4-diClPh SO2 Single bond Sub-11
2-3516 Sub-42 3,4-diClPh SO2 Single bond Sub-12
2-3517 Sub-42 3,4-diClPh SO2 Single bond Sub-13
2-3518 Sub-42 3,4-diClPh SO2 Single bond Sub-14
2-3519 Sub-42 3,4-diClPh SO2 SheetKey with a key body Sub-15
2-3520 Sub-42 3,4-diClPh SO2 Single bond Sub-16
2-3521 Sub-42 3,4-diClPh SO2 Single bond Sub-17
2-3522 Sub-42 3,4-diClPh SO2 Single bond Sub-18
2-3523 Sub-42 3,4-diClPh SO2 Single bond Sub-19
2-3524 Sub-42 3,4-diClPh SO2 Single bond Sub-20
2-3525 Sub-42 3,4-diClPh SO2 Single bond Sub-21
2-3526 Sub-42 3,4-diClPh SO2 Single bond Sub-22
2-3527 Sub-42 3,4-diClPh SO2 Single bond Sub-23
2-3528 Sub-42 3,4-diClPh SO2 Single bond Sub-24
2-3529 Sub-42 3,4-diClPh SO2 Single bond Sub-25
2-3530 Sub-42 3,4-diClPh SO2 Single bond Sub-26
2-3531 Sub-42 3,4-diClPh SO2 Single bond Sub-27
2-3532 Sub-42 3,4-diClPh SO2 Single bond Sub-28
2-3533 Sub-42 3,4-diClPh SO2 Single bond Sub-29
2-3534 Sub-42 3,4-diClPh SO2 Single bond Sub-30
2-3535 Sub-42 3,4-diClPh SO2 Single bond Sub-31
2-3536 Sub-42 3,4-diClPh SO2 Single bond Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3537 Sub-42 3,4-diClPh SO2 Single bond Sub-65
2-3538 Sub-42 3,4-diClPh SO2 Single bond Sub-66
2-3539 Sub-42 3,4-diClPh SO2 Single bond Sub-67
2-3540 Sub-42 3,4-diClPh SO2 Single bond Sub-68
2-3541 Sub-42 3,4-diClPh SO2 Single bond Sub-69
2-3542 Sub-42 3,4-diClPh SO2 Single bond Sub-70
2-3543 Sub-42 3,4-diClPh SO2 Single bond Sub-71
2-3544 Sub-42 3,4-diClPh SO2 Single bond Sub-72
2-3545 Sub-42 3,4-diClPh SO2 Single bond Sub-73
2-3546 Sub-42 3,4-diClPh SO2 Single bond Sub-74
2-3547 Sub-42 3,4-diClPh SO2 Single bond Sub-75
2-3548 Sub-42 3,4-diClPh SO2 Single bond Sub-76
2-3549 Sub-42 -,4-diClPh SO2 Single bond Sub-77
2-3550 Sub-42 3,4-diClPh SO2 Single bond Sub-78
2-3551 Sub-42 3,4-diClPh SO2 Single bond Sub-79
2-3552 Sub-42 3,4-diClPh SO2 Single bond Sub-80
2-3553 Sub-43 3,4-diClPh SO2 Single bond Sub-1
2-3554 Sub-43 3,4-diClPh SO2 Single bond Sub-2
2-3555 Sub-43 3,4-diClPh SO2 Single bond Sub-3
2-3556 Sub-43 3,4-diClPh SO2 Single bond Sub-4
2-3557 Sub-43 3,4-diClPh SO2 Single bond Sub-5
2-3558 Sub-43 3,4-diClPh SO2 Single bond Sub-6
2-3559 Sub-43 3,4-diClPh SO2 Single bond Sub-7
2-3560 Sub-43 3,4-diClPh SO2 Single bond Sub-8
2-3561 Sub-43 3,4-diClPh SO2 Single bond Sub-9
2-3562 Sub-43 3,4-diClPh SO2 Single bond Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3563 Sub-43 3,4-diClPh SO2 Single bond Sub-11
2-3564 Sub-43 3,4-diClPh SO2 Single bond Sub-12
2-3565 Sub-43 3,4-diClPh SO2 Single bond Sub-13
2-3566 Sub-43 3,4-diClPh SO2 Single bond Sub-14
2-3567 Sub-43 3,4-diClPh SO2 Single bond Sub-15
2-3568 Sub-43 3,4-diClPh SO2 Single bond Sub-16
2-3569 Sub-43 3,4-diClPh SO2 Single bond Sub-17
2-3570 Sub-43 3,4-diClPh SO2 Single bond Sub-18
2-3571 Sub-43 3,4-diClPh SO2 Single bond Sub-19
2-3572 Sub-43 3,4-diClPh SO2 Single bond Sub-20
2-3573 Sub-43 3,4-diClPh SO2 Single bond Sub-21
2-3574 Sub-43 3,4-diClPh SO2 Single bond Sub-22
2-3575 Sub-43 3,4-diClPh SO2 Single bond Sub-23
2-3576 Sub-43 3,4-diClPh SO2 Single bond Sub-24
2-3577 Sub-43 3,4-diClPh SO2 Single bond Sub-25
2-3578 Sub-43 3,4-diClPh SO2 Single bond Sub-26
2-3579 Sub-43 3,4-diClPh SO2 Single bond Sub-27
2-3580 Sub-43 3,4-diClPh SO2 Single bond Sub-28
2-3581 Sub-43 3,4-diClPh SO2 Single bond Sub-29
2-3582 Sub-43 3,4-diClPh SO2 Single bond Sub-30
2-3583 Sub-43 3,4-diClPh SO2 Single bond Sub-31
2-3584 Sub-43 3,4-diClPh SO2 Single bond Sub-32
2-3585 Sub-43 3,4-diClPh SO2 Single bond Sub-65
2-3586 Sub-43 3,4-diClPh SO2 Single bond Sub-66
2-3587 Sub-43 3,4-diClPh SO2 Single bond Sub-67
2-3588 Sub-43 3,4-diClPh SO2 Single bond Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3589 Sub-43 3,4-diC-Ph SO2 Single bond Sub-69
2-3590 Sub-43 3,4-diClPh SO2 Single bond Sub-70
2-3591 Sub-43 3,4-diClPh SO2 Single bond Sub-71
2-3592 Sub-43 3,4-diClPh SO2 Single bond Sub-72
2-3593 Sub-43 3,4-diClPh SO2 Single bond Sub-73
2-3594 Sub-43 3,4-diClPh SO2 Single bond Sub-74
2-3595 Sub-43 3,4-diClPh SO2 Single bond Sub-75
2-3596 Sub-43 3,4-diClPh SO2 Single bond Sub-76
2-3597 Sub-43 3,4-diClPh SO2 Single bond Sub-77
2-3598 Sub-43 3,4-diClPh SO2 Single bond Sub-78
2-3599 Sub-43 3,4-diClPh SO2 Single bond Sub-79
2-3600 Sub-43 3,4-diClPh SO2 Single bond Sub-80
2-3601 Sub-44 3,4-diClPh SO2 Single bond Sub-1
2-3602 Sub-44 3,4-diClPh SO2 Single bond Sub-2
2-3603 Sub-44 3,4-diClPh SO2 Single bond Sub-3
2-3604 Sub-44 3,4-diClPh SO2 Single bond Sub-4
2-3605 Sub-44 3,4-diClPh SO2 Single bond Sub-5
2-3606 Sub-44 3,4-diClPh SO2 Single bond Sub-6
2-3607 Sub-44 3,4-diClPh SO2 Single bond Sub-7
2-3608 Sub-44 3,4-diClPh SO2 Single bond Sub-8
2-3609 Sub-44 3,4-diClPh SO2 Single bond Sub-9
2-3610 Sub-44 3,4-diClPh SO2 Single bond Sub-10
2-3611 Sub-44 3,4-diClPh SO2 Single bond Sub-11
2-3612 Sub-44 3,4-diClPh SO2 Single bond Sub-12
2-3613 Sub-44 3,4-diClPh SO2 Single bond Sub-13
2-3614 Sub-44 3,4-diClPh SO2 Single bond Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3615 Sub-44 3,4-diClPh SO2 Single bond Sub-15
2-3616 Sub-44 3,4-diClPh SO2 Single bond Sub-16
2-3617 Sub-44 3,4-diClPh SO2 Single bond Sub-17
2-3618 Sub-44 3,4-diClPh SO2 Single bond Sub-18
2-3619 Sub-44 3,4-diClPh SO2 Single bond Sub-19
2-3620 Sub-44 3,4-diClPh SO2 Single bond Sub-20
2-3621 Sub-44 3,4-diClPh SO2 Single bond Sub-21
2-3622 Sub-44 3,4-diClPh SO2 Single bond Sub-22
2-3623 Sub-44 3,4-diClPh SO2 Single bond Sub-23
2-3624 Sub-44 3,4-diClPh SO2 Single bond Sub-24
2-3625 Sub-44 3,4-diClPh SO2 Single bond Sub-25
2-3626 Sub-44 3,4-diClPh SO2 Single bond Sub-26
2-3627 Sub-44 3,4-diClPh SO2 Single bond Sub-27
2-3628 Sub-44 3,4-diClPh SO2 Single bond Sub-28
2-3629 Sub-44 3,4-diClPh SO2 Single bond Sub-29
2-3630 Sub-44 3,4-diClPh SO2 Single bond Sub-30
2-3631 Sub-44 3,4-diClPh SO2 Single bond Sub-31
2-3632 Sub-44 3,4-diClPh SO2 Single bond Sub-32
2-3633 Sub-44 3,4-diClPh SO2 Single bond Sub-65
2-3634 Sub-44 3,4-diClPh SO2 Single bond Sub-66
2-3635 Sub-44 3,4-diClPh SO2 Single bond Sub-67
2-3636 Sub-44 3,4-diClPh SO2 Single bond Sub-68
2-3637 Sub-44 3,4-diClPh SO2 Single bond Sub-69
2-3638 Sub-44 3,4-diClPh SO2 Single bond Sub-70
2-3639 Sub-44 3,4-diClPh SO2 Single bond Sub-71
2-3640 Sub-44 3,4-diClPh SO2 Single bond Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3641 Sub-44 3,4-diClPh SO2 Single bond Sub-73
2-3642 Sub-44 3,4-diClPh SO2 Single bond Sub-74
2-3643 Sub-44 3,4-diClPh SO2 Single bond Sub-75
2-3644 Sub-44 3,4-diClPh SO2 Single bond Sub-76
2-3645 Sub-44 3,4-diClPh SO2 Single bond Sub-77
2-3646 Sub-44 3,4-diClPh SO2 Single bond Sub-78
2-3647 Sub-44 3,4-diClPh SO2 Single bond Sub-79
2-3648 Sub-44 3,4-diClPh SO2 Single bond Sub-80
2-3649 Sub-45 3,4-diClPh SO2 Single bond Sub-1
2-3650 Sub-45 3,4-diClPh SO2 Single bond Sub-2
2-3651 Sub-45 3,4-diClPh SO2 Single bond Sub-3
2-3652 Sub-45 3,4-diClPh SO2 Single bond Sub-4
2-3653 Sub-45 3,4-diClPh SO2 Single bond Sub-5
2-3654 Sub-45 3,4-diClPh SO2 Single bond Sub-6
2-3655 Sub-45 3,4-diClPh SO2 Single bond Sub-7
2-3656 Sub-45 3,4-diClPh SO2 Single bond Sub-8
2-3657 Sub-45 3,4-diClPh SO2 Single bond Sub-9
2-3658 Sub-45 3,4-diClPh SO2 Single bond Sub-10
2-3659 Sub-45 3,4-diClPh SO2 Single bond Sub-11
2-3660 Sub-45 3,4-diClPh SO2 Single bond Sub-12
2-3661 Sub-45 3,4-diClPh SO2 Single bond Sub-13
2-3662 Sub-45 3,4-diClPh SO2 Single bond Sub-14
2-3663 Sub-45 3,4-diClPh SO2 Single bond Sub-15
2-3664 Sub-45 3,4-diClPh SO2 Single bond Sub-16
2-3665 Sub-45 3,4-diClPh SO2 Single bond Sub-17
2-3666 Sub-45 3,4-diClPh SO2 Single bond Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3667 Sub-45 3,4-diClPh SO2 Single bond Sub-19
2-3668 Sub-45 3,4-diClPh SO2 Single bond Sub-20
2-3669 Sub-45 3,4-diClPh SO2 Single bond Sub-21
2-3670 Sub-45 3,4-diClPh SO2 Single bond Sub-22
2-3671 Sub-45 3,4-diClPh SO2 Single bond Sub-23
2-3672 Sub-45 3,4-diClPh SO2 Single bond Sub-24
2-3673 Sub-45 3,4-diClPh SO2 Single bond Sub-25
2-3674 Sub-45 3,4-diClPh SO2 Single bond Sub-26
2-3675 Sub-45 3,4-diClPh SO2 Single bond Sub-27
2-3676 Sub-45 3,4-diClPh SO2 Single bond Sub-28
2-3677 Sub-45 3,4-diClPh SO2 Single bond Sub-29
2-3678 Sub-45 3,4-diClPh SO2 Single bond Sub-30
2-3679 Sub-45 3,4-diClPh SO2 Single bond Sub-31
2-3680 Sub-45 3,4-diClPh SO2 Single bond Sub-32
2-3681 Sub-45 3,4-diClPh SO2 Single bond Sub-65
2-3682 Sub-45 3,4-diClPh SO2 Single bond Sub-66
2-3683 Sub-45 3,4-diClPh SO2 Single bond Sub-67
2-3684 Sub-45 3,4-diClPh SO2 Single bond Sub-68
2-3685 Sub-45 3,4-diClPh SO2 Single bond Sub-69
2-3686 Sub-45 3,4-diClPh SO2 Single bond Sub-70
2-3687 Sub-45 3,4-diClPh SO2 Single bond Sub-71
2-3688 Sub-45 3,4-diClPh SO2 Single bond Sub-72
2-3689 Sub-45 3,4-diClPh SO2 Single bond Sub-73
2-3690 Sub-45 3,4-diClPh SO2 Single bond Sub-74
2-3691 Sub-45 3,4-diClPh SO2 Single bond Sub-75
2-3692 Sub-45 3,4-diClPh SO2 Single bond Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3693 Sub-45 3,4-diClPh SO2 Single bond Sub-77
2-3694 Sub-45 3,4-diClPh SO2 Single bond Sub-78
2-3695 Sub-45 3,4-diClPh SO2 Single bond Sub-79
2-3696 Sub-45 3,4-diClPh SO2 Single bond Sub-80
2-3697 Sub-46 3,4-diClPh SO2 Single bond Sub-1
2-3698 Sub-46 3,4-diClPh SO2 Single bond Sub-2
2-3699 Sub-46 3,4-diClPh SO2 Single bond Sub-3
2-3700 Sub-46 3,4-diClPh SO2 Single bond Sub-4
2-3701 Sub-46 3,4-diClPh SO2 Single bond Sub-5
2-3702 Sub-46 3,4-diClPh SO2 Single bond Sub-6
2-3703 Sub-46 3,4-diClPh SO2 Single bond Sub-7
2-3704 Sub-46 3,4-diClPh SO2 Single bond Sub-8
2-3705 Sub-46 3,4-diClPh SO2 Single bond Sub-9
2-3706 Sub-46 3,4-diClPh SO2 Single bond Sub-10
2-3707 Sub-46 3,4-diClPh SO2 Single bond Sub-11
2-3708 Sub-46 3,4-diClPh SO2 Single bond Sub-12
2-3709 Sub-46 3,4-diClPh SO2 Single bond Sub-13
2-3710 Sub-46 3,4-diClPh SO2 Single bond Sub-14
2-3711 Sub-46 3,4-diClPh SO2 Single bond Sub-15
2-3712 Sub-46 3,4-diClPh SO2 Single bond Sub-16
2-3713 Sub-46 3,4-diClPh SO2 Single bond Sub-17
2-3714 Sub-46 3,4-diClPh SO2 Single bond Sub-18
2-3715 Sub-46 3,4-diClPh SO2 Single bond Sub-19
2-3716 Sub-46 3,4-diClPh SO2 Single bond Sub-20
2-3717 Sub-46 3,4-diClPh SO2 Single bond Sub-21
2-3718 Sub-46 3,4-diClPh SO2 Single bond Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3719 Sub-46 3,4-diClPh SO2 Single bond Sub-23
2-3720 Sub-46 3,4-diClPh SO2 Single bond Sub-24
2-3721 Sub-46 3,4-diClPh SO2 Single bond Sub-25
2-3722 Sub-46 3,4-diClPh SO2 Single bond Sub-26
2-3723 Sub-46 3,4-diClPh SO2 Single bond Sub-27
2-3724 Sub-46 3,4-diClPh SO2 Single bond Sub-28
2-3725 Sub-46 3,4-diClPh SO2 Single bond Sub-29
2-3726 Sub-46 3,4-diClPh SO2 Single bond Sub-30
2-3727 Sub-46 3,4-diClPh SO2 Single bond Sub-31
2-3728 Sub-46 3,4-diClPh SO2 Single bond Sub-32
2-3729 Sub-46 3,4-diClPh SO2 Single bond Sub-65
2-3730 Sub-46 3,4-diClPh SO2 Single bond Sub-66
2-3731 Sub-46 3,4-diClPh SO2 Single bond Sub-67
2-3732 Sub-46 3,4-diClPh SO2 Single bond Sub-68
2-3733 Sub-46 3,4-diClPh SO2 Single bond Sub-69
2-3734 Sub-46 3,4-diClPh SO2 Single bond Sub-70
2-3735 Sub-46 3,4-diClPh SO2 Single bond Sub-71
2-3736 Sub-46 3,4-diClPh SO2 Single bond Sub-72
2-3737 Sub-46 3,4-diClPh SO2 Single bond Sub-73
2-3738 Sub-46 3,4-diClPh SO2 Single bond Sub-74
2-3739 Sub-46 3,4-diClPh SO2 Single bond Sub-75
2-3740 Sub-46 3,4-diClPh SO2 Single bond Sub-76
2-3741 Sub-46 3,4-diClPh SO2 Single bond Sub-77
2-3742 Sub-46 3,4-diClPh SO2 Single bond Sub-78
2-3743 Sub-46 3,4-diClPh SO2 Single bond Sub-79
2-3744 Sub-46 3,4-diClPh SO2 Single bond Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3745 Sub-47 3,4-diClPh SO2 Single bond Sub-1
2-3746 Sub-47 3,4-diClPh SO2 Single bond Sub-2
2-3747 Sub-47 3,4-diClPh SO2 Single bond Sub-3
2-3748 Sub-47 3,4-diClPh SO2 Single bond Sub-4
2-3749 Sub-47 3,4-diClPh SO2 Single bond Sub-5
2-3750 Sub-47 3,4-diClPh SO2 Single bond Sub-6
2-3751 Sub-47 3,4-diClPh SO2 Single bond Sub-7
2-3752 Sub-47 3,4-diClPh SO2 Single bond Sub-8
2-3753 Sub-47 3,4-diClPh SO2 Single bond Sub-9
2-3754 Sub-47 3,4-diClPh SO2 Single bond Sub-10
2-3755 Sub-47 3,4-diClPh SO2 Single bond Sub-11
2-3756 Sub-47 3,4-diClPh SO2 Single bond Sub-12
2-3757 Sub-47 3,4-diClPh SO2 Single bond Sub-13
2-3758 Sub-47 3,4-diClPh SO2 Single bond Sub-14
2-3759 Sub-47 3,4-diClPh SO2 Single bond Sub-15
2-3760 Sub-47 3,4-diClPh SO2 Single bond Sub-16
2-3761 Sub-47 3,4-diClPh SO2 Single bond Sub-17
2-3762 Sub-47 3,4-diClPh SO2 Single bond Sub-18
2-3763 Sub-47 3,4-diClPh SO2 Single bond Sub-19
2-3764 Sub-47 3,4-diClPh SO2 Single bond Sub-20
2-3765 Sub-47 3,4-diClPh SO2 Single bond Sub-21
2-3766 Sub-47 3,4-diClPh SO2 Single bond Sub-22
2-3767 Sub-47 3,4-diClPh SO2 Single bond Sub-23
2-3768 Sub-47 3,4-diClPh SO2 Single bond Sub-24
2-3769 Sub-47 3,4-diClPh SO2 Single bond Sub-25
2-3770 Sub-47 3,4-diClPh SO2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3771 Sub-47 3,4-diClPh SO2 Single bond Sub-27
2-3772 Sub-47 3,4-diClPh SO2 Single bond Sub-28
2-3773 Sub-47 3,4-diClPh SO2 Single bond Sub-29
2-3774 Sub-47 3,4-diClPh SO2 Single bond Sub-30
2-3775 Sub-47 3,4-diClPh SO2 Single bond Sub-31
2-3776 Sub-47 3,4-diClPh SO2 Single bond Sub-32
2-3777 Sub-47 3,4-diClPh SO2 Single bond Sub-65
2-3778 Sub-47 3,4-diClPh SO2 Single bond Sub-66
2-3779 Sub-47 3,4-diClPh SO2 Single bond Sub-67
2-3780 Sub-47 3,4-diClPh SO2 Single bond Sub-68
2-3781 Sub-47 3,4-diClPh SO2 Single bond Sub-69
2-3782 Sub-47 3,4-diClPh SO2 Single bond Sub-7O
2-3783 Sub-47 3,4-diClPh SO2 Single bond Sub-71
2-3784 Sub-47 3,4-diClPh SO2 Single bond Sub-72
2-3785 Sub-47 3,4-diClPh SO2 Single bond Sub-73
2-3786 Sub-47 3,4-diClPh SO2 Single bond Sub-74
2-3787 Sub-47 3,4-diClPh SO2 Single bond Sub-75
2-3788 Sub-47 3,4-diClPh SO2 Single bond Sub-76
2-3789 Sub-47 3,4-diClPh SO2 Single bond Sub-77
2-3790 Sub-47 3,4-diClPh SO2 Single bond Sub-78
2-3791 Sub-47 3,4-diClPh SO2 Single bond Sub-79
2-3792 Sub-47 3,4-diClPh SO2 Single bond Sub-80
2-3793 Sub-81 3,4-diClPh SO2 Single bond Sub-1
2-3794 Sub-81 3,4-diClPh SO2 Single bond Sub-2
2-3795 Sub-81 3,4-diClPh SO2 Single bond Sub-3
2-3796 Sub-81 3,4-diClPh SO2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3797 Sub-81 3,4-diClPh SO2 Single bond Sub-5
2-3798 Sub-81 3,4-diClPh SO2 Single bond Sub-6
2-3799 Sub-81 3,4-diClPh SO2 Single bond Sub-7
2-3800 Sub-81 3,4-diClPh SO2 Single bond Sub-8
2-3801 Sub-81 3,4-diClPh SO2 Single bond Sub-9
2-3802 Sub-81 3,4-diClPh SO2 Single bond Sub-10
2-3803 Sub-81 3,4-diClPh SO2 Single bond Sub-11
2-3804 Sub-81 3,4-diClPh SO2 Single bond Sub-12
2-3805 Sub-81 3,4-diClPh SO2 Single bond Sub-13
2-3806 Sub-81 3,4-diClPh SO2 Single bond Sub-14
2-3807 Sub-81 3,4-diClPh SO2 Single bond Sub-15
2-3808 Sub-81 3,4-diClPh SO2 Single bond Sub-16
2-3809 Sub-81 3,4-diClPh SO2 Single bond Sub-17
2-3810 Sub-81 3,4-diClPh SO2 Single bond Sub-18
2-3811 Sub-81 3,4-diClPh SO2 Single bond Sub-19
2-3812 Sub-81 3,4-diClPh SO2 Single bond Sub-20
2-3813 Sub-81 3,4-diClPh SO2 Single bond Sub-21
2-3814 Sub-81 3,4-diClPh SO2 Single bond Sub-22
2-3815 Sub-81 3,4-diClPh SO2 Single bond Sub-23
2-3816 Sub-81 3,4-diClPh SO2 Single bond Sub-24
2-3817 Sub-81 3,4-diClPh SO2 Single bond Sub-25
2-3818 Sub-81 3,4-diClPh SO2 Single bond Sub-26
2-3819 Sub-81 3,4-diClPh SO2 Single bond Sub-27
2-3820 Sub-81 3,4-diClPh SO2 Single bond Sub-28
2-3821 Sub-81 3,4-diClPh SO2 Single bond Sub-29
2-3822 Sub-81 3,4-diClPh SO2 Single bond Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3823 Sub-81 3,4-diClPh SO2 Single bond Sub-31
2-3824 Sub-81 3,4-diClPh SO2 Single bond Sub-32
2-3825 Sub-81 3,4-diClPh SO2 Single bond Sub-65
2-3826 Sub-81 3,4-diClPh SO2 Single bond Sub-66
2-3827 Sub-81 3,4-diClPh SO2 Single bond Sub-67
2-3828 Sub-81 3,4-diClPh SO2 Single bond Sub-68
2-3829 Sub-81 3,4-diClPh SO2 Single bond Sub-69
2-3830 Sub-81 3,4-diClPh SO2 Single bond Sub-70
2-3831 Sub-81 3,4-diClPh SO2 Single bond Sub-71
2-3832 Sub-81 3,4-diClPh S02 Single bond Sub-72
2-3833 Sub-81 3,4-diClPh SO2 Single bond Sub-73
2-3834 Sub-81 3,4-diClPh SO2 Single bond Sub-74
2-3835 Sub-81 3,4-diClPh SO2 Single bond Sub-75
2-3836 Sub-81 3,4-diClPh SO2 Single bond Sub-76
2-3837 Sub-81 3,4-diClPh SO2 Single bond Sub-77
2-3838 Sub-81 3,4-diClPh SO2 Single bond Sub-78
2-3839 Sub-81 3,4-diClPh SO2 Single bond Sub-79
2-3840 Sub-81 3,4-diClPh SO2 Single bond Sub-80
2-3841 Sub-48 3,4-diClPh SO2 Single bond Sub-1
2-3842 Sub-48 3,4-diClPh SO2 Single bond Sub-2
2-3843 Sub-48 3,4-diClPh SO2 Single bond Sub-3
2-3844 Sub-48 3,4-diClPh SO2 Single bond Sub-4
2-3845 Sub-48 3,4-diClPh SO2 Single bond Sub-5
2-3846 Sub-48 3,4-diClPh SO2 Single bond Sub-6
2-3847 Sub-48 3,4-diClPh SO2 Single bond Sub-7
2-3848 Sub-48 3,4-diClPh SO2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3849 Sub-48 3,4-diClPh SO2 Single bond Sub-9
2-3850 Sub-48 3,4-diClPh SO2 Single bond Sub-10
2-3851 Sub-48 3,4-diClPh SO2 Single bond Sub-11
2-3852 Sub-48 3,4-diClPh SO2 Single bond Sub-12
2-3853 Sub-48 3,4-diClPh SO2 Single bond Sub-13
2-3854 Sub-48 3,4-diClPh SO2 Single bond Sub-14
2-3855 Sub-48 3,4-diClPh SO2 Single bond Sub-15
2-3856 Sub-48 3,4-diClPh SO2 Single bond Sub-16
2-3857 Sub-48 3,4-diClPh SO2 Single bond Sub-17
2-3858 Sub-48 3,4-diClPh SO2 Single bond Sub-18
2-3859 Sub48 3,4-diClPh SO2 Single bond Sub-19
2-3860 Sub-48 3,4-diClPh SO2 Single bond Sub-20
2-3861 Sub-48 3,4-diClPh SO2 Single bond Sub-21
2-3862 Sub-48 3,4-diClPh SO2 Single bond Sub-22
2-3863 Sub-48 3,4-diClPh SO2 Single bond Sub-23
2-3864 Sub-48 3,4-diClPh SO2 Single bond Sub-24
2-3865 Sub-48 3,4-diClPh SO2 Single bond Sub-25
2-3866 Sub-48 3,4-diClPh SO2 Single bond Sub-26
2-3867 Sub-48 3,4-diClPh SO2 Single bond Sub-27
2-3868 Sub-48 3,4-diClPh SO2 Single bond Sub-28
2-3869 Sub-48 3,4-diClPh SO2 Single bond Sub-29
2-3870 Sub-48 3,4-diClPh SO2 Single bond Sub-30
2-3871 Sub-48 3,4-diClPh SO2 Single bond Sub-31
2-3872 Sub-48 3,4-diClPh SO2 Single bond Sub-32
2-3873 Sub-48 3,4-diClPh SO2 Single bond Sub-S5
2-3874 Sub-48 3,4-diClPh SO2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3875 Sub-48 3,4-diClPh SO2 Single bond Sub-67
2-3876 Sub-48 3,4-diClPh SO2 Single bond Sub-68
2-3877 Sub-48 3,4-diClPh SO2 Single bond Sub-69
2-3878 Sub-48 3,4-diClPh SO2 Single bond Sub-70
2-3879 Sub-48 3,4-diClPh SO2 Single bond Sub-71
2-3880 Sub-48 3,4-diClPh SO2 Single bond Sub-72
2-3881 Sub-48 3,4-diClPh SO2 Single bond Sub-73
2-3882 Sub-48 3,4-diClPh SO2 Single bond Sub-74
2-3883 Sub-48 3,4-diClPh SO2 Single bond Sub-75
2-3884 Sub-48 3,4-diClPh SO2 Single bond Sub-76
2-3885 Sub-48 3,4-diClPh SO2 Single bond Sub-77
2-3886 Sub-48 3,4-diClPh SO2 Single bond Sub-78
2-3887 Sub-48 3,4-diClPh SO2 Single bond Sub-79
2-3888 Sub-48 3,4-diClPh SO2 Single bond Sub-80
2-3889 Sub-49 3,4-diClPh SO2 Single bond Sub-1
2-3890 Sub-49 3,4-diClPh SO2 Single bond Sub-2
2-3891 Sub-49 3,4-diClPh SO2 Single bond Sub-3
2-3892 Sub-49 3,4-diClPh SO2 Single bond Sub-4
2-3893 Sub-49 3,4-diClPh SO2 Single bond Sub-5
2-3894 Sub-49 3,4-diClPh SO2 Single bond Sub-6
2-3895 Sub-49 3,4-diClPh SO2 Single bond Sub-7
2-3896 Sub-49 3,4-diClPh SO2 Single bond Sub-8
2-3897 Sub-49 3,4-diClPh SO2 Single bond Sub-9
2-3898 Sub-49 3,4-diClPh SO2 Single bond Sub-10
2-3899 Sub-49 3,4-diClPh SO2 Single bond Sub-11
2-3900 Sub-49 3,4-diClPh SO2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3901 Sub-49 3,4-diClPh SO2 Single bond Sub-13
2-3902 Sub-49 3,4-diClPh SO2 Single bond Sub-14
2-3903 Sub-49 3,4-diClPh SO2 Single bond Sub-15
2-3904 Sub-49 3,4-diClPh SO2 Single bond Sub-16
2-3905 Sub-49 3,4-diClPh SO2 Single bond Sub-17
2-3906 Sub-49 3,4-diClPh SO2 Single bond Sub-18
2-3907 Sub-49 3,4-diClPh SO2 Single bond Sub-19
2-3908 Sub-49 3,4-diClPh SO2 Single bond Sub-20
2-3909 Sub-49 3,4-diClPh SO2 Single bond Sub-21
2-3910 Sub-49 3,4-diClPh SO2 Single bond Sub-22
2-3911 Sub-49 3,4-diClPh SO2 Single bond Sub-23
2-3912 Sub-49 3,4-diClPh SO2 Single bond Sub-24
2-3913 Sub-49 3,4-diClPh SO2 Single bond Sub-25
2-3914 Sub-49 3,4-diClPh SO2 Single bond Sub-26
2-3915 Sub-49 3,4-diClPh SO2 Single bond Sub-27
2-3916 Sub-49 3,4-diClPh SO2 Single bond Sub-28
2-3917 Sub-49 3,4-diClPh SO2 Single bond Sub-29
2-3918 Sub-49 3,4-diClPh SO2 Single bond Sub-30
2-3919 Sub-49 3,4-diClPh SO2 Single bond Sub-31
2-3920 Sub-49 3,4-diClPh SO2 Single bond Sub-32
2-3921 Sub-49 3,4-diClPh SO2 Single bond Sub-65
2-3922 Sub-49 3,4-diClPh SO2 Single bond Sub-66
2-3923 Sub-49 3,4-diClPh SO2 Single bond Sub-67
2-3924 Sub-49 3,4-diClPh SO2 Single bond Sub-68
2-3925 Sub-49 3,4-diClPh SO2 Single bond Sub-69
2-3926 Sub-49 3,4-diClPh SO2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3927 Sub-49 3,4-diClPh SO2 Single bond Sub-71
2-3928 Sub-49 3,4-diClPh SO2 Single bond Sub-72
2-3929 Sub-49 3,4-diClPh SO2 Single bond Sub-73
2-3930 Sub-49 3,4-diClPh SO2 Single bond Sub-74
2-3931 Sub-49 3,4-diClPh SO2 Single bond Sub-75
2-3932 Sub-49 3,4-diClPh SO2 Single bond Sub-76
2-3933 Sub-49 3,4-diClPh SO2 Single bond Sub-77
2-3934 Sub-49 3,4-diClPh SO2 Single bond Sub-78
2-3935 Sub-49 3,4-diClPh SO2 Single bond Sub-79
2-3936 Sub-49 3,4-diClPh SO2 Single bond Sub-80
2-3937 Sub-50 3,4-diClPh SO2 Single bond Sub-1
2-3938 Sub-50 3,4-diClPh SO2 Single bond Sub-2
2-3939 Sub-50 3,4-diClPh SO2 Single bond Sub-3
2-3940 Sub-50 3,4-diClPh SO2 Single bond Sub-4
2-3941 Sub-50 3,4-diClPh SO2 Single bond Sub-5
2-3942 Sub-50 3,4-diClPh SO2 Single bond Sub-6
2-3943 Sub-50 3,4-diClPh SO2 Single bond Sub-7
2-3944 Sub-50 3,4-diClPh SO2 Single bond Sub-8
2-3945 Sub-50 3,4-diClPh SO2 Single bond Sub-9
2-3946 Sub-50 3,4-diClPh SO2 SheetKey with a key body Sub-10
2-3947 Sub-50 3,4-diClPh SO2 Single bond Sub-11
2-3948 Sub-50 3,4-diClPh SO2 Single bond Sub-12
2-3949 Sub-50 3,4-diClPh SO2 Single bond Sub-13
2-3950 Sub-50 3,4-diClPh SO2 Single bond Sub-14
2-3951 Sub-50 3,4-diClPh SO2 Single bond Sub-15
2-3952 Sub-50 3,4-diClPh SO2 Single bond Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3953 Sub-50 3,4-diClPh SO2 Single bond Sub-17
2-3954 Sub-50 3,4-diClPh SO2 Single bond Sub-18
2-3955 Sub-50 3,4-diClPh SO2 Single bond Sub-19
2-3956 Sub-50 3,4-diClPh SO2 Single bond Sub-20
2-3957 Sub-50 3,4-diClPh SO2 Single bond Sub-21
2-3958 Sub-50 3,4-diClPh SO2 Single bond Sub-22
2-3959 Sub-50 3,4-diClPh SO2 Single bond Sub-23
2-3960 Sub-50 3,4-diClPh SO2 Single bond Sub-24
2-3961 Sub-50 3,4-diClPh SO2 Single bond Sub-25
2-3962 Sub-50 3,4-diClPh SO2 Single bond Sub-26
2-3963 Sub-50 3,4-diClPh SO2 Single bond Sub-27
2-3964 Sub-50 3,4-diClPh SO2 Single bond Sub-28
2-3965 Sub-50 3,4-diClPh SO2 Single bond Sub-29
2-3966 Sub-50 3,4-diClPh SO2 Single bond Sub-30
2-3967 Sub-50 3,4-diClPh SO2 Single bond Sub-31
2-3968 Sub-50 3,4-diClPh SO2 Single bond Sub-32
2-3969 Sub-50 3,4-diClPh SO2 Single bond Sub-65
2-3970 Sub-50 3,4-diClPh SO2 Single bond Sub-66
2-3971 Sub-50 3,4-diClPh SO2 Single bond Sub-67
2-3972 Sub-50 3,4-diClPh SO2 Single bond Sub-68
2-3973 Sub-50 3,4-diClPh SO2 Single bond Sub-69
2-3974 Sub-5O 3,4-diClPh SO2 Single bond Sub-70
2-3975 Sub-50 3,4-diClPh SO2 Single bond Sub-71
2-3976 Sub-50 3,4-diClPh SO2 Single bond Sub-72
2-3977 Sub-50 3,4-diClPh SO2 Single bond Sub-73
2-3978 Sub-50 3,4-diClPh SO2 Single bond Sub-74
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-3979 Sub-50 3,4-diClPh SO2 Single bond Sub-75
2-3980 Sub-50 3,4-diClPh SO2 Single bond Sub-76
2-3981 Sub-50 3,4-diClPh SO2 Single bond Sub-77
2-3982 Sub-50 3,4-diClPh SO2 Single bond Sub-78
2-3983 Sub-50 3,4-diClPh SO2 Single bond Sub-79
2-3984 Sub-50 3,4-diClPh SO2 Single bond Sub-80
2-3985 Sub-51 3,4-diClPh SO2 Single bond Sub-1
2-3986 Sub-51 3,4-diClPh SO2 Single bond Sub-2
2-3987 Sub-51 3,4-diClPh SO2 Single bond Sub-3
2-3988 Sub-51 3,4-diClPh SO2 Single bond Sub-4
2-3989 Sub-51 3,4-diClPh SO2 Single bond Sub-5
2-3990 Sub-51 3,4-diClPh SO2 Single bond Sub-6
2-3991 Sub-51 3,4-diClPh SO2 Single bond Sub-7
2-3992 Sub-51 3,4-diClPh SO2 Single bond Sub-8
2-3993 Sub-51 3,4-diClPh SO2 Single bond Sub-9
2-3994 Sub-51 3,4-diClPh SO2 Single bond Sub-10
2-3995 Sub-51 3,4-diClPh SO2 Single bond Sub-11
2-3996 Sub-51 3,4-diClPh SO2 Single bond Sub-12
2-3997 Sub-51 3,4-diClPh SO2 Single bond Sub-13
2-3998 Sub-5l 3,4-diClPh SO2 Single bond Sub-14
2-3999 Sub-51 3,4-diClPh SO2 Single bond Sub-15
2-4000 Sub-51 3,4-diClPh SO2 Single bond Sub-16
2-4001 Sub-51 3,4-diClPh SO2 Single bond Sub-17
2-4002 Sub-51 3,4-diClPh SO2 Single bond Sub-18
2-4003 Sub-51 3,4-diClPh SO2 Single bond Sub-19
2-4004 Sub-51 3,4-diClPh SO2 Single bond Sub-20
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4005 Sub-51 3,4-diClPh SO2 Single bond Sub-21
2-4006 Sub-51 3,4-diClPh SO2 Single bond Sub-22
2-4007 Sub-51 3,4-diClPh SO2 Single bond Sub-23
2-4008 Sub-51 3,4-diClPh SO2 Single bond Sub-24
2-4009 Sub-51 3,4-diClPh SO2 Single bond Sub-25
2-4010 Sub-51 3,4-diClPh SO2 Single bond Sub-26
2-4011 Sub-51 3,4-diClPh SO2 Single bond Sub-27
2-4012 Sub-51 3,4-diClPh SO2 Single bond Sub-28
2-4013 Sub-51 3,4-diClPh SO2 Single bond Sub-29
2-4014 Sub-51 3,4-diClPh SO2 Single bond Sub-30
2-4015 Sub-51 3,4-diClPh SO2 Single bond Sub-31
2-4016 Sub-51 3,4-diClPh SO2 Single bond Sub-32
2-4017 Sub-51 3,4-diClPh SO2 Single bond Sub-65
2-4018 Sub-51 3,4-diClPh SO2 Single bond Sub-66
2-4019 Sub-51 3,4-diClPh SO2 Single bond Sub-67
2-4020 Sub-51 3,4-diClPh SO2 Single bond Sub-68
2-4021 Sub-51 3,4-diClPh SO2 Single bond Sub-69
2-4022 Sub-51 3,4-diClPh SO2 Single bond Sub-70
2-4023 Sub-51 3,4-diClPh SO2 Single bond Sub-71
2-4024 Sub-51 3,4-diClPh SO2 Single bond Sub-72
2-4025 Sub-51 3,4-diClPh SO2 Single bond Sub-73
2-4026 Sub-51 3,4-diClPh SO2 Single bond Sub-74
2-4027 Sub-51 3,4-diClPh SO2 Single bond Sub-75
2-4028 Sub-51 3,4-diClPh SO2 Single bond Sub-76
2-4029 Sub-51 3,4-diClPh SO2 Single bond Sub-77
2-4030 Sub-51 3,4-diClPh SO2 Single bond Sub-78
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4031 Sub-51 3,4-diClPh SO2 Single bond Sub-79
2-4032 Sub-51 3,4-diClPh SO2 Single bond Sub-80
2-4033 Sub-52 3,4-diClPh SO2 Single bond Sub-1
2-4034 Sub-52 3,4-diClPh SO2 Single bond Sub-2
2-4035 Sub-52 3,4-diClPh SO2 Single bond Sub-3
2-4036 Sub-52 3,4-diClPh SO2 Single bond Sub-4
2-4037 Sub-52 3,4-diClPh SO2 Single bond Sub-5
2-4038 Sub-52 3,4-diClPh SO2 Single bond Sub-6
2-4039 Sub-52 3,4-diClPh SO2 Single bond Sub-7
2-4040 Sub-52 3,4-diClPh SO2 Single bond Sub-8
2-4041 Sub-52 3,4-diClPh SO2 Single bond Sub-9
2-4042 Sub-52 3,4-diClPh SO2 Single bond Sub-10
2-4043 Sub-52 3,4-diClPh SO2 Single bond Sub-11
2-4044 Sub-52 3,4-diClPh SO2 Single bond Sub-12
2-4045 Sub-52 3,4-diClPh SO2 Single bond Sub-13
2-4046 Sub-52 3,4-diClPh SO2 Single bond Sub-14
2-4047 Sub-52 3,4-diClPh SO2 Single bond Sub-15
2-4048 Sub-52 3,4-diClPh SO2 Single bond Sub-16
2-4049 Sub-52 3,4-diClPh SO2 Single bond Sub-17
2-4050 Sub-52 3,4-diClPh SO2 Single bond Sub-18
2-4051 Sub-52 3,4-diClPh SO2 Single bond Sub-19
2-4052 Sub-52 3,4-diClPh SO2 Single bond Sub-20
2-4053 Sub-52 3,4-diClPh SO2 Single bond Sub-21
2-4054 Sub-52 3,4-diClPh SO2 Single bond Sub-22
2-4055 Sub-52 3,4-diClPh SO2 Single bond Sub-23
2-4056 Sub-52 3,4-diClPh SO2 Single bond Sub-24
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4057 Sub-52 3,4-diClPh SO2 Single bond Sub-25
2-4058 Sub-52 3,4-diClPh SO2 Single bond Sub-26
2-4059 Sub-52 3,4-diClPh SO2 Single bond Sub-27
2-4060 Sub-52 3,4-diClPh SO2 Single bond Sub-28
2-4061 Sub-52 3,4-diClPh SO2 Single bond Sub-29
2-4062 Sub-52 3,4-diClPh SO2 Single bond Sub-30
2-4063 Sub-52 3,4-diClPh SO2 Single bond Sub-31
2-4064 Sub-52 3,4-diClPh SO2 Single bond Sub-32
2-4065 Sub-52 3,4-diClPh SO2 Single bond Sub-65
2-4066 Sub-52 3,4-diClPh SO2 Single bond Sub-66
2-4067 Sub-52 3,4-diClPh SO2 Single bond Sub-67
2-4068 Sub-52 3,4-diClPh SO2 Single bond Sub-68
2-4069 Sub-52 3,4-diClPh SO2 Single bond Sub-69
2-4070 Sub-52 3,4-diClPh SO2 Single bond Sub-70
2-4071 Sub-52 3,4-diClPh SO2 Single bond Sub-71
2-4072 Sub-52 3,4-diClPh SO2 Single bond Sub-72
2-4073 Sub-52 3,4-diClPh SO2 Single bond Sub-73
2-4074 Sub-52 3,4-diClPh SO2 Single bond Sub-74
2-4075 Sub-52 3,4-diClPh SO2 Single bond Sub-75
2-4076 Sub-52 -,4-diClPh SO2 Single bond Sub-76
2-4077 Sub-52 3,4-diClPh SO2 Single bond Sub-77
2-4078 Sub-52 3,4-diClPh SO2 Single bond Sub-78
2-4079 Sub-52 3,4-diClPh SO2 Single bond Sub-79
2-4080 Sub-52 3,4-diClPh SO2 Single bond Sub-80
2-4081 Sub-53 3,4-diClPh SO2 Single bond Sub-1
2-4082 Sub-53 3,4-diClPh SO2 Single bond Sub-2
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4083 Sub-53 3,4-diClPh SO2 Single bond Sub-3
2-4084 Sub-53 3,4-diClPh SO2 Single bond Sub-4
2-4085 Sub-53 3,4-diClPh SO2 Single bond Sub-5
2-4086 Sub-53 3,4-diClPh SO2 Single bond Sub-6
2-4087 Sub-53 3,4-diClPh SO2 Single bond Sub-7
2-4088 Sub-53 3,4-diClPh SO2 Single bond Sub-8
2-4089 Sub-53 3,4-diClPh SO2 Single bond Sub-9
2-4090 Sub-53 3,4-diClPh SO2 Single bond Sub-10
2-4091 Sub-53 3,4-diClPh SO2 Single bond Sub-11
2-4092 Sub-53 3,4-diClPh SO2 Single bond Sub-12
2-4093 Sub-53 3,4-diClPh SO2 Single bond Sub-13
2-4094 Sub-53 3,4-diClPh SO2 Single bond Sub-14
2-4095 Sub-53 3,4-diClPh SO2 Single bond Sub-15
2-4096 Sub-53 3,4-diClPh SO2 Single bond Sub-16
2-4097 Sub-53 3,4-diClPh SO2 Single bond Sub-17
2-4098 Sub-53 3,4-diClPh SO2 Single bond Sub-18
2-4099 Sub-53 3,4-diClPh SO2 Single bond Sub-19
2-4100 Sub-53 3,4-diClPh SO2 Single bond Sub-20
2-4101 Sub-53 3,4-diClPh SO2 Single bond Sub-21
2-4102 Sub-53 3,4-diClPh SO2 Single bond Sub-22
2-4103 Sub-53 3,4-diClPh SO2 Single bond Sub-23
2-4104 Sub-53 3,4-diClPh SO2 Single bond Sub-24
2-4105 Sub-53 3,4-diClPh SO2 Single bond Sub-25
2-4106 Sub-53 3,4-diClPh SO2 Single bond Sub-26
2-4107 Sub-53 3,4-diClPh SO2 Single bond Sub-27
2-4108 Sub-53 3,4-diClPh SO2 Single bond Sub-28
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4109 Sub-53 3,4-diClPh SO2 Single bond Sub-29
2-4110 Sub-53 3,4-diClPh SO2 Single bond Sub-30
2-4111 Sub-53 3,4-diClPh SO2 Single bond Sub-31
2-4112 Sub-53 3,4-diClPh SO2 Single bond Sub-32
2-4113 Sub-53 3,4-diClPh SO2 Single bond Sub-65
2-4114 Sub-53 3,4-diClPh SO2 Single bond Sub-66
2-4115 Sub-53 3,4-diClPh SO2 Single bond Sub-67
2-4116 Sub-53 3,4-diClPh SO2 Single bond Sub-68
2-4117 Sub-53 3,4-diClPh SO2 Single bond Sub-69
2-4118 Sub-53 3,4-diClPh SO2 Single bond Sub-70
2-4119 Sub-53 3,4-diClPh SO2 Single bond Sub-71
2-4120 Sub-53 3,4-diClPh SO2 Single bond Sub-72
2-4121 Sub-53 3,4-diClPh SO2 Single bond Sub-73
2-4122 Sub-53 3,4-diClPh SO2 Single bond Sub-74
2-4123 Sub-53 3,4-diClPh SO2 Single bond Sub-75
2-4124 Sub-53 3,4-diClPh SO2 Single bond Sub-76
2-4125 Sub-53 3,4-diClPh SO2 Single bond Sub-77
2-4126 Sub-53 3,4-diClPh SO2 Single bond Sub-78
2-4127 Sub-53 3,4-diClPh SO2 Single bond Sub-79
2-4128 Sub-53 3,4-diClPh SO2 Single bond Sub-80
2-4129 Sub-54 3,4-diClPh SO2 Single bond Sub-1
2-4130 Sub-54 3,4-diClPh SO2 Single bond Sub-2
2-4131 Sub-54 3,4-diClPh SO2 Single bond Sub-3
2-4132 Sub-54 3,4-diClPh SO2 Single bond Sub-4
2-4133 Sub-54 3,4-diClPh SO2 Single bond Sub-5
2-4134 Sub-54 3,4-diClPh SO2 Single bond Sub-6
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4135 Sub-54 3,4-diClPh SO2 Single bond Sub-7
2-4136 Sub-54 3,4-diClPh SO2 Single bond Sub-8
2-4137 Sub-54 3,4-diClPh SO2 Single bond Sub-9
2-4138 Sub-54 3,4-diClPh SO2 Single bond Sub-10
2-4139 Sub-54 3,4-diClPh SO2 Single bond Sub-11
2-4140 Sub-54 3,4-diClPh SO2 Single bond Sub-12
2-4141 Sub-54 3,4-diClPh SO2 Single bond Sub-13
2-4142 Sub-54 3,4-diClPh SO2 Single bond Sub-14
2-4143 Sub-54 3,4-diClPh SO2 Single bond Sub-15
2-4144 Sub-54 3,4-diClPh SO2 Single bond Sub-16
2-4145 Sub-54 3,4-diClPh SO2 Single bond Sub-17
2-4146 Sub-54 3,4-diClPh SO2 Single bond Sub-18
2-4147 Sub-54 3,4-diClPh SO2 Single bond Sub-19
2-4148 Sub-54 3,4-diClPh SO2 Single bond Sub-20
2-4149 Sub-54 3,4-diClPh SO2 Single bond Sub-21
2-4150 Sub-54 3,4-diClPh SO2 Single bond Sub-22
2-4151 Sub-54 3,4-diClPh SO2 Single bond Sub-23
2-4152 Sub-54 3,4-diClPh SO2 Single bond Sub-24
2-4153 Sub-54 3,4-diClPh SO2 Single bond Sub-25
2-4154 Sub-54 3,4-diClPh SO2 Single bond Sub-26
2-4155 Sub-54 3,4-diClPh SO2 Single bond Sub-27
2-4156 Sub-54 3,4-diClPh SO2 Single bond Sub-28
2-4157 Sub-54 3,4-diClPh SO2 Single bond Sub-29
2-4158 Sub-54 3,4-diClPh SO2 Single bond Sub-30
2-4159 Sub-54 3,4-diClPh SO2 Single bond Sub-31
2-4160 Sub-54 3,4-diClPh SO2 Single bond Sub-32
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4161 Sub-54 3,4-diClPh SO2 Single bond Sub-65
2-4162 Sub-54 3,4-diClPh SO2 Single bond Sub-66
2-4163 Sub-54 3,4-diClPh SO2 Single bond Sub-67
2-4164 Sub-54 3,4-diClPh SO2 Single bond Sub-68
2-4165 Sub-54 3,4-diClPh SO2 Single bond Sub-69
2-4166 Sub-54 3,4-diClPh SO2 Single bond Sub-70
2-4167 Sub-54 3,4-diClPh SO2 Single bond Sub-71
2-4168 Sub-54 3,4-diClPh SO2 Single bond Sub-72
2-4169 Sub-54 3,4-diClPh SO2 Single bond Sub-73
2-4170 Sub-54 3,4-diClPh SO2 Single bond Sub-74
2-4171 Sub-54 3,4-diClPh SO2 Single bond Sub-75
2-4172 Sub-54 3,4-diClPh SO2 Single bond Sub-76
2-4173 Sub-54 3,4-diClPh SO2 Single bond Sub-77
2-4174 Sub-54 3,4-diClPh SO2 Single bond Sub-78
2-4175 Sub-54 3,4-diClPh SO2 Single bond Sub-79
2-4176 Sub-54 3,4-diClPh SO2 Single bond Sub-80
2-4177 Sub-55 3,4-diClPh SO2 Single bond Sub-1
2-4178 Sub-55 3,4-diClPh SO2 Single bond Sub-2
2-4179 Sub-55 3,4-diCiPh SO2 Single bond Sub-3
2-4180 Sub-55 3,4-diClPh SO2 Single bond Sub-4
2-4181 Sub-55 3,4-diClPh SO2 Single bond Sub-5
2-4182 Sub-55 3,4-diClPh SO2 Single bond Sub-6
2-4183 Sub-55 3,4-diClPh SO2 Single bond Sub-7
2-4184 Sub-55 3,4-diClPh SO2 Single bond Sub-8
2-4185 Sub-55 3,4-diClPh SO2 Single bond Sub-9
2-4186 Sub-55 3,4-diClPh SO2 Single bond Sub-10
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4187 Sub-55 3,4-diClPh SO2 Single bond Sub-11
2-4188 Sub-55 3,4-diClPh SO2 Single bond Sub-12
2-4189 Sub-55 3,4-diClPh SO2 Single bond Sub-13
2-4190 Sub-55 3,4-diClPh SO2 Single bond Sub-14
2-4191 Sub-55 3,4-diClPh SO2 Single bond Sub-15
2-4192 Sub-55 3,4-diClPh SO2 Single bond Sub-16
2-4193 Sub-55 3,4-diClPh SO2 Single bond Sub-17
2-4194 Sub-55 3,4-diClPh SO2 Single bond Sub-18
2-4195 Sub-55 3,4-diClPh SO2 Single bond Sub-19
2-4196 Sub-55 3,4-diClPh SO2 Single bond Sub-20
2-4197 Sub-55 3,4-diClPh SO2 Single bond Sub-21
2-4198 Sub-55 3,4-diClPh SO2 Single bond Sub-22
2-4199 Sub-55 3,4-diClPh SO2 Single bond Sub-23
2-4200 Sub-55 3,4-diClPh SO2 Single bond Sub-24
2-4201 Sub-55 3,4-diClPh SO2 Single bond Sub-25
2-4202 Sub-55 3,4-diClPh SO2 Single bond Sub-26
2-4203 Sub-55 3,4-diClPh SO2 Single bond Sub-27
2-4204 Sub-55 3,4-diClPh SO2 Single bond Sub-28
2-4205 Sub-55 3,4-diClPh SO2 Single bond Sub-29
2-4206 Sub-55 3,4-diClPh SO2 Single bond Sub-30
2-4207 Sub-55 3,4-diClPh SO2 Single bond Sub-31
2-4208 Sub-55 3,4-diClPh SO2 Single bond Sub-32
2-4209 Sub-55 3,4-diClPh SO2 Single bond Sub-65
2-4210 Sub-55 3,4-diClPh SO2 Single bond Sub-66
2-4211 Sub-55 3,4-diClPh SO2 Single bond Sub-67
2-4212 Sub-55 3,4-diClPh SO2 Single bond Sub-68
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4213 Sub-55 3,4-diClPh SO2 Single bond Sub-69
2-4214 Sub-55 3,4-diClPh SO2 Single bond Sub-70
2-4215 Sub-55 3,4-diClPh SO2 Single bond Sub-71
2-4216 Sub-55 3,4-diClPh SO2 Single bond Sub-72
2-4217 Sub-55 3,4-diClPh SO2 Single bond Sub-73
2-4218 Sub-55 3,4-diClPh SO2 Single bond Sub-74
2-4219 Sub-55 3,4-diClPh SO2 Single bond Sub-75
2-4220 Sub-55 3,4-diClPh SO2 Single bond Sub-76
2-4221 Sub-55 3,4-diClPh SO2 Single bond Sub-77
2-4222 Sub-55 3,4-diClPh SO2 Single bond Sub-78
2-4223 Sub-55 3,4-diClPh SO2 Single bond Sub-79
2-4224 Sub-55 3,4-diClPh SO2 Single bond Sub-80
2-4225 Sub-56 3,4-diClPh SO2 Single bond Sub-1
2-4226 Sub-56 3,4-diClPh SO2 Single bond Sub-2
2-4227 Sub-56 3,4-diClPh SO2 Single bond Sub-3
2-4228 Sub-56 3,4-diClPh SO2 Single bond Sub-4
2-4229 Sub-56 3,4-diClPh SO2 Single bond Sub-5
2-4230 Sub-56 3,4-diClPh SO2 Single bond Sub-6
2-4231 Sub-56 3,4-diClPh SO2 Single bond Sub-7
2-4232 Sub-56 3,4-diClPh SO2 Single bond Sub-8
2-4233 Sub-56 3,4-diClPh SO2 Single bond Sub-9
2-4234 Sub-56 3,4-diClPh SO2 Single bond Sub-10
2-4235 Sub-56 3,4-diClPh SO2 Single bond Sub-11
2-4236 Sub-56 3,4-diClPh SO2 SheetKey with a key body Sub-12
2-4237 Sub-56 3,4-diClPh SO2 Single bond Sub-13
2-4238 Sub-56 3,4-diClPh SO2 Single bond Sub-14
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4239 Sub-56 3,4-diClPh SO2 Single bond Sub-15
2-4240 Sub-56 3,4-diClPh SO2 Single bond Sub-16
2-4241 Sub-56 3,4-diClPh SO2 Single bond Sub-17
2-4242 Sub-56 3,4-diClPh SO2 Single bond Sub-18
2-4243 Sub-56 3,4-diClPh SO2 Single bond Sub-19
2-4244 Sub-56 3,4-diClPh SO2 Single bond Sub-20
2-4245 Sub-56 3,4-diClPh SO2 Single bond Sub-21
2-4246 Sub-56 3,4-diClPh SO2 Single bond Sub-22
2-4247 Sub-56 3,4-diClPh SO2 Single bond Sub-23
2-4248 Sub-56 3,4-diClPh SO2 Single bond Sub-24
2-4249 Sub-56 3,4-diClPh SO2 Single bond Sub-25
2-4250 Sub-56 3,4-diClPh SO2 Single bond Sub-26
2-4251 Sub-56 3,4-diClPh SO2 Single bond Sub-27
2-4252 Sub-56 3,4-diClPh SO2 Single bond Sub-28
2-4253 Sub-56 3,4-diClPh SO2 Single bond Sub-29
2-4254 Sub-56 3,4-diClPh SO2 Single bond Sub-30
2-4255 Sub-56 3,4-diClPh SO2 Single bond Sub-31
2-4256 Sub-56 3,4-diClPh SO2 Single bond Sub-32
2-4257 Sub-56 3,4-diClPh SO2 Single bond Sub-65
2-4258 Sub-56 3,4-diClPh SO2 Single bond Sub-66
2-4259 Sub-56 3,4-diClPh SO2 Single bond Sub-67
2-4260 Sub-56 3,4-diClPh SO2 Single bond Sub-68
2-4261 Sub-56 3,4-diClPh SO2 Single bond Sub-69
2-4262 Sub-56 3,4-diClPh SO2 Single bond Sub-70
2-4263 Sub-56 3,4-diClPh SO2 Single bond Sub-71
2-4264 Sub-56 3,4-diClPh SO2 Single bond Sub-72
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4265 Sub-56 3,4-diClPh SO2 Single bond Sub-73
2-4266 Sub-56 3,4-diClPh SO2 Single bond Sub-74
2-4267 Sub-56 3,4-diClPh SO2 Single bond Sub-75
2-4268 Sub-56 3,4-diClPh SO2 Single bond Sub-76
2-4269 Sub-56 3,4-diClPh SO2 Single bond Sub-77
2-4270 Sub-56 3,4-diClPh SO2 Single bond Sub-78
2-4271 Sub-56 3,4-diClPh SO2 Single bond Sub-79
2-4272 Sub-56 3,4-diClPh SO2 Single bond Sub-80
2-4273 Sub-57 3,4-diClPh SO2 Single bond Sub-1
2-4274 Sub-57 3,4-diClPh SO2 Single bond Sub-2
2-4275 Sub-57 3,4-diClPh SO2 Single bond Sub-3
2-4276 Sub-57 3,4-diClPh SO2 Single bond Sub-4
2-4277 Sub-57 3,4-diClPh SO2 Single bond Sub-5
2-4278 Sub-57 3,4-diClPh SO2 Single bond Sub-6
2-4279 Sub-57 3,4-diClPh SO2 Single bond Sub-7
2-4280 Sub-57 3,4-diClPh SO2 Single bond Sub-8
2-4281 Sub-57 3,4-diClPh SO2 Single bond Sub-9
2-4282 Sub-57 3,4-diClPh SO2 Single bond Sub-10
2-4283 Sub-57 3,4-diClPh SO2 Single bond Sub-11
2-4284 Sub-57 3,4-diClPh SO2 Single bond Sub-12
2-4285 Sub-57 3,4-diClPh SO2 Single bond Sub-13
2-4286 Sub-57 3,4-diClPh SO2 Single bond Sub-14
2-4287 Sub-57 3,4-diClPh SO2 Single bond Sub-15
2-4288 Sub-57 3,4-diClPh SO2 Single bond Sub-16
2-4289 Sub-57 3,4-diClPh SO2 Single bond Sub-17
2-4290 Sub-57 3,4-diClPh SO2 Single bond Sub-18
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4291 Sub-56 3,4-diClPh SO2 Single bond Sub-19
2-4292 Sub-56 3,4-diClPh SO2 Single bond Sub-20
2-4293 Sub-56 3,4-diClPh SO2 Single bond Sub-21
2-4294 Sub-56 3,4-diClPh SO2 Single bond Sub-22
2-4295 Sub-56 3,4-diClPh SO2 Single bond Sub-23
2-4296 Sub-56 3,4-diClPh SO2 Single bond Sub-24
2-4297 Sub-56 3,4-diClPh SO2 Single bond Sub-25
2-4298 Sub-56 3,4-diClPh SO2 Single bond Sub-26
2-4299 Sub-57 3,4-diClPh SO2 Single bond Sub-27
2-4300 Sub-57 3,4-diClPh SO2 Single bond Sub-28
2-4301 Sub-57 3,4-diClPh SO2 Single bond Sub-29
2-4302 Sub-57 3,4-diClPh SO2 Single bond Sub-30
2-4303 Sub-57 3,4-diClPh SO2 Single bond Sub-31
2-4304 Sub-57 3,4-diClPh SO2 Single bond Sub-32
2-4305 Sub-57 3,4-diClPh SO2 Single bond Sub-65
2-4306 Sub-57 3,4-diClPh SO2 Single bond Sub-66
2-4307 Sub-57 3,4-diClPh SO2 Single bond Sub-67
2-4308 Sub-57 3,4-diClPh SO2 Single bond Sub-68
2-4309 Sub-57 3,4-diClPh SO2 Single bond Sub-69
2-4310 Sub-57 3,4-diClPh SO2 Single bond Sub-70
2-4311 Sub-57 3,4-diClPh SO2 Single bond Sub-71
2-4312 Sub-57 3,4-diClPh SO2 Single bond Sub-72
2-4313 Sub-57 3,4-diClPh SO2 Single bond Sub-73
2-4314 Sub-57 3,4-diClPh SO2 Single bond Sub-74
2-4315 Sub-57 3,4-diClPh SO2 Single bond Sub-75
2-4316 Sub-57 3,4-diClPh SO2 Single bond Sub-76
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4317 Sub-57 3,4-diClPh SO2 Single bond Sub-77
2-4318 Sub-57 3,4-diClPh SO2 Single bond Sub-78
2-4319 Sub-57 3,4-diClPh SO2 Single bond Sub-79
2-4320 Sub-57 3,4-diClPh SO2 Single bond Sub-80
2-4321 Sub-58 3 ,4-diClPh SO2 Single bond Sub-1
2-4322 Sub-58 3,4-diClPh SO2 Single bond Sub-2
2-4323 Sub-58 3,4-diClPh SO2 Single bond Sub-3
2-4324 Sub-58 3,4-diClPh SO2 Single bond Sub-4
2-4325 Sub-58 3,4-diClPh SO2 Single bond Sub-5
2-4326 Sub-58 3,4-diClPh SO2 Single bond Sub-6
2-4327 Sub-58 3,4-diClPh SO2 Single bond Sub-7
2-4328 Sub-58 3,4-diClPh SO2 Single bond Sub-8
2-4329 Sub-58 3,4-diClPh SO2 Single bond Sub-9
2-4330 Sub-58 3,4-diClPh SO2 Single bond Sub-10
2-4331 Sub-58 3,4-diClPh SO2 Single bond Sub-11
2-4332 Sub-58 3,4-diClPh SO2 Single bond Sub-12
2-4333 Sub-58 3,4-diClPh SO2 Single bond Sub-13
2-4334 Sub-58 3,4-diClPh SO2 Single bond Sub-14
2-4335 Sub-58 3,4-diClPh SO2 Single bond Sub-15
2-4336 Sub-58 3,4-diClPh SO2 Single bond Sub-16
2-4337 Sub-58 3,4-diClPh SO2 Single bond Sub-17
2-4338 Sub-58 3,4-diClPh SO2 Single bond Sub-18
2-4339 Sub-58 3,4-diClPh SO2 Single bond Sub-19
2-4340 Sub-58 3,4-diClPh SO2 Single bond Sub-20
2-4341 Sub-58 3,4-diClPh SO2 Single bond Sub-21
2-4342 Sub-58 3,4-diClPh SO2 Single bond Sub-22
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4343 Sub-58 3,4-diClPh SO2 Single bond Sub-23
2-4344 Sub-58 3,4-diClPh SO2 Single bond Sub-24
2-4345 Sub-58 3,4-diClPh SO2 Single bond Sub-25
2-4346 Sub-58 3,4-diClPh SO2 Single bond Sub-26
2-4347 Sub-58 3,4-diClPh SO2 Single bond Sub-27
2-4348 Sub-58 3,4-diClPh SO2 Single bond Sub-28
2-4349 Sub-58 3,4-diClPh SO2 Single bond Sub-29
2-4350 Sub-58 3,4-diClPh SO2 Single bond Sub-30
2-4351 Sub-58 3,4-diClPh SO2 Single bond Sub-31
2-4352 Sub-58 3,4-diClPh SO2 Single bond Sub-32
2-4353 Sub-58 3,4-diClPh SO2 Single bond Sub-65
2-4354 Sub-58 3,4-diClPh SO2 Single bond Sub-66
2-4355 Sub-58 3,4-diClPh SO2 Single bond Sub-67
2-4356 Sub-58 3,4-diClPh SO2 Single bond Sub-68
2-4357 Sub-58 3,4-diClPh SO2 Single bond Sub-69
2-4358 Sub-58 3,4-diClPh SO2 Single bond Sub-70
2-4359 Sub-58 3,4-diClPh SO2 Single bond Snb-71
2-4360 Sub-58 3,4-diClPh SO2 Single bond Sub-72
2-4361 Sub-58 3,4-diClPh SO2 Single bond Sub-73
2-4362 Sub-58 3,4-diClPh SO2 Single bond Sub-74
2-4363 Sub-58 3,4-diClPh SO2 Single bond Sub-75
2-4364 Sub-58 3,4-diClPh SO2 Single bond Sub-76
2-4365 Sub-58 3,4-diClPh SO2 Single bond Sub-77
2-4366 Sub-58 3,4-diClPh SO2 Single bond Sub-78
2-4367 Sub-58 3,4-diClPh SO2 Single bond Sub-79
2-4368 Sub-58 3,4-diClPh SO2 Single bond Sub-80
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4369 Sub-59 3,4-diClPh SO2 Single bond Sub-1
2-4370 Sub-59 3,4-diClPh SO2 Single bond Sub-2
2-4371 Sub-59 3,4-diClPh SO2 Single bond Sub-3
2-4372 Sub-59 3,4-diClPh SO2 Single bond Sub-4
2-4373 Sub-59 3,4-diClPh SO2 Single bond Sub-5
2-4374 Sub-59 3,4-diClPh SO2 Single bond Sub-6
2-4375 Sub-59 3,4-diClPh SO2 Single bond Sub-7
2-4376 Sub-59 3,4-diClPh SO2 Single bond Sub-8
2-4377 Sub-59 3,4-diClPh SO2 Single bond Sub-9
2-4378 Sub-59 3,4-diClPh SO2 Single bond Sub-10
2-4379 Sub-59 3,4-diClPh SO2 Single bond Sub-11
2-4380 Sub-59 3,4-diClPh SO2 Single bond Sub-12
2-4381 Sub-59 3,4-diClPh SO2 Single bond Sub-13
2-4382 Sub-59 3,4-diClPh SO2 Single bond Sub-14
2-4383 Sub-59 3,4-diClPh SO2 Single bond Sub-15
2-4384 Sub-59 3,4-diClPh SO2 Single bond Sub-16
2-4385 Sub-59 3,4-diClPh SO2 Single bond Sub-17
2-4386 Sub-59 3,4-diClPh SO2 Single bond Sub-18
2-4387 Sub-59 3,4-diClPh SO2 Single bond Sub-19
2-4388 Sub-59 3,4-diClPh SO2 Single bond Sub-20
2-4389 Sub-59 3,4-diClPh SO2 Single bond Sub-21
2-4390 Sub-59 3,4-diClPh SO2 Single bond Sub-22
2-4391 Sub-59 3,4-diClPh SO2 Single bond Sub-23
2-4392 Sub-59 3,4-diCiCh SO2 Single bond Sub-24
2-4393 Sub-59 3,4-diClPh SO2 Single bond Sub-25
2-4394 Sub-59 3,4-diClPh SO2 Single bond Sub-26
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4395 Sub-59 3,4-diClPh SO2 Single bond Sub-27
2-4396 Sub-59 3,4-diClPh SO2 Single bond Sub-28
2-4397 Sub-59 3,4-diClPh SO2 Single bond Sub-29
2-4398 Sub-59 3,4-diClPh SO2 Single bond Sub-30
2-4399 Sub-59 3,4-diClPh SO2 Single bond Sub-31
3-4400 Sub-59 3,4-diClPh SO2 Single bond Sub-32
2-4401 Sub-59 3,4-diClPh SO2 Single bond Sub-65
2-4402 Sub-59 3,4-diClPh SO2 Single bond Sub-66
2-4403 Sub-59 3,4-diClPh SO2 Single bond Sub-67
2-4404 Sub-59 3,4-diClPh SO2 Single bond Sub-68
2-4405 Sub-59 3,4-diClPh SO2 Single bond Sub-69
2-4406 Sub-59 3,4-diClPh SO2 Single bond Sub-70
2-4407 Sub-59 3,4-diClPh SO2 Single bond Sub-71
2-4408 Sub-59 3,4-diClPh SO2 Single bond Sub-72
2-4409 Sub-59 3,4-diClPh SO2 Single bond Sub-73
2-4410 Sub-59 3,4-diClPh SO2 Single bond Sub-74
2-4411 Sub-59 3,4-diClPh SO2 Single bond Sub-75
2-4412 Sub-59 3,4-diClPh SO2 Single bond Sub-76
2-4413 Sub-59 3,4-diClPh SO2 Single bond Sub-77
2-4414 Sub-59 3,4-diClPh SO2 Single bond Sub-78
2-4415 Sub-59 3,4-diClPh SO2 Single bond Sub-79
2-4416 Sub-59 3,4-diClPh SO2 Single bond Sub-80
2-4417 Sub-82 3,4-diClPh SO2 Single bond Sub-1
2-4418 Sub-82 3,4-diClPh SO2 Single bond Sub-2
2-4419 Sub-82 3,4-diClPh SO2 Single bond Sub-3
2-4420 Sub-82 3,4-diClPh SO2 Single bond Sub-4
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4421 Sub-82 3,4-diClPh SO2 Single bond Sub-5
2-4422 Sub-82 3,4-diClPh SO2 Single bond Sub-6
2-4423 Sub-82 3,4-diClPh SO2 Single bond Sub-7
2-4424 Sub-82 3,4-diClPh SO2 Single bond Sub-8
2-4425 Sub-82 3,4-diClPh SO2 Single bond Sub-9
3-4426 Sub-82 3,4-diClPh SO2 Single bond Sub-10
2-4427 Sub-82 3,4-diClPh SO2 Single bond Sub-11
2-4428 Sub-82 3,4-diClPh SO2 Single bond Sub-12
2-4429 Sub-82 3,4-diClPh SO2 Single bond Sub-13
2-4430 Sub-82 3,4-diClPh SO2 Single bond Sub-14
2-4431 Sub-82 3,4-diClPh SO2 Single bond Sub-15
2-4432 Sub-82 3,4-diClPh SO2 Single bond Sub-16
2-4433 Sub-82 3,4-diClPh SO2 Single bond Sub-17
2-4434 Sub-82 3,4-diClPh SO2 Single bond Sub-18
2-4435 Sub-82 3,4-diClPh SO2 Single bond Sub-19
2-4436 Sub-82 3,4-diClPh SO2 Single bond Sub-20
2-4437 Sub-82 3,4-diClPh SO2 Single bond Sub-21
2-4438 Sub-82 3,4-diClPh SO2 Single bond Sub-22
2-4439 Sub-82 3,4-diClPh SO2 Single bond Sub-23
2-4440 Sub-82 3,4-diClPh SO2 Single bond Sub-24
2-4441 Sub-82 3,4-diClPh SO2 Single bond Sub-25
2-4442 Sub-82 3,4-diClPh SO2 Single bond Sub-26
2-4443 Sub-82 3,4-diClPh SO2 Single bond Sub-27
2-4444 Sub-82 3,4-diClPh SO2 Single bond Sub-28
2-4445 Sub-82 3,4-diClPh SO2 Single bond Sub-29
2-4446 Sub-82 3,4-diClPh SO2 Single bond Sub-30
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4447 Sub-82 3,4-diClPh SO2 Single bond Sub-31
2-4448 Sub-82 3,4-diClPh SO2 Single bond Sub-32
2-4449 Sub-82 3,4-diClPh SO2 Single bond Sub-65
2-4450 Sub-82 3,4-diClPh SO2 Single bond Sub-66
2-4451 Sub-82 3,4-diClPh SO2 Single bond Sub-67
2-4452 Sub-82 3,4-diClPh SO2 Single bond Sub-68
2-4453 Sub-82 3,4-diClPh SO2 Single bond Sub-69
2-4454 Sub-82 3,4-diClPh SO2 Single bond Sub-70
2-4455 Sub-82 3,4-diClPh SO2 Single bond Sub-71
2-4456 Sub-82 3,4-diClPh SO2 Single bond Sub-72
2-4457 Sub-82 3,4-diClPh SO2 Single bond Sub-73
2-4458 Sub-82 3,4-diClPh SO2 Single bond Sub-74
2-4459 Sub-82 3,4-diClPh SO2 Single bond Sub-75
2-4460 Sub-82 3,4-diClPh SO2 Single bond Sub-76
2-4461 Sub-82 3,4-diClPh SO2 Single bond Sub-77
2-4462 Sub-82 3,4-diClPh SO2 Single bond Sub-78
2-4463 Sub-82 3,4-diClPh SO2 Single bond Sub-79
2-4464 Sub-82 3,4-diClPh SO2 Single bond Sub-80
2-4465 Sub-83 3,4-diClPh SO2 Single bond Sub-1
2-4466 Sub-83 3,4-diClPh SO2 Single bond Sub-2
2-4467 Sub-83 3,4-diClPh SO2 Single bond Sub-3
2-4468 Sub-83 3,4-diClPh SO2 Single bond Sub-4
2-4469 Sub-83 3,4-diClPh SO2 Single bond Sub-5
2-4470 Sub-83 3,4-diClPh SO2 Single bond Sub-6
2-4471 Sub-83 3,4-diClPh SO2 Single bond Sub-7
2-4472 Sub-83 3,4-diClPh SO2 Single bond Sub-8
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4473 Sub-83 3,4-diClPh SO2 Single bond Sub-9
2-4474 Sub-83 3,4-diClPh SO2 Single bond Sub-10
2-4475 Sub-83 3,4-diClPh SO2 Single bond Sub-11
2-4476 Sub-83 3,4-diClPh SO2 Single bond Sub-12
2-4477 Sub-83 3,4-diClPh SO2 Single bond Sub-13
2-4478 Sub-83 3,4-diClPh SO2 Single bond Sub-14
2-4479 Sub-83 3,4-diClPh SO2 Single bond Sub-15
2-4480 Sub-83 3,4-diClPh SO2 Single bond Sub-16
2-4481 Sub-83 3,4-diClPh SO2 Single bond Sub-17
2-4482 Sub-83 3,4-diClPh SO2 Single bond Sub-18
2-4483 Sub-83 3,4-diClPh SO2 Single bond Sub-19
2-4484 Sub-83 3,4-diClPh SO2 Single bond Sub-20
2-4485 Sub-83 3,4-diClPh SO2 Single bond Sub-21
2-4486 Sub-83 3,4-diClPh SO2 Single bond Sub-22
2-4487 Sub-83 3,4-diClPh SO2 Single bond Sub-23
2-4488 Sub-83 3,4-diClPh SO2 Single bond Sub-24
2-4489 Sub-83 3,4-diClPh SO2 Single bond Sub-25
2-4490 Sub-83 3,4-diClPh SO2 Single bond Sub-26
2-4491 Sub-83 3,4-diClPh SO2 Single bond Sub-27
2-4492 Sub-83 3,4-diClPh SO2 Single bond Sub-28
2-4493 Sub-83 3,4-diClPh SO2 Single bond Sub-29
2-4494 Sub-83 3,4-diClPh SO2 Single bond Sub-30
2-4495 Sub-83 3,4-diClPh SO2 Single bond Sub-31
2-4496 Sub-83 3,4-diClPh SO2 Single bond Sub-32
2-4497 Sub-83 3,4-diClPh SO2 Single bond Sub-65
2-4498 Sub-83 3,4-diClPh SO2 Single bond Sub-66
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4499 Sub-83 3,4-diClPh SO2 Single bond Sub-67
2-4500 Sub-83 3,4-diClPh SO2 Single bond Sub-68
2-4501 Sub-83 3,4-diClPh SO2 Single bond Sub-69
2-4502 Sub-83 3,4-diClPh SO2 Single bond Sub-70
2-4503 Sub-83 3,4-diClPh SO2 Single bond Sub-71
2-4504 Sub-83 3,4-diClPh SO2 Single bond Sub-72
2-4505 Sub-83 3,4-diClPh SO2 Single bond Sub-73
2-4506 Sub-83 3,4-diClPh SO2 Single bond Sub-74
2-4507 Sub-83 3,4-diClPh SO2 Single bond Sub-75
2-4508 Sub-83 3,4-diClPh SO2 Single bond Sub-76
2-4509 Sub-83 3,4-diClPh SO2 Single bond Sub-77
2-4510 Sub-83 3,4-diClPh SO2 Single bond Sub-78
2-4511 Sub-83 3,4-diClPh SO2 Single bond Sub-79
2-4512 Sub-83 3,4-diClPh SO2 Single bond Sub-80
2-4513 Sub-61 3,4-diClPh SO2 Single bond Sub-1
2-4514 Sub-61 3,4-diClPh SO2 Single bond Sub-2
2-4515 Sub-61 3,4-diClPh SO2 Single bond Sub-3
2-4516 Sub-61 3,4-diClPh SO2 Single bond Sub-4
2-4517 Sub-61 3,4-diClPh SO2 Single bond Sub-5
2-4518 Sub-61 3,4-diClPh SO2 Single bond Sub-6
2-4519 Sub-61 3,4-diClPh SO2 Single bond Sub-7
2-4520 Sub-61 3,4-diClPh SO2 Single bond Sub-8
2-4521 Sub-61 3,4-diClPh SO2 Single bond Sub-9
2-4522 Sub-61 3,4-diClPh SO2 Single bond Sub-10
2-4523 Sub-61 3,4-diClPh SO2 Single bond Sub-11
2-4524 Sub-61 3,4-diClPh SO2 Single bond Sub-12
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4525 Sub-61 3,4-diClPh SO2 Single bond Sub-13
2-4526 Sub-61 3,4-diClPh SO2 Single bond Sub-14
2-4527 Sub-61 3,4-diClPh SO2 Single bond Sub-15
2-4528 Sub-61 3,4-diClPh SO2 Single bond Sub-16
2-4529 Sub-61 3,4-diClPh SO2 Single bond Sub-17
2-4530 Sub-61 3,4-diClPh SO2 Single bond Sub-18
2-4531 Sub-61 3,4-diClPh SO2 Single bond Sub-19
2-4532 Sub-61 3,4-diClPh SO2 Single bond Sub-20
2-4533 Sub-61 3,4-diClPh SO2 Single bond Sub-21
2-4534 Sub-61 3,4-diClPh SO2 Single bond Sub-22
2-4535 Sub-61 3,4-diClPh SO2 Single bond Sub-23
2-4536 Sub-61 3,4-diClPh SO2 Single bond Sub-24
2-4537 Sub-61 3,4-diClPh SO2 Single bond Sub-25
2-4538 Sub-61 3,4-diClPh SO2 Single bond Sub-26
2-4539 Sub-61 3,4-diClPh SO2 Single bond Sub-27
2-4540 Sub-61 3,4-diClPh SO2 Single bond Sub-28
2-4541 Sub-61 3,4-diClPh SO2 Single bond Sub-29
2-4542 Sub-61 3,4-diClPh SO2 Single bond Sub-30
2-4543 Sub-61 3,4-diClPh SO2 Single bond Sub-31
2-4544 Sub-61 3,4-diClPh SO2 Single bond Sub-32
2-4545 Sub-61 3,4-diClPh SO2 Single bond Sub-65
2-4546 Sub-61 3,4-diClPh SO2 Single bond Sub-66
2-4547 Sub-61 3,4-diClPh SO2 Single bond Sub-67
2-4548 Sub-61 3,4-diClPh SO2 Single bond Sub-68
2-4549 Sub-61 3,4-diClPh SO2 Single bond Sub-69
2-4550 Sub-61 3,4-diClPh SO2 Single bond Sub-70
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4551 Sub-61 3,4-diClPh SO2 Single bond Sub-71
2-4552 Sub-61 3,4-diClPh SO2 Single bond Sub-72
2-4553 Sub-61 3,4-diClPh SO2 Single bond Sub-73
2-4554 Sub-61 3,4-diClPh SO2 Single bond Sub-74
2-4555 Sub-61 3,4-diClPh SO2 Single bond Sub-75
2-4556 Sub-61 3,4-diClPh SO2 Single bond Sub-76
2-4557 Sub-61 3,4-diClPh SO2 Single bond Sub-77
2-4558 Sub-61 3,4-diClPh SO2 Single bond Sub-78
2-4559 Sub-61 3,4-diClPh SO2 Single bond Sub-79
2-4560 Sub-61 3,4-diClPh SO2 Single bond Sub-80
2-4561 Sub-60 3,4-diClPh SO2 Single bond Sub-1
2-4562 Sub-6u 3,4-diClPh SO2 Single bond Sub-2
2-4563 Sub-60 3,4-diClPh SO2 Single bond Sub-3
2-4564 Sub-60 3,4-diClPh SO2 Single bond Sub-4
2-4565 Sub-60 3,4-diClPh SO2 Single bond Sub-5
2-4566 Sub-60 3,4-diClPh SO2 Single bond Sub-6
2-4567 Sub-60 3,4-diClPh SO2 Single bond Sub-7
2-4568 Sub-60 3,4-diClPh SO2 SheetKey with a key body Sub-8
2-4569 Sub-60 3,4-diClPh SO2 Single bond Sub-9
2-4570 Sub-60 3,4-diClPh SO2 Single bond Sub-10
2-4571 Sub-60 3,4-diClPh SO2 Single bond Sub-11
2-4572 Sub-60 3,4-diClPh SO2 Single bond Sub-12
2-4573 Sub-60 3,4-diClPh SO2 Single bond Sub-13
2-4574 Sub-60 3,4-diClPh SO2 Single bond Sub-14
2-4575 Sub-60 3,4-diClPh SO2 Single bond Sub-15
2-4576 Sub-60 3,4-diClPh SO2 Single bond Sub-16
Table 2(cont.)
Compound (I) Serial number R1 R2 A B Z
2-4577 Sub-60 3,4-diClPh SO2 Single bond Sub-17
2-4578 Sub-60 3,4-diClPh SO2 Single bond Sub-18
2-4579 Sub-60 3,4-diClPh SO2 Single bond Sub-19
2-4580 Sub-60 3,4-diClPh SO2 Single bond Sub-20
2-4581 Sub-60 3,4-diClPh SO2 Single bond Sub-21
2-4582 Sub-60 3,4-diClPh SO2 Single bond Sub-22
2-4583 Sub-60 3,4-diClPh SO2 Single bond Sub-23
2-4584 Sub-60 3,4-diClPh SO2 Single bond Sub-24
2-4585 Sub-60 3,4-diClPh SO2 Single bond Sub-25
2-4586 Sub-60 3,4-diClPh SO2 Single bond Sub-26
2-4587 Sub-60 3,4-diClPh SO2 Single bond Sub-27
2-4588 Sub-60 3,4-diClPh SO2 Single bond Sub-28
2-4589 Sub-60 3,4-diClPh SO2 Single bond Sub-29
2-4590 Sub-60 3,4-diClPh SO2 Single bond Sub-30
2-4591 Sub-60 3,4-diClPh SO2 Single bond Sub-31
2-4592 Sub-60 3,4-diClPh SO2 Single bond Sub-32
2-4593 Sub-60 3,4-diClPh SO2 Single bond Sub-65
2-4594 Sub-60 3,4-diClPh SO2 Single bond Sub-66
2-4595 Sub-60 3,4-diClPh SO2 Single bond Sub-67
2-4596 Sub-60 3,4-diClPh SO2 Single bond Sub-68
2-4597 Sub-60 3,4-diClPh SO2 Single bond Sub-69
2-4598 Sub-60 3,4-diClPh SO2 Single bond Sub-70
2-4599 Sub-60 3,4-diClPh SO2 Single bond Sub-71
2-4600 Sub-60 3,4-diClPh SO2 Single bond Sub-72
2-4601 Sub-60 3,4-diClPh SO2 Single bond Sub-73
2-4602 Sub-60 3,4-diClPh SO2 Single bond Sub-74
Table 2(contc)
Compound (I) Serial number R1 R2 A B Z
2-4603 Sub-60 3,4-diClPh SO2 Single bond Sub-75
2-4604 Sub-60 3,4-diClPh SO2 Single bond Sub-76
2-4605 Sub-60 3,4-diClPh SO2 Single bond Sub-77
2-4606 Sub-60 3,4-diClPh SO2 Single bond Sub-78
2-4607 Sub-60 3,4-diClPh SO2 Single bond Sub-79
2-4608 Sub-60 3,4-diClPh SO2 Single bond Sub-80
TABLE 3
Compound (I) Serial number R1 R2 A B E
3-1 Sub-33 3,4-diClPh -CO- Single bond -CH2-
3-2 Sub-34 3,4-diClPh -CO- Single bond -CH2-
3-3 Sub-35 3,4-diClPh -CO- Single bond -CH2-
3-4 Sub-36 3,4-diClPh -CO- Single bond -CH2-
3-5 Sub-37 3,4-diClPh -CO- Single bond -CH2-
3-6 Sub-38 3,4-diClPh -CO- Single bond -CH2-
3-7 Sub-39 3,4-diClPh -CO- Single bond -CH2-
3-8 Sub-40 3,4-diClPh -CO- Single bond -CH2-
3-9 Sub-41 3,4-diClPh -CO- Single bond -CH2-
3-10 Sub-42 3,4-diClPh -CO- Single bond -CH2-
3-11 Sub-84 3,4-diClPh -CO- Single bond -CH2-
3-12 Sub-43 3,4-diClPh -CO- Single bond -CH2-
3-13 Sub-44 3,4-diClPh -CO- Single bond -CH2-
3-14 Sub-45 3,4-diClPh -CO- Single bond -CH2-
3-15 Sub-46 3,4-diClPh -CO- Single bond -CH2-
3-16 Sub-47 3,4-diClPh -CO- Single bond -CH2-
3-17 Sub-81 3,4-diClPh -CO- Single bond -CH2-
3-18 Sub-48 3,4-diClPh -CO- Single bond -CH2-
3-19 Sub-49 3,4-diClPh -CO- Single bond -CH2-
3-20 Sub-50 3,4-diClPh -CO- Single bond -CH2-
3-21 Sub-51 3,4-diClPh -CO- Single bond -CH2-
3-22 Sub-52 3,4-diClPh -CO- Single bond -CH2-
3-23 Sub-53 3,4-diClPh -CO- Single bond -CH2-
3-24 Sub-54 3,4-diClPh -CO- Single bond -CH2-
3-25 Sub-56 3,4-diClPh -CO- Single bond -CH2-
3-26 Sub-57 3,4-diClPh -CO- Single bond -CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-27 Sub-58 3,4-diClPh -CO- Single bond -CH2-
3-28 Sub-59 3,4-diClPh -CO- Single bond -CH2-
3-29 Sub-82 3,4-diClPh -CO- Single bond -CH2-
3-30 Sub-83 3,4-diClPh -CO- Single bond -CH2-
3-31 Sub-61 3,4-diClPh -CO- Single bond -CH2-
3-32 Sub-55 3,4-diClPh -CO- Single bond -CH2-
3-33 Sub-33 3,4-diClPh -CO- Single bond -CH2CH2-
3-34 Sub-34 3,4-diClPh -CO- Single bond -CH2CH2-
3-35 Sub-35 3,4-diClPh -CO- Single bond -CH2CH2-
3-36 Sub-36 3,4-diClPh -CO- Single bond -CH2CH2-
3-37 Sub-37 3,4-diClPh -CO- Single bond -CH2CH2-
3-38 Sub-38 3,4-diClPh -CO- Single bond -CH2CH2-
3-39 Sub-39 3,4-diClPh -CO- Single bond -CH2CH2-
3-40 Sub-40 3,4-diClPh -CO- Single bond -CH2CH2-
3-41 Sub-41 3,4-diClPh -CO- Single bond -CH2CH2-
3-42 Sub-42 3,4-diClPh -CO- Single bond -CH2CH2-
3-43 Sub-84 3,4-diClPh -CO- Single bond -CH2CH2-
3-44 Sub-43 3,4-diClPh -CO- Single bond -CH2CH2-
3-45 Sub-44 3,4-diClPh -CO- Single bond -CH2CH2-
3-46 Sub-45 3,4-diClPh -CO- Single bond -CH2CH2-
3-47 Sub-46 3,4-diClPh -CO- Single bond -CH2CH2-
3-48 Sub-47 3,4-diClPh -CO- Single bond -CH2CH2-
3-49 Sub-81 3,4-diClPh -CO- Single bond -CH2CH2-
3-50 Sub-48 3,4-diClPh -CO- Single bond -CH2CH2-
3-51 Sub-49 3,4-diClPh -CO- Single bond -CH2CH2-
3-52 Sub-50 3,4-diClPh -CO- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-53 Sub-51 3,4-diClPh -CO- Single bond -CH2CH2-
3-54 Sub-52 3,4-diClPh -CO- Single bond -CH2CH2-
3-55 Sub-53 3,4-diClPh -CO- Single bond -CH2CH2-
3-56 Sub-54 3,4-diClPh -CO- Single bond -CH2CH2-
3-57 Sub-56 3,4-diClPh -CO- Single bond -CH2CH2-
3-58 Sub-57 3,4-diClPh -CO- Single bond -CH2CH2-
3-59 Sub-58 3,4-diClPh -CO- Single bond -CH2CH2-
3-60 Sub-59 3,4-diClPh -CO- Single bond -CH2CH2-
3-61 Sub-82 3,4-diClPh -CO- Single bond -CH2CH2-
3-62 Sub-83 3,4-diClPh -CO- Single bond -CH2CH2-
3-63 Sub-61 3,4-diClPh -CO- Single bond -CH2CH2-
3-64 Sub-55 3,4-diClPh -CO- Single bond -CH2CH2-
3-65 Sub-33 3,4-diClPh -CO- Single bond -(CH2)3-
3-66 Sub-34 3,4-diClPh -CO- Single bond -(CH2)3-
3-67 Sub-35 3,4-diClPh -CO- Single bond -(CH2)3-
3-68 Sub-36 3,4-diClPh -CO- Single bond -(CH2)3-
3-69 Sub-37 3,4-diClPh -CO- Single bond -(CH2)3-
3-70 Sub-38 3,4-diClPh -CO- Single bond -(CH2)3-
3-71 Sub-39 3,4-diClPh -CO- Single bond -(CH2)3-
3-72 Sub-40 3,4-diClPh -CO- Single bond -(CH2)3-
3-73 Sub-41 3,4-diClPh -CO- Single bond -(CH2)3-
3-74 Sub-42 3,4-diClPh -CO- Single bond -(CH2)3-
3-75 Sub-84 3,4-diClPh -CO- Single bond -(CH2)3-
3-76 Sub-43 3,4-diClPh -CO- Single bond -(CH2)3-
3-77 Sub-44 3,4-diClPh -CO- Single bond -(CH2)3-
3-78 Sub-45 3,4-diClPh -CO- Single bond -(CH2)3-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-79 Sub-46 3,4-diClPh -CO- Single bond -(CH2)3-
3-80 Sub-47 3,4-diClPh -CO- Single bond -(CH2)3-
3-81 Sub-81 3,4-diClPh -CO- Single bond -(CH2)3-
3-82 Sub-48 3,4-diClPh -CO- Single bond -(CH2)3-
3-83 Sub-49 3,4-diClPh -CO- Single bond -(CH2)3-
3-84 Sub-50 3,4-diClPh -CO- Single bond -(CH2)3-
3-85 Sub-51 3,4-diClPh -CO- Single bond -(CH2)3-
3-86 Sub-52 3,4-diClPh -CO- Single bond -(CH2)3-
3-87 Sub-53 3,4-diClPh -CO- Single bond -(CH2)3-
3-88 Sub-54 3,4-diClPh -CO- Single bond -(CH2)3-
3-89 Sub-56 3,4-diClPh -CO- Single bond -(CH2)3-
3-90 Sub-57 3,4-diClPh -CO- Single bond -(CH2)3-
3-91 Sub-58 3,4-diClPh -CO- Single bond -(CH2)3-
3-92 Sub-59 3,4-diClPh -CO- Single bond -(CH2)3-
3-93 Sub-82 3,4-diClPh -CO- Single bond -(CH2)3-
3-94 Sub-83 3,4-diClPh -CO- Single bond -(CH2)3-
3-95 Sub-61 3,4-diClPh -CO- Single bond -(CH2)3-
3-96 Sub-55 3,4-diClPh -CO- Single bond -(CH2)3-
3-97 Sub-33 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-98 Sub-34 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-99 Sub-35 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-100 Sub-36 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-101 Sub-37 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-102 Sub-38 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-103 Sub-39 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-104 Sub-40 3,4-diClPh -CO- Single bond -CH2C(Me)2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-105 Sub-41 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-106 Sub-42 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-107 Sub-84 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-108 Sub-43 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-109 Sub-44 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-110 Sub-45 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-111 Sub-46 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-112 Sub-47 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-113 Sub-81 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-114 Sub-48 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-115 Sub-49 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-116 Sub-50 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-117 Sub-51 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-118 Sub-52 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-119 Sub-53 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-120 Sub-54 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-121 Sub-56 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-122 Sub-57 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-123 Sub-58 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-124 Sub-59 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-125 Sub-82 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-126 Sub-83 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-127 Sub-61 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-128 Sub-55 3,4-diClPh -CO- Single bond -CH2C(Me)2-
3-129 Sub-33 3,4-diClPh -CO- Single bond -CH2-cPR-
3-130 Sub-34 3,4-diClPh -CO- Single bond -CH2-cPR-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-131 Sub-35 3,4-diClPh -CO- Single bond -CH2-cPr-
3-132 Sub-36 3,4-diClPh -CO- Single bond -CH2-cPr-
3-133 Sub-37 3,4-diClPh -CO- Single bond -CH2-cPr-
3-134 Sub-38 3,4-diClPh -CO- Single bond -CH2-cPr-
3-135 Sub-39 3,4-diClPh -CO- Single bond -CH2-cPr-
3-136 Sub-40 3,4-diClPh -CO- Single bond -CH2-cPr-
3-137 Sub-41 3,4-diClPh -CO- Single bond -CH2-cPr-
3-138 Sub-42 3,4-diClPh -CO- Single bond -CH2-cPr-
3-139 Sub-84 3,4-diClPh -CO- Single bond -CH2-cPr-
3-140 Sub-43 3,4-diClPh -CO- Single bond -CH2-cPr-
3-141 Sub-44 3,4-diClPh -CO- Single bond -CH2-cPr-
3-142 Sub-45 3,4-diClPh -CO- Single bond -CH2-cPr-
3-143 Sub-46 3,4-diClPh -CO- Single bond -CH2-cPr-
3-144 Sub-47 3,4-diClPh -CO- Single bond -CH2-cPr-
3-145 Sub-81 3,4-diClPh -CO- Single bond -CH2-cPr-
3-146 Sub-48 3,4-diClPh -CO- Single bond -CH2-cPr-
3-147 Sub-49 3,4-diClPh -CO- Single bond -CH2-cPr-
3-148 Sub-50 3,4-diClPh -CO- Single bond -CH2-cPr-
3-149 Sub-51 3,4-diClPh -CO- Single bond -CH2-cPr-
3-150 Sub-52 3,4-diClPh -CO- Single bond -CH2-cPr-
3-151 Sub-53 3,4-diClPh -CO- Single bond -CH2-cPr-
3-152 Sub-54 3,4-diClPh -CO- Single bond -CH2-cPr-
3-153 Sub-56 3,4-diClPh -CO- Single bond -CH2-cPr-
3-154 Sub-57 3,4-diClPh -CO- Single bond -CH2-cPr-
3-155 Sub-58 3,4-diClPh -CO- Single bond -CH2-cPr-
3-156 Sub-59 3,4-diClPh -CO- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-157 Sub-82 3,4-diClPh -CO- Single bond -CH2-cPr-
3-158 Sub-83 3,4-diClPh -CO- Single bond -CH2-cPr-
3-159 Sub-61 3,4-diClPh -CO- Single bond -CH2-cPr-
3-160 Sub-55 3,4-diClPh -CO- Single bond -CH2-cPr-
3-161 Sub-33 3,4-diClPh -CO- Single bond -CH2-cBu-
3-162 Sub-34 3,4-diClPh -CO- Single bond -CH2-cBu-
3-163 Sub-35 3,4-diClPh -CO- Single bond -CH2-cBu-
3-164 Sub-36 3,4-diClPh -CO- Single bond -CH2-cBu-
3-165 Sub-37 3,4-diClPh -CO- Single bond -CH2-cBu-
3-166 Sub-38 3,4-diClPh -CO- Single bond -CH2-cBu-
3-167 Sub-39 3,4-diClPh -CO- Single bond -CH2-cBu-
3-168 Sub-40 3,4-diClPh -CO- Single bond -CH2-cBu-
3-169 Sub-41 3,4-diClPh -CO- Single bond -CH2-cBu-
3-170 Sub-42 3,4-diClPh -CO- Single bond -CH2-cBu-
3-171 Sub-84 3,4-diClPh -CO- Single bond -CH2-cBu-
3-172 Sub-43 3,4-diClPh -CO- Single bond -CH2-cBu-
3-173 Sub-44 3,4-diClPh -CO- Single bond -CH2-cBu-
3-174 Sub-45 3,4-diClPh -CO- Single bond -CH2-cBu-
3-175 Sub-46 3,4-diClPh -CO- Single bond -CH2-cBu-
3-176 Sub-47 3,4-diClPh -CO- Single bond -CH2-cBu-
3-177 Sub-81 3,4-diClPh -CO- Single bond -CH2-cBu-
3-178 Sub-48 3,4-diClPh -CO- Single bond -CH2-cBu-
3-179 Sub-49 3,4-diClPh -CO- Single bond -CH2-cBu-
3-180 Sub-50 3,4-diClPh -CO- Single bond -CH2-cBu-
3-181 Sub-51 3,4-diClPh -CO- Single bond -CH2-cBu-
3-182 Sub-52 3,4-diClPh -CO- Single bond -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-183 Sub-53 3,4-diClPh -CO- Single bond -CH2-cBu-
3-184 Sub-54 3,4-diClPh -CO- Single bond -CH2-cBu-
3-185 Sub-56 3,4-diClPh -CO- Single bond -CH2-cBu-
3-186 Sub-57 3,4-diClPh -CO- Single bond -CH2-cBu-
3-187 Sub-58 3,4-diClPh -CO- Single bond -CH2-cBu-
3-188 Sub-59 3,4-diClPh -CO- Single bond -CH2-cBu-
3-189 Sub-82 3,4-diClPh -CO- Single bond -CH2-cBu-
3-190 Sub-83 3,4-diClPh -CO- Single bond -CH2-cBu-
3-191 Sub-61 3,4-diClPh -CO- Single bond -CH2-cBu-
3-192 Sub-55 3,4-diClPh -CO- Single bond -CH2-cBu-
3-193 Sub-33 3,4-diClPh -CO- Single bond -CH2-cPn-
3-194 Sub-34 3,4-diClPh -CO- Single bond -CH2-cPn-
3-195 Sub-35 3,4-diClPh -CO- Single bond -CH2-cPn-
3-196 Sub-36 3,4-diClPh -CO- Single bond -CH2-cPn-
3-197 Sub-37 3,4-diClPh -CO- Single bond -CH2-cPn-
3-198 Sub-38 3,4-diClPh -CO- Single bond -CH2-cPn-
3-199 Sub-39 3,4-diClPh -CO- Single bond -CH2-cPn-
3-200 Sub-40 3,4-diClPh -CO- Single bond -CH2-cPn-
3-201 Sub-41 3,4-diClPh -CO- Single bond -CH2-cPn-
3-202 Sub-42 3,4-diClPh -CO- Single bond -CH2-cPn-
3-203 Sub-84 3,4-diClPh -CO- Single bond -CH2-cPn-
3-204 Sub-43 3,4-diClPh -CO- Single bond -CH2-cPn-
3-205 Sub-44 3,4-diClPh -CO- Single bond -CH2-cPn-
3-206 Sub-45 3,4-diClPh -CO- Single bond -CH2-cPn-
3-207 Sub-46 3,4-diClPh -CO- Single bond -CH2-cPn-
3-208 Sub-47 3,4-diClPh -CO- Single bond -CH2-cPn-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-209 Sub-81 3,4-diClPh -CO- Single bond -CH2-cPn-
3-210 Sub-48 3,4-diClPh -CO- Single bond -CH2-cPn-
3-211 Sub-49 3,4-diClPh -CO- Single bond -CH2-cPn-
3-212 Sub-50 3,4-diClPh -CO- Single bond -CH2-cPn-
3-213 Sub-51 3,4-diClPh -CO- Single bond -CH2-cPn-
3-214 Sub-52 3,4-diClPh -CO- Single bond -CH2-cPn-
3-215 Sub-53 3,4-diClPh -CO- Single bond -CH2-cPn-
3-216 Sub-54 3,4-diClPh -CO- Single bond -CH2-cPn-
3-217 Sub-56 3,4-diClPh -CO- Single bond -CH2-cPn-
3-218 Sub-57 3,4-diClPh -CO- Single bond -CH2-cPn-
3-219 Sub-58 3,4-diClPh -CO- Single bond -CH2-cPn-
3-220 Sub-59 3,4-diClPh -CO- Single bond -CH2-cPn-
3-221 Sub-82 3,4-diClPh -CO- Single bond -CH2-cPn-
3-222 Sub-83 3,4-diClPh -CO- Single bond -CH2-cPn-
3-223 Sub-61 3,4-diClPh -CO- Single bond -CH2-cPn-
3-224 Sub-55 3,4-diClPh -CO- Single bond -CH2-cPn-
3-225 Sub-33 3,4-diClPh -CO- Single bond -CH2-cHx-
3-226 Sub-34 3,4-diClPh -CO- Single bond -CH2-cHx-
3-227 Sub-35 3,4-diClPh -CO- Single bond -CH2-cHx-
3-228 Sub-36 3,4-diClPh -CO- Single bond -CH2-cHx-
3-229 Sub-37 3,4-diClPh -CO- Single bond -CH2-cHx-
3-230 Sub-38 3,4-diClPh -CO- Single bond -CH2-cHx-
3-231 Sub-39 3,4-diClPh -CO- Single bond -CH2-cHx-
3-232 Sub-40 3,4-diClPh -CO- Single bond -CH2-cHx-
3-233 Sub-41 3,4-diClPh -CO- Single bond -CH2-cHx-
3-234 Sub-42 3,4-diClPh -CO- Single bond -CH2-cHx-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-235 Sub-84 3,4-diClPh -CO- Single bond -CH2-cHx-
3-236 Sub-43 3,4-diClPh -CO- Single bond -CH2-cHx-
3-237 Sub-44 3,4-diClPh -CO- Single bond -CH2-cHx-
3-238 Sub-45 3,4-diClPh -CO- Single bond -CH2-cHx-
3-239 Sub-46 3,4-diClPh -CO- Single bond -CH2-cHx-
3-240 Sub-47 3,4-diClPh -CO- Single bond -CH2-cHx-
3-241 Sub-81 3,4-diClPh -CO- Single bond -CH2-cHx-
3-242 Sub-48 3,4-diClPh -CO- Single bond -CH2-cHx-
3-243 Sub-49 3,4-diClPh -CO- Single bond -CH2-cHx-
3-244 Sub-50 3,4-diClPh -CO- Single bond -CH2-cHx-
3-245 Sub-51 3,4-diClPh -CO- Single bond -CH2-cHx-
3-246 Sub-52 3,4-diClPh -CO- Single bond -CH2-cHx-
3-247 Sub-53 3,4-diClPh -CO- Single bond -CH2-cHx-
3-248 Sub-54 3,4-diClPh -CO- Single bond -CH2-cHx-
3-249 Sub-56 3,4-diClPh -CO- Single bond -CH2-cHx-
3-250 Sub-57 3,4-diClPh -CO- Single bond -CH2-cHx-
3-251 Sub-58 3,4-diClPh -CO- Single bond -CH2-cHx-
3-252 Sub-59 3,4-diClPh -CO- Single bond -CH2-cHx-
3-253 Sub-82 3,4-diClPh -CO- Single bond -CH2-cHx-
3-254 Sub-83 3,4-diClPh -CO- Single bond -CH2-cHx-
3-255 Sub-61 3,4-diClPh -CO- Single bond -CH2-cHx-
3-256 Sub-55 3,4-diClPh -CO- Single bond -CH2-cHx-
3-257 Sub-33 4-ClPh -CO- Single bond -CH2-
3-258 Sub-34 4-ClPh -CO- Single bond -CH2-
3-259 Sub-35 4-ClPh -CO- Single bond -CH2-
3-260 Sub-36 4-ClPh -CO- Single bond -CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-261 Sub-37 4-ClPh -CO- Single bond -CH2-
3-262 Sub-38 4-ClPh -CO- Single bond -CH2-
3-263 Sub-39 4-ClPh -CO- Single bond -CH2-
3-264 Sub-40 4-ClPh -CO- Single bond -CH2-
3-265 Sub-41 4-ClPh -CO- Single bond -CH2-
3-266 Sub-42 4-ClPh -CO- Single bond -CH2-
3-267 Sub-84 4-ClPh -CO- Single bond -CH2-
3-268 Sub-43 4-ClPh -CO- Single bond -CH2-
3-269 Sub-44 4-ClPh -CO- Single bond -CH2-
3-270 Sub-45 4-ClPh -CO- Single bond -CH2-
3-271 Sub-46 4-ClPh -CO- Single bond -CH2-
3-272 Sub-47 4-ClPh -CO- Single bond -CH2-
3-273 Sub-81 4-ClPh -CO- Single bond -CH2-
3-274 Sub-48 4-ClPh -CO- Single bond -CH2-
3-275 Sub-49 4-ClPh -CO- Single bond -CH2-
3-276 Sub-50 4-ClPh -CO- Single bond -CH2-
3-277 Sub-51 4-ClPh -CO- Single bond -CH2-
3-278 Sub-52 4-ClPh -CO- Single bond -CH2-
3-279 Sub-53 4-ClPh -CO- Single bond -CH2-
3-280 Sub-54 4-ClPh -CO- Single bond -CH2-
3-281 Sub-56 4-ClPh -CO- Single bond -CH2-
3-282 Sub-57 4-ClPh -CO- Single bond -CH2-
3-283 Sub-58 4-ClPh -CO- Single bond -CH2-
3-284 Sub-59 4-ClPh -CO- Single bond -CH2-
3-285 Sub-82 4-ClPh -CO- Single bond -CH2-
3-286 Sub-83 4-ClPh -CO- Single bond -CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-287 Sub-61 4-ClPh -CO- Single bond -CH2-
3-288 Sub-55 4-ClPh -CO- Single bond -CH2-
3-289 Sub-33 4-ClPh -CO- Single bond -CH2CH2-
3-290 Sub-34 4-ClPh -CO- Single bond -CH2CH2-
3-291 Sub-35 4-ClPh -CO- Single bond -CH2CH2-
3-292 Sub-36 4-ClPh -CO- Single bond -CH2CH2-
3-293 Sub-37 4-ClPh -CO- Single bond -CH2CH2-
3-294 Sub-38 4-ClPh -CO- Single bond -CH2CH2-
3-295 Sub-39 4-ClPh -CO- Single bond -CH2CH2-
3-296 Sub-40 4-ClPh -CO- Single bond -CH2CH2-
3-297 Sub-41 4-ClPh -CO- Single bond -CH2CH2-
3-298 Sub-42 4-ClPh -CO- Single bond -CH2CH2-
3-299 Sub-84 4-ClPh -CO- Single bond -CH2CH2-
3-300 Sub-43 4-ClPh -CO- Single bond -CH2CH2-
3-301 Sub-44 4-ClPh -CO- Single bond -CH2CH2-
3-302 Sub-45 4-ClPh -CO- Single bond -CH2CH2-
3-303 Sub-46 4-ClPh -CO- Single bond -CH2CH2-
3-304 Sub-47 4-ClPh -CO- Single bond -CH2CH2-
3-305 Sub-81 4-ClPh -CO- Single bond -CH2CH2-
3-306 Sub-48 4-ClPh -CO- Single bond -CH2CH2-
3-307 Sub-49 4-ClPh -CO- Single bond -CH2CH2-
3-308 Sub-50 4-ClPh -CO- Single bond -CH2CH2-
3-309 Sub-51 4-ClPh -CO- Single bond -CH2CH2-
3-310 Sub-52 4-ClPh -CO- Single bond -CH2CH2-
3-311 Sub-53 4-ClPh -CO- Single bond -CH2CH2-
3-312 Sub-54 4-ClPh -CO- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-313 Sub-56 4-ClPh -CO- Single bond -CH2CH2-
3-314 Sub-57 4-ClPh -CO- Single bond -CH2CH2-
3-315 Sub-58 4-ClPh -CO- Single bond -CH2CH2-
3-316 Sub-59 4-ClPh -CO- Single bond -CH2CH2-
3-317 Sub-82 4-ClPh -CO- Single bond -CH2CH2-
3-318 Sub-83 4-ClPh -CO- Single bond -CH2CH2-
3-319 Sub-61 4-ClPh -CO- Single bond -CH2CH2-
3-320 Sub-55 4-ClPh -CO- Single bond -CH2CH2-
3-321 Sub-33 4-ClPh -CO- Single bond -(CH2)3-
3-322 Sub-34 4-ClPh -CO- Single bond -(CH2)3-
3-323 Sub-35 4-ClPh -CO- Single bond -(CH2)3-
3-324 Sub-36 4-ClPh -CO- Single bond -(CH2)3-
3-325 Sub-37 4-ClPh -CO- Single bond -(CH2)3-
3-326 Sub-38 4-ClPh -CO- Single bond -(CH2)3-
3-327 Sub-39 4-ClPh -CO- Single bond -(CH2)3-
3-328 Sub-40 4-ClPh -CO- Single bond -(CH2)3-
3-329 Sub-41 4-ClPh -CO- Single bond -(CH2)3-
3-330 Sub-42 4-ClPh -CO- Single bond -(CH2)3-
3-331 Sub-84 4-ClPh -CO- Single bond -(CH2)3-
3-332 Sub-43 4-ClPh -CO- Single bond -(CH2)3-
3-333 Sub-44 4-ClPh -CO- Single bond -(CH2)3-
3-334 Sub-45 4-ClPh -CO- Single bond -(CH2)3-
3-335 Sub-46 4-ClPh -CO- Single bond -(CH2)3-
3-336 Sub-47 4-ClPh -CO- Single bond -(CH2)3-
3-337 Sub-81 4-ClPh -CO- Single bond -(CH2)3-
3-338 Sub-48 4-ClPh -CO- Single bond -(CH2)3-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-339 Sub-49 4-ClPh -CO- Single bond -(CH2)3-
3-340 Sub-50 4-ClPh -CO- Single bond -(CH2)3-
3-341 Sub-51 4-ClPh -CO- Single bond -(CH2)3-
3-342 Sub-52 4-ClPh -CO- Single bond -(CH2)3-
3-343 Sub-53 4-ClPh -CO- Single bond -(CH2)3-
3-344 Sub-54 4-ClPh -CO- Single bond -(CH2)3-
3-345 Sub-56 4-ClPh -CO- Single bond -(CH2)3-
3-346 Sub-57 4-ClPh -CO- Single bond -(CH2)3-
3-347 Sub-58 4-ClPh -CO- Single bond -(CH2)3-
3-348 Sub-59 4-ClPh -CO- Single bond -(CH2)3-
3-349 Sub-82 4-ClPh -CO- Single bond -(CH2)3-
3-350 Sub-83 4-ClPh -CO- Single bond -(CH2)3-
3-351 Sub-61 4-ClPh -CO- Single bond -(CH2)3-
3-352 Sub-55 4-ClPh -CO- Single bond -(CH2)3-
3-353 Sub-33 4-ClPh -CO- Single bond -CH2C(Me)2-
3-354 Sub-34 4-ClPh -CO- Single bond -CH2C(Me)2-
3-355 Sub-35 4-ClPh -CO- Single bond -CH2C(Me)2-
3-356 Sub-36 4-ClPh -CO- Single bond -CH2C(Me)2-
3-357 Sub-37 4-ClPh -CO- Single bond -CH2C(Me)2-
3-358 Sub-38 4-ClPh -CO- Single bond -CH2C(Me)2-
3-359 Sub-39 4-ClPh -CO- Single bond -CH2C(Me)2-
3-360 Sub-40 4-ClPh -CO- Single bond -CH2C(Me)2-
3-361 Sub-41 4-ClPh -CO- Single bond -CH2C(Me)2-
3-362 Sub-42 4-ClPh -CO- Single bond -CH2C(Me)2-
3-363 Sub-84 4-ClPh -CO- Single bond -CH2C(Me)2-
3-364 Sub-43 4-ClPh -CO- Single bond -CH2C(Me)2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-365 Sub-44 4-ClPh -CO- Single bond -CH2C(Me)2-
3-366 Sub-45 4-ClPh -CO- Single bond -CH2C(Me)2-
3-367 Sub-46 4-ClPh -CO- Single bond -CH2C(Me)2-
3-368 Sub-47 4-ClPh -CO- Single bond -CH2C(Me)2-
3-369 Sub-81 4-ClPh -CO- Single bond -CH2C(Me)2-
3-370 Sub-48 4-ClPh -CO- Single bond -CH2C(Me)2-
3-371 Sub-49 4-ClPh -CO- Single bond -CH2C(Me)2-
3-372 Sub-50 4-ClPh -CO- Single bond -CH2C(Me)2-
3-373 Sub-51 4-ClPh -CO- Single bond -CH2C(Me)2-
3-374 Sub-52 4-ClPh -CO- Single bond -CH2C(Me)2-
3-375 Sub-53 4-ClPh -CO- Single bond -CH2C(Me)2-
3-376 Sub-54 4-ClPh -CO- Single bond -CH2C(Me)2-
3-377 Sub-56 4-ClPh -CO- Single bond -CH2C(Me)2-
3-378 Sub-57 4-ClPh -CO- Single bond -CH2C(Me)2-
3-379 Sub-58 4-ClPh -CO- Single bond -CH2C(Me)2-
3-380 Sub-59 4-ClPh -CO- Single bond -CH2C(Me)2-
3-381 Sub-82 4-ClPh -CO- Single bond -CH2C(Me)2-
3-382 Sub-83 4-ClPh -CO- Single bond -CH2C(Me)2-
3-383 Sub-61 4-ClPh -CO- Single bond -CH2C(Me)2-
3-384 Sub-55 4-ClPh -CO- Single bond -CH2C(Me)2-
3-385 Sub-33 4-ClPh -CO- Single bond -CH2-cPr-
3-386 Sub-34 4-ClPh -CO- Single bond -CH2-cPr-
3-387 Sub-35 4-ClPh -CO- Single bond -CH2-cPr-
3-388 Sub-36 4-ClPh -CO- Single bond -CH2-cPr-
3-389 Sub-37 4-ClPh -CO- Single bond -CH2-cPr-
3-390 Sub-38 4-ClPh -CO- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-391 Sub-39 4-ClPh -CO- Single bond -CH2-cPr-
3-392 Sub-40 4-ClPh -CO- Single bond -CH2-cPr-
3-393 Sub-41 4-ClPh -CO- Single bond -CH2-cPr-
3-394 Sub-42 4-ClPh -CO- Single bond -CH2-cPr-
3-395 Sub-84 4-ClPh -CO- Single bond -CH2-cPr-
3-396 Sub-43 4-ClPh -CO- Single bond -CH2-cPr-
3-397 Sub-44 4-ClPh -CO- Single bond -CH2-cPr-
3-398 Sub-45 4-ClPh -CO- Single bond -CH2-cPr-
3-399 Sub-46 4-ClPh -CO- Single bond -CH2-cPr-
3-400 Sub-47 4-ClPh -CO- Single bond -CH2-cPr-
3-401 Sub-81 4-ClPh -CO- Single bond -CH2-cPr-
3-402 Sub-48 4-ClPh -CO- Single bond -CH2-cPr-
3-403 Sub-49 4-ClPh -CO- Single bond -CH2-cPr-
3-404 Sub-50 4-ClPh -CO- Single bond -CH2-cPr-
3-405 Sub-51 4-ClPh -CO- Single bond -CH2-cPr-
3-406 Sub-52 4-ClPh -CO- Single bond -CH2-cPr-
3-407 Sub-53 4-ClPh -CO- Single bond -CH2-cPr-
3-408 Sub-54 4-ClPh -CO- Single bond -CH2-cPr-
3-409 Sub-56 4-ClPh -CO- Single bond -CH2-cPr-
3-410 Sub-57 4-ClPh -CO- Single bond -CH2-cPr-
3-411 Sub-58 4-ClPh -CO- Single bond -CH2-cPr-
3-412 Sub-59 4-ClPh -CO- Single bond -CH2-cPr-
3-413 Sub-82 4-ClPh -CO- Single bond -CH2-cPr-
3-414 Sub-83 4-ClPh -CO- Single bond -CH2-cPr-
3-415 Sub-61 4-ClPh -CO- Single bond -CH2-cPr-
3-416 Sub-55 4-ClPh -CO- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-417 Sub-33 4-ClPh -CO- Single bond -CH2-cBu-
3-418 Sub-34 4-ClPh -CO- Single bond -CH2-cBu-
3-419 Sub-35 4-ClPh -CO- Single bond -CH2-cBu-
3-420 Sub-36 4-ClPh -CO- Single bond -CH2-cBu-
3-421 Sub-37 4-ClPh -CO- Single bond -CH2-cBu-
3-422 Sub-38 4-ClPh -CO- Single bond -CH2-cBu-
3-423 Sub-39 4-ClPh -CO- Single bond -CH2-cBu-
3-424 Sub-40 4-ClPh -CO- Single bond -CH2-cBu-
3-425 Sub-41 4-ClPh -CO- Single bond -CH2-cBu-
3-426 Sub-42 4-ClPh -CO- Single bond -CH2-cBu-
3-427 Sub-84 4-ClPh -CO- Single bond -CH2-cBu-
3-428 Sub-43 4-ClPh -CO- Single bond -CH2-cBu-
3-429 Sub-44 4-ClPh -CO- Single bond -CH2-cBu-
3-430 Sub-45 4-ClPh -CO- Single bond -CH2-cBu-
3-431 Sub-46 4-ClPh -CO- Single bond -CH2-cBu-
3-432 Sub-47 4-ClPh -CO- Single bond -CH2-cBu-
3-433 Sub-81 4-ClPh -CO- Single bond -CH2-cBu-
3-434 Sub-48 4-ClPh -CO- Single bond -CH2-cBu-
3-435 Sub-49 4-ClPh -CO- Single bond -CH2-cBu-
3-436 Sub-50 4-ClPh -CO- Single bond -CH2-cBu-
3-437 Sub-51 4-ClPh -CO- Single bond -CH2-cBu-
3-438 Sub-52 4-ClPh -CO- Single bond -CH2-cBu-
3-439 Sub-53 4-ClPh -CO- Single bond -CH2-cBu-
3-440 Sub-54 4-ClPh -CO- Single bond -CH2-cBu-
3-441 Sub-56 4-ClPh -CO- Single bond -CH2-cBu-
3-442 Sub-57 4-ClPh -CO- Single bond -CH2-cBu-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-443 Sub-58 4-ClPh -CO- Single bond -CH2-cBu-
3-444 Sub-59 4-ClPh -CO- Single bond -CH2-cBu-
3-445 Sub-82 4-ClPh -CO- Single bond -CH2-cBu-
3-446 Sub-83 4-ClPh -CO- Single bond -CH2-cBu-
3-447 Sub-61 4-ClPh -CO- Single bond -CH2-cBu-
3-448 Sub-55 4-ClPh -CO- Single bond -CH2-cBu-
3-449 Sub-33 4-ClPh -CO- Single bond -CH2-cPn-
3-450 Sub-34 4-ClPh -CO- Single bond -CH2-cPn-
3-451 Sub-35 4-ClPh -CO- Single bond -CH2-cPn-
3-452 Sub-36 4-ClPh -CO- Single bond -CH2-cPn-
3-453 Sub-37 4-ClPh -CO- Single bond -CH2-cPn-
3-454 Sub-38 4-ClPh -CO- Single bond -CH2-cPn-
3-455 Sub-39 4-ClPh -CO- Single bond -CH2-cPn-
3-456 Sub-40 4-ClPh -CO- Single bond -CH2-cPn-
3-457 Sub-41 4-ClPh -CO- Single bond -CH2-cPn-
3-458 Sub-42 4-ClPh -CO- Single bond -CH2-cPn-
3-459 Sub-84 4-ClPh -CO- Single bond -CH2-cPn-
3-460 Sub-43 4-ClPh -CO- Single bond -CH2-cPn-
3-461 Sub-44 4-ClPh -CO- Single bond -CH2-cPn-
3-462 Sub-45 4-ClPh -CO- Single bond -CH2-cPn-
3-463 Sub-46 4-ClPh -CO- Single bond -CH2-cPn-
3-464 Sub-47 4-ClPh -CO- Single bond -CH2-cPn-
3-465 Sub-81 4-ClPh -CO- Single bond -CH2-cPn-
3-466 Sub-48 4-ClPh -CO- Single bond -CH2-cPn-
3-467 Sub-49 4-ClPh -CO- Single bond -CH2-cPn-
3-468 Sub-50 4-ClPh -CO- Single bond -CH2-cPn-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-469 Sub-51 4-ClPh -CO- Single bond -CH2-cPn-
3-470 Sub-52 4-ClPh -CO- Single bond -CH2-cPn-
3-471 Sub-53 4-ClPh -CO- Single bond -CH2-cPn-
3-472 Sub-54 4-ClPh -CO- Single bond -CH2-cPn-
3-473 Sub-56 4-ClPh -CO- Single bond -CH2-cPn-
3-474 Sub-57 4-ClPh -CO- Single bond -CH2-cPn-
3-475 Sub-58 4-ClPh -CO- Single bond -CH2-cPn-
3-476 Sub-59 4-ClPh -CO- Single bond -CH2-cPn-
3-477 Sub-82 4-ClPh -CO- Single bond -CH2-cPn-
3-478 Sub-83 4-ClPh -CO- Single bond -CH2-cPn-
3-479 Sub-61 4-ClPh -CO- Single bond -CH2-cPn-
3-480 Sub-55 4-ClPh -CO- Single bond -CH2-cPn-
3-481 Sub-33 4-ClPh -CO- Single bond -CH2-cHx-
3-482 Sub-34 4-ClPh -CO- Single bond -CH2-cHx-
3-483 Sub-35 4-ClPh -CO- Single bond -CH2-cHx-
3-484 Sub-36 4-ClPh -CO- Single bond -CH2-cHx-
3-485 Sub-37 4-ClPh -CO- Single bond -CH2-cHx-
3-486 Sub-38 4-ClPh -CO- Single bond -CH2-cHx-
3-487 Sub-39 4-ClPh -CO- Single bond -CH2-cHx-
3-488 Sub-40 4-ClPh -CO- Single bond -CH2-cHx-
3-489 Sub-41 4-ClPh -CO- Single bond -CH2-cHx-
3-490 Sub-42 4-ClPh -CO- Single bond -CH2-cHx-
3-491 Sub-84 4-ClPh -CO- Single bond -CH2-cHx-
3-492 Sub-43 4-ClPh -CO- Single bond -CH2-cHx-
3-493 Sub-44 4-ClPh -CO- Single bond -CH2-cHx-
3-494 Sub-45 4-ClPh -CO- Single bond -CH2-cHx-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-495 Sub-46 4-ClPh -CO- Single bond -CH2-cHx-
3-496 Sub-47 4-ClPh -CO- Single bond -CH2-cHx-
3-497 Sub-81 4-ClPh -CO- Single bond -CH2-cHx-
3-498 Sub-48 4-ClPh -CO- Single bond -CH2-cHx-
3-499 Sub-49 4-ClPh -CO- Single bond -CH2-cHx-
3-500 Sub-50 4-ClPh -CO- Single bond -CH2-cHx-
3-501 Sub-51 4-ClPh -CO- Single bond -CH2-cHx-
3-502 Sub-52 4-ClPh -CO- Single bond -CH2-cHx-
3-503 Sub-53 4-ClPh -CO- Single bond -CH2-cHx-
3-504 Sub-54 4-ClPh -CO- Single bond -CH2-cHx-
3-505 Sub-56 4-ClPh -CO- Single bond -CH2-cHx-
3-506 Sub-57 4-ClPh -CO- Single bond -CH2-cHx-
3-507 Sub-58 4-ClPh -CO- Single bond -CH2-cHx-
3-508 Sub-59 4-ClPh -CO- Single bond -CH2-cHx-
3-509 Sub-82 4-ClPh -CO- Single bond -CH2-cHx-
3-510 Sub-83 4-ClPh -CO- Single bond -CH2-cHx-
3-511 Sub-61 4-ClPh -CO- Single bond -CH2-cHx-
3-512 Sub-55 4-ClPh -CO- Single bond -CH2-cHx-
3-513 Sub-33 4-FPh -CO- Single bond -CH2-
3-514 Sub-34 4-FPh -CO- Single bond -CH2-
3-515 Sub-35 4-FPh -CO- Single bond -CH2-
3-516 Sub-36 4-FPh -CO- Single bond -CH2-
3-517 Sub-37 4-FPh -CO- Single bond -CH2-
3-518 Sub-38 4-FPh -CO- Single bond -CH2-
3-519 Sub-39 4-FPh -CO- Single bond -CH2-
3-520 Sub-40 4-FPh -CO- Single bond -CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-521 Sub-41 4-FPh -CO- Single bond -CH2-
3-522 Sub-42 4-FPh -CO- Single bond -CH2-
3-523 Sub-84 4-FPh -CO- Single bond -CH2-
3-524 Sub-43 4-FPh -CO- Single bond -CH2-
3-525 Sub-44 4-FPh -CO- Single bond -CH2-
3-526 Sub-45 4-FPh -CO- Single bond -CH2-
3-527 SuB-46 4-FPh -CO- Single bond -CH2-
3-528 Sub-47 4-FPh -CO- Single bond -CH2-
3-529 Sub-81 4-FPh -CO- Single bond -CH2-
3-530 Sub-48 4-FPh -CO- Single bond -CH2-
3-531 Sub-49 4-FPh -CO- Single bond -CH2-
3-532 Sub-50 4-FPh -CO- Single bond -CH2-
3-533 Sub-51 4-FPh -CO- Single bond -CH2-
3-534 Sub-52 4-FPh -CO- Single bond -CH2-
3-535 Sub-53 4-FPh -CO- Single bond -CH2-
3-536 Sub-54 4-FPh -CO- Single bond -CH2-
3-537 Sub-56 4-FPh -CO- Single bond -CH2-
3-538 Sub-57 4-FPh -CO- Single bond -CH2-
3-539 Sub-58 4-FPh -CO- Single bond -CH2-
3-540 Sub-59 4-FPh -CO- Single bond -CH2-
3-541 Sub-82 4-FPh -CO- Single bond -CH2-
3-542 Sub-83 4-FPh -CO- Single bond -CH2-
3-543 Sub-61 4-FPh -CO- Single bond -CH2-
3-544 Sub-55 4-FPh -CO- Single bond -CH2-
3-545 Sub-33 4-FPh -CO- Single bond -CH2CH2-
3-546 Sub-34 4-FPh -CO- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-547 Sub-35 4-FPh -CO- Single bond -CH2CH2-
3-548 Sub-36 4-FPh -CO- Single bond -CH2CH2-
3-549 Sub-37 4-FPh -CO- Single bond -CH2CH2-
3-550 Sub-38 4-FPh -CO- Single bond -CH2CH2-
3-551 Sub-39 4-FPh -CO- Single bond -CH2CH2-
3-552 Sub-40 4-FPh -CO- Single bond -CH2CH2-
3-553 Sub-41 4-FPh -CO- Single bond -CH2CH2-
3-554 Sub-42 4-FPh -CO- Single bond -CH2CH2-
3-555 Sub-84 4-FPh -CO- Single bond -CH2CH2-
3-556 Sub-43 4-FPh -CO- Single bond -CH2CH2-
3-557 Sub-44 4-FPh -CO- Single bond -CH2CH2-
3-558 Sub-45 4-FPh -CO- Single bond -CH2CH2-
3-559 Sub-46 4-FPh -CO- Single bond -CH2CH2-
3-560 Sub-47 4-FPh -CO- Single bond -CH2CH2-
3-561 Sub-81 4-FPh -CO- Single bond -CH2CH2-
3-562 Sub-48 4-FPh -CO- Single bond -CH2CH2-
3-563 Sub-49 4-FPh -CO- Single bond -CH2CH2-
3-564 Sub-50 4-FPh -CO- Single bond -CH2CH2-
3-565 Sub-51 4-FPh -CO- Single bond -CH2CH2-
3-566 Sub-52 4-FPh -CO- Single bond -CH2CH2-
3-567 Sub-53 4-FPh -CO- Single bond -CH2CH2-
3-568 Sub-54 4-FPh -CO- Single bond -CH2CH2-
3-569 Sub-56 4-FPh -CO- Single bond -CH2CH2-
3-570 Sub-57 4-FPh -CO- Single bond -CH2CH2-
3-571 Sub-58 4-FPh -CO- Single bond -CH2CH2-
3-572 Sub-59 4-FPh -CO- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-573 Sub-82 4-FPh -CO- Single bond -CH2CH2-
3-574 Sub-83 4-FPh -CO- Single bond -CH2CH2-
3-575 Sub-61 4-FPh -CO- Single bond -CH2CH2-
3-576 Sub-55 4-FPh -CO- Single bond -CH2CH2-
3-577 Sub-33 4-FPh -CO- Single bond -(CH2)3-
3-578 Sub-34 4-FPh -CO- Single bond -(CH2)3-
3-579 Sub-35 4-FPh -CO- Single bond -(CH2)3-
3-580 Sub-36 4-FPh -CO- Single bond -(CH2)3-
3-581 Sub-37 4-FPh -CO- Single bond -(CH2)3-
3-582 Sub-38 4-FPh -CO- Single bond -(CH2)3-
3-583 Sub-39 4-FPh -CO- Single bond -(CH2)3-
3-584 Sub-40 4-FPh -CO- Single bond -(CH2)3-
3-585 Sub-41 4-FPh -CO- Single bond -(CH2)3-
3-586 Sub-42 4-FPh -CO- Single bond -(CH2)3-
3-587 Sub-84 4-FPh -CO- Single bond -(CH2)3-
3-588 Sub-43 4-FPh -CO- Single bond -(CH2)3-
3-589 Sub-44 4-FPh -CO- Single bond -(CH2)3-
3-590 Sub-45 4-FPh -CO- Single bond -(CH2)3-
3-591 Sub-46 4-FPh -CO- Single bond -(CH2)3-
3-592 Sub-47 4-FPh -CO- Single bond -(CH2)3-
3-593 Sub-81 4-FPh -CO- Single bond -(CH2)3-
3-594 Sub-48 4-FPh -CO- Single bond -(CH2)3-
3-595 Sub-49 4-FPh -CO- Single bond -(CH2)3-
3-596 Sub-50 4-FPh -CO- Single bond -(CH2)3-
3-597 Sub-51 4-FPh -CO- Single bond -(CH2)3-
3-598 Sub-52 4-FPh -CO- Single bond -(CH2)3-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-599 Sub-53 4-FPh -CO- Single bond -(CH2)3-
3-600 Sub-54 4-FPh -CO- Single bond -(CH2)3-
3-601 Sub-56 4-FPh -CO- Single bond -(CH2)3-
3-602 Sub-57 4-FPh -CO- Single bond -(CH2)3-
3-603 Sub-58 4-FPh -CO- Single bond -(CH2)3-
3-604 Sub-59 4-FPh -CO- Single bond -(CH2)3-
3-605 Sub-82 4-FPh -CO- Single bond -(CH2)3-
3-606 Sub-83 4-FPh -CO- Single bond -(CH2)3-
3-607 Sub-61 4-FPh -CO- Single bond -(CH2)3-
3-608 Sub-55 4-FPh -CO- Single bond -(CH2)3-
3-609 Sub-33 4-FPh -CO- Single bond -CH2C(Me)2-
3-610 Sub-34 4-FPh -CO- Single bond -CH2C(Me)2-
3-611 Sub-35 4-FPh -CO- Single bond -CH2C(Me)2-
3-612 Sub-36 4-FPh -CO- Single bond -CH2C(Me)2-
3-613 Sub-37 4-FPh -CO- Single bond -CH2C(Me)2-
3-614 Sub-38 4-FPh -CO- Single bond -CH2C(Me)2-
3-615 Sub-39 4-FPh -CO- Single bond -CH2C(Me)2-
3-616 Sub-40 4-FPh -CO- Single bond -CH2C(Me)2-
3-617 Sub-41 4-FPh -CO- Single bond -CH2C(Me)2-
3-618 Sub-42 4-FPh -CO- Single bond -CH2C(Me)2-
3-619 Sub-84 4-FPh -CO- Single bond -CH2C(Me)2-
3-620 Sub-43 4-FPh -CO- Single bond -CH2C(Me)2-
3-621 Sub-44 4-FPh -CO- Single bond -CH2C(Me)2-
3-622 Sub-45 4-FPh -CO- Single bond -CH2C(Me)2-
3-623 Sub-46 4-FPh -CO- Single bond -CH2C(Me)2-
3-624 Sub-47 4-FPh -CO- Single bond -CH2C(Me)2-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-625 Sub-81 4-FPh -CO- Single bond -CH2C(Me)2-
3-626 Sub-48 4-FPh -CO- Single bond -CH2C(Me)2-
3-627 Sub-49 4-FPh -CO- Single bond -CH2C(Me)2-
3-628 Sub-50 4-FPh -CO- Single bond -CH2C(Me)2-
3-629 Sub-51 4-FPh -CO- Single bond -CH2C(Me)2-
3-630 Sub-52 4-FPh -CO- Single bond -CH2C(Me)2-
3-631 Sub-53 4-FPh -CO- Single bond -CH2C(Me)2-
3-632 Sub-54 4-FPh -CO- Single bond -CH2C(Me)2-
3-633 Sub-56 4-FPh -CO- Single bond -CH2C(Me)2-
3-634 Sub-57 4-FPh -CO- Single bond -CH2C(Me)2-
3-635 Sub-58 4-FPh -CO- Single bond -CH2C(Me)2-
3-636 Sub-59 4-FPh -CO- Single bond -CH2C(Me)2-
3-637 Sub-82 4-FPh -CO- Single bond -CH2C(Me)2-
3-638 Sub-83 4-FPh -CO- Single bond -CH2C(Me)2-
3-639 Sub-61 4-FPh -CO- Single bond -CH2C(Me)2-
3-640 Sub-55 4-FPh -CO- Single bond -CH2C(Me)2-
3-641 Sub-33 4-FPh -CO- Single bond -CH2-cPr-
3-642 Sub-34 4-FPh -CO- Single bond -CH2-cPr-
3-643 Sub-35 4-FPh -CO- Single bond -CH2-cPr-
3-644 Sub-36 4-FPh -CO- Single bond -CH2-cPr-
3-645 Sub-37 4-FPh -CO- Single bond -CH2-cPr-
3-646 Sub-38 4-FPh -CO- Single bond -CH2-cPr-
3-647 Sub-39 4-FPh -CO- Single bond -CH2-cPr-
3-648 Sub-40 4-FPh -CO- Single bond -CH2-cPr-
3-649 Sub-41 4-FPh -CO- Single bond -CH2-cPr-
3-650 Sub-42 4-FPh -CO- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) Serial number R1 R2 A B E
3-651 Sub-84 4-FPh -CO- Single bond -CH2-cPr-
3-652 Sub-43 4-FPh -CO- Single bond -CH2-cPr-
3-653 Sub-44 4-FPh -CO- Single bond -CH2-cPr-
3-654 Sub-45 4-FPh -CO- Single bond -CH2-cPr-
3-655 Sub-46 4-FPh -CO- Single bond -CH2-cPr-
3-656 Sub-47 4-FPh -CO- Single bond -CH2-cPr-
3-657 Sub-81 4-FPh -CO- Single bond -CH2-cPr-
3-658 Sub-48 4-FPh -CO- Single bond -CH2-cPr-
3-659 Sub-49 4-FPh -CO- Single bond -CH2-cPr-
3-660 Sub-50 4-FPh -CO- Single bond -CH2-cPr-
3-661 Sub-51 4-FPh -CO- Single bond -CH2-cPr-
3-662 Sub-52 4-FPh -CO- Single bond -CH2-cPr-
3-663 Sub-53 4-FPh -CO- Single bond -CH2-cPr-
3-664 Sub-54 4-FPh -CO- Single bond -CH2-cPr-
3-665 Sub-56 4-FPh -CO- Single bond -CH2-cPr-
3-666 Sub-57 4-FPh -CO- Single bond -CH2-cPr-
3-667 Sub-58 4-FPh -CO- Single bond -CH2-cPr-
3-668 Sub-59 4-FPh -CO- Single bond -CH2-cPr-
3-669 Sub-82 4-FPh -CO- Single bond -CH2-cPr-
3-670 Sub-83 4-FPh -CO- Single bond -CH2-cPr-
3-671 Sub-61 4-FPh -CO- Single bond -CH2-cPr-
3-672 Sub-55 4-FPh -CO- Single bond -CH2-cPr-
3-673 Sub-33 4-FPh -CO- Single bond -CH2-cBu-
3-674 Sub-34 4-FPh -CO- Single bond -CH2-cBu-
3-675 Sub-35 4-FPh -CO- Single bond -CH2-cBu-
3-676 Sub-36 4-FPh -CO- Single bond -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-677 Sub-37 4-FPh -CO- Single bond -CH2-cBu-
3-678 Sub-38 4-FPh -CO- Single bond -CH2-cBu-
3-679 Sub-39 4-FPh -CO- Single bond -CH2-cBu-
3-680 Sub-40 4-FPh -CO- Single bond -CH2-cBu-
3-681 Sub-41 4-FPh -CO- Single bond -CH2-cBu-
3-682 Sub-42 4-FPh -CO- Single bond -CH2-cBu-
3-683 Sub-84 4-FPh -CO- Single bond -CH2-cBu-
3-684 Sub-43 4-FPh -CO- Single bond -CH2-cBu-
3-685 Sub-44 4-FPh -CO- Single bond -CH2-cBu-
3-686 Sub-45 4-FPh -CO- Single bond -CH2-cBu-
3-687 Sub-46 4-FPh -CO- Single bond -CH2-cBu-
3-688 Sub-47 4-FPh -CO- Single bond -CH2-cBu-
3-689 Sub-81 4-FPh -CO- Single bond -CH2-cBu-
3-690 Sub-48 4-FPh -CO- Single bond -CH2-cBu-
3-691 Sub-49 4-FPh -CO- Single bond -CH2-cBu-
3-692 Sub-50 4-FPh -CO- Single bond -CH2-cBu-
3-693 Sub-51 4-FPh -CO- Single bond -CH2-cBu-
3-694 Sub-52 4-FPh -CO- Single bond -CH2-cBu-
3-695 Sub-53 4-FPh -CO- Single bond -CH2-cBu-
3-696 Sub-54 4-FPh -CO- Single bond -CH2-cBu-
3-697 Sub-56 4-FPh -CO- Single bond -CH2-cBu-
3-698 Sub-57 4-FPh -CO- Single bond -CH2-cBu-
3-699 Sub-58 4-FPh -CO- Single bond -CH2-cBu-
3-700 Sub-59 4-FPh -CO- Single bond -CH2-cBu-
3-701 Sub-82 4-FPh -CO- Single bond -CH2-cBu-
3-702 Sub-83 4-FPh -CO- Single bond -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-703 Sub-61 4-FPh -CO- Single bond -CH2-cBu-
3-704 Sub-55 4-FPh -CO- Single bond -CH2-cBu-
3-705 Sub-33 4-FPh -CO- Single bond -CH2-cPn-
3-706 Sub-34 4-FPh -CO- Single bond -CH2-cPn-
3-707 Sub-35 4-FPh -CO- Single bond -CH2-cPn-
3-708 Sub-36 4-FPh -CO- Single bond -CH2-cPn-
3-709 Sub-37 4-FPh -CO- Single bond -CH2-cPn-
3-710 Sub-38 4-FPh -CO- Single bond -CH2-cPn-
3-711 Sub-39 4-FPh -CO- Single bond -CH2-cPn-
3-712 Sub-40 4-FPh -CO- Single bond -CH2-cPn-
3-713 Sub-41 4-FPh -CO- Single bond -CH2-cPn-
3-714 Sub-42 4-FPh -CO- Single bond -CH2-cPn-
3-715 Sub-84 4-FPh -CO- Single bond -CH2-cPn-
3-716 Sub-43 4-FPh -CO- Single bond -CH2-cPn-
3-717 Sub-44 4-FPh -CO- Single bond -CH2-cPn-
3-718 Sub-45 4-FPh -CO- Single bond -CH2-cPn-
3-719 Sub-46 4-FPh -CO- Single bond -CH2-cPn-
3-720 Sub-47 4-FPh -CO- Single bond -CH2-cPn-
3-721 Sub-81 4-FPh -CO- Single bond -CH2-cPn-
3-722 Sub-48 4-FPh -CO- Single bond -CH2-cPn-
3-723 Sub-49 4-FPh -CO- Single bond -CH2-cPn-
3-724 Sub-50 4-FPh -CO- Single bond -CH2-cPn-
3-725 Sub-51 4-FPh -CO- Single bond -CH2-cPn-
3-726 Sub-52 4-FPh -CO- Single bond -CH2-cPn-
3-727 Sub-53 4-FPh -CO- Single bond -CH2-cPn-
3-728 Sub-54 4-FPh -CO- Single bond -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-729 Sub-56 4-FPh -CO- Single bond -CH2-cPn-
3-730 Sub-57 4-FPh -CO- Single bond -CH2-cPn-
3-731 Sub-58 4-FPh -CO- Single bond -CH2-cPn-
3-732 Sub-59 4-FPh -CO- Single bond -CH2-cPn-
3-733 Sub-82 4-FPh -CO- Single bond -CH2-cPn-
3-734 Sub-83 4-FPh -CO- Single bond -CH2-cPn-
3-735 Sub-61 4-FPh -CO- Single bond -CH2-cPn-
3-736 Sub-55 4-FPh -CO- Single bond -CH2-cPn-
3-737 Sub-33 4-FPh -CO- Single bond -CH2-cHx-
3-738 Sub-34 4-FPh -CO- Single bond -CH2-cHx-
3-739 Sub-35 4-FPh -CO- Single bond -CH2-cHx-
3-740 Sub-36 4-FPh -CO- Single bond -CH2-cHx-
3-741 Sub-37 4-FPh -CO- Single bond -CH2-cHx-
3-742 Sub-38 4-FPh -CO- Single bond -CH2-cHx-
3-743 Sub-39 4-FPh -CO- Single bond -CH2-cHx-
3-744 Sub-40 4-FPh -CO- Single bond -CH2-cHx-
3-745 Sub-41 4-FPh -CO- Single bond -CH2-cHx-
3-746 Sub-42 4-FPh -CO- Single bond -CH2-cHx-
3-747 Sub-84 4-FPh -CO- Single bond -CH2-cHx-
3-748 Sub-43 4-FPh -CO- Single bond -CH2-cHx-
3-749 Sub-44 4-FPh -CO- Single bond -CH2-cHx-
3-750 Sub-45 4-FPh -CO- Single bond -CH2-cHx-
3-751 Sub-46 4-FPh -CO- Single bond -CH2-cHx-
3-752 Sub-47 4-FPh -CO- Single bond -CH2-cHx-
3-753 Sub-81 4-FPh -CO- Single bond -CH2-cHx-
3-754 Sub-48 4-FPh -CO- Single bond -CH2-cHx-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-755 Sub-49 4-FPh -CO- Single bond -CH2-cHx-
3-756 Sub-50 4-FPh -CO- Single bond -CH2-cHx-
3-757 Sub-51 4-FPh -CO- Single bond -CH2-cHx-
3-758 Sub-52 4-FPh -CO- Single bond -CH2-cHx-
3-759 Sub-53 4-FPh -CO- Single bond -CH2-cHx-
3-760 Sub-54 4-FPh -CO- Single bond -CH2-cHx-
3-761 Sub-56 4-FPh -CO- Single bond -CH2-cHx-
3-762 Sub-57 4-FPh -CO- Single bond -CH2-cHx-
3-763 Sub-58 4-FPh -CO- Single bond -CH2-cHx-
3-764 Sub-59 4-FPh -CO- Single bond -CH2-cHx-
3-765 Sub-82 4-FPh -CO- Single bond -CH2-cHx-
3-766 Sub-83 4-FPh -CO- Single bond -CH2-cHx-
3-767 Sub-61 4-FPh -CO- Single bond -CH2-cHx-
3-768 Sub-55 4-FPh -CO- Single bond -CH2-cHx-
3-769 Sub-33 3,4-diClPh -CO- -CH2- -CH2-
3-770 Sub-34 3,4-diClPh -CO- -CH2- -CH2-
3-771 Sub-35 3,4-dClPh -CO- -CH2- -CH2-
3-772 Sub-36 3,4-diClPh -CO- -CH2- -CH2-
3-773 Sub-37 3,4-diClPh -CO- -CH2- -CH2-
3-774 Sub-38 3,4-diClPh -CO- -CH2- -CH2-
3-775 Sub-39 3-4-diClPh -CO- -CH2- -CH2-
3-776 Sub-40 3,4-diClPh -CO- -CH2- -CH2-
3-777 Sub-41 3,4-diClPh -CO- -CH2- -CH2-
3-778 Sub-42 3,4-diClPh -CO- -CH2- -CH2-
3-779 Sub-84 3,4-diClPh -CO- -CH2- -CH2-
3-780 Sub-43 3,4-diClPh -CO- -CH2- -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-781 Sub-44 3,4-diClPh -CO- -CH2- -CH2-
3-782 Sub-45 3,4-diClPh -CO- -CH2- -CH2-
3-783 Sub-46 3,4-diClPh -CO- -CH2- -CH2-
3-784 Sub-47 3,4-diClPh -CO- -CH2- -CH2-
3-785 Sub-81 3,4-diClPh -CO- -CH2- -CH2-
3-786 Sub-48 3,4-diClPh -CO- -CH2- -CH2-
3-787 Sub-49 3,4-diClPh -CO- -CH2- -CH2-
3-788 Sub-50 3,4-diClPh -CO- -CH2- -CH2-
3-789 Sub-51 3,4-diClPh -CO- -CH2- -CH2-
3-790 Sub-52 3,4-diClPh -CO- -CH2- -CH2-
3-791 Sub-53 3,4-diClPh -CO- -CH2- -CH2-
3-792 Sub-54 3,4-diCPh -CO- -CH2- -CH2-
3-793 Sub-56 3,4-diClPh -CO- -CH2- -CH2-
3-794 Sub-57 3,4-diClPh -CO- -CH2- -CH2-
3-795 Sub-58 3,4-diClPh -CO- -CH2- -CH2-
3-796 Sub-59 3,4-diClPh -CO- -CH2- -CH2-
3-797 Sub-82 3,4-diClPh -CO- -CH2- -CH2-
3-798 Sub-83 3,4-diClPh -CO- -CH2- -CH2-
3-799 Sub-61 3,4-diClPh -CO- -CH2- -CH2-
3-800 Sub-55 3,4-diClPh -CO- -CH2- -CH2-
3-801 Sub-33 3,4-diClPh -CO- -CH2- -CH2CH2-
3-802 Sub-34 3,4-diClPh -CO- -CH2- -CH2CH2-
3-803 Sub-35 3,4-diClPh -CO- -CH2- -CH2CH2-
3-804 Sub-36 3,4-diCHph -CO- -CH2- -CH2CH2-
3-805 Sub-37 3,4-diClPh -CO- -CH2- -CH2CH2-
3-806 Sub-38 3,4-diClPh -CO- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-807 Sub-39 3,4-diClPh -CO- -CH2- -CH2CH2-
3-808 Sub-40 3,4-diClPh -CO- -CH2- -CH2CH2-
3-809 Sub-41 3,4-diClPh -CO- -CH2- -CH2CH2-
3-810 Sub-42 3,4-diClPh -CO- -CH2- -CH2CH2-
3-811 Sub-84 3,4-diClPh -CO- -CH2- -CH2CH2-
3-812 Sub-43 3,4-diClPh -CO- -CH2- -CH2CH2-
3-813 Sub-44 3,4-diClPh -CO- -CH2- -CH2CH2-
3-814 Sub-45 3,4-diClPh -CO- -CH2- -CH2CH2-
3-815 Sub-46 3,4-diClPh -CO- -CH2- -CH2CH2-
3-816 Sub-47 3,4-diClPh -CO- -CH2- -CH2CH2-
3-817 Sub-81 3,4-diClPh -CO- -CH2- -CH2CH2-
3-818 Sub-48 3,4-diClPh -CO- -CH2- -CH2CH2-
3-819 Sub-49 3,4-diClPh -CO- -CH2- -CH2CH2-
3-820 Sub-50 3,4-diClPh -CO- -CH2- -CH2CH2-
3-821 Sub-51 3,4-diClPh -CO- -CH2- -CH2CH2-
3-822 Sub-52 3,4-diClPh -CO- -CH2- -CH2CH2-
3-823 Sub-53 3,4-diClPh -CO- -CH2- -CH2CH2-
3-824 Sub-54 3,4-diClPh -CO- -CH2- -CH2CH2-
3-825 Sub-56 3,4-diClPh -CO- -CH2- -CH2CH2-
3-826 Sub-57 3,4-diClPh -CO- -CH2- -CH2CH2-
3-827 Sub-58 3,4-diClPh -CO- -CH2- -CH2CH2-
3-828 Sub-59 3,4-diClPh -CO- -CH2- -CH2CH2-
3-829 Sub-82 3,4-diClPh -CO- -CH2- -CH2CH2-
3-830 Sub-83 3,4-diClPh -CO- -CH2- -CH2CH2-
3-831 Sub-61 3,4-diClPh -CO- -CH2- -CH2CH2-
3-832 Sub-55 3,4-diClPh -CO- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-833 Sub-33 3,4-diClPh -CO- -CH2- -(CH2)3-
3-834 Sub-34 3,4-diClPh -CO- -CH2- -(CH2)3-
3-835 Sub-35 3,4-diClPh -CO- -CH2- -(CH2)3-
3-836 Sub-36 3,4-diClPh -CO- -CH2- -(CH2)3-
3-837 Sub-37 3,4-diClPh -CO- -CH2- -(CH2)3-
3-838 Sub-38 3,4-diClPh -CO- -CH2- -(CH2)3-
3-839 Sub-39 3,4-diClPh -CO- -CH2- -(CH2)3-
3-840 Sub-40 3,4-diClPh -CO- -CH2- -(CH2)3-
3-841 Sub-41 3,4-diClPh -CO- -CH2- -(CH2)3-
3-842 Sub-42 3,4-diClPh -CO- -CH2- -(CH2)3-
3-843 Sub-84 3,4-diClPh -CO- -CH2- -(CH2)3-
3-844 Sub-43 3,4-diClPh -CO- -CH2- -(CH2)3-
3-845 Sub-44 3,4-diClPh -CO- -CH2- -(CH2)3-
3-846 Sub-45 3,4-diClPh -CO- -CH2- -(CH2)3-
3-847 Sub-46 3,4-diClPh -CO- -CH2- -(CH2)3-
3-848 Sub-47 3,4-diClPh -CO- -CH2- -(CH2)3-
3-849 Sub-81 3,4-diClPh -CO- -CH2- -(CH2)3-
3-850 Sub-48 3,4-diClPh -CO- -CH2- -(CH2)3-
3-851 Sub-49 3,4-diClPh -CO- -CH2- -(CH2)3-
3-852 Sub-50 3,4-diClPh -CO- -CH2- -(CH2)3-
3-853 Sub-51 3,4-diClPh -CO- -CH2- -(CH2)3-
3-854 Sub-52 3,4-diClPh -CO- -CH2- -(CH2)3-
3-855 Sub-53 3,4-diClPh -CO- -CH2- -(CH2)3-
3-856 Sub-54 3,4-diClPh -CO- -CH2- -(CH2)3-
3-857 Sub-56 3,4-diClPh -CO- -CH2- -(CH2)3-
3-858 Sub-57 3,4-diClPh -CO- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-859 Sub-58 3,4-diClPh -CO- -CH2- -(CH2)3-
3-860 Sub-59 3,4-diClPh -CO- -CH2- -(CH2)3-
3-861 Sub-82 3,4-diClPh -CO- -CH2- -(CH2)3-
3-862 Sub-83 3,4-diClPh -CO- -CH2- -(CH2)3-
3-863 Sub-61 3,4-diClPh -CO- -CH2- -(CH2)3-
3-864 Sub-55 3,4-diClPh -CO- -CH2- -(CH2)3-
3-865 Sub-33 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-866 Sub-34 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-867 Sub-35 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-868 Sub-36 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-869 Sub-37 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-870 Sub-38 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-871 Sub-39 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-872 Sub-40 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-873 Sub-41 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-874 Sub-42 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-875 Sub-84 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-876 Sub-43 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-877 Sub-44 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-878 Sub-45 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-879 Sub-46 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-880 Sub-47 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-881 Sub-81 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-882 Sub-48 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-883 Sub-49 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-884 Sub-50 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
TABLE 3 (cont)
Compound (I) A serial number. R1 R2 A B E
3-885 Sub-51 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-886 Sub-52 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-887 Sub-53 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-888 Sub-54 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-889 Sub-56 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-890 Sub-57 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-891 Sub-58 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-892 Sub-59 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-893 Sub-82 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-894 Sub-83 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-895 Sub-61 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-896 Sub-55 3,4-diClPh -CO- -CH2- -CH2C(Me)2-
3-897 Sub-33 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-898 Sub-34 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-899 Sub-35 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-900 Sub-36 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-901 Sub-37 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-902 Sub-38 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-903 Sub-39 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-904 Sub-40 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-905 Sub-41 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-906 Sub-42 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-907 Sub-84 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-908 Sub-43 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-909 Sub-44 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-910 Sub-45 3,4-diClPh -CO- -CH2- -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-911 Sub-46 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-912 Sub-47 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-913 Sub-81 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-914 Sub-48 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-915 Sub-49 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-916 Sub-50 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-917 Sub-51 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-918 Sub-52 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-919 Sub-53 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-920 Sub-54 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-921 Sub-56 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-922 Sub-57 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-923 Sub-58 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-924 Sub-59 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-925 Sub-82 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-926 Sub-83 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-927 Sub-61 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-928 Sub-55 3,4-diClPh -CO- -CH2- -CH2-cPr-
3-929 Sub-33 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-930 Sub-34 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-931 Sub-35 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-932 Sub-36 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-933 Sub-37 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-934 Sub-38 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-935 Sub-39 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-936 Sub-40 3,4-diClPh -CO- -CH2- -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-937 Sub-41 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-938 Sub-42 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-939 Sub-84 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-940 Sub-43 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-941 Sub-44 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-942 Sub-45 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-943 Sub-46 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-944 Sub-47 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-945 Sub-81 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-946 Sub-48 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-947 Sub-49 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-948 Sub-50 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-949 Sub-51 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-950 Sub-52 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-951 Sub-53 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-952 Sub-54 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-953 Sub-56 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-954 Sub-57 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-955 Sub-58 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-956 Sub-59 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-957 Sub-82 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-958 Sub-83 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-959 Sub-61 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-960 Sub-55 3,4-diClPh -CO- -CH2- -CH2-cBu-
3-961 Sub-33 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-962 Sub-34 3,4-diClPh -CO- -CH2- -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-963 Sub-35 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-964 Sub-36 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-965 Sub-37 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-966 Sub-38 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-967 Sub-39 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-968 Sub-40 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-969 Sub-41 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-970 Sub-42 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-971 Sub-84 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-972 Sub-43 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-973 Sub-44 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-974 Sub-45 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-975 Sub-46 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-976 Sub-47 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-977 Sub-81 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-978 Sub-48 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-979 Sub-49 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-980 Sub-50 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-981 Sub-51 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-982 Sub-52 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-983 Sub-53 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-984 Sub-54 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-985 Sub-56 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-986 Sub-57 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-987 Sub-58 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-988 Sub-59 3,4-diClPh -CO- -CH2- -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-989 Sub-82 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-990 Sub-83 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-991 Sub-61 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-992 Sub-55 3,4-diClPh -CO- -CH2- -CH2-cPn-
3-993 Sub-33 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-994 Sub-34 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-995 Sub-35 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-996 Sub-36 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-997 Sub-37 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-998 Sub-38 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-999 Sub-39 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1000 Sub-40 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1001 Sub-41 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1002 Sub-42 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1003 Sub-84 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1004 Sub-43 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1005 Sub-44 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1006 Sub-45 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1007 Sub-46 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1008 Sub-47 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1009 Sub-81 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1010 Sub-48 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1011 Sub-49 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1012 Sub-50 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1013 Sub-51 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1014 Sub-52 3,4-diClPh -CO- -CH2- -CH2-cHx-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1015 Sub-53 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1016 Sub-54 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1017 Sub-56 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1018 Sub-57 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1019 Sub-58 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1020 Sub-59 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1021 Sub-82 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1022 Sub-83 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1023 Sub-61 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1024 Sub-55 3,4-diClPh -CO- -CH2- -CH2-cHx-
3-1025 Sub-33 4-ClPh -CO- -CH2- -CH2-
3-1026 Sub-34 4-ClPh -CO- -CH2- -CH2-
3-1027 Sub-35 4-ClPh -CO- -CH2- -CH2-
3-1028 Sub-36 4-ClPh -CO- -CH2- -CH2-
3-1029 Sub-37 4-ClPh -CO- -CH2- -CH2-
3-1030 Sub-38 4-ClPh -CO- -CH2- -CH2-
3-1031 Sub-39 4-ClPh -CO- -CH2- -CH2-
3-1032 Sub-40 4-ClPh -CO- -CH2- -CH2-
3-1033 Sub-41 4-ClPh -CO- -CH2- -CH2-
3-1034 Sub-42 4-ClPh -CO- -CH2- -CH2-
3-1035 Sub-84 4-ClPh -CO- -CH2- -CH2-
3-1036 Sub-43 4-ClPh -CO- -CH2- -CH2-
3-1037 Sub-44 4-ClPh -CO- -CH2- -CH2-
3-1038 Sub-45 4-ClPh -CO- -CH2- -CH2-
3-1039 Sub-46 4-ClPh -CO- -CH2- -CH2-
3-1040 Sub-47 4-ClPh -CO- -CH2- -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1041 Sub-81 4-ClPh -CO- -CH2- -CH2-
3-1042 Sub-48 4-ClPh -CO- -CH2- -CH2-
3-1043 Sub-49 4-ClPh -CO- -CH2- -CH2-
3-1044 Sub-50 4-ClPh -CO- -CH2- -CH2-
3-1045 Sub-51 4-ClPh -CO- -CH2- -CH2-
3-1046 Sub-52 4-ClPh -CO- -CH2- -CH2-
3-1047 Sub-53 4-ClPh -CO- -CH2- -CH2-
3-1048 Sub-54 4-ClPh -CO- -CH2- -CH2-
3-1049 Sub-56 4-ClPh -CO- -CH2- -CH2-
3-1050 Sub-57 4-ClPh -CO- -CH2- -CH2-
3-1051 Sub-58 4-ClPh -CO- -CH2- -CH2-
3-1052 Sub-59 4-ClPh -CO- -CH2- -CH2-
3-1053 Sub-82 4-ClPh -CO- -CH2- -CH2-
3-1054 Sub-83 4-ClPh -CO- -CH2- -CH2-
3-1055 Sub-61 4-ClPh -CO- -CH2- -CH2-
3-1056 Sub-55 4-ClPh -CO- -CH2- -CH2-
3-1057 Sub-33 4-ClPh -CO- -CH2- -CH2CH2-
3-1058 Sub-34 4-ClPh -CO- -CH2- -CH2CH2-
3-1059 Sub-35 4-ClPh -CO- -CH2- -CH2CH2-
3-1060 Sub-36 4-ClPh -CO- -CH2- -CH2CH2-
3-1061 Sub-37 4-ClPh -CO- -CH2- -CH2CH2-
3-1062 Sub-38 4-ClPh -CO- -CH2- -CH2CH2-
3-1063 Sub-39 4-ClPh -CO- -CH2- -CH2CH2-
3-1064 Sub-40 4-ClPh -CO- -CH2- -CH2CH2-
3-1065 Sub-41 4-ClPh -CO- -CH2- -CH2CH2-
3-1066 Sub-42 4-ClPh -CO- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1067 Sub-84 4-ClPh -CO- -CH2- -CH2CH2-
3-1068 Sub-43 4-ClPh -CO- -CH2- -CH2CH2-
3-1069 Sub-44 4-ClPh -CO- -CH2- -CH2CH2-
3-1070 Sub-45 4-ClPh -CO- -CH2- -CH2CH2-
3-1071 Sub-46 4-ClPh -CO- -CH2- -CH2CH2-
3-1072 Sub-47 4-ClPh -CO- -CH2- -CH2CH2-
3-1073 Sub-81 4-ClPh -CO- -CH2- -CH2CH2-
3-1074 Sub-48 4-ClPh -CO- -CH2- -CH2CH2-
3-1075 Sub-49 4-ClPh -CO- -CH2- -CH2CH2-
3-1076 Sub-50 4-ClPh -CO- -CH2- -CH2CH2-
3-1077 Sub-51 4-ClPh -CO- -CH2- -CH2CH2-
3-1078 Sub-52 4-ClPh -CO- -CH2- -CH2CH2-
3-1079 Sub-53 4-ClPh -CO- -CH2- -CH2CH2-
3-1080 Sub-54 4-ClPh -CO- -CH2- -CH2CH2-
3-1081 Sub-56 4-ClPh -CO- -CH2- -CH2CH2-
3-1082 Sub-57 4-ClPh -CO- -CH2- -CH2CH2-
3-1083 Sub-58 4-ClPh -CO- -CH2- -CH2CH2-
3-1084 Sub-59 4-ClPh -CO- -CH2- -CH2CH2-
3-1085 Sub-82 4-ClPh -CO- -CH2- -CH2CH2-
3-1086 Sub-83 4-ClPh -CO- -CH2- -CH2CH2-
3-1087 Sub-61 4-ClPh -CO- -CH2- -CH2CH2-
3-1088 Sub-55 4-ClPh -CO- -CH2- -CH2CH2-
3-1089 Sub-33 4-ClPh -CO- -CH2- -(CH2)3-
3-1090 Sub-34 4-ClPh -CO- -CH2- -(CH2)3-
3-1091 Sub-35 4-ClPh -CO- -CH2- -(CH2)3-
3-1092 Sub-36 4-ClPh -CO- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1093 Sub-37 4-ClPh -CO- -CH2- -(CH2)3-
3-1094 Sub-38 4-ClPh -CO- -CH2- -(CH2)3-
3-1095 Sub-39 4-ClPh -CO- -CH2- -(CH2)3-
3-1096 Sub-40 4-ClPh -CO- -CH2- -(CH2)3-
3-1097 Sub-41 4-ClPh -CO- -CH2- -(CH2)3-
3-1098 Sub-42 4-ClPh -CO- -CH2- -(CH2)3-
3-1099 Sub-84 4-ClPh -CO- -CH2- -(CH2)3-
3-1100 Sub-43 4-ClPh -CO- -CH2- -(CH2)3-
3-1101 Sub-44 4-ClPh -CO- -CH2- -(CH2)3-
3-1102 Sub-45 4-ClPh -CO- -CH2- -(CH2)3-
3-1103 Sub-46 4-ClPh -CO- -CH2- -(CH2)3-
3-1104 Sub-47 4-ClPh -CO- -CH2- -(CH2)3-
3-1105 Sub-81 4-ClPh -CO- -CH2- -(CH2)3-
3-1106 Sub-48 4-ClPh -CO- -CH2- -(CH2)3-
3-1107 Sub-49 4-ClPh -CO- -CH2- -(CH2)3-
3-1108 Sub-50 4-ClPh -CO- -CH2- -(CH2)3-
3-1109 Sub-51 4-ClPh -CO- -CH2- -(CH2)3-
3-1110 Sub-52 4-ClPh -CO- -CH2- -(CH2)3-
3-1111 Sub-53 4-ClPh -CO- -CH2- -(CH2)3-
3-1112 Sub-54 4-ClPh -CO- -CH2- -(CH2)3-
3-1113 Sub-56 4-ClPh -CO- -CH2- -(CH2)3-
3-1114 Sub-57 4-ClPh -CO- -CH2- -(CH2)3-
3-1115 Sub-58 4-ClPh -CO- -CH2- -(CH2)3-
3-1116 Sub-59 4-ClPh -CO- -CH2- -(CH2)3-
3-1117 Sub-82 4-ClPh -CO- -CH2- -(CH2)3-
3-1118 Sub-83 4-ClPh -CO- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1119 Sub-61 4-ClPh -CO- -CH2- -(CH2)3-
3-1120 Sub-55 4-ClPh -CO- -CH2- -(CH2)3-
3-1121 Sub-33 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1122 Sub-34 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1123 Sub-35 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1124 Sub-36 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1125 Sub-37 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1126 Sub-38 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1127 Sub-39 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1128 Sub-40 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1129 Sub-41 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1130 Sub-42 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1131 Sub-84 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1132 Sub-43 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1133 Sub-44 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1134 Sub-45 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1135 Sub-46 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1136 Sub-47 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1137 Sub-81 4-C lPh -CO- -CH2- -CH2C(Me)2-
3-1138 Sub-48 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1139 Sub-49 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1140 Sub-50 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1141 Sub-51 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1142 Sub-52 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1143 Sub-53 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1144 Sub-54 4-ClPh -CO- -CH2- -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1145 Sub-56 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1146 Sub-57 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1147 Sub-58 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1148 Sub-59 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1149 Sub-82 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1150 Sub-83 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1151 Sub-61 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1152 Sub-55 4-ClPh -CO- -CH2- -CH2C(Me)2-
3-1153 Sub-33 4-ClPh -CO- -CH2- -CH2-cPr-
3-1154 Sub-34 4-ClPh -CO- -CH2- -CH2-cPr-
3-1155 Sub-35 4-ClPh -CO- -CH2- -CH2-cPr-
3-1156 Sub-36 4-ClPh -CO- -CH2- -CH2-cPr-
3-1157 Sub-37 4-ClPh -CO- -CH2- -CH2-cPr-
3-1158 Sub-38 4-ClPh -CO- -CH2- -CH2-cPr-
3-1159 Sub-39 4-ClPh -CO- -CH2- -CH2-cPr-
3-1160 Sub-40 4-ClPh -CO- -CH2- -CH2-cPr-
3-1161 Sub-41 4-ClPh -CO- -CH2- -CH2-cPr-
3-1162 Sub-42 4-ClPh -CO- -CH2- -CH2-cPr-
3-1163 Sub-84 4-ClPh -CO- -CH2- -CH2-cPr-
3-1164 Sub-43 4-ClPh -CO- -CH2- -CH2-cPr-
3-1165 Sub-44 4-ClPh -CO- -CH2- -CH2-cPr-
3-1166 Sub-45 4-ClPh -CO- -CH2- -CH2-cPr-
3-1167 Sub-46 4-ClPh -CO- -CH2- -CH2-cPr-
3-1168 Sub-47 4-ClPh -CO- -CH2- -CH2-cPr-
3-1169 Sub-81 4-ClPh -CO- -CH2- -CH2-cPr-
3-1170 Sub-48 4-ClPh -CO- -CH2- -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1171 Sub-49 4-ClPh -CO- -CH2- -CH2-cPr-
3-1172 Sub-50 4-ClPh -CO- -CH2- -CH2-cPr-
3-1173 Sub-51 4-ClPh -CO- -CH2- -CH2-cPr-
3-1174 Sub-52 4-ClPh -CO- -CH2- -CH2-cPr-
3-1175 Sub-53 4-ClPh -CO- -CH2- -CH2-cPr-
3-1176 Sub-54 4-ClPh -CO- -CH2- -CH2-cPr-
3-1177 Sub-56 4-ClPh -CO- -CH2- -CH2-cPr-
3-1178 Sub-57 4-ClPh -CO- -CH2- -CH2-cPr-
3-1179 Sub-58 4-ClPh -CO- -CH2- -CH2-cPr-
3-1180 Sub-59 4-ClPh -CO- -CH2- -CH2-cPr-
3-1181 Sub-82 4-ClPh -CO- -CH2- -CH2-cPr-
3-1182 Sub-83 4-ClPh -CO- -CH2- -CH2-cPr-
3-1183 Sub-61 4-ClPh -CO- -CH2- -CH2-cPr-
3-1184 Sub-55 4-ClPh -CO- -CH2- -CH2-cPr-
3-1185 Sub-33 4-ClPh -CO- -CH2- -CH2-cBu-
3-1186 Sub-34 4-ClPh -CO- -CH2- -CH2-cBu-
3-1187 Sub-35 4-ClPh -CO- -CH2- -CH2-cBu-
3-1188 Sub-36 4-ClPh -CO- -CH2- -CH2-cBu-
3-1189 Sub-37 4-ClPh -CO- -CH2- -CH2-cBu-
3-1190 Sub-38 4-ClPh -CO- -CH2- -CH2-cBu-
3-1191 Sub-39 4-ClPh -CO- -CH2- -CH2-cBu-
3-1192 Sub-40 4-ClPh -CO- -CH2- -CH2-cBu-
3-1193 Sub-41 4-ClPh -CO- -CH2- -CH2-cBu-
3-1194 Sub-42 4-ClPh -CO- -CH2- -CH2-cBu-
3-1195 Sub-84 4-ClPh -CO- -CH2- -CH2-cBu-
3-1196 Sub-43 4-ClPh -CO- -CH2- -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1197 Sub-44 4-ClPh -CO- -CH2- -CH2-cBu-
3-1198 Sub-45 4-ClPh -CO- -CH2- -CH2-cBu-
3-1199 Sub-46 4-ClPh -CO- -CH2- -CH2-cBu-
3-1200 Sub-47 4-ClPh -CO- -CH2- -CH2-cBu-
3-1201 Sub-81 4-ClPh -CO- -CH2- -CH2-cBu-
3-1202 Sub-48 4-ClPh -CO- -CH2- -CH2-cBu-
3-1203 Sub-49 4-ClPh -CO- -CH2- -CH2-cBu-
3-1204 Sub-50 4-ClPh -CO- -CH2- -CH2-cBu-
3-1205 Sub-51 4-ClPh -CO- -CH2- -CH2-cBu-
3-1206 Sub-52 4-ClPh -CO- -CH2- -CH2-cBu-
3-1207 Sub-53 4-ClPh -CO- -CH2- -CH2-cBu-
3-1208 Sub-54 4-ClPh -CO- -CH2- -CH2-cBu-
3-1209 Sub-56 4-ClPh -CO- -CH2- -CH2-cBu-
3-1210 Sub-57 4-ClPh -CO- -CH2- -CH2-cBu-
3-1211 Sub-58 4-ClPh -CO- -CH2- -CH2-cBu-
3-1212 Sub-59 4-ClPh -CO- -CH2- -CH2-cBu-
3-1213 Sub-82 4-ClPh -CO- -CH2- -CH2-cBu-
3-1214 Sub-83 4-ClPh -CO- -CH2- -CH2-cBu-
3-1215 Sub-61 4-ClPh -CO- -CH2- -CH2-cBu-
3-1216 Sub-55 4-ClPh -CO- -CH2- -CH2-cBu-
3-1217 Sub-33 4-ClPh -CO- -CH2- -CH2-cPn-
3-1218 Sub-34 4-ClPh -CO- -CH2- -CH2-cPn-
3-1219 Sub-35 4-ClPh -CO- -CH2- -CH2-cPn-
3-1220 Sub-36 4-ClPh -CO- -CH2- -CH2-cPn-
3-1221 Sub-37 4-ClPh -CO- -CH2- -CH2-cPn-
3-1222 Sub-38 4-ClPh -CO- -CH2- -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1223 Sub-39 4-ClPh -CO- -CH2- -CH2-cPn-
3-1224 Sub-40 4-ClPh -CO- -CH2- -CH2-cPn-
3-1225 Sub-41 4-ClPh -CO- -CH2- -CH2-cPn-
3-1226 Sub-42 4-ClPh -CO- -CH2- -CH2-cPn-
3-1227 Sub-84 4-ClPh -CO- -CH2- -CH2-cPn-
3-1228 Sub-43 4-ClPh -CO- -CH2- -CH2-cPn-
3-1229 Sub-44 4-ClPh -CO- -CH2- -CH2-cPn-
3-1230 Sub-45 4-ClPh -CO- -CH2- -CH2-cPn-
3-1231 Sub-46 4-ClPh -CO- -CH2- -CH2-cPn-
3-1232 Sub-47 4-ClPh -CO- -CH2- -CH2-cPn-
3-1233 Sub-81 4-ClPh -CO- -CH2- -CH2-cPn-
3-1234 Sub-48 4-ClPh -CO- -CH2- -CH2-cPn-
3-1235 Sub-49 4-ClPh -CO- -CH2- -CH2-cPn-
3-1236 Sub-50 4-ClPh -CO- -CH2- -CH2-cPn-
3-1237 Sub-51 4-ClPh -CO- -CH2- -CH2-cPn-
3-1238 Sub-52 4-ClPh -CO- -CH2- -CH2-cPn-
3-1239 Sub-53 4-ClPh -CO- -CH2- -CH2-cPn-
3-1240 Sub-54 4-ClPh -CO- -CH2- -CH2-cPn-
3-1241 Sub-56 4-ClPh -CO- -CH2- -CH2-cPn-
3-1242 Sub-57 4-ClPh -CO- -CH2- -CH2-cPn-
3-1243 Sub-58 4-ClPh -CO- -CH2- -CH2-cPn-
3-1244 Sub-59 4-ClPh -CO- -CH2- -CH2-cPn-
3-1245 Sub-82 4-ClPh -CO- -CH2- -CH2-cPn-
3-1246 Sub-83 4-ClPh -CO- -CH2- -CH2-cPn-
3-1247 Sub-61 4-ClPh -CO- -CH2- -CH2-cPn-
3-1248 Sub-55 4-ClPh -CO- -CH2- -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1249 Sub-33 4-ClPh -CO- -CH2- -CH2-cHx-
3-1250 Sub-34 4-ClPh -CO- -CH2- -CH2-cHx-
3-1251 Sub-35 4-ClPh -CO- -CH2- -CH2-cHx-
3-1252 Sub-36 4-ClPh -CO- -CH2- -CH2-cHx-
3-1253 Sub-37 4-ClPh -CO- -CH2- -CH2-cHx-
3-1254 Sub-38 4-ClPh -CO- -CH2- -CH2-cHx-
3-1255 Sub-39 4-ClPh -CO- -CH2- -CH2-cHx-
3-1256 Sub-40 4-ClPh -CO- -CH2- -CH2-cHx-
3-1257 Sub-41 4-ClPh -CO- -CH2- -CH2-cHx-
3-1258 Sub-42 4-ClPh -CO- -CH2- -CH2-cHx-
3-1259 Sub-84 4-ClPh -CO- -CH2- -CH2-cHx-
3-1260 Sub-43 4-ClPh -CO- -CH2- -CH2-cHx-
3-1261 Sub-44 4-ClPh -CO- -CH2- -CH2-cHx-
3-1262 Sub-45 4-ClPh -CO- -CH2- -CH2-cHx-
3-1263 Sub-46 4-ClPh -CO- -CH2- -CH2-cHx-
3-1264 Sub-47 4-ClPh -CO- -CH2- -CH2-cHx-
3-1265 Sub-81 4-ClPh -CO- -CH2- -CH2-cHx-
3-1266 Sub-48 4-ClPh -CO- -CH2- -CH2-cHx-
3-1267 Sub-49 4-ClPh -CO- -CH2- -CH2-cHx-
3-1268 Sub-50 4-ClPh -CO- -CH2- -CH2-cHx-
3-1269 Sub-51 4-ClPh -CO- -CH2- -CH2-cHx-
3-1270 Sub-52 4-ClPh -CO- -CH2- -CH2-cHx-
3-1271 Sub-53 4-ClPh -CO- -CH2- -CH2-cHx-
3-1272 Sub-54 4-ClPh -CO- -CH2- -CH2-cHx-
3-1273 Sub-56 4-ClPh -CO- -CH2- -CH2-cHx-
3-1274 Sub-57 4-ClPh -CO- -CH2- -CH2-cHx-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1275 Sub-58 4-ClPh -CO- -CH2- -CH2-cHx-
3-1276 Sub-59 4-ClPh -CO- -CH2- -CH2-cHx-
3-1277 Sub-82 4-ClPh -CO- -CH2- -CH2-cHx-
3-1278 Sub-83 4-ClPh -CO- -CH2- -CH2-cHx-
3-1279 Sub-61 4-ClPh -CO- -CH2- -CH2-cHx-
3-1280 Sub-55 4-ClPh -CO- -CH2- -CH2-cHx-
3-1281 Sub-33 4-FPh -CO- -CH2- -CH2-
3-1282 Sub-34 4-FPh -CO- -CH2- -CH2-
3-1283 Sub-35 4-FPh -CO- -CH2- -CH2-
3-1284 Sub-36 4-FPh -CO- -CH2- -CH2-
3-1285 Sub-37 4-FPh -CO- -CH2- -CH2-
3-1286 Sub-38 4-FPh -CO- -CH2- -CH2-
3-1287 Sub-39 4-FPh -CO- -CH2- -CH2-
3-1288 Sub-40 4-FPh -CO- -CH2- -CH2-
3-1289 Sub-41 4-FPh -CO- -CH2- -CH2-
3-1290 Sub-42 4-FPh -CO- -CH2- -CH2-
3-1291 Sub-84 4-FPh -CO- -CH2- -CH2-
3-1292 Sub-43 4-FPh -CO- -CH2- -CH2-
3-1293 Sub-44 4-FPh -CO- -CH2- -CH2-
3-1294 Sub-45 4-FPh -CO- -CH2- -CH2-
3-1295 Sub-46 4-FPh -CO- -CH2- -CH2-
3-1296 Sub-47 4-FPh -CO- -CH2- -CH2-
3-1297 Sub-81 4-FPh -CO- -CH2- -CH2-
3-1298 Sub-48 4-FPh -CO- -CH2- -CH2-
3-1299 Sub-49 4-FPh -CO- -CH2- -CH2-
3-1300 Sub-50 4-FPh -CO- -CH2- -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1301 Sub-51 4-FPh -CO- -CH2- -CH2-
3-1302 Sub-52 4-FPh -CO- -CH2- -CH2-
3-1303 Sub-53 4-FPh -CO- -CH2- -CH2-
3-1304 Sub-54 4-FPh -CO- -CH2- -CH2-
3-1305 Sub-56 4-FPh -CO- -CH2- -CH2-
3-1306 Sub-57 4-FPh -CO- -CH2- -CH2-
3-1307 Sub-58 4-FPh -CO- -CH2- -CH2-
3-1308 Sub-59 4-FPh -CO- -CH2- -CH2-
3-1309 Sub-82 4-FPh -CO- -CH2- -CH2-
3-1310 Sub-83 4-FPh -CO- -CH2- -CH2-
3-1311 Sub-61 4-FPh -CO- -CH2- -CH2-
3-1312 Sub-55 4-FPh -CO- -CH2- -CH2-
3-1313 Sub-33 4-FPh -CO- -CH2- -CH2CH2-
3-1314 Sub-34 4-FPh -CO- -CH2- -CH2CH2-
3-1315 Sub-35 4-FPh -CO- -CH2- -CH2CH2-
3-1316 Sub-36 4-FPh -CO- -CH2- -CH2CH2-
3-1317 Sub-37 4-FPh -CO- -CH2- -CH2CH2-
3-1318 Sub-38 4-FPh -CO- -CH2- -CH2CH2-
3-1319 Sub-39 4-FPh -CO- -CH2- -CH2CH2-
3-1320 Sub-40 4-FPh -CO- -CH2- -CH2CH2-
3-1321 Sub-41 4-FPh -CO- -CH2- -CH2CH2-
3-1322 Sub-42 4-FPh -CO- -CH2- -CH2CH2-
3-1323 Sub-84 4-FPh -CO- -CH2- -CH2CH2-
3-1324 Sub-43 4-FPh -CO- -CH2- -CH2CH2-
3-1325 Sub-44 4-FPh -CO- -CH2- -CH2CH2-
3-1326 Sub-45 4-FPh -CO- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1327 Sub-46 4-FPh -CO- -CH2- -CH2CH2-
3-1328 Sub-47 4-FPh -CO- -CH2- -CH2CH2-
3-1329 Sub-81 4-FPh -CO- -CH2- -CH2CH2-
3-1330 Sub-48 4-FPh -CO- -CH2- -CH2CH2-
3-1331 Sub-49 4-FPh -CO- -CH2- -CH2CH2-
3-1332 Sub-5O 4-FPh -CO- -CH2- -CH2CH2-
3-1333 Sub-51 4-FPh -CO- -CH2- -CH2CH2-
3-1334 Sub-52 4-FPh -CO- -CH2- -CH2CH2-
3-1335 Sub-53 4-FPh -CO- -CH2- -CH2CH2-
3-1336 Sub-54 4-FPh -CO- -CH2- -CH2CH2-
3-1337 Sub-56 4-FPh -CO- -CH2- -CH2CH2-
3-1338 Sub-57 4-FPh -CO- -CH2- -CH2CH2-
3-1339 Sub-58 4-FPh -CO- -CH2- -CH2CH2-
3-1340 Sub-59 4-FPh -CO- -CH2- -CH2CH2-
3-1341 Sub-82 4-FPh -CO- -CH2- -CH2CH2-
3-1342 Sub-83 4-FPh -CO- -CH2- -CH2CH2-
3-1343 Sub-61 4-FPh -CO- -CH2- -CH2CH2-
3-1344 Sub-55 4-FPh -CO- -CH2- -CH2CH2-
3-1345 Sub-33 4-FPh -CO- -CH2- -(CH2)3-
3-1346 Sub-34 4-FPh -CO- -CH2- -(CH2)3-
3-1347 Sub-35 4-FPh -CO- -CH2- -(CH2)3-
3-1348 Sub-36 4-FPh -CO- -CH2- -(CH2)3-
3-1349 Sub-37 4-FPh -CO- -CH2- -(CH2)3-
3-1350 Sub-38 4-FPh -CO- -CH2- -(CH2)3-
3-1351 Sub-39 4-FPh -CO- -CH2- -(CH2)3-
3-1352 Sub-40 4-FPh -CO- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1353 Sub-41 4-FPh -CO- -CH2- -(CH2)3-
3-1354 Sub-42 4-FPh -CO- -CH2- -(CH2)3-
3-1355 Sub-84 4-FPh -CO- -CH2- -(CH2)3-
3-1356 Sub-43 4-FPh -CO- -CH2- -(CH2)3-
3-1357 Sub-44 4-FPh -CO- -CH2- -(CH2)3-
3-1358 Sub-45 4-FPh -CO- -CH2- -(CH2)3-
3-1359 Sub-46 4-FPh -CO- -CH2- -(CH2)3-
3-1360 Sub-47 4-FPh -CO- -CH2- -(CH2)3-
3-1361 Sub-81 4-FPh -CO- -CH2- -(CH2)3-
3-1362 Sub-48 4-FPh -CO- -CH2- -(CH2)3-
3-1363 Sub-49 4-FPh -CO- -CH2- -(CH2)3-
3-1364 Sub-50 4-FPh -CO- -CH2- -(CH2)3-
3-1365 Sub-51 4-FPh -CO- -CH2- -(CH2)3-
3-1366 Sub-52 4-FPh -CO- -CH2- -(CH2)3-
3-1367 Sub-53 4-FPh -CO- -CH2- -(CH2)3-
3-1368 Sub-54 4-FPh -CO- -CH2- -(CH2)3-
3-1369 Sub-56 4-FPh -CO- -CH2- -(CH2)3-
3-1370 Sub-57 4-FPh -CO- -CH2- -(CH2)3-
3-1371 Sub-58 4-FPh -CO- -CH2- -(CH2)3-
3-1372 Sub-59 4-FPh -CO- -CH2- -(CH2)3-
3-1373 Sub-82 4-FPh -CO- -CH2- -(CH2)3-
3-1374 Sub-83 4-FPh -CO- -CH2- -(CH2)3-
3-1375 Sub-61 4-FPh -CO- -CH2- -(CH2)3-
3-1376 Sub-55 4-FPh -CO- -CH2- -(CH2)3-
3-1377 Sub-33 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1378 Sub-34 4-FPh -CO- -CH2- -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1379 Sub-35 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1380 Sub-36 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1381 Sub-37 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1382 Sub-38 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1383 Sub-39 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1384 Sub-40 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1385 Sub-41 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1386 Sub-42 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1387 Sub-84 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1388 Sub-43 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1389 Sub-44 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1390 Sub-45 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1391 Sub-46 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1392 Sub-47 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1393 Sub-81 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1394 Sub-48 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1395 Sub-49 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1396 Sub-50 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1397 Sub-51 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1398 Sub-52 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1399 Sub-53 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1400 Sub-54 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1401 Sub-56 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1402 Sub-57 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1403 Sub-58 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1404 Sub-59 4-FPh -CO- -CH2- -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1405 Sub-82 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1406 Sub-83 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1407 Sub-6l 4-FPh -CO- -CH2- -CH2C(Me)2-
3-1408 Sub-55 4-rPh -CO- -CH2- -CH2C(Me)2-
3-1409 Sub-33 4-FPh -CO- -CH2- -CH2-cPr-
3-1410 Sub-34 4-FPh -CO- -CH2- -CH2-cPr-
3-1411 Sub-35 4-FPh -CO- -CH2- -CH2-cPr-
3-1412 Sub-36 4-FPh -CO- -CH2- -CH2-cPr-
3-1413 Sub-37 4-FPh -CO- -CH2- -CH2-cPr-
3-1414 Sub-38 4-FPh -CO- -CH2- -CH2-cPr-
3-1415 Sub-39 4-FPh -CO- -CH2- -CH2-cPr-
3-1416 Sub-40 4-FPh -CO- -CH2- -CH2-cPr-
3-1417 Sub-41 4-FPh -CO- -CH2- -CH2-cPr-
3-1418 Sub-42 4-FPh -CO- -CH2- -CH2-cPr-
3-1419 Sub-84 4-FPh -CO- -CH2- -CH2-cPr-
3-1420 Sub-43 4-FPh -CO- -CH2- -CH2-cPr-
3-1421 Sub-44 4-FPh -CO- -CH2- -CH2-cPr-
3-1422 Sub-45 4-FPh -CO- -CH2- -CH2-cPr-
3-1423 Sub-46 4-FPh -CO- -CH2- -CH2-cPr-
3-1424 Sub-47 4-FPh -CO- -CH2- -CH2-cPr-
3-1425 Sub-81 4-FPh -CO- -CH2- -CH2-cPr-
3-1426 Sub-48 4-FPh -CO- -CH2- -CH2-cPr-
3-1427 Sub-49 4-FPh -CO- -CH2- -CH2-cPr-
3-1428 Sub-50 4-FPh -CO- -CH2- -CH2-cPr-
3-1429 Sub-51 4-FPh -CO- -CH2- -CH2-cPr-
3-1430 Sub-52 4-FPh -CO- -CH2- -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1431 Sub-53 4-FPh -CO- -CH2- -CH2-cPr-
3-1432 Sub-54 4-FPh -CO- -CH2- -CH2-cPr-
3-1433 Sub-56 4-FPh -CO- -CH2- -CH2-cPr-
3-1434 Sub-57 4-FPh -CO- -CH2- -CH2-cPr-
3-1435 Sub-58 4-FPh -CO- -CH2- -CH2-cPr-
3-1436 Sub-59 4-FPh -CO- -CH2- -CH2-cPr-
3-1437 Sub-82 4-FPh -CO- -CH2- -CH2-cPr-
3-1438 Sub-83 4-FPh -CO- -CH2- -CH2-cPr-
3-1439 Sub-61 4-FPh -CO- -CH2- -CH2-cPr-
3-1440 Sub-55 4-FPh -CO- -CH2- -CH2-cPr-
3-1441 Sub-33 4-FPh -CO- -CH2- -CH2-cBu-
3-1442 Sub-34 4-FPh -CO- -CH2- -CH2-cBu-
3-1443 Sub-35 4-FPh -CO- -CH2- -CH2-cBu-
3-1444 Sub-36 4-FPh -CO- -CH2- -CH2-cBu-
3-1445 Sub-37 4-FPh -CO- -CH2- -CH2-cBu-
3-1446 Sub-38 4-FPh -CO- -CH2- -CH2-cBu-
3-1447 Sub-39 4-FPh -CO- -CH2- -CH2-cBu-
3-1448 Sub-40 4-FPh -CO- -CH2- -CH2-cBu-
3-1449 Sub-41 4-FPh -CO- -CH2- -CH2-cBu-
3-1450 Sub-42 4-FPh -CO- -CH2- -CH2-cBu-
3-1451 Sub-84 4-FPh -CO- -CH2- -CH2-cBu-
3-1452 Sub-43 4-FPh -CO- -CH2- -CH2-cBu-
3-1453 Sub-44 4-FPh -CO- -CH2- -CH2-cBu-
3-1454 Sub-45 4-FPh -CO- -CH2- -CH2-cBu-
3-1455 Sub-46 4-FPh -CO- -CH2- -CH2-cBu-
3-1456 Sub-47 4-FPh -CO- -CH2- -CH2-cBu-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1457 Sub-81 4-FPh -CO- -CH2- -CH2-cBu-
3-1458 Sub-48 4-FPh -CO- -CH2- -CH2-cBu-
3-1459 Sub-49 4-FPh -CO- -CH2- -CH2-cBu-
3-1460 Sub-50 4-FPh -CO- -CH2- -CH2-cBu-
3-1461 Sub-51 4-FPh -CO- -CH2- -CH2-cBu-
3-1462 Sub-52 4-FPh -CO- -CH2- -CH2-cBu-
3-1463 Sub-53 4-FPh -CO- -CH2- -CH2-cBu-
3-1464 Sub-54 4-FPh -CO- -CH2- -CH2-cBu-
3-1465 Sub-56 4-FPh -CO- -CH2- -CH2-cBu-
3-1466 Sub-57 4-FPh -CO- -CH2- -CH2-cBu-
3-1467 Sub-58 4-FPh -CO- -CH2- -CH2-cBu-
3-1468 Sub-59 4-FPh -CO- -CH2- -CH2-cBu-
3-1469 Sub-82 4-FPh -CO- -CH2- -CH2-cBu-
3-1470 Sub-83 4-FPh -CO- -CH2- -CH2-cBu-
3-1471 Sub-61 4-FPh -CO- -CH2- -CH2-cBu-
3-1472 Sub-55 4-FPh -CO- -CH2- -CH2-cBu-
3-1473 Sub-33 4-FPh -CO- -CH2- -CH2-cPn-
3-1474 Sub-34 4-FPh -CO- -CH2- -CH2-cPn-
3-1475 Sub-35 4-FPh -CO- -CH2- -CH2-cPn-
3-1476 Sub-36 4-FPh -CO- -CH2- -CH2-cPn-
3-1477 Sub-37 4-FPh -CO- -CH2- -CH2-cPn-
3-1478 Sub-38 4-FPh -CO- -CH2- -CH2-cPn-
3-1479 Sub-39 4-FPh -CO- -CH2- -CH2-cPn-
3-1480 Sub-40 4-FPh -CO- -CH2- -CH2-cPn-
3-1481 Sub-41 4-FPh -CO- -CH2- -CH2-cPn-
3-1482 Sub-42 4-FPh -CO- -CH2- -CH2-cPn-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1483 Sub-84 4-FPh -CO- -CH2- -CH2-cPn-
3-1484 Sub-43 4-FPh -CO- -CH2- -CH2-cPn-
3-1485 Sub-44 4-FPh -CO- -CH2- -CH2-cPn-
3-1486 Sub-45 4-FPh -CO- -CH2- -CH2-cPn-
3-1487 Sub-46 4-FPh -CO- -CH2- -CH2-cPn-
3-1488 Sub-47 4-FPh -CO- -CH2- -CH2-cPn-
3-1489 Sub-81 4-FPh -CO- -CH2- -CH2-cPn-
3-1490 Sub-48 4-FPh -CO- -CH2- -CH2-cPn-
3-1491 Sub-49 4-FPh -CO- -CH2- -CH2-cPn-
3-1492 Sub-50 4-FPh -CO- -CH2- -CH2-cPn-
3-1493 Sub-51 4-FPh -CO- -CH2- -CH2-cPn-
3-1494 Sub-52 4-FPh -CO- -CH2- -CH2-cPn-
3-1495 Sub-53 4-FPh -CO- -CH2- -CH2-cPn-
3-1496 Sub-54 4-FPh -CO- -CH2- -CH2-cPn-
3-1497 Sub-56 4-FPh -CO- -CH2- -CH2-cPn-
3-1498 Sub-57 4-FPh -CO- -CH2- -CH2-cPn-
3-1499 Sub-58 4-FPh -CO- -CH2- -CH2-cPn-
3-1500 Sub-59 4-FPh -CO- -CH2- -CH2-cPn-
3-1501 Sub-82 4-FPh -CO- -CH2- -CH2-cPn-
3-1502 Sub-83 4-FPh -CO- -CH2- -CH2-cPn-
3-1503 Sub-61 4-FPh -CO- -CH2- -CH2-cPn-
3-1504 Sub-55 4-FPh -CO- -CH2- -CH2-cPn-
3-1505 Sub-33 4-FPh -CO- -CH2- -CH2-cHx-
3-1506 Sub-34 4-FPh -CO- -CH2- -CH2-cHx-
3-1507 Sub-35 4-FPh -CO- -CH2- -CH2-cHx-
3-1508 Sub-36 4-FPh -CO- -CH2- -CH2-cHx-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1509 Sub-37 4-FPh -CO- -CH2- -CH2-cHx-
3-1510 Sub-38 4-FPh -CO- -CH2- -CH2-cHx-
3-1511 Sub-39 4-FPh -CO- -CH2- -CH2-cHx-
3-1512 Sub-40 4-FPh -CO- -CH2- -CH2-cHx-
3-1513 Sub-41 4-FPh -CO- -CH2- -CH2-cHx-
3-1514 Sub-42 4-FPh -CO- -CH2- -CH2-cHx-
3-1515 Sub-84 4-FPh -CO- -CH2- -CH2-cHx-
3-1516 Sub-43 4-FPh -CO- -CH2- -CH2-cHx-
3-1517 Sub-44 4-FPh -CO- -CH2- -CH2-cHx-
3-1518 Sub-45 4-FPh -CO- -CH2- -CH2-cHx-
3-1519 Sub-46 4-FPh -CO- -CH2- -CH2-cHx-
3-1520 Sub-47 4-FPh -CO- -CH2- -CH2-cHx-
3-1521 Sub-81 4-FPh -CO- -CH2- -CH2-cHx-
3-1522 Sub-48 4-FPh -CO- -CH2- -CH2-cHx-
3-1523 Sub-49 4-FPh -CO- -CH2- -CH2-cHx-
3-1524 Sub-50 4-FPh -CO- -CH2- -CH2-cHx-
3-1525 Sub-51 4-FPh -CO- -CH2- -CH2-cHx-
3-1526 Sub-52 4-FPh -CO- -CH2- -CH2-cHx-
3-1527 Sub-53 4-FPh -CO- -CH2- -CH2-cHx-
3-1528 Sub-54 4-FPh -CO- -CH2- -CH2-cHx-
3-1529 Sub-56 4-FPh -CO- -CH2- -CH2-cHx-
3-1530 Sub-57 4-FPh -CO- -CH2- -CH2-cHx-
3-1531 Sub-58 4-FPh -CO- -CH2- -CH2-cHx-
3-1532 Sub-59 4-FPh -CO- -CH2- -CH2-cHx-
3-1533 Sub-82 4-FPh -CO- -CH2- -CH2-cHx-
3-1534 Sub-83 4-FPh -CO- -CH2- -CH2-cHx-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1535 Sub-61 4-FPh -CO- -CH2- -CH2-cHx-
3-1536 Sub-55 4-FPh -CO- -CH2- -CH2-cHx-
3-1537 Sub-33 3,4-diClPh -CO- Single bond -C(Me)2-
3-1538 Sub-34 3,4-diClPh -CO- Single bond -C(Me)2-
3-1539 Sub-35 3,4-diClPh -CO- Single bond -C(Me)2-
3-1540 Sub-36 3,4-diClPh -CO- Single bond -C(Me)2-
3-1541 Sub-37 3,4-diClPh -CO- Single bond -C(Me)2-
3-1542 Sub-38 3,4-diClPh -CO- Single bond -C(Me)2-
3-1543 Sub-39 3,4-diClPh -CO- Single bond -C(Me)2-
3-1544 Sub-40 3,4-diClPh -CO- Single bond -C(Me)2-
3-1545 Sub-41 3,4-diClPh -CO- Single bond -C(Me)2-
3-1546 Sub-42 3,4-diClPh -CO- Single bond -C(Me)2-
3-1547 Sub-84 3,4-diClPh -CO- Single bond -C(Me)2-
3-1548 Sub-43 3,4-diClPh -CO- Single bond -C(Me)2-
3-1549 Sub-44 3,4-diClPh -CO- Single bond -C(Me)2-
3-1550 Sub-45 3,4-diClPh -CO- Single bond -C(Me)2-
3-1551 Sub-46 3,4-diClPh -CO- Single bond -C(Me)2-
3-1552 Sub-47 3,4-diClPh -CO- Single bond -C(Me)2-
3-1553 Sub-81 3,4-diClPh -CO- Single bond -C(Me)2-
3-1554 Sub-48 3,4-diClPh -CO- Single bond -C(Me)2-
3-1555 Sub-49 3,4-diClPh -CO- Single bond -C(Me)2-
3-1556 Sub-50 3,4-diClPh -CO- Single bond -C(Me)2-
3-1557 Sub-51 3,4-diClPh -CO- Single bond -C(Me)2-
3-1558 Sub-52 3,4-diClPh -CO- Single bond -C(Me)2-
3-1559 Sub-53 3,4-diClPh -CO- Single bond -C(Me)2-
3-1560 Sub-54 3,4-diClPh -CO- Single bond -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1561 Sub-56 3,4-diClPh -CO- Single bond -C(Me)2-
3-1562 Sub-57 3,4-diClPh -CO- Single bond -C(Me)2-
3-1563 Sub-58 3,4-diClPh -CO- Single bond -C(Me)2-
3-1564 Sub-59 3,4-diClPh -CO- Single bond -C(Me)2-
3-1565 Sub-82 3,4-diClPh -CO- Single bond -C(Me)2-
3-1566 Sub-83 3,4-diClPh -CO- Single bond -C(Me)2-
3-1567 Sub-61 3,4-diClPh -CO- Single bond -C(Me)2-
3-1568 Sub-55 3,4-diClPh -CO- Single bond -C(Me)2-
3-1569 Sub-33 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1570 Sub-34 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1571 Sub-35 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1572 Sub-36 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1573 Sub-37 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1574 Sub-38 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1575 Sub-39 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1576 Sub-40 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1577 Sub-41 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1578 Sub-42 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1579 Sub-84 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1580 Sub-43 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1581 Sub-44 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1582 Sub-45 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1583 Sub-46 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1584 Sub-47 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1585 Sub-81 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1586 Sub-48 3,4-diClPh -CO- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1587 Sub-49 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1588 Sub-50 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1589 Sub-51 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1590 Sub-52 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1591 Sub-53 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1592 Sub-54 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1593 Sub-56 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1594 Sub-57 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1595 Sub-58 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1596 Sub-59 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1597 Sub-82 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1598 Sub-83 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1599 Sub-61 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1600 Sub-55 3,4-diClPh -CO- -CH2- -C(Me)2-
3-1601 Sub-33 4-ClPh -CO- Single bond -C(Me)2-
3-1602 Sub-34 4-ClPh -CO- Single bond -C(Me)2-
3-1603 Sub-35 4-ClPh -CO- Single bond -C(Me)2-
3-1604 Sub-36 4-ClPh -CO- Single bond -C(Me)2-
3-1605 Sub-37 4-ClPh -CO- Single bond -C(Me)2-
3-1606 Sub-38 4-ClPh -CO- Single bond -C(Me)2-
3-1607 Sub-39 4-ClPh -CO- Single bond -C(Me)2-
3-1608 Sub-40 4-ClPh -CO- Single bond -C(Me)2-
3-1609 Sub-41 4-ClPh -CO- Single bond -C(Me)2-
3-1610 Sub-42 4-ClPh -CO- Single bond -C(Me)2-
3-1611 Sub-84 4-ClPh -CO- Single bond -C(Me)2-
3-1612 Sub-43 4-ClPh -CO- Single bond -C(Me)2-
Table 3(cont.)
Chemical combination A serial number. R1 R2 A B E
3-1613 Sub-44 4-ClPh -CO- Single bond -C(Me)2-
3-1614 Sub-45 4-ClPh -CO- Single bond -C(Me)2-
3-1615 Sub-46 4-ClPh -CO- Single bond -C(Me)2-
3-1616 Sub-47 4-ClPh -CO- Single bond -C(Me)2-
3-1617 Sub-81 4-ClPh -CO- Single bond -C(Me)2-
3-1618 Sub-48 4-ClPh -CO- Single bond -C(Me)2-
3-1619 Sub-49 4-ClPh -CO- Single bond -C(Me)2-
3-1620 Sub-5O 4-ClPh -CO- Single bond -C(Me)2-
3-1621 Sub-51 4-ClPh -CO- Single bond -C(Me)2-
3-1622 Sub-52 4-ClPh -CO- Single bond -C(Me)2-
3-1623 Sub-53 4-ClPh -CO- Single bond -C(Me)2-
3-1624 Sub-54 4-ClPh -CO- Single bond -C(Me)2-
3-1625 Sub-56 4-ClPh -CO- Single bond -C(Me)2-
3-1626 Sub-57 4-ClPh -CO- Single bond -C(Me)2-
3-1627 Sub-58 4-ClPh -CO- Single bond -C(Me)2-
3-1628 Sub-59 4-ClPh -CO- Single bond -C(Me)2-
3-1629 Sub-82 4-ClPh -CO- Single bond -C(Me)2-
3-1630 Sub-83 4-ClPh -CO- Single bond -C(Me)2-
3-1631 Sub-61 4-ClPh -CO- Single bond -C(Me)2-
3-1632 Sub-55 4-ClPh -CO- Single bond -C(Me)2-
3-1633 Sub-33 4-ClPh -CO- -CH2- -C(Me)2-
3-1634 Sub-34 4-ClPh -CO- -CH2- -C(Me)2-
3-1635 Sub-35 4-ClPh -CO- -CH2- -C(Me)2-
3-1636 Sub-36 4-ClPh -CO- -CH2- -C(Me)2-
3-1637 Sub-37 4-ClPh -CO- -CH2- -C(Me)2-
3-1638 Sub-38 4-ClPh -CO- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1639 Sub-39 4-ClPh -CO- -CH2- -C(Me)2-
3-1640 Sub-40 4-ClPh -CO- -CH2- -C(Me)2-
3-1641 Sub-41 4-ClPh -CO- -CH2- -C(Me)2-
3-1642 Sub-42 4-ClPh -CO- -CH2- -C(Me)2-
3-1643 Sub-84 4-ClPh -CO- -CH2- -C(Me)2-
3-1644 Sub-43 4-ClPh -CO- -CH2- -C(Me)2-
3-1645 Sub-44 4-ClPh -CO- -CH2- -C(Me)2-
3-1646 Sub-45 4-ClPh -CO- -CH2- -C(Me)2-
3-1647 Sub-46 4-ClPh -CO- -CH2- -C(Me)2-
3-1648 Sub-47 4-ClPh -CO- -CH2- -C(Me)2-
3-1649 Sub-81 4-ClPh -CO- -CH2- -C(Me)2-
3-1650 Sub-48 4-ClPh -CO- -CH2- -C(Me)2-
3-1651 Sub-49 4-ClPh -CO- -CH2- -C(Me)2-
3-1652 Sub-50 4-ClPh -CO- -CH2- -C(Me)2-
3-1653 Sub-51 4-ClPh -CO- -CH2- -C(Me)2-
3-1654 Sub-52 4-ClPh -CO- -CH2- -C(Me)2-
3-1655 Sub-53 4-ClPh -CO- -CH2- -C(Me)2-
3-1656 Sub-54 4-ClPh -CO- -CH2- -C(Me)2-
3-1657 Sub-56 4-ClPh -CO- -CH2- -C(Me)2-
3-1658 Sub-57 4-ClPh -CO- -CH2- -C(Me)2-
3-1659 Sub-58 4-ClPh -CO- -CH2- -C(Me)2-
3-1660 Sub-59 4-ClPh -CO- -CH2- -C(Me)2-
3-1661 Sub-82 4-ClPh -CO- -CH2- -C(Me)2-
3-1662 Sub-83 4-ClPh -CO- -CH2- -C(Me)2-
3-1663 Sub-61 4-ClPh -CO- -CH2- -C(Me)2-
3-1664 Sub-55 4-ClPh -CO- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1665 Sub-33 4-FPh -CO- Single bond -C(Me)2-
3-1666 Sub-34 4-FPh -CO- Single bond -C(Me)2-
3-1667 Sub-35 4-FPh -CO- Single bond -C(Me)2-
3-1668 Sub-36 4-FPh -CO- Single bond -C(Me)2-
3-1669 Sub-37 4-FPh -CO- Single bond -C(Me)2-
3-1670 Sub-38 4-FPh -CO- Single bond -C(Me)2-
3-1671 Sub-39 4-FPh -CO- Single bond -C(Me)2-
3-1672 Sub-40 4-FPh -CO- Single bond -C(Me)2-
3-1673 Sub-41 4-FPh -CO- Single bond -C(Me)2-
3-1674 Sub-42 4-FPh -CO- Single bond -C(Me)2-
3-1675 Sub-84 4-FPh -CO- Single bond -C(Me)2-
3-1676 Sub-43 4-FPh -CO- Single bond -C(Me)2-
3-1677 Sub-44 4-FPh -CO- Single bond -C(Me)2-
3-1678 Sub-45 4-FPh -CO- Single bond -C(Me)2-
3-1679 Sub-46 4-FPh -CO- Single bond -C(Me)2-
3-1680 Sub-47 4-FPh -CO- Single bond -C(Me)2-
3-1681 Sub-81 4-FPh -CO- Single bond -C(Me)2-
3-1682 Sub-48 4-FPh -CO- Single bond -C(Me)2-
3-1683 Sub-49 4-FPh -CO- Single bond -C(Me)2-
3-1684 Sub-50 4-FPh -CO- Single bond -C(Me)2-
3-1685 Sub-51 4-FPh -CO- Single bond -C(Me)2-
3-1686 Sub-52 4-FPh -CO- Single bond -C(Me)2-
3-1687 Sub-53 4-FPh -CO- Single bond -C(Me)2-
3-1688 Sub-54 4-FPh -CO- Single bond -C(Me)2-
3-1689 Sub-56 4-FPh -CO- Single bond -C(Me)2-
3-1690 Sub-57 4-FPh -CO- Single bond -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1691 Sub-58 4-FPh -CO- Single bond -C(Me)2-
3-1692 Sub-59 4-FPh -CO- Single bond -C(Me)2-
3-1693 Sub-82 4-FPh -CO- Single bond -C(Me)2-
3-1694 Sub-83 4-FPh -CO- Single bond -C(Me)2-
3-1695 Sub-61 4-FPh -CO- Single bond -C(Me)2-
3-1696 Sub-55 4-FPh -CO- Single bond -C(Me)2-
3-1697 Sub-33 4-FPh -CO- -CH2- -C(Me)2-
3-1698 Sub-34 4-FPh -CO- -CH2- -C(Me)2-
3-1699 Sub-35 4-FPh -CO- -CH2- -C(Me)2-
3-1700 Sub-36 4-FPh -CO- -CH2- -C(Me)2-
3-1701 Sub-37 4-FPh -CO- -CH2- -C(Me)2-
3-1702 Sub-38 4-FPh -CO- -CH2- -C(Me)2-
3-1703 Sub-39 4-FPh -CO- -CH2- -C(Me)2-
3-1704 Sub-40 4-FPh -CO- -CH2- -C(Me)2-
3-1705 Sub-41 4-FPh -CO- -CH2- -C(Me)2-
3-1706 Sub-42 4-FPh -CO- -CH2- -C(Me)2-
3-1707 Sub-84 4-FPh -CO- -CH2- -C(Me)2-
3-1708 Sub-43 4-FPh -CO- -CH2- -C(Me)2-
3-1709 Sub-44 4-FPh -CO- -CH2- -C(Me)2-
3-1710 Sub-45 4-FPh -CO- -CH2- -C(Me)2-
3-1711 Sub-46 4-FPh -CO- -CH2- -C(Me)2-
3-1712 Sub-47 4-FPh -CO- -CH2- -C(Me)2-
3-1713 Sub-81 4-FPh -CO- -CH2- -C(Me)2-
3-1714 Sub-48 4-FPh -CO- -CH2- -C(Me)2-
3-1715 Sub-49 4-FPh -CO- -CH2- -C(Me)2-
3-1716 Sub-50 4-FPh -CO- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1717 Sub-51 4-FPh -CO- -CH2- -C(Me)2-
3-1718 Sub-52 4-FPh -CO- -CH2- -C(Me)2-
3-1719 Sub-53 4-FPh -CO- -CH2- -C(Me)2-
3-1720 Sub-54 4-FPh -CO- -CH2- -C(Me)2-
3-1721 Sub-56 4-FPh -CO- -CH2- -C(Me)2-
3-1722 Sub-57 4-FPh -CO- -CH2- -C(Me)2-
3-1723 Sub-58 4-FPh -CO- -CH2- -C(Me)2-
3-1724 Sub-59 4-FPh -CO- -CH2- -C(Me)2-
3-1725 Sub-82 4-FPh -CO- -CH2- -C(Me)2-
3-1726 Sub-83 4-FPh -CO- -CH2- -C(Me)2-
3-1727 Sub-61 4-FPh -CO- -CH2- -C(Me)2-
3-1728 Sub-55 4-FPh -CO- -CH2- -C(Me)2-
3-1729 Sub-37 3,4-diClPh -CH2- Single bond -CH2-
3-1730 Sub-38 3,4-diClPh -CH2- Single bond -CH2-
3-1731 Sub-39 3,4-diClPh -CH2- Single bond -CH2-
3-1732 Sub-40 3,4-diClPh -CH2- Single bond -CH2-
3-1733 Sub-41 3,4-diClPh -CH2- Single bond -CH2-
3-1734 Sub-42 3,4-diClPh -CH2- Single bond -CH2-
3-1735 Sub-84 3,4-diClPh -CH2- Single bond -CH2-
3-1736 Sub-81 3,4-diClPh -CH2- Single bond -CH2-
3-1737 Sub-48 3,4-diClPh -CH2- Single bond -CH2-
3-1738 Sub-37 4-ClPh -CH2- Single bond -CH2-
3-1739 Sub-38 4-ClPh -CH2- Single bond -CH2-
3-1740 Sub-39 4-ClPh -CH2- Single bond -CH2-
3-1741 Sub-40 4-ClPh -CH2- Single bond -CH2-
3-1742 Sub-41 4-ClPh -CH2- Single bond -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1743 Sub-42 4-ClPh -CH2- Single bond -CH2-
3-1744 Sub-84 4-ClPh -CH2- Single bond -CH2-
3-1745 Sub-81 4-ClPh -CH2- Single bond -CH2-
3-1746 Sub-48 4-ClPh -CH2- Single bond -CH2-
3-1747 Sub-37 4-FPh -CH2- Single bond -CH2-
3-1748 Sub-38 4-FPh -CH2- Single bond -CH2-
3-1749 Sub-39 4-FPh -CH2- Single bond -CH2-
3-1750 Sub-40 4-FPh -CH2- Single bond -CH2-
3-1751 Sub-41 4-FPh -CH2- Single bond -CH2-
3-1752 Sub-42 4-FPh -CH2- Single bond -CH2-
3-1753 Sub-84 4-FPh -CH2- Single bond -CH2-
3-1754 Sub-81 4-FPh -CH2- Single bond -CH2-
3-1755 Sub-48 4-FPh -CH2- Single bond -CH2-
3-1756 Sub-37 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1757 Sub-38 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1758 Sub-39 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1759 Sub-40 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1760 Sub-41 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1761 Sub-42 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1762 Sub-84 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1763 Sub-81 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1764 Sub-48 3,4-diClPh -CH2- Single bond -CH2CH2-
3-1765 Sub-37 4-ClPh -CH2- Single bond -CH2CH2-
3-1766 Sub-38 4-ClPh -CH2- Single bond -CH2CH2-
3-1767 Sub-39 4-ClPh -CH2- Single bond -CH2CH2-
3-1768 Sub-40 4-ClPh -CH2- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1769 Sub-41 4-ClPh -CH2- Single bond -CH2CH2-
3-1770 Sub-42 4-ClPh -CH2- Single bond -CH2CH2-
3-1771 Sub-84 4-ClPh -CH2- Single bond -CH2CH2-
3-1772 Sub-81 4-ClPh -CH2- Single bond -CH2CH2-
3-1773 Sub-48 4-ClPh -CH2- Single bond -CH2CH2-
3-1774 Sub-37 4-FPh -CH2- Single bond -CH2CH2-
3-1775 Sub-38 4-FPh -CH2- Single bond -CH2CH2-
3-1776 Sub-39 4-FPh -CH2- Single bond -CH2CH2-
3-1777 Sub-40 4-FPh -CH2- Single bond -CH2CH2-
3-1778 Sub-41 4-FPh -CH2- Single bond -CH2CH2-
3-1779 Sub-42 4-FPh -CH2- Single bond -CH2CH2-
3-1780 Sub-84 4-FPh -CH2- Single bond -CH2CH2-
3-1781 Sub-81 4-FPh -CH2- Single bond -CH2CH2-
3-1782 Sub-48 4-FPh -CH2- Single bond -CH2CH2-
3-1783 Sub-37 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1784 Sub-38 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1785 Sub-39 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1786 Sub-40 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1787 Sub-41 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1788 Sub-42 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1789 Sub-84 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1790 Sub-81 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1791 Sub-48 3,4-diClPh -CH2- Single bond -(CH2)3-
3-1792 Sub-37 4-ClPh -CH2- Single bond -(CH2)3-
3-1793 Sub-38 4-ClPh -CH2- Single bond -(CH2)3-
3-1794 Sub-39 4-ClPh -CH2- Single bond -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1795 Sub-40 4-ClPh -CH2- Single bond -(CH2)x-
3-1796 Sub-41 4-ClPh -CH2- Single bond -(CH2)3-
3-1797 Sub-42 4-ClPh -CH2- Single bond -(CH2)3-
3-1798 Sub-84 4-ClPh -CH2- Single bond -(CH2)3-
3-1799 Sub-81 4-ClPh -CH2- Single bond -(CH2)3-
3-1800 Sub-48 4-ClPh -CH2- Single bond -(CH2)3-
3-1801 Sub-37 4-FPh -CH2- Single bond -(CH2)3-
3-1802 Sub-38 4-FPh -CH2- Single bond -(CH2)3-
3-1803 Sub-39 4-FPh -CH2- Single bond -(CH2)3-
3-1804 Sub-40 4-FPh -CH2- Single bond -(CH2)3-
3-1805 Sub-41 4-FPh -CH2- Single bond -(CH2)3-
3-1806 Sub-42 4-FPh -CH2- Single bond -(CH2)3-
3-1807 Sub-84 4-FPh -CH2- Single bond -(CH2)3-
3-1808 Sub-81 4-FPh -CH2- Single bond -(CH2)3-
3-1809 Sub-48 4-FPh -CH2- Single bond -(CH2)3-
3-1810 Sub-37 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1811 Sub-38 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1812 Sub-39 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1813 Sub-40 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1814 Sub-41 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1815 Sub-42 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1816 Sub-84 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1817 Sub-81 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1818 Sub-48 3,4-diClPh -CH2- Single bond -CH2C(Me)2-
3-1819 Sub-37 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1820 Sub-38 4-ClPh -CH2- Single bond -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1821 Sub-39 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1822 Sub-40 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1823 Sub-41 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1824 Sub-42 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1825 Sub-84 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1826 Sub-81 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1827 Sub-48 4-ClPh -CH2- Single bond -CH2C(Me)2-
3-1828 Sub-37 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1829 Sub-38 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1830 Sub-39 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1831 Sub-40 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1832 Sub-41 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1833 Sub-42 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1834 Sub-84 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1835 Sub-81 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1836 Sub-48 4-FPh -CH2- Single bond -CH2C(Me)2-
3-1837 Sub-37 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1838 Sub-38 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1839 Sub-39 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1840 Sub-40 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1841 Sub-41 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1842 Sub-42 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1843 Sub-84 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1844 Sub-81 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1845 Sub-48 3,4-diClPh -CH2- Single bond -CH2-cPr-
3-1846 Sub-37 4-ClPh -CH2- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1847 Sub-38 4-ClPh -CH2- Single bond -CH2-cPr-
3-1848 Sub-39 4-ClPh -CH2- Single bond -CH2-cPr-
3-1849 Sub-40 4-ClPh -CH2- Single bond -CH2-cPr-
3-1850 Sub-41 4-ClPh -CH2- Single bond -CH2-cPr-
3-1851 Sub-42 4-ClPh -CH2- Single bond -CH2-cPr-
3-1852 Sub-84 4-ClPh -CH2- Single bond -CH2-cPr-
3-1853 Sub-81 4-ClPh -CH2- Single bond -CH2-cPr-
3-1854 Sub-48 4-ClPh -CH2- Single bond -CH2-cPr-
3-1855 Sub-37 4-FPh -CH2- Single bond -CH2-cPr-
3-1856 Sub-38 4-FPh -CH2- Single bond -CH2-cPr-
3-1857 Sub-39 4-FPh -CH2- Single bond -CH2-cPr-
3-1858 Sub-40 4-FPh -CH2- Single bond -CH2-cPr-
3-1859 Sub-41 4-FPh -CH2- Single bond -CH2-cPr-
3-1860 Sub-42 4-FPh -CH2- Single bond -CH2-cPr-
3-1861 Sub-84 4-FPh -CH2- Single bond -CH2-cPr-
3-1862 Sub-81 4-FPh -CH2- Single bond -CH2-cPr-
3-1863 Sub-48 4-FPh -CH2- Single bond -CH2-cPr-
3-1864 Sub-37 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1865 Sub-38 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1866 Sub-39 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1867 Sub-40 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1868 Sub-41 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1869 Sub-42 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1870 Sub-84 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1871 Sub-81 3,4-diClPh -CH2- Single bond -C(Me)2-
3-1872 Sub-48 3,4-diClPh -CH2- Single bond -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1873 Sub-37 4-ClPh -CH2- Single bond -C(Me)2-
3-1874 Sub-38 4-ClPh -CH2- Single bond -C(Me)2-
3-1875 Sub-39 4-ClPh -CH2- Single bond -C(Me)2-
3-1876 Sub-40 4-ClPh -CH2- Single bond -C(Me)2-
3-1877 Sub-41 4-ClPh -CH2- Single bond -C(Me)2-
3-1878 Sub-42 4-ClPh -CH2- Single bond -C(Me)2-
3-1879 Sub-84 4-ClPh -CH2- Single bond -C(Me)2-
3-1880 Sub-81 4-ClPh -CH2- Single bond -C(Me)2-
3-1881 Sub-48 4-ClPh -CH2- Single bond -C(Me)2-
3-1882 Sub-37 4-FPh -CH2- Single bond -C(Me)2-
3-1883 Sub-38 4-FPh -CH2- Single bond -C(Me)2-
3-1884 Sub-39 4-FPh -CH2- Single bond -C(Me)2-
3-1885 Sub-40 4-FPh -CH2- Single bond -C(Me)2-
3-1886 Sub-41 4-FPh -CH2- Single bond -C(Me)2-
3-1887 Sub-42 4-FPh -CH2- Single bond -C(Me)2-
3-1888 Sub-84 4-FPh -CH2- Single bond -C(Me)2-
3-1889 Sub-81 4-FPh -CH2- Single bond -C(Me)2-
3-1890 Sub-48 4-FPh -CH2- Single bond -C(Me)2-
3-1891 Sub-37 3,4-diClPh -CH2- -CH2- -CH2-
3-1892 Sub-38 3,4-diClPh -CH2- -CH2- -CH2-
3-1893 Sub-39 3,4-diClPh -CH2- -CH2- -CH2-
3-1894 Sub-40 3,4-diClPh -CH2- -CH2- -CH2-
3-1895 Sub-41 3,4-diClPh -CH2- -CH2- -CH2-
3-1896 Sub-42 3,4-diClPh -CH2- -CH2- -CH2-
3-1897 Sub-84 3,4-diClPh -CH2- -CH2- -CH2-
3-1898 Sub-81 3,4-diClPh -CH2- -CH2- -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1899 Sub-48 3,4-diClPh -CH2- -CH2- -CH2-
3-1900 Sub-37 4-ClPh -CH2- -CH2- -CH2-
3-1901 Sub-38 4-ClPh -CH2- -CH2- -CH2-
3-1902 Sub-39 4-ClPh -CH2- -CH2- -CH2-
3-1903 Sub-40 4-ClPh -CH2- -CH2- -CH2-
3-1904 Sub-41 4-ClPh -CH2- -CH2- -CH2-
3-1905 Sub-42 4-ClPh -CH2- -CH2- -CH2-
3-1906 Sub-84 4-ClPh -CH2- -CH2- -CH2-
3-1907 Sub-81 4-ClPh -CH2- -CH2- -CH2-
3-1908 Sub-48 4-ClPh -CH2- -CH2- -CH2-
3-1909 Sub-37 4-FPh -CH2- -CH2- -CH2-
3-1910 Sub-38 4-FPh -CH2- -CH2- -CH2-
3-1911 Sub-39 4-FPh -CH2- -CH2- -CH2-
3-1912 Sub-40 4-FPh -CH2- -CH2- -CH2-
3-1913 Sub-41 4-FPh -CH2- -CH2- -CH2-
3-1914 Sub-42 4-FPh -CH2- -CH2- -CH2-
3-1915 Sub-84 4-FPh -CH2- -CH2- -CH2-
3-1916 Sub-81 4-FPh -CH2- -CH2- -CH2-
3-1917 Sub-48 4-FPh -CH2- -CH2- -CH2-
3-1918 Sub-37 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1919 Sub-38 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1920 Sub-39 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1921 Sub-40 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1922 Sub-41 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1923 Sub-42 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1924 Sub-84 3,4-diClPh -CH2- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1925 Sub-81 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1926 Sub-48 3,4-diClPh -CH2- -CH2- -CH2CH2-
3-1927 Sub-37 4-ClPh -CH2- -CH2- -CH2CH2-
3-1928 Sub-38 4-ClPh -CH2- -CH2- -CH2CH2-
3-1929 Sub-39 4-ClPh -CH2- -CH2- -CH2CH2-
3-1930 Sub-40 4-ClPh -CH2- -CH2- -CH2CH2-
3-1931 Sub-41 4-ClPh -CH2- -CH2- -CH2CH2-
3-1932 Sub-42 4-ClPh -CH2- -CH2- -CH2CH2-
3-1933 Sub-84 4-ClPh -CH2- -CH2- -CH2CH2-
3-1934 Sub-81 4-ClPh -CH2- -CH2- -CH2CH2-
3-1935 Sub-48 4-ClPh -CH2- -CH2- -CH2CH2-
3-1936 Sub-37 4-FPh -CH2- -CH2- -CH2CH2-
3-1937 Sub-38 4-FPh -CH2- -CH2- -CH2CH2-
3-1938 Sub-39 4-FPh -CH2- -CH2- -CH2CH2-
3-1939 Sub-40 4-FPh -CH2- -CH2- -CH2CH2-
3-1940 Sub-41 4-FPh -CH2- -CH2- -CH2CH2-
3-1941 Sub-42 4-FPh -CH2- -CH2- -CH2CH2-
3-1942 Sub-84 4-FPh -CH2- -CH2- -CH2CH2-
3-1943 Sub-81 4-FPh -CH2- -CH2- -CH2CH2-
3-1944 Sub-48 4-FPh -CH2- -CH2- -CH2CH2-
3-1945 Sub-37 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1946 Sub-38 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1947 Sub-39 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1948 Sub-40 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1949 Sub-41 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1950 Sub-42 3,4-diClPh -CH2- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1951 Sub-84 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1952 Sub-81 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1953 Sub-48 3,4-diClPh -CH2- -CH2- -(CH2)3-
3-1954 Sub-37 4-ClPh -CH2- -CH2- -(CH2)3-
3-1955 Sub-38 4-ClPh -CH2- -CH2- -(CH2)3-
3-1956 Sub-39 4-ClPh -CH2- -CH2- -(CH2)3-
3-1957 Sub-40 4-ClPh -CH2- -CH2- -(CH2)3-
3-1958 Sub-41 4-ClPh -CH2- -CH2- -(CH2)3-
3-1959 Sub-42 4-ClPh -CH2- -CH2- -(CH2)3-
3-1960 Sub-84 4-ClPh -CH2- -CH2- -(CH2)3-
3-1961 Sub-81 4-ClPh -CH2- -CH2- -(CH2)3-
3-1962 Sub-48 4-ClPh -CH2- -CH2- -(CH2)3-
3-1963 Sub-37 4-FPh -CH2- -CH2- -(CH2)3-
3-1964 Sub-38 4-FPh -CH2- -CH2- -(CH2)3-
3-1965 Sub-39 4-FPh -CH2- -CH2- -(CH2)3-
3-1966 Sub-40 4-FPh -CH2- -CH2- -(CH2)3-
3-1967 Sub-41 4-FPh -CH2- -CH2- -(CH2)3-
3-1968 Sub-42 4-FPh -CH2- -CH2- -(CH2)3-
3-1969 Sub-84 4-FPh -CH2- -CH2- -(CH2)3-
3-1970 Sub-81 4-FPh -CH2- -CH2- -(CH2)3-
3-1971 Sub-48 4-FPh -CH2- -CH2- -(CH2)3-
3-1972 Sub-37 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1973 Sub-38 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1974 Sub-39 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1975 Sub-40 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1976 Sub-41 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-1977 Sub-42 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1978 Sub-84 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1979 Sub-81 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1980 Sub-48 3,4-diClPh -CH2- -CH2- -CH2C(Me)2-
3-1981 Sub-37 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1982 Sub-38 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1983 Sub-39 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1984 Sub-40 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1985 Sub-41 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1986 Sub-42 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1987 Sub-84 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1988 Sub-81 4-ClPh -CH2- -CHx- -CH2C(Me)2-
3-1989 Sub-48 4-ClPh -CH2- -CH2- -CH2C(Me)2-
3-1990 Sub-37 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1991 Sub-38 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1992 Sub-39 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1993 Sub-40 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1994 Sub-41 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1995 Sub-42 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1996 Sub-84 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1997 Sub-81 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1998 Sub-48 4-FPh -CH2- -CH2- -CH2C(Me)2-
3-1999 Sub-37 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2000 Sub-38 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2001 Sub-39 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2002 Sub-40 3,4-diClPh -CH2- -CH2- -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2003 Sub-41 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2004 Sub-42 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2005 Sub-84 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2006 Sub-81 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2007 Sub-48 3,4-diClPh -CH2- -CH2- -CH2-cPr-
3-2008 Sub-37 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2009 Sub-38 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2010 Sub-39 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2011 Sub-40 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2012 Sub-41 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2013 Sub-42 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2014 Sub-84 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2015 Sub-81 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2016 Sub-48 4-ClPh -CH2- -CH2- -CH2-cPr-
3-2017 Sub-37 4-FPh -CH2- -CH2- -CH2-cPr-
3-2018 Sub-38 4-FPh -CH2- -CH2- -CH2-cPr-
3-2019 Sub-39 4-FPh -CH2- -CH2- -CH2-cPr-
3-2020 Sub-40 4-FPh -CH2- -CH2- -CH2-cPr-
3-2021 Sub-41 4-FPh -CH2- -CH2- -CH2-cPr-
3-2022 Sub-42 4-FPh -CH2- -CH2- -CH2-cPr-
3-2023 Sub-84 4-FPh -CH2- -CH2- -CH2-cPr-
3-2024 Sub-81 4-FPh -CH2- -CH2- -CH2-cPr-
3-2025 Sub-48 4-FPh -CH2- -CH2- -CH2-cPr-
3-2026 Sub-37 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2027 Sub-38 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2028 Sub-39 3,4-diClPh -CH2- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2029 Sub-40 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2030 Sub-41 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2031 Sub-42 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2032 Sub-84 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2033 Sub-81 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2034 Sub-48 3,4-diClPh -CH2- -CH2- -C(Me)2-
3-2035 Sub-37 4-ClPh -CH2- -CH2- -C(Me)2-
3-2036 Sub-38 4-ClPh -CH2- -CH2- -C(Me)2-
3-2037 Sub-39 4-ClPh -CH2- -CH2- -C(Me)2-
3-2038 Sub-40 4-ClPh -CH2- -CH2- -C(Me)2-
3-2039 Sub-41 4-ClPh -CH2- -CH2- -C(Me)2-
3-2040 Sub-42 4-ClPh -CH2- -CH2- -C(Me)2-
3-2041 Sub-84 4-ClPh -CH2- -CH2- -C(Me)2-
3-2042 Sub-81 4-ClPh -CH2- -CH2- -C(Me)2-
3-2043 Sub-48 4-ClPh -CH2- -CH2- -C(Me)2-
3-2044 Sub-37 4-FPh -CH2- -CH2- -C(Me)2-
3-2045 Sub-38 4-FPh -CH2- -CH2- -C(Me)2-
3-2046 Sub-39 4-FPh -CH2- -CH2- -C(Me)2-
3-2047 Sub-40 4-FPh -CH2- -CH2- -C(Me)2-
3-2048 Sub-41 4-FPh -CH2- -CH2- -C(Me)2-
3-2049 Sub-42 4-FPh -CH2- -CH2- -C(Me)2-
3-2050 Sub-84 4-FPh -CH2- -CH2- -C(Me)2-
3-2051 Sub-81 4-FPh -CH2- -CH2- -C(Me)2-
3-2052 Sub-48 4-FPh -CH2- -CH2- -C(Me)2-
3-2053 Sub-37 3,4-diClPh -SO2- Single bond -CH2-
3-2054 Sub-38 3,4-diClPh -SO2- Single bond -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2055 Sub-39 3,4-diClPh -SO2- Single bond -CH2-
3-2056 Sub-40 3,4-diClPh -SO2- Single bond -CH2-
3-2057 Sub-41 3,4-diClPh -SO2- Single bond -CH2-
3-2058 Sub-42 3,4-diClPh -SO2- Single bond -CH2-
3-2059 Sub-84 3,4-diClPh -SO2- Single bond -CH2-
3-2060 Sub-81 3,4-diClPh -SO2- Single bond -CH2-
3-2061 Sub-48 3,4-diClPh -SO2- Single bond -CH2-
3-2062 Sub-37 4-ClPh -SO2- Single bond -CH2-
3-2063 Sub-38 4-ClPh -SO2- Single bond -CH2-
3-2064 Sub-39 4-ClPh -SO2- Single bond -CH2-
3-2065 Sub-40 4-ClPh -SO2- Single bond -CH2-
3-2066 Sub-41 4-ClPh -SO2- Single bond -CH2-
3-2067 Sub-42 4-ClPh -SO2- Single bond -CH2-
3-2068 Sub-84 4-ClPh -SO2- Single bond -CH2-
3-2069 Sub-81 4-ClPh -SO2- Single bond -CH2-
3-2070 Sub-48 4-ClPh -SO2- Single bond -CH2-
3-2071 Sub-37 4-FPh -SO2- Single bond -CH2-
3-2072 Sub-38 4-FPh -SO2- Single bond -CH2-
3-2073 Sub-39 4-FPh -SO2- Single bond -CH2-
3-2074 Sub-40 4-FPh -SO2- Single bond -CH2-
3-2075 Sub-41 4-FPh -SO2- Single bond -CH2-
3-2076 Sub-42 4-FPh -SO2- Single bond -CH2-
3-2077 Sub-84 4-FPh -SO2- Single bond -CH2-
3-2078 Sub-81 4-FPh -SO2- Single bond -CH2-
3-2079 Sub-48 4-FPh -SO2- Single bond -CH2-
3-2080 Sub-37 3,4-diClPh -SO2- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2081 Sub-38 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2082 Sub-39 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2083 Sub-40 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2084 Sub-41 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2085 Sub-42 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2086 Sub-84 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2087 Sub-81 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2088 Sub-48 3,4-diClPh -SO2- Single bond -CH2CH2-
3-2089 Sub-37 4-ClPh -SO2- Single bond -CH2CH2-
3-2090 Sub-38 4-ClPh -SO2- Single bond -CH2CH2-
3-2091 Sub-39 4-ClPh -SO2- Single bond -CH2CH2-
3-2092 Sub-40 4-ClPh -SO2- Single bond -CH2CH2-
3-2093 Sub-41 4-ClPh -SO2- Single bond -CH2CH2-
3-2094 Sub-42 4-ClPh -SO2- Single bond -CH2CH2-
3-2095 Sub-84 4-ClPh -SO2- Single bond -CH2CH2-
3-2096 Sub-81 4-ClPh -SO2- Single bond -CH2CH2-
3-2097 Sub-48 4-ClPh -SO2- Single bond -CH2CH2-
3-2098 Sub-37 4-FPh -SO2- Single bond -CH2CH2-
3-2099 Sub-38 4-FPh -SO2- Single bond -CH2CH2-
3-2100 Sub-39 4-FPh -SO2- Single bond -CH2CH2-
3-2101 Sub-40 4-FPh -SO2- Single bond -CH2CH2-
3-2202 Sub-41 4-FPh -SO2- Single bond -CH2CH2-
3-2103 Sub-42 4-FPh -SO2- Single bond -CH2CH2-
3-2104 Sub-84 4-FPh -SO2- Single bond -CH2CH2-
3-2105 Sub-81 4-FPh -SO2- Single bond -CH2CH2-
3-2106 Sub-48 4-FPh -SO2- Single bond -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2107 Sub-37 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2108 Sub-38 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2109 Sub-39 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2110 Sub-40 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2111 Sub-41 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2112 Sub-42 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2113 Sub-84 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2114 Sub-81 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2115 Sub-48 3,4-diClPh -SO2- Single bond -(CH2)3-
3-2116 Sub-37 4-ClPh -SO2- Single bond -(CH2)3-
3-2117 Sub-38 4-ClPh -SO2- Single bond -(CH2)3-
3-2118 Sub-39 4-ClPh -SO2- Single bond -(CH2)3-
3-2119 Sub-40 4-ClPh -SO2- Single bond -(CH2)3-
3-2120 Sub-41 4-ClPh -SO2- Single bond -(CH2)3-
3-2121 Sub-42 4-ClPh -SO2- Single bond -(CH2)3-
3-2122 Sub-84 4-ClPh -SO2- Single bond -(CH2)3-
3-2123 Sub-81 4-ClPh -SO2- Single bond -(CH2)3-
3-2124 Sub-48 4-ClPh -SO2- Single bond -(CH2)3-
3-2125 Sub-37 4-FPh -SO2- Single bond -(CH2)3-
3-2126 Sub-38 4-FPh -SO2- Single bond -(CH2)3-
3-2127 Sub-39 4-FPh -SO2- Single bond -(CH2)3-
3-2128 Sub-40 4-FPh -SO2- Single bond -(CH2)3-
3-2129 Sub-41 4-FPh -SO2- Single bond -(CH2)3-
3-2130 Sub-42 4-FPh -SO2- Single bond -(CH2)3-
3-2131 Sub-84 4-FPh -SO2- Single bond -(CH2)3-
3-2132 Sub-81 4-FPh -SO2- Single bond -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2133 Sub-48 4-FPh -SO2- Single bond -(CH2)3-
3-2134 Sub-37 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2135 Sub-38 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2136 Sub-39 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2137 Sub-40 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2138 Sub-41 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2139 Sub-42 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2140 Sub-84 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2141 Sub-81 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-2142 Sub-48 3,4-diClPh -SO2- Single bond -CH2C(Me)2-
3-143 Sub-37 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2144 Sub-38 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2145 Sub-39 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2146 Sub-4O 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2147 Sub-41 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2148 Sub-42 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2149 Sub-84 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2150 Sub-81 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2151 Sub-48 4-ClPh -SO2- Single bond -CH2C(Me)2-
3-2152 Sub-37 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2153 Sub-38 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2154 Sub-39 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2155 Sub-40 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2156 Sub-41 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2157 Sub-42 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2158 Sub-84 4-FPh -SO2- Single bond -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2159 Sub-81 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2160 Sub-48 4-FPh -SO2- Single bond -CH2C(Me)2-
3-2161 Sub-37 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2162 Sub-38 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2163 Sub-39 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2164 Sub-40 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2165 Sub-41 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2166 Sub-42 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2167 Sub-84 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2168 Sub-81 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2169 Sub-48 3,4-diClPh -SO2- Single bond -CH2-cPr-
3-2170 Sub-37 4-ClPh -SO2- Single bond -CH2-cPr-
3-2171 Sub-38 4-ClPh -SO2- Single bond -CH2-cPr-
3-2172 Sub-39 4-ClPh -SO2- Single bond -CH2-cPr-
3-2173 Sub-40 4-ClPh -SO2- Single bond -CH2-cPr-
3-2174 Sub-41 4-ClPh -SO2- Single bond -CH2-cPr-
3-2175 Sub-42 4-ClPh -SO2- Single bond -CH2-cPr-
3-2176 Sub-84 4-ClPh -SO2- Single bond -CH2-cPr-
3-2177 Sub-81 4-ClPh -SO2- Single bond -CH2-cPr-
3-2178 Sub-48 4-ClPh -SO2- Single bond -CH2-cPr-
3-2179 Sub-37 4-FPh -SO2- Single bond -CH2-cPr-
3-2180 Sub-38 4-FPh -SO2- Single bond -CH2-cPr-
3-2181 Sub-39 4-FPh -SO2- Single bond -CH2-cPr-
3-2182 Sub-40 4-FPh -SO2- Single bond -CH2-cPr-
3-2183 Sub-41 4-FPh -SO2- Single bond -CH2-cPr-
3-2184 Sub-42 4-FPh -SO2- Single bond -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2185 Sub-84 4-FPh -SO2- Single bond -CH2-cPr-
3-2186 Sub-81 4-FPh -SO2- Single bond -CH2-cPr-
3-2187 Sub-48 4-FPh -SO2- Single bond -CH2-cPr-
3-2188 Sub-37 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2189 Sub-38 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2190 Sub-39 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2191 Sub-40 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2192 Sub-41 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2193 Sub-42 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2194 Sub-84 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2195 Sub-81 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2196 Sub-48 3,4-diClPh -SO2- Single bond -C(Me)2-
3-2197 Sub-37 4-ClPh -SO2- Single bond -C(Me)2-
3-2198 Sub-38 4-ClPh -SO2- Single bond -C(Me)2-
3-2199 Sub-39 4-ClPh -SO2- Single bond -C(Me)2-
3-2200 Sub-40 4-ClPh -SO2- Single bond -C(Me)2-
3-2201 Sub-41 4-ClPh -SO2- Single bond -C(Me)2-
3-2202 Sub-42 4-ClPh -SO2- Single bond -C(Me)2-
3-2203 Sub-84 4-ClPh -SO2- Single bond -C(Me)2-
3-2204 Sub-81 4-ClPh -SO2- Single bond -C(Me)2-
3-2205 Sub-48 4-ClPh -SO2- Single bond -C(Me)2-
3-2206 Sub-37 4-FPh -SO2- Single bond -C(Me)2-
3-2207 Sub-38 4-FPh -SO2- Single bond -C(Me)2-
3-2208 Sub-39 4-FPh -SO2- Single bond -C(Me)2-
3-2209 Sub-40 4-FPh -SO2- Single bond -C(Me)2-
3-2210 Sub-41 4-FPh -SO2- Single bond -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2211 Sub-42 4-FPh -SO2- Single bond -C(Me)2-
3-2212 Sub-84 4-FPh -SO2- Single bond -C(Me)2-
3-2213 Sub-81 4-FPh -SO2- Single bond -C(Me)2-
3-2214 Sub-48 4-FPh -SO2- Single bond -C(Me)2-
3-2215 Sub-37 3,4-diClPh -SO2- -CH2- -CH2-
3-2216 Sub-38 3,4-diClPh -SO2- -CH2- -CH2-
3-2217 Sub-39 3,4-diClPh -SO2- -CH2- -CH2-
3-2218 Sub-40 3,4-diClPh -SO2- -CH2- -CH2-
3-2219 Sub-41 3,4-diClPh -SO2- -CH2- -CH2-
3-2220 Sub-42 3,4-diClPh -SO2- -CH2- -CH2-
3-2221 Sub-84 3,4-diClPh -SO2- -CH2- -CH2-
3-2222 Sub-81 3,4-diClPh -SO2- -CH2- -CH2-
3-2223 Sub-48 3,4-diClPh -SO2- -CH2- -CH2-
3-2224 Sub-37 4-ClPh -SO2- -CH2- -CH2-
3-2225 Sub-38 4-ClPh -SO2- -CH2- -CH2-
3-2226 Sub-39 4-ClPh -SO2- -CH2- -CH2-
3-2227 Sub-40 4-ClPh -SO2- -CH2- -CH2-
3-2228 Sub-41 4-ClPh -SO2- -CH2- -CH2-
3-2229 Sub-42 4-ClPh -SO2- -CH2- -CH2-
3-2230 Sub-84 4-ClPh -SO2- -CH2- -CH2-
3-2231 Sub-81 4-ClPh -SO2- -CH2- -CH2-
3-2232 Sub-48 4-ClPh -SO2- -CH2- -CH2-
3-2233 Sub-37 4-FPh -SO2- -CH2- -CH2-
3-2234 Sub-38 4-FPh -SO2- -CH2- -CH2-
3-2235 Sub-39 4-FPh -SO2- -CH2- -CH2-
3-2236 Sub-40 4-FPh -SO2- -CH2- -CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2237 Sub-41 4-FPh -SO2- -CH2- -CH2-
3-2238 Sub-42 4-FPh -SO2- -CH2- -CH2-
3-2239 Sub-84 4-FPh -SO2- -CH2- -CH2-
3-2240 Sub-81 4-FPh -SO2- -CH2- -CH2-
3-2241 Sub-48 4-FPh -SO2- -CH2- -CH2-
3-2242 Sub-37 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2243 Sub-38 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2244 Sub-39 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2245 Sub-40 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2246 Sub-41 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2247 Sub-42 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2248 Sub-84 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2249 Sub-81 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2250 Sub-48 3,4-diClPh -SO2- -CH2- -CH2CH2-
3-2251 Sub-37 4-ClPh -SO2- -CH2- -CH2CH2-
3-2252 Sub-38 4-ClPh -SO2- -CH2- -CH2CH2-
3-2253 Sub-39 4-ClPh -SO2- -CH2- -CH2CH2-
3-2254 Sub-40 4-ClPh -SO2- -CH2- -CH2CH2-
3-2255 Sub-4l 4-ClPh -SO2- -CH2- -CH2CH2-
3-2256 Sub-42 4-ClPh -SO2- -CH2- -CH2CH2-
3-2257 Sub-84 4-ClPh -SO2- -CH2- -CH2CH2-
3-2258 Sub-81 4-ClPh -SO2- -CH2- -CH2CH2-
3-2259 Sub-48 4-ClPh -SO2- -CH2- -CH2CH2-
3-2260 Sub-37 4-FPh -SO2- -CH2- -CH2CH2-
3-2261 Sub-38 4-FPh -SO2- -CH2- -CH2CH2-
3-2262 Sub-39 4-FPh -SO2- -CH2- -CH2CH2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2263 Sub-40 4-FPh -SO2- -CH2- -CH2CH2-
3-2264 Sub-41 4-FPh -SO2- -CH2- -CH2CH2-
3-2265 Sub-42 4-FPh -SO2- -CH2- -CH2CH2-
3-2266 Sub-84 4-FPh -SO2- -CH2- -CH2CH2-
3-2267 Sub-81 4-FPh -SO2- -CH2- -CH2CH2-
3-2268 Sub-48 4-FPh -SO2- -CH2- -CH2CH2-
3-2269 Sub-37 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2270 Sub-38 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2271 Sub-39 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2272 Sub-40 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2273 Sub-41 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2274 Sub-42 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2275 Sub-84 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2276 Sub-81 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2277 Sub-48 3,4-diClPh -SO2- -CH2- -(CH2)3-
3-2278 Sub-37 4-ClPh -SO2- -CH2- -(CH2)3-
3-2279 Sub-38 4-ClPh -SO2- -CH2- -(CH2)3-
3-2280 Sub-39 4-ClPh -SO2- -CH2- -(CH2)3-
3-2281 Sub-40 4-ClPh -SO2- -CH2- -(CH2)3-
3-2282 Sub-41 4-ClPh -SO2- -CH2- -(CH2)3-
3-2283 Sub-42 4-ClPh -SO2- -CH2- -(CH2)3-
3-2284 Sub-84 4-ClPh -SO2- -CH2- -(CH2)3-
3-2285 Sub-81 4-ClPh -SO2- -CH2- -(CH2)3-
3-2286 Sub-48 4-ClPh -SO2- -CH2- -(CH2)3-
3-2287 Sub-37 4-FPh -SO2- -CH2- -(CH2)3-
3-2288 Sub-38 4-FPh -SO2- -CH2- -(CH2)3-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2289 Sub-39 4-FPh -SO2- -CH2- -(CH2)3-
3-2290 Sub-40 4-FPh -SO2- -CH2- -(CH2)3-
3-2291 Sub-41 4-FPh -SO2- -CH2- -(CH2)3-
3-2292 Sub-42 4-FPh -SO2- -CH2- -(CH2)3-
3-2293 Sub-84 4-FPh -SO2- -CH2- -(CH2)3-
3-2294 Sub-81 4-FPh -SO2- -CH2- -(CH2)3-
3-2295 Sub-48 4-FPh -SO2- -CH2- -(CH2)3-
3-2296 Sub-37 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2297 Sub-38 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2298 Sub-39 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2299 Sub-40 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2300 Sub-41 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2301 Sub-42 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2302 Sub-84 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2303 Sub-81 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2304 Sub-48 3,4-diClPh -SO2- -CH2- -CH2C(Me)2-
3-2305 Sub-37 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2306 Sub-38 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2307 Sub-39 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2308 Sub-40 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2309 Sub-41 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2310 Sub-42 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2311 Sub-84 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2312 Sub-81 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2313 Sub-48 4-ClPh -SO2- -CH2- -CH2C(Me)2-
3-2314 Sub-37 4-FPh -SO2- -CH2- -CH2C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2315 Sub-38 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2316 Sub-39 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2317 Sub-40 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2318 Sub-41 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2319 Sub-42 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2320 Sub-84 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2321 Sub-81 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2322 Sub-48 4-FPh -SO2- -CH2- -CH2C(Me)2-
3-2323 Sub-37 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2324 Sub-38 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2325 Sub-39 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2326 Sub-40 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2327 Sub-41 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2328 Sub-42 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2329 Sub-84 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2330 Sub-81 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2331 Sub-48 3,4-diClPh -SO2- -CH2- -CH2-cPr-
3-2332 Sub-37 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2333 Sub-38 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2334 Sub-39 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2335 Sub-40 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2336 Sub-41 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2337 Sub-42 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2338 Sub-84 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2339 Sub-81 4-ClPh -SO2- -CH2- -CH2-cPr-
3-2340 Sub-48 4-ClPh -SO2- -CH2- -CH2-cPr-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2341 Sub-37 4-FPh -SO2- -CH2- -CH2-cPr-
3-2342 Sub-38 4-FPh -SO2- -CH2- -CH2-cPr-
3-2343 Sub-39 4-FPh -SO2- -CH2- -CH2-cPr-
3-2344 Sub-40 4-FPh -SO2- -CH2- -CH2-cPr-
3-2345 Sub-41 4-FPh -SO2- -CH2- -CH2-cPr-
3-2346 Sub-42 4-FPh -SO2- -CH2- -CH2-cPr-
3-2347 Sub-84 4-FPh -SO2- -CH2- -CH2-cPr-
3-2348 Sub-81 4-FPh -SO2- -CH2- -CH2-cPr-
3-2349 Sub-48 4-FPh -SO2- -CH2- -CH2-cPr-
3-2350 Sub-37 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2351 Sub-38 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2352 Sub-39 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2353 Sub-40 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2354 Sub-41 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2355 Sub-42 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2356 Sub-84 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2357 Sub-81 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2358 Sub-48 3,4-diClPh -SO2- -CH2- -C(Me)2-
3-2359 Sub-37 4-ClPh -SO2- -CH2- -C(Me)2-
3-2360 Sub-38 4-ClPh -SO2- -CH2- -C(Me)2-
3-2361 Sub-39 4-ClPh -SO2- -CH2- -C(Me)2-
3-2362 Sub-40 4-ClPh -SO2- -CH2- -C(Me)2-
3-2363 Sub-41 4-ClPh -SO2- -CH2- -C(Me)2-
3-2364 Sub-42 4-ClPh -SO2- -CH2- -C(Me)2-
3-2365 Sub-84 4-ClPh -SO2- -CH2- -C(Me)2-
3-2366 Sub-81 4-ClPh -SO2- -CH2- -C(Me)2-
Table 3(cont.)
Compound (I) A serial number. R1 R2 A B E
3-2367 Sub-48 4-ClPh -SO2- -CH2- -C(Me)2-
3-2368 Sub-37 4-FPh -SO2- -CH2- -C(Me)2-
3-2369 Sub-38 4-FPh -SO2- -CH2- -C(Me)2-
3-2370 Sub-39 4-FPh -SO2- -CH2- -C(Me)2-
3-2371 Sub-40 4-FPh -SO2- -CH2- -C(Me)2-
3-2372 Sub-41 4-FPh -SO2- -CH2- -C(Me)2-
3-2373 Sub-42 4-FPh -SO2- -CH2- -C(Me)2-
3-2374 Sub-84 4-FPh -SO2- -CH2- -C(Me)2-
3-2375 Sub-81 4-FPh -SO2- -CH2- -C(Me)2-
3-2376 Sub-48 4-FPh -SO2- -CH2- -C(Me)2-
Among the compounds listed above, the following compounds, i.e., compounds No.1-1025 to 1-1536, 2-1537 to 2-1728, 2-1825 to 2-19202-1969 to 2-2016, 2-2113 to 2-2160, 2-2257 to 2-2352, 3-1 to 3-64, and 3-97 to 3-160 are preferred.
More preferred are the compounds No.1-1089 to 1-1120, 1-1217 to 1-1280, 1-1313 to 1-1344, 1-1505 to 1-1536, 2-1825 to 2-1920, 2-1969 to 2-2016, 2-2257 to 2-2352, 3-5 to 3-11, 3-17, 3-18, 3-37 to 3-43, 3-49, 3-50, 3-101 to 3-107, 3-113, 3-114, 3-133 to 3-139, 3-145 and 3-146.
Still more preferred are the compounds No.1-1089 to 1-1120, 1-1313 to 1-1344, 2-1969 to 2-2016, 3-7, 3-8, 3-10, 3-11, 3-39, 3-40, 3-42, 3-43, 3-103,3-104, 3-106, 3-107, 3-135, 3-136, 3-138, and 3-139.
The most preferred compounds of the invention are:
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-N, N-dimethylformamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenyl-4 (pyrrol-1-ylcarbonyl) piperidine;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-morpholinocarbonyl-4-phenylpiperidine;
1- {2- [2- (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isobenzofuran-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]-2-oxide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidin]-3(4H) -one;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isobenzofuran-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]-2-oxide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidin]-3(4H) -one;
1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (5R) - (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (5R) - (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide; and
1- {2- [ (2R) - (4-fluorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2 yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4-piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -5, 5-dimethyl-4- (3, 4, 5) -trimethoxybenzoyl) -morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
the compounds of the present invention can be prepared according to known methods for preparing such compounds, for example, as shown in reaction schemes A and J below.
Reaction scheme A:wherein R is1,R2A, B, D, E, G and L are as defined above.
X, X ', Y, Y ' and Y ' may be any group or atom capable of being eliminated as a nucleophilic residue, without particular limitation. Examples of preferred such groups and atoms include: halogen atoms such as chlorine, bromine and iodine atoms; trihalomethoxy, such as trichloromethoxy; alkylsulfonyloxy groups having 1 to 6 carbon atoms, such as methylsulfonyloxyand ethylsulfonyloxy; haloalkanesulfonyloxy having 1 to 6 carbon atoms, such as trifluoromethanesulfonyloxy and pentafluoroethanesulfonyloxy; and arylsulfonyloxy groups such as benzenesulfonyloxy, p-toluenesulfonyloxy and p-nitrobenzenesulfonyloxy. Among these groups, a halogen atom and an alkylsulfonyloxy group are preferable.
X may be bound to R10The bonds form single bonds. In this case, the compound of formula (III) becomes an acid anhydride.
The group represented by E' corresponds to the group represented by E, but the number of carbon atoms therein is one less than that in an alkylene or cycloalkane-1, 1-diylmethyl or cycloalkane-1, 1-di (ylmethyl) group having 1 to 4 carbon atoms.
The group represented by G' corresponds to the group represented by G, but the number of carbon atoms therein is one less than that in an alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 4 carbon atoms.
R10Represents a carboxyl protecting group which can be eliminated chemically, for example by hydrogenolysis, hydrolysis, electrolysis or photolysis. Examples of such protecting groups preferred in the reaction include:
alkyl groups having 1 to 6 carbon atoms, e.g. those at R5The examples listed in (1);
alkenyl groups having 2 to 6 carbon atoms such as vinyl, 1-propenyl, 2-propenyl, 1-methyl-1-propenyl, 2-methyl-2-propenyl, 2-ethyl-2-propenyl, 1-butenyl, 2-butenyl, 1-methyl-1-butenyl, 3-methyl-2-butenyl, 1-ethyl-2-butenyl, 3-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl, 1-ethyl-3-butenyl, 1-pentenyl, 2-pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-pentenyl, 1-methylalen-3-pentenyl, 2-methyl-3-pentenyl, 4-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, and 5-hexenyl.
Alkynyl having 2 to 6 carbon atoms such as ethynyl, 2-propynyl, 1-methyl-2-propynyl, 2-butynyl, 1-methyl-2-butynyl, 1-ethyl-2-butynyl, 3-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 1-ethyl-3-butynyl, 2-pentynyl, 1-methyl-2-pentynyl, 4-methyl-2-pentynyl, 3-pentynyl, 1-methyl-3-pentynyl, 2-methyl-3-pentynyl, 4-pentynyl, 1-methyl-4-pentynyl, 2-methyl-4-pentynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, and 5-hexynyl groups;
haloalkyl having 1 to 6 carbon atoms as exemplified above for substituent α;
hydroxyalkyl groups such as hydroxymethyl, 2-hydroxyethyl, 2, 3-dihydroxypropyl, 3-hydroxypropyl, 3, 4-dihydroxybutyl, and 4-hydroxybutyl;
fatty acyl substituted alkyl groups such as an acetylmethyl group;
aralkyl radicals, such as those previously mentioned R5The examples listed in (1) and the like; and silyl groups such as those exemplified in the aforementioned ester groups.
R11Represents a hydroxyl protecting group which can be removed by chemical means, such as hydrogenolysis, hydrolysis, electrolysis, or photolysis. Examples of preferred protecting groups such as hydroxyl include:
acyl (including alkanoyl, haloalkanoyl, alkoxyalkyl acyl, alkenylacyl and alkynoyl) groups, such as those described above for R5The examples listed in (1);
arylacyl (including halo-substituted, alkyl-substituted, alkoxy-substituted, nitro-substituted, alkoxycarbonyl-substituted and aryl-substituted aromatic acyl groups), such as those described above for R5The examples listed in (1);
tetrahydrofuran or tetrahydrothiopyran groups, such as those exemplified above for the ester groups;
tetrahydrofuran or tetrahydrothienyl, such as those exemplified above forthe ester group;
silyl groups such as those exemplified in the above ester groups;
alkoxymethyl groups such as those exemplified in the above ester groups;
substituted ethyl groups such as those exemplified in the above ester groups;
aralkyl radicals, such as those mentioned above for R5Examples of which are listed above;
alkoxycarbonyl groups such as those exemplified above for substituent α;
alkenyloxycarbonyl radicals, such as those exemplified above for the ester radical; and
an aralkyloxycarbonyl group such as those exemplified above for the ester group.
R12Represents a hydrogen atom or11The hydroxyl protecting groups listed in (1). Step A1
In this step, the Friedel-Crafts reaction of the compound of the formula (II) with the acid derivative of the formula (III) is carried out in a solvent in the presence of a Lewis acid (step A1a), optionally with R when the acid derivative of the formula (III) is an acid anhydride10Esterifying the resulting free carboxylic acid group (step A1b), and then converting the carbonyl group by a Wittig reaction in a solvent in the presence of a baseExomethylene (step A1c), thus producing a compound of formula (IV). Step A1a
There is no particular restriction on the nature of the Lewis acid used in the Friedel-Crafts reaction, and any Lewis acid commonly used in this type of reaction may be used. Examples of such Lewis acids include: III (C)1-C6Alkyl) silyl triflates, such as trimethylsilyl triflate; aluminum salts such as aluminum chloride; tin salts, such as tin tetrachloride; zinc salts, such as zinc bromide; titanium salts, such astitanium tetrachloride; perchlorates, such as trimethylsilyl perchlorate or triphenylmethyl perchlorate. Among them, aluminum salts and titanium salts are preferable, and aluminum chloride is particularly preferable.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, isopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diethylene glycol dimethyl ether; nitro compounds, such as nitromethane and nitrobenzene. Among them, halogenated hydrocarbons are particularly preferable.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the purposes of the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. In general, however, we carry out the reaction at a temperature in the range from-10 to 150 ℃ and preferably from 0 to 100 ℃. The reaction time may also vary over a wide time range, depending on many factors, such as, inter alia, the reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferable conditions, the reaction is generally carried out for 30 minutes to 24 hours, preferably 1 to 12 hours. Step A1b
When the esterification in this step is an alkylation reaction, the reaction can be completed by any of the following steps. Step A1b (i)
The resulting carboxylic acids may be used with formulaWherein:
R10is as defined above, and
x' represents a residue which can be eliminated as a nucleophile, such as a halogen atom (e.g., chlorine, bromine or iodine atom), an alkylcarbonacyloxy group having 1 to 6 carbon atoms (e.g., methanesulfonyloxy or ethanesulfonyloxy); haloalkanesulfonyloxy having 1 to 6 carbon atoms (e.g., trifluoromethanesulfonyloxy or pentafluoroethanesulfonyloxy); arylsulfonyloxy (e.g., benzenesulfonyloxy, p-toluenesulfonyloxy, or p-nitrobenzenesulfonyloxy).
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane or heptane; aromatic hydrocarbons such as benzene, toluene or xylene; halogenated hydrocarbons, such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene or dichlorobenzene; an ether; such as diethyl ether, isopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane or diglyme; ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isopropyl ketone or cyclohexanone; nitriles, such as acetonitrile or isobutyronitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone and hexamethylphosphoric triamide.
The reaction is generally and preferably carried out in the presence of a base. Likewise, there is no particular limitation on the nature of the base used, and any base that has been used in this type of reaction may be used here. Examples of such bases include: alkali metal carbonates, sodium carbonate, potassium carbonate and lithium carbonate; alkali metal bicarbonates, such as sodium bicarbonate, carbocyclic potassium bicarbonate and lithium bicarbonate; alkali metal hydrides such as lithium hydride, sodium hydride, potassium hydride; alkali metal hydroxides such as sodium hydroxide, potassium hydroxide, barium hydroxide, lithium hydroxide; alkali metal fluorides such as lithium fluoride, sodium fluoride and potassium fluoride; alkali metal alkoxides such as sodium methoxide, sodium ethoxide, potassium methoxide, potassium ethoxide, potassium tert-butoxide, and lithium methoxide; alkali metal mercaptides such as sodium methyl mercaptide and sodium ethyl mercaptide; organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyridopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N-dimethylaniline, N-diethylaniline, 1, 5-diazabicyclo [4, 3, 0]non-5-ene (DBN), 1, 4-diazabicyclo [2, 2, 2]octane (DABCO), 1, 8-diazabicyclo [5, 4, 0]undec-7-ene (DBU); and organometallic bases such as butyllithium, lithium diisopropylamide and lithium bis (trimethylsilyl) amide.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. In general, however, we carry out the reaction at a temperature in the range from-20 to 120 ℃ and preferably from 0 to 80 ℃. The reaction time may also vary over a wide time range, depending on many factors, such as, inter alia, the reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 0.5 to 10 hours. Step A1b (ii)
The resulting carboxylic acids may be used with formulaCompound of [ in which R10As defined above]The alkylation is accomplished using a condensation reagent reaction.
There are no particular restrictions on the nature of the condensing agent used, and any condensing agent which has been used in reactions of this type can be used here. Examples of such condensing agents include: (1) a combination of phosphate esters including (e.g., diphenylphosphoryl azide or diethylcyanophosphate) and one or more of the following bases; (2) carbodiimides (e.g., 1, 3-dicyclohexylcarbodiimide, 1, 3-diisopropylcarbodiimide or 1-2 yl-3- (3-dimethylaminopropyl) carbodiimide); a combination of one or more of the above carbodiimides and one or more of the following bases; or a combination of one or more of the above carbodiimides and an N-hydroxy compound (e.g., N-hydroxysuccinimide, 1-hydroxybenzotriazole or N-hydroxy-5-norbornene-2, 3-dicarboximide); (3) combinations of disulfides (e.g., 2, 2 '-dipyridyl disulfide or 2, 2' -dibenzothiazolyl disulfide, etc.) and phosphines (e.g., triphenylphosphine or tributylphosphine); (4) carbonates [ e.g. N, N-disuccinimidyl carbonate, di-2-pyridyl carbonate or S, S' -bis (1-phenyl-1H-tetrazol-5-yl) dithiocarbonate](ii) a (5) Phosphinophosphonic acid chlorides [ e.g., N, N' -bis (2-oxo-3-oxazolidinyl) phosphinic acid chloride phosphonic acid chloride](ii) a (6) Oxalate [ e.g., N, N '-disuccinimidyl oxalate, N, N' -diphosphthalimide oxalate, N, N '-bis (5-norbornene-2, 3-dienimiyl) oxalate, 1, 1' -bis (benzotriazolyl) oxalate, 1, 1 '-bis (6-chlorobenzotriazolyl) oxalate or 1, 1' -bis (6-trifluoromethylbenzotriazolyl) oxalate](ii) a (7) One or more of the above phosphines and one or more of azodicarboxylate or azodicarboxylate amide (e.g. diethyl azodicarboxylate, 1, 1' - (azodicarbonyl) dipiperidine]Or a mixture of one or more of the above phosphines with one or more of the following bases; (8) n-alkyl-5-aryl isoxazolium-3' -iodates with the alkyl moiety having 1-6 carbon atoms and the aryl moiety as defined above for R1Examples of which are listed above. (e.g., N-ethyl-5-phenylisoxazolium-3' -sulfonate); (9) a diheterocyclic aryl diselenide (e.g., bis-2-pyridyl diselenide); (10) arylsulfonyltriazoles in which the aryl radical is as defined for R above1Examples of which are listed above. (for example,p-nitrobenzenesulfonyltriazolate); (11) 2-halo-1-alkylpyridinium halides in which the alkyl moiety has 1 to 6 carbon atoms (e.g., 2-chloro-1-methylpyridinium iodide); (12) imidazoles (e.g., 1, 1 '-oxalyl diimidazole, N' -carbonyldiimidazole); (13) 3-alkyl-2-halo-benzothiazolium fluoroborates in which the alkyl moiety has 1 to 6 carbon atoms (e.g., 3-ethyl-2-chloro-benzothiazolium fluoroborate); (14) 3-alkylbenzothiazol-2-Serone wherein the alkyl moiety has 1 to 6 carbon atoms (e.g., 3-methylbenzothiazole-2-Serone); (15) phosphate esters (e.g., phenyl dichlorophosphate or polyphosphate) (16) halosulfonylisocyanates (e.g., chlorosulfonyl isocyanate); (17) halosilanes (e.g., trimethylsilyl chloride or triethylsilyl chloride); (18) combinations of alkyl sulfonyl halides having 1 to 6 carbon atoms (e.g., methanesulfonyl chloride) and one or more of the following bases; and (19) N, N, N ', N' -tetraalkylhaloformamidinium chlorides wherein each alkyl group has from 1 to 6 carbon atoms (e.g., N, N, N ', N' -tetramethylchloroformamidinium chloride).
Of these, we prefer compositions of carbodiimides or phosphines with azodicarboxylic acid esters or azodicarboxylic acid amides.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, so long as it does not adversely affect the reaction or the reagents used, and at leastsome amount of the reagents may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and glyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline.
If desired, 4- (N, N-dimethylamino) pyridine or 4-pyrrolidinopyridine may be used in catalytic amounts, in combination with one or more other bases. If desired, the reaction may be carried out in the presence of one or more of the following reagents to enhance the efficiency of the reaction: a dehydrating agent (e.g., a molecular sieve), a quaternary ammonium salt (e.g., benzyltriethylammonium chloride or tetrabutylammonium chloride), a crown ether (e.g., dibenzo-18-crown-6), and an acid scavenger (e.g., 3, 4-dihydro-2H-pyrido [1, 2-a]pyrimidin-2-one).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularlyrequired for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step A1b (iii)
The resulting carboxylic acid may be alkylated by reaction with the corresponding alcohol (e.g., methanol, ethanol, propanol, or butanol) to introduce a lower alkyl protecting group.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: the same alcohols as the reactants; aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane or glyme; ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone or cyclohexanone; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) or hexamethylphosphoric triamide. Among them, the same alcohol as the reactant is preferable.
The reaction is carried out in the presence of an acid catalyst. Likewise, there is no particular limitation on the nature of the acid catalyst used, and any acid catalyst commonly used in this type of reaction may be used here. Examples of such acid catalysts include: bronsted acids such as inorganic acids (e.g., hydrochloric acid, hydrobromic acid, sulfuric acid, perchloric acid or phosphoric acid) and organic acids (e.g., acetic acid, formic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, trifluoroacetic acid or trifluoromethanesulfonic acid); and Lewis acids (e.g., boron trichloride, boron trifluoride, boron tribromide) or acid ion exchange resins.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of from 0 to 150 ℃ and preferably from 50 to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 5 hours. Step A1c
In the Wittig reaction, too, there is no particular restriction on the nature of the Wittig reagent used, and any Wittig-type reagent commonly used in this type of reaction can be used here. Examples of such Wittig reagents include: methyl triphenyl halides such as methyl triphenyl phosphonium bromide and methyl triphenyl phosphonium iodide.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran; nitriles such as acetonitrile and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, and hexamethylphosphoric triamide; and sulfoxides such as dimethyl sulfoxide and sulfolane. Among them, we prefer aromatic hydrocarbons, and particularly prefer benzene.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal bicarbonates, such as sodium bicarbonate, potassium bicarbonate and lithium bicarbonate; alkali metal hydrides such as lithium hydride, sodium hydride, potassium hydride; alkali metal and alkaline earth metal hydroxides such as sodium hydroxide, potassium hydroxide, barium hydroxide and lithium hydroxide; alkali metal fluorides such as sodium fluoride, potassium fluoride; and alkali metal alcoholates such as sodium methylate, sodium ethylate, potassium methylate, potassium ethylate, potassium tert-butylate and lithium methylate. Among them, alkali metal hydrides and alkali metal alcoholates are preferred, and metal alcoholates are particularly preferred.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, thestarting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 100 ℃ and preferably 0 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 12 hours. Step A2
In this step, the ester group in the compound of formula (IV) (prepared from step A1) is reduced in a solvent using a reducing agent to convert it to a primary hydroxyl group, and R is used11The hydroxyl group is protected.
There is no particular limitation on the nature of the reducing agent used, and any reducing agent commonly used in this type of reaction may be used here. Examples of such reducing agents include: hydride reagents such as alkali metal borohydrides (e.g., sodium borohydride or lithium borohydride), aluminum hydride compounds (e.g., lithium aluminum hydride or lithium tri-t-butoxide hydride), sodium tellurite hydride, and organic aluminum hydride reducing agents [ e.g., diisobutylaluminum hydride or sodium bis (methoxyethoxy) aluminum hydride]. Among them, we prefer an aluminum hydride compound and an organic aluminum hydride reducing agent, and particularly prefer an aluminum hydride compound.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; and ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and glyme. Among them, we prefer ethers, and particularly prefer diethyl ether and tetrahydrofuran.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature of-78 to 50 ℃ and preferably-20 to 20 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 5 minutes to 24 hours, preferably 10 minutes to 2 hours.
The protecting group R may be introduced by any of the following methods11. Step A2(i)
Can be used without protectionWith a suitable amount, preferably 1-4 equivalents (more preferably 2-3 equivalents), of a compound of the formulaCompound orCompound (in the latter compound)R11Acyl) to introduce a protecting group R11. Wherein the content of the first and second substances,
R11as defined above, silyl groups are preferred, with tert-butyldimethylsilyl group being particularly preferred;
x' represents any group which can be eliminated as a nucleophilic residue, for example, a halogen atom such as a chlorine, bromine or iodine atom; an alkoxycarbonyloxy group such as a methoxycarbonyloxy group or an ethoxycarbonyloxy group having 1 to 6 carbon atoms in the alkoxy moiety; haloalkoyloxy having 2 to 6 carbon atoms, such as chloroacetyloxy, dichloroacetoxy, trichloroacetoxy or trifluoroacetyloxy; alkylsulfonyloxy groups having 1 to 6 carbon atoms, such as methanesulfonyloxy or ethanesulfonyloxy groups; haloalkanesulfonyloxy having 1 to 6 carbon atoms, such as trifluoromethanesulfonyloxy or pentafluoroethanesulfonyloxy; arylsulfonyloxy groups in which the aryl moiety is as above R1Examples of the above-mentioned groups include benzenesulfonyloxy, p-toluenesulfonyloxy and p-nitrobenzenesulfonyloxy groups. Among them, we prefer a halogen atom, an alkylsulfonyloxy group and an arylsulfonyloxy group.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, so long as it does not adversely affect the reaction or the reagents used, and at least some of the reactants are soluble. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diethylene glycol dimethyl ether; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide. Among them, we prefer amides.
The reaction may be carried out in the presence of a base. Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, imidazole, quinoline, N, N-dimethylaniline, N, N-diethylaniline. Among them, 4- (N, N-dimethylamino) pyridine is preferable.
Additionally, 4- (N, N-dimethylamino) pyridine or 4-pyrrolidinopyridine may be used in catalytic amounts, in combination with one or more other bases. If desired, the reaction may be carried out in the presence of one or more of the following reagents to enhance the efficiency of the reaction: quaternary ammonium salts (e.g., benzyltriethylammonium chloride or tetrabutylammonium chloride), crown ethers (e.g., dibenzo-18-crown-6).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 100 ℃, preferably-10 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 1 day, preferably 30 minutes to 10 hours.
General formula (VII)Specific examples of the representative compounds include: acyl halides such as aliphatic acyl halides (e.g., acetyl chloride, propionyl chloride, butyryl chloride, valeryl chloride and hexanoyl chloride); alkoxycarbonyl halides having 1 to 6 carbon atoms in the alkoxy moiety (e.g., methoxycarbonyl chloride, methoxycarbonyl bromide, ethoxycarbonyl chloride, propoxycarbonyl chloride, butoxycarbonyl chloride and hexyloxycarbonyl chloride); aryl carbonylRadical halides (e.g., benzoyl chloride, benzoyl bromide, naphthoyl chloride); and silyl halides, and tert-butyldimethylsilyl chloride, trimethylsilyl chloride, triethylsilyl bromide, triisopropylsilyl chloride, dimethylisopropylsilyl chloride, diethylisopropylsilyl chloride, tert-butyldiphenylsilyl chloride, diphenylmethylsilyl chloride, triphenylsilyl chloride, or the corresponding silyl triflates; aralkyl halides such as benzyl chloride and benzyl bromide; carbonyloxyalkyl halides having from 1 to 6 carbon atoms in the alkyl moiety, such as pivaloyloxymethyl chloride and ethoxycarbonyloxymethyl chloride.
General formula (VII)Specific examples of the representative compounds include: aliphatic carboxylic anhydrides, such as acetic anhydride, propionic anhydride, valeric anhydride and hexanoic anhydride. Mixed anhydrides (e.g., of formic acid and acetic acid) may also be used. Step A2(ii)
By reacting an unprotected compound with a compound of formula[ wherein R11Groups which are in acyl form include those defined above]The reaction of the compound (2) is carried out in a solvent in the presence of a condensing agent, which is exemplified by the above-mentioned step A1b (ii), and the reaction may be carried out in the presence or absence of a base, and a protecting group R may be introduced11
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does notadversely affect the reagents used in the reaction and can dissolve at least some amount of the reactants. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
The base used in step a2(ii) may be any of the bases listed in step a2 (i).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step A2(iii)
By reacting an unprotected compound with a compound of formula[ wherein R11Groups which are in acyl form include those defined above]In a solvent and in the presence of a dialkyl halophosphate (e.g., diethyl chlorophosphate) and a base, a protecting group R may be introduced11
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and can dissolve at least some of the reactants. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; quinones such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
The base used in step a2(iii) may be any of the bases listed in step a2 (i).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, we carry out the reaction at a temperature ranging from 0 ℃ to the reflux temperature using the solvent, preferably from room temperature to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step A3
In this step, exomethylene group in the compound of formula (V) is oxidized in a solvent using an oxidizing agent to convert the compound into a diol form to prepare a compound of formula (VI).
Likewise, there is no particular limitation on the nature of the oxidizing agent used, and any oxidizing agent commonly used in this type of reaction may be used here. Examples of such oxidizing agents include: oxides of manganese, such as potassium permanganate and manganese dioxide; ruthenium oxides, such as ruthenium (IV) oxide; selenium compounds, such as selenium dioxide; and osmium compounds, e.g. osmium tetroxide and potassium osmate dihydrate: (). We prefer to use catalytic amounts of osmium tetroxide and reoxidant agents of osmium compounds. Examples of such reoxidants include: metal ferricyanides such as potassium ferricyanide (III); amine oxides such as 4-methylmorpholine oxide; inorganic oxidizing agents such as persulfate salts (e.g., potassium persulfate or sodium persulfate); peroxides, such as tert-butyl hydroperoxide; hypochlorite compounds such as tert-butyl hypochlorite; and nitrites, methyl nitrite. Among them, we prefer metal ferricyanides and amine oxides.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons, in particular halogenated aliphatic hydrocarbons, such as dichloromethane, chloroform; ethers such as diethyl ether, tetrahydrofuran, dioxane and dimethoxyethane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, isobutanol, tert-butanol and isoamyl alcohol; esters such as ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; dilute acids, such as aqueous sulfuric acid; dilute bases such as aqueous sodium hydroxide; water; ketones such as acetone and methyl ethyl ketone; organic bases, such as pyridine, nitriles, such as acetonitrile; or a mixture of any two or more of the above solvents. Among these, we prefer acetone and a mixture of acetone and water.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 5 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 1 to 24 hours, preferably 2 to 12 hours.
An optically active diol derivative having a specific absolute configuration can be prepared by an asymmetric dihydroxylation reaction using a chiral ligand. This asymmetric dihydroxylation reaction can be carried out, for example, as described by Sharpless et al (chemical review, Vol.94, page2483 (1994)).
Examples of the oxidizing agent used for this reaction include 0.0001 to 0.1 equivalent (more preferably 0.001 to 0.005 equivalent) of osmium tetroxide. Examples of chiral ligands include hydrogenated quinidine 1, 4-phthalazinediyl diether (DHQD)2-PHAL) and hydrogenated quinidine 2, 5-diphenyl-4, 6-pyrimidinediyl diether (DHQD)2-PYR) (preferably (DHQD) 2-PHAL). Examples of the oxidizing agent used for reoxidizing the osmium compound include potassium ferricyanide (III) and potassium carbonate.
Examples of the solvent used include water and a mixture of one or more of the following organic solvents: halogenated hydrocarbons, in particular halogenated aliphatic hydrocarbons, such as dichloromethane, chloroform; ethers such as diethyl ether, tetrahydrofuran, dioxane and dimethoxyethane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, isobutanol, tert-butanol and isoamyl alcohol; ketones such as acetone and methyl ethyl ketone; an ester; such as ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; nitriles, such as acetonitrile; mixtures of water and alcohols are preferred. Among these, a mixture of water and t-butanol is particularly preferable.
The compound of formula (VI) wherein D represents a sulfur atom can be prepared by converting the exomethylene group of the compound of formula (V) into thiirane by a conventional method and then opening the ring with a hydroxyl ion. Step A4
In this step a compound of formula (VII) is prepared by: (a) converting the primary hydroxyl group in formula (VI) into an eliminable group (this reaction is carried out in the presence of a base, with or without a solvent); and (b) then reacting the resulting compound with an azidation reagent, the reaction being carried out in a solvent, with or without a catalyst, to convert it to an azido group.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons, particularly halogenated aliphatic hydrocarbons such as dichloromethane and chloroform; ethers such as diethyl ether, tetrahydrofuran, dioxane and dimethoxyethane; nitriles such as acetonitrile and amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone and hexamethylphosphoric triamide; more preferred are halogenated hydrocarbons or ethers in the first reaction step or amides in the second reaction step.
There is no particular limitation on the nature of the base used in the first step, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tripropylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline, 1, 5-diazabicyclo [4, 3, 0]non-5-ene (DBN), 1, 4-diazabicyclo [2, 2, 2]octane (DABCO) and 1, 8-diazabicyclo [5, 4, 0]undec 7-ene (DBU). Among them, triethylamine, pyridine and 4- (N, N-dimethylamino) pyridine are preferable.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 50 ℃ and preferably 10 to 20 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature andthe nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 15 minutes to 24 hours, preferably 30 minutes to 6 hours.
Groups which can be eliminated are the same as those defined for X above. Reagents for forming the eliminating group, preferably corresponding halides, examples of such reagents include sulfonyl halides such as methanesulfonyl chloride and p-toluenesulfonyl chloride. The reaction may be carried out with introduction of a protecting group R11The same conditions were used.
Likewise, there is no particular limitation on the nature of the azidation reagent used in the second step, and any azidation reagent commonly used in this type of reaction may be used here. Examples of such azidation reagents include: diarylphosphoryl azides, such as diphenylphosphoryl azide; trialkylsilyl azides, such as trimethylsilyl azide and triethylsilyl azide; and alkali metal azides such as sodium azide, potassium azide and lithium azide. Among them, we prefer alkali metal azides.
Examples of useful catalysts include trialkylsilyl triflates, such as trimethylsilyl triflate, trimethylsilyl triflate; lewis acids, such as boron trifluoride etherate, aluminum chloride and zinc chloride.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of 20 to 180 ℃, preferably 50 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 8 hours. Step A5
In this step, the amino compound of the general formula (VIII) is prepared by reducing the compound of the general formula (VII) in a solvent.
Any reagent that can reduce an azide group to an amino group can be used in the reaction, and is not particularly limited. Preferably, the reaction is carried out at 20 to 150 deg.C (more preferably 50 to 100 deg.C) for 15 minutes to 1 day (more preferably 1 to 12 hours), and the reaction is carried out in an aqueous solvent (preferably an ether such as tetrahydrofuran) using triphenylphosphine as a reducing agent.
In addition, the reaction may be carried out by catalytic hydrogenation at-10 to 100 ℃ (preferably 0 to 50 ℃) for 1 hour to 4 days (preferably 2 hours to 2 days), in an organic solvent such as an alcohol (e.g., methanol or ethanol), an ester (e.g., ethyl acetate, propyl acetate, butyl acetate or diethyl carbonate), an ether (e.g., tetrahydrofuran or dioxane) or a fatty acid (e.g., acetic acid) or a mixture of any one or more organic solvents with water (preferably an alcohol), using a catalyst such as palladium on carbon, platinum or Raney nickel. Step A6
In this step, a compound of the formula (X) is prepared, and the amino group in the compound of the formula (VIII) is acylated with a compound of the formula (IX) in a solvent in the presence of a base (step A6a), followed by ring closure of the alkylated DH group to form a cyclic amide (step A6 b). Step A6a
The acylation reaction in this step is generally and preferably carried out in a solvent. There is no particular limitation on the natureof the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline.
If desired, 4- (N, N-dimethylamino) pyridine or 4-pyrrolidinopyridine may be used in catalytic amounts, in combination with one or more other bases. If desired, the reaction may be carried out in the presence of one or more of the following reagents to enhance the efficiency of the reaction: a dehydrating agent (e.g., a molecular sieve), a quaternary ammonium salt (e.g., benzyltriethylammonium chloride or tetrabutylammonium chloride), a crown ether (e.g., dibenzo-18-crown-6), and an acid scavenger (e.g., 3, 4-dihydro-2H-pyrido [1, 2-a]pyrimidin-2-one).
The reaction can be carried out over a widetemperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day.
In the case where the group X' in the carboxylic acid derivative of the formula (IX) represents a hydroxyl group, the reaction is carried out by reacting the compound of the formula (VIII) with the compound of the formula (IX) in the presence of the condensing agent described in step A1b (ii) in the above-mentioned solvent in the presence or absence of the above-mentioned base. Step A6b
The cycloalkylation reaction in this step is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile, propionitrile, and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide; and sulfoxides such as dimethyl sulfoxide and sulfolane. Among them, we prefer ethers and amides, and particularly prefer tetrahydrofuran and dimethylformamide.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal bicarbonates, such as sodium bicarbonate, potassium bicarbonate and lithium bicarbonate; alkali metal hydrides such as lithium hydride, sodium hydride, potassium hydride; alkali metal hydroxides such as sodium hydroxide, potassium hydroxide, barium hydroxide and lithium hydroxide; alkali metal fluorides such as sodium fluoride, potassium fluoride; and alkali metal alcoholates such as sodium methylate, sodium ethylate, potassium methylate, potassium ethylate, potassium tert-butylate and lithium methylate. Among them, alkali metal hydrides and alkali metal alcoholates are preferred.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 100 ℃ and preferably 0 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 12 hours. Step A7
In this step, the amide group in the general formula (X) is converted into an imino group by reducing it in a solvent using a reducing agent, and then optionally with the group R12Protection is carried out to prepare the compound of the general formula (XI).
The reaction is generally and preferably carried out in a solvent in the main step. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme. Among these, we prefer ethers, particularly diethyl ether or tetrahydrofuran.
Likewise, there is no particular limitation on the nature of the reducing agent used, and any reducing agent commonly used in this type of reaction may be used here. Examples of such reducing agents include: hydride reagents such as alkali metal borohydrides (e.g., sodium borohydride or lithium borohydride), aluminum hydride compounds (e.g., lithium aluminum hydride or lithium tri-t-butoxide hydride), sodium tellurite hydride and organic aluminum hydride reducing agents [ e.g., diisobutylaluminum hydride or sodium bis (methoxyethoxy) aluminum hydride]and borane reducing agents (e.g., borane-dimethyl sulfide complex, or borane-tetrahydrofuran complex, etc.). Among them, we prefer an aluminum hydride compound and a borane reducing agent, and particularly prefer a borane-dimethyl sulfide complex.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-78 to 150 ℃, preferably-20 to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 5 minutes to 24 hours, preferably 10 minutes to 2 hours. Step A8
In this step, a compound of the formula (XIII) is prepared by using the imino group of the formula (XI) with-A-B-R1(A, B and R1Same as defined above) is prepared by reacting a compound of formula (XI) with a compound of formula (XII) in a solvent in the presence of a base.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane, ligroin and petroleum ether; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone and cyclohexanone; nitro compounds such as nitroethane and nitrobenzene; nitriles such as acetonitrile and isobutyl nitrile. Among them, halogenated hydrocarbons and ethers are preferable, and dichloromethane and tetrahydrofuran are particularly preferable.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tripropylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline, 1, 5-diazabicyclo [4, 3, 0]non-5-ene (DBN), 1, 4-diazabicyclo [2, 2, 2]octane (DABCO) and, 1, 8-diazabicyclo [5, 4, 0]undec-7-ene (DBU). Among them, triethylamine or diisopropylethylamine is preferable.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 100 ℃ and preferably 0 to 20 ℃. The reaction time may also vary within wide limits depending on many factors, the main reaction temperature and the nature of the reagents and solvents used, but, assuming that the reaction is carried out under the conditions described above, it is sufficient to carry out the reaction generally from 5 minutes to 24 hours, preferably from 10 minutes to 12 hours.
When A represents a carbonyl group, this step can also be carried out by reacting a compound of the formula (XI) with a compound of the formula(wherein A, B, R1As defined above) is completed, the reaction is carried out in the presence of a condensing agent, in a solvent, with or without a base.
Examples of the condensing agent that can be used include those exemplified in the above-mentioned reaction step A1b (ii). Among these, we prefer a combination of phosphate and one or more of the following bases.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline and N, N-diethylaniline.
If desired, 4- (N, N-dimethylamino) pyridine or 4-pyrrolidinopyridine may be used in catalytic amounts, in combination with one or more other bases. If desired, the reaction may be carried out in the presence of one or more of the following reagents to enhance the efficiency of the reaction: a dehydrating agent (e.g., a molecular sieve), a quaternary ammonium salt (e.g., benzyltriethylammonium chloride or tetrabutylammonium chloride), a crown ether (e.g., dibenzo-18-crown-6), and an acid scavenger (e.g., 3, 4-dihydro-2H-pyrido [1, 2-a]pyrimidin-2-one).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step A9
In this step, a compound of formula (XIV) is prepared by reacting R in a compound of formula (XIII)12(R12Not a hydrogen atom) and converting the resulting hydroxyl group into an eliminating group Y' which can be passed through the second step in step A4The one step method is completed.
Depending on the nature of the radical, R can be removed by different methods12. However, methods for removing such groups are known in the art.
For example, when R is12When it is a silyl group, it is generally removed by treatment with a compound capable of forming a fluoride ion (e.g., tetrabutylammonium fluoride, hydrogen fluoride-pyridine or potassium fluoride), or with an organic acid (e.g., acetic acid, methanesulfonic acid, p-toluenesulfonic acid, trifluoromethanesulfonic acid or B-bromocatechol borane), or with an inorganic salt (e.g., hydrochloric acid).
When the group R12When removed by fluoride ion, the reaction may be accelerated by the addition of an organic acid such as formic acid, acetic acid or propionic acid.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; water; and an organic acid, such as acetic acid, or a mixture of any two or more thereof.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of from 0 to 150 ℃, preferably from 10 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, the reaction is carried out for generally 1 to 48 hours, preferably 2 to 12 hours, sufficiently.
When R is12In the case of an aralkyl group or an aralkyloxy group, it is preferable to remove this group by contacting with a reducing agent (preferably catalytic hydrogenation in the presence of a catalyst at room temperature) in a solvent, or to use an oxidizing agent.
The catalytic hydrogenation reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: alcohols, such as methanol, ethanol, propanol; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran and dioxane; aromatic hydrocarbons such as benzene, toluene and xylene; aliphatic hydrocarbons such as hexane and cyclohexane; esters, such as ethyl acetate and propyl acetate; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone and hexamethylphosphoric triamide; fatty acids such as formic acid and acetic acid; water; or a mixture of any two or more thereof. Among these, we prefer alcohols, mixtures of fatty acids and alcohols and ethers, mixtures of alcohols and water or mixtures of fatty acids and water.
Likewise, there is no particular limitation on the nature of the catalyst used, and any catalyst commonly used in this type of reaction may be used here. Examples of such catalysts include: palladium on carbon, palladium black, Raney nickel, platinum oxide, platinum black, alumina-rhodium, triphenylphosphine-rhodium chloride and palladium-barium sulfate.
The pressure of the reaction is not particularly limited, but the reaction is generally carried out in the range of 1 to 10 atmospheres.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature of 0 to 100 ℃ and preferably20 to 70 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 5 minutes to 48 hours, preferably 1 to 24 hours.
If the protecting group is removed by oxidation, the reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Preferably, an aqueous organic solvent is used. Examples of suitable solvents include: ketones, such as acetone; halogenated hydrocarbons, preferably halogenated aliphatic hydrocarbons, such as dichloromethane, chloroform and carbon tetrachloride; nitriles, such as acetonitrile; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran and dioxane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide; and sulfoxides, such as dimethyl sulfoxide.
Likewise, there is no particular limitation on the nature of the oxidizing agent used, and any oxidizing agent commonly used in this type of reaction may be used here. Examples of such oxidizing agents include: potassium persulfate, sodium persulfate, Cesium Ammonium Nitrate (CAN), and 2, 3-dichloro-5, 6-dicyano-p-benzoquinone (DDQ).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 0 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours.
It is also possible to remove the protecting group by reaction with an alkali metal (e.g., metallic lithium or metallic sodium) in liquid ammonia or with an alcohol (e.g., methanol or ethanol) at a temperature in the range of-78 to-20 ℃.
The protecting group may also be removed using reaction with aluminum chloride-sodium iodide or an alkylsilyl halide (e.g., trimethylsilyliodide) in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: nitriles, such as acetonitrile; halogenated hydrocarbons, preferably halogenated aliphatic hydrocarbons, such as dichloromethane, chloroform; or a mixture of any two or more thereof.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of 0 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 5 minutes to 3 days.
When the reaction substrate contains a sulfur atom, aluminum chloride-sodium iodide is preferably used.
When R is12When the group is an aliphatic acyl group, an aromatic acyl group or an alkoxycarbonyl group, the protecting group is preferably removed in a solvent using a base.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal alcoholates, such as sodium methylate; alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal hydroxides such as sodium hydroxide, potassium hydroxide, lithium hydroxide and barium hydroxide; or various forms of ammonia such as aqueous ammonia or concentrated ammonia-methanol.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and can dissolve at least some amount of the reactants. Any solvent commonly used in this type of reaction may be used here. Examples of suitable solvents include: water; organic solvents such as alcohols (e.g., methanol, ethanol, propanol) and ethers (e.g., tetrahydrofuran and dioxane); or preferably a mixture of water and one or more of the above organic solvents.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in order to avoid side reactions, the reaction is generally carried out at a temperature of 0 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 1 to 10 hours.
When R is12When it is an alkoxymethyl group, a tetrahydropyranyl group, a tetrahydrothiopyranyl group, a tetrahydrofuranyl group, a tetrahydrothiofuranyl group or a substituted ethyl group, the protecting group is removed in a solvent using an acid.
Likewise, there is no particular limitation on the nature of the acid used, and any acid commonly used in this type of reaction may be used here. Examples of such acids include: bronsted acids such as mineral acids (e.g., hydrochloric acid, sulfuric acid, or nitric acid); organic acids (e.g., acetic acid, trifluoroacetic acid, methanesulfonic acid, or p-toluenesulfonic acid); and Lewis acids such as boron trifluoride. Strong acid ion exchange resins such as Dowex (trade mark) 50W may also be used.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane, heptane, ligroin and petroleum ether; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; alcohols, methanol, ethanol, propanol, isopropanol, butanol, isobutanol, tert-butanol, isoamyl alcohol, diethylene glycol, glycerol,octanol, cyclohexanol and methyl cellosolve; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone and cyclohexanone; water; and mixtures of any one or more thereof. Among these, halogenated hydrocarbons, esters and ethers are preferred.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-10 to 100 ℃, preferably-5 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 5 minutes to 48 hours, preferably 30 minutes to 10 hours.
When R is12When it is an alkenyloxycarbonyl radical, it is preferred to use a base in combination with the removal of R12Is an aliphatic acyl group, an aromatic acyl group or an alkoxycarbonyl group, under the same conditions to remove R12
In the case of allyloxycarbonyl, palladium and triphenylphosphine or bis (methyldiphenylphosphine) (1, 5-cyclooctadiene) -iridium (I) hexafluorophosphate can be used for removal, so that the reaction can be carried out simply and few side reactions occur. Step A10
In this step, the compound of the present invention of the general formula (I) is prepared by reacting the compound of the general formula (XIV) with the compound of the general formula (XV) in a solvent in the presence of a base.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane, ligroin and petroleum ether; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene, esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone and cyclohexanone; nitro compounds such as nitroethane and nitrobenzene; nitriles such as acetonitrile and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide; and sulfoxides such as dimethyl sulfoxide and sulfolane. Among them, we prefer amides, ethers, nitriles, and particularly prefer amides.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: a combination of a metal iodide (e.g., potassium iodide) and an inorganic base, such as an alkali metal carbonate (e.g., sodium carbonate, potassium carbonate and lithium carbonate), an alkali metal hydrogencarbonate, (e.g., sodium hydrogencarbonate, potassium hydrogencarbonate and lithium hydrogencarbonate), an alkali metal hydride, (e.g., lithium hydride, sodium hydride, potassium hydride), an alkali metal hydroxide, (e.g., sodium hydroxide, potassium hydroxide, barium hydroxide and lithium hydroxide) or an alkali metal fluoride, (e.g., sodium fluoride or potassium fluoride); or an organic base such as N-methylmorpholine, triethylamine, tripropylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridinoquinoline, N, N-dimethylaniline, N, N-diethylaniline, 1, 5-diazabicyclo [4, 3, 0]non-5-ene (DBN), 1, 4-diazabicyclo [2, 2, 2]octane (DABCO) and 1, 8-diazabicyclo [5, 4, 0]undec-7-ene (DBU). Among them, we prefer a combination of a metal iodide and an inorganic base, and particularly prefer a combination of a metal iodide and an alkali metal bicarbonate.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of from 0 to 150 ℃, preferably from 20 to 120 ℃. The reaction time can also be within a wide range, depending on many factors, the main reaction temperature and the nature of the reagents and solvents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 48 hours, preferably 1 to 12 hours.
After completion of the above-mentioned reaction steps, the reaction product can be collected from the reaction mixture using a conventional method.
For example, in one suitable separation method, the reaction mixture is neutralized, if insoluble, filtered to remove, and any water-immiscible solvent (e.g., ethyl acetate) is added. The organic layer is separated, and then washed with, for example, water, and the desired compound is dried using, for example, anhydrous magnesium sulfateor anhydrous sodium sulfate. The solvent was then distilled off to give the desired compound.
The resulting compound may, if desired, be purified by one or more of the following methods: recrystallizing; then precipitating; or other methods commonly used for separation and purification of organic compounds, for example, adsorption column chromatography using a chromatographic column, adsorption column chromatography using a carrier such as silica gel, alumina or magnesium-silica gel, Florisil; a partition column chromatography using a synthetic adsorbent, for example, Sephadex (trademark) LH-20 (manufactured by Pharmacia Co., Ltd.), Diaion (trademark) HP-20 (manufactured by Mitsubishi Kasei Co., Ltd.); methods using ion exchange chromatography; or normal/reverse phase liquid chromatography (preferably high performance liquid chromatography) using silica gel or alkylated silica gel.
When it is necessary to separate isomers, the separation can be carried out using the above separation and purification methods after completion of each reaction described above or after completion of the desired step. Reaction scheme B:
an alternative process for the preparation of compounds of the general formula (IV) is provided, after which the preparation of the compounds according to the invention can also be continued using step A.
In the above formula R2As defined above. Step B1
In this step, the compound of formula (IV) is prepared as follows: grignard reagents are prepared by reacting a compound of general formula (XVI) with magnesium metal according to the method described by Ito et al [ Bull. chem. Soc. Jpn., Vol.64, page 3746(1991)]; coupling the Grignard reagent with a compound of general formula (XVII) in a solvent, in the presence or absenceof a Lewis acid, and in the presence of a catalytic amount (preferably 0.1 to 0.5 equivalent) of a palladium catalyst; the resulting carboxylic acid was esterified according to any of the steps of step A1.
This is preferred because the reaction can be carried out in good yield in the presence of a Lewis acid with almost no by-products. There is no particular restriction on the nature of the Lewis acid used, and any Lewis acid commonly used in this type of reaction may be used here. Examples of such Lewis acids include: trialkylsilyl trifluoromethanesulfonate having 1 to 6 carbon atoms in the alkyl moiety; aluminum salts such as aluminum chloride; tin salts, such as tin tetrachloride; zinc salts, such as zinc bromide or zinc chloride; titanium salts, such as titanium tetrachloride; or perchlorate, trimethylsilyl perchlorate or triphenylmethyl perchlorate. Among them, zinc salts are preferable, and zinc chloride is particularly preferable.
Any palladium-containing palladium catalyst may be used without particular limitation. Preferred examples include organophosphinic palladium compounds such as dichlorobis (triphenylphosphine) palladium (II).
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and glyme. Among them, diethyl ether is preferred.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or thereagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 50 ℃ and preferably 0 to 20 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 15 minutes to 8 hours, preferably 30 minutes to 2 hours.
After completion of the above reaction, the desired compound of the formula (IV) can be isolated from the reaction mixture by a conventional method.
For example, in one suitable separation method, the reaction mixture is neutralized, if insoluble, filtered to remove, and any water-immiscible solvent (e.g., ethyl acetate) is added. The organic layer is separated, and then washed with, for example, water, and the resulting compound is dried using, for example, anhydrous magnesium sulfate or anhydrous sodium sulfate. The solvent was then distilled off to give the desired compound.
The resulting compound may, if desired, be purified by one or more of the following methods: recrystallizing; then precipitating; or other methods commonly used for the separation and purification of organic compounds, for example, using a carrier such as silica gel, alumina or magnesium-silica gel; florisil adsorption column chromatography; a partition column chromatography using a synthetic adsorbent, for example, Sephadex (trademark) LH-20 (manufactured by Pharmacia Co., Ltd.), Diaion (trademark) HP-20 (manufactured by Mitsubishi Kasei Co., Ltd.); using ion exchange chromatography; or normal/reverse phase liquid chromatography (preferably high performance liquid chromatography) using silica gel or alkylated silica gel. Scheme C
An alternative process for the preparation of compounds of the general formula (XI) is provided, after which the preparation of the compounds of the invention can also be continued using step A.
In the above formula R2,R11,R12D, E and G are as defined above.
R13A hydrogen atom or a hydroxyl protecting group, and may be substituted with R as described above11The groups listed in (a) are the same.
R14Represents an amino-protecting group, and examples thereof include aliphatic acyl groups, aromatic acyl groups, alkoxycarbonyl groups, alkenyloxycarbonyl groups, aralkyloxycarbonyl groups and silyl groups as defined below, with alkoxycarbonyl groups being preferred. Among these, tert-butoxycarbonyl is particularly preferable.
Step C1
In this step, the exomethylene group in the compound of the general formula (V) is reacted with an oxidizing agent in a solvent to prepare an epoxy compound of the general formula (XVIII).
Likewise, there is no particular limitation on the nature of the oxidizing agent used, and any oxidizing agent commonly used in olefin epoxidation reactions can be used here. Examples of such oxidizing agents include: peracids, such as m-chloroperbenzoic acid, 3, 5-dinitroperbenzoic acid, o-carboxyperbenzoic acid, peracetic acid, pertrifluoroacetic acid and perphthalic acid; a hydroperoxide; peroxides, such as t-butyl hydroperoxide (which may be used in combination with vanadium or molybdenum complexes); and a combination of a succinimide (e.g., N-bromosuccinimide) and a base. Among them, peracids are preferable, and m-chloroperbenzoic acid is particularly preferable.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons, particularly halogenated aliphatic hydrocarbons such as dichloromethane and chloroform; ethers, such as diethyl ether, tetrahydrofuran, dioxane, dimethoxyethane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, isobutanol, tert-butanol and isoamyl alcohol; dilute acids, such as aqueous sulfuric acid; dilute bases such as aqueous sodium hydroxide; water; ketones such as acetone and methyl ethyl ketone; organic bases, such as pyridine, nitriles, such as acetonitrile; or a mixture of any two or more of the above solvents. Among them, methylene chloride is preferred.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature of-20 to 80 ℃ and preferably at a temperature of-5 to 50 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 1 to 24 hours, preferably 2 to 12 hours.
Optically active epoxy compounds having a specific absolute configuration can be prepared by asymmetric epoxidation using chiral ligands. This reaction can be carried out, for example, by Sharpless et al or by Jacobsen et al [ see catalysis A systematic Synthesis, VCH Publishers Inc. (1993) The process is complete. Step C2
In this step, the ring opening of the epoxide group in the compound of the formula (XVIII) is carried out using an amino alcohol of the formula (XIX) in the presence or absence of a base (step C2a) and the secondary ammonia is then protectedRadical-forming radicals R14(step C2b) to prepare a compound of formula (XX). Step C2a
The ring-opening reaction of the first step is generally preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile, propionitrile, and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide and sulfolane. Among them, we prefer nitrile.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal perchlorates such as lithium perchlorate and sodium perchlorate; alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal bicarbonates, such as sodium bicarbonate, potassium bicarbonate and lithium bicarbonate; alkali metal hydrides such as lithium hydride, sodium hydride, potassium hydride; alkali metal hydroxides such as sodium hydroxide, potassium hydroxide, barium hydroxide and lithium hydroxide; alkali metal fluorides such as sodium fluoride, potassium fluoride; and alkali metal alcoholates such as sodium methylate, sodium ethylate, potassium methylate, potassium ethylate, potassium tert-butylate and lithium methylate; alkali metal mercaptides, such as sodium methyl mercaptide, sodium ethyl mercaptide; and organic bases such as N-methylmorpholine, triethylamine, tripropylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline, 1, 5-diazabicyclo [4, 3, 0]non-5-ene (DBN), 1, 4-diazabicyclo [2, 2, 2]octane (DABC0) and 1, 8-diazabicyclo [5, 4, 0]undec-7-ene (DBI).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 150 ℃ and preferably from room temperature to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step C2b
In this step, a secondary amino-protecting group R is introduced as follows14. Step C2b (i)
The unprotected compound is admixed with a suitable amount, for example, 1 to 4 equivalents (preferably 2 to 3 equivalents) of the compound of the formula in a solvent, in the presence or absence of a baseCompound (wherein R14As defined above, and X' represents a group capable of elimination as a nucleophilic residue, with special restrictions), or with the general formulaCompound of (2) (wherein R is14Selected from the group consisting of R as defined above14Acyl type group of (1). Examples of preferred such scavenging groups include: a halogen atom such as a chlorine, bromine or iodine atom; alkoxycarbonyloxy having 1 to 6 carbon atoms in the alkoxy moiety, such as methoxycarbonyloxy and ethoxycarbonyloxy; haloalkylcarbonyloxy having 1 to 6 carbon atoms in the alkyl moiety, such as chloroacetyloxy, dichloroacetoxy, trichloroacetoxy and trifluoroacetyloxy; alkylsulfonyloxy groups having 1 to 6 carbon atoms, such as methanesulfonyloxy and ethanesulfonyloxy groups; halogenated alkylsulfonyloxy groups having 1 to 6 carbon atoms, such as trifluoromethanesulfonyloxy and pentafluoroethanesulfonyloxy groups; arylsulfonyloxy groups in which the aryl moiety is as above R1Examples of the above-mentioned groups include benzenesulfonyloxy, p-toluenesulfonyloxy and p-nitrobenzenesulfonyloxy groups. Among them, we prefer a halogen atom, a haloalkylsulfonyloxy group and an arylsulfonyloxy group.
General formula (VII)Specific examples of (a) include: acyl halides such as aliphatic acyl halides (e.g., acetyl chloride, propionyl chloride, butyryl chloride, valeryl chloride and hexanoyl chloride); in thatAlkoxycarbonyl halides in which the alkoxy moiety has 1 to 6 carbon atoms (e.g., methoxycarbonyl chloride, methoxycarbonyl bromide, ethoxycarbonyl chloride, propoxycarbonyl chloride, butoxycarbonyl chloride and hexyloxycarbonyl chloride); arylcarbonyl halides (e.g., benzoyl chloride, benzoyl bromide, naphthoyl chloride); silyl halides, such as tert-butyldimethylsilyl chloride, trimethylsilyl chloride, triethylsilyl bromide, triisopropylsilyl chloride, dimethylisopropylsilyl chloride, diethylisopropylsilyl chloride, tert-butyldiphenylsilyl chloride, diphenylmethylsilyl chloride, triphenylsilyl chloride or the corresponding silyl triflates; aralkyl halides such as benzyl chloride and benzyl bromide; or carbonyloxyalkyl halides, such as pivaloyloxymethyl chloride and ethoxycarbonyloxymethyl chloride.
General formula (VII)Specific examples of the representative compounds include: aliphatic carboxylic anhydrides, such as acetic anhydride, propionic anhydride or valeric anhydride, and carbonates, such as di-tert-butyl dicarbonate or hexanoic anhydride. Mixed anhydrides (e.g., a mixed anhydride of formic acid and acetic acid) may also be used.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane, ligroin and petroleum ether; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: organic bases, such as N-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline, 4- (N, N-dimethylamino) pyridine, 2, 6-di (tert-butyl) -4-methylpyridine, quinoline, N, N-dimethylaniline, N, N-diethylaniline.
If desired, 4- (N, N-dimethylamino) pyridine or 4-pyrrolidinopyridine may be used in catalytic amounts in combination with one or more other bases, and if desired, in the presence of one or more of the following reagents to enhance the efficiency of the reaction: quaternary ammonium salts (e.g., benzyltriethylammonium chloride or tetrabutylammonium chloride), crown ethers (e.g., dibenzo-18-crown-6).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. In general, however, we carry out the reaction at temperatures ranging from-20 ℃ to the reflux temperature of the solvent used, preferably from 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 1 hour to 1 day. Step C2b (ii)
Unprotected compound with general formula (I) in solvent in the presence of condensing agent and in the presence or absence of base(wherein R is14Is selected from R as defined above14Acyl type group) of (a).
The condensing agents given above in step A1b (ii) may be used.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; and amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide.
Bases which can be used in this step are the bases given above in step C2b (i).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly critical to the present invention, and is preferably determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 1 day. Step C2b (iii)
Preferably, when R is14Is tert-butoxycarbonyl or benzyloxycarbonyl, by reacting the compound formed in step C1b with a tert-butoxycarbonylating agent or a benzyloxycarbonylating agent in a solvent in the presence of a base and then reacting with R14The group protects the secondary amino group.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide; water; and mixtures of water with any one or more of the above organic solvents.
Any of the bases given above for step C1C (i) may be used in this step.
Likewise, there is no particular limitation on the nature of the t-butyloxycarbonylating agent used, and any t-butyloxycarbonylating agent commonly used in reactions of this type may be used here. Examples of such t-butyloxycarbonylating agents include: di-tert-butyl dicarbonate, 2- (tert-butoxycarbonyloxyimino) -2-phenylacetonitrile, tert-butyl S- (4, 6-dimethylpyridin-2-yl) thiocarboxylate and 1, 2, 2, 2-tetrachloroethyl tert-butyl carbonate, more preferably di-tert-butyl dicarbonate.
Likewise, there is no particular limitation on the nature of the benzyloxycarbonylating reagent used, and any benzyloxycarbonylating reagent commonly used in this type of reaction can be used here. Examples of such benzyloxycarbonylation reagents include: benzyloxycarbonyl chloride, benzyloxycarbonyl cyanide and dibenzyl dicarbonate.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃ and preferably 0 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 24 hours. Step C3
In this step, the compound of formula (XXI) is prepared by dehydrating the compound of formula (XX) using a Mitsunobu reaction.
There is no particular limitation on the nature of the reagent used in the Mitsunobu reaction, and any reagent commonly used in this type of reaction may be used here. Examples of such agentsThe sub-steps include: compositions of azo compounds, such as dialkyl azodicarboxylates having 1-6 carbon atoms in the alkyl moiety (e.g., diethyl azodicarboxylate or diisopropyl azodicarboxylate) or azodicarbonyl compounds [ e.g., 1, 1- (azodicarbonyl) bipiperidine](ii) a And phosphines, e.g. triarylphosphines, wherein the aryl moiety is as R above1A trialkyl phosphine (e.g., tributylphosphine) having 1 to 6 carbon atoms per alkyl moiety or (e.g., triphenylphosphine). Among these, we prefer a combination of dialkyl azodicarboxylate and triarylphosphine, and particularly prefer a combination of diethyl azodicarboxylate and triphenylphosphine.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide; and sulfoxides such as dimethyl sulfoxide and sulfolane. Among them, we prefer aromatic hydrocarbons and ethers.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 100 ℃ and preferably 0 to50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 30 minutes to 12 hours.
In carrying out the reaction of this step, R is sometimes removed11. In this case, the hydroxyl group may be re-protected as in the second part of step a 2. Step C4
In this step, the following steps are carried out simultaneously or separately to prepare the compound of formula (XI):
(i) removal of the amino-protecting group R14Exposing the amino group, and
(ii) when R is12In the case of a hydroxyl-protecting group, the hydroxyl group is optionally removed. Step C4(i)
The radical R can be removed by various reactions, depending on the nature of the radical14Reactions useful for removing such groups are known in the art. Step C4(i) a
For example, if the amino protecting group is a silyl group, the group is typically removed by treatment with a fluoride ion-forming compound, such as tetrabutylammonium fluoride.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: ethers, such as tetrahydrofuran or dioxane.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly requiredfor the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general we carry out the reaction at about room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 18 hours. Step C4(i) b
When the amino protecting group is an aliphatic acyl group, an aromatic acyl group, an alkoxycarbonyl group or a substituted methylene group to form a Sohiff base, it can be treated with an acid or a base in an aqueous solvent.
There are no particular restrictions on the nature of the acid used, and any acid commonly used in reactions of this type may be used here. Examples of such acids include: inorganic acids such as hydrochloric acid, sulfuric acid, phosphoric acid and hydrobromic acid; and Lewis acids such as B-bromocatechol borane. Among them, B-bromocatechol borane or hydrochloric acid is preferable.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and can dissolve at least some amount of the reactants. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and ethylene glycol dimethyl ether; nitro compounds, such as nitroethane and nitrobenzene. Among them, halogenated hydrocarbons are particularly preferable.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal alcoholates, such as sodium methylate; alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal bicarbonates, such as sodium bicarbonate, potassium bicarbonate and lithium bicarbonate; alkali metal hydroxides such as sodium hydroxide, potassium hydroxide and lithium hydroxide; different forms of ammonia, such as aqueous ammonia and concentrated methanolic ammonia.
When a base is used for hydrolysis, isomerization sometimes occurs.
The reaction is preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, provided that it adversely affects the reaction or the reagents used, and that at least some amount of the reactants may be dissolved. Examples of suitable solvents include: water; organic solvents such as alcohols (e.g., methanol, ethanol or propanol) and ethers (e.g., tetrahydrofuran or dioxane); or a mixture of water and one or more of the above organic solvents.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 0 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferable conditions, it is sufficient that the reaction is carried out for 1 to 10 hours in general. Step C4(i) C
When the amino protecting group is an aralkyl or aralkyloxycarbonyl group, we prefer to remove the protecting group by treatment with a reducing agent in a solvent (preferably catalytic hydrogenation at room temperature in the presence of a catalyst) or treatment with an oxidizing agent.
The catalytic hydrogenation reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: organic solvents such as alcohols (e.g. methanol, ethanol or isopropanol), ethers (e.g. diethyl ether, tetrahydrofuran or dioxane), aromatic hydrocarbons (e.g. benzene, toluene, xylene), esters (e.g. ethyl acetate or ethyl propyl acetate) and fatty acids (e.g. acetic acid) or mixtures of any one or more of these organic solvents with water.
Likewise, there is no particular limitation on the nature of the catalyst used in the catalytic hydrogenation reaction, and any catalyst commonly used in this type of reaction may be used here. Examples of such catalysts include: palladium on carbon, palladium black, Raney nickel, platinum oxide, platinum black, rhodium-aluminum oxide, triphenylphosphine-rhodium chloride and palladium-barium sulfate.
The pressure of the reaction is not particularly limited, and the reaction is generally carried out in the range of 1 to 10 atmospheres.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of 0 to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for 1 to 24 hours in general.
The oxidation reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable organic solvents include: ketones, such as acetone; halogenated hydrocarbons, in particular aliphatic halogenated hydrocarbons, such as dichloromethane, chloroform and carbon tetrachloride; nitriles, such as acetonitrile; ethers such as diethyl ether, tetrahydrofuran and dioxane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide.
Likewise, there is no particular limitation on the nature of the oxidizing agent used, and any oxidizing agent commonly used in this type of reaction may function here. Examples of such oxidizing agents include: potassium persulfate, sodium persulfate, Cesium Ammonium Nitrate (CAN) and 2, 3-dichloro-5, 6-dicyano-p-benzoquinone (DDQ).
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 0 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and thenature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours. Step C4(i) d
When the amino protecting group is an alkenyloxycarbonyl group, the amino protecting group is preferably removed using a base which is treated under the same conditions as when the amino protecting group is an aliphatic acyl group, an aromatic acyl group or an alkoxycarbonyl group or a substituted methylene group to form a Schiff base.
In the case of allyloxycarbonyl, palladium and triphenylphosphine or nickel tetracarbonyl can be used for removal, so that the reaction can be carried out simply and few side reactions occur. Step C4(ii)
The removal of the group R can be carried out in the same manner as in step A912
After completion of the above-mentioned reaction steps, the desired reaction product can be collected from the reaction mixture using a conventional method.
For example, in one suitable separation method, the reaction mixture is neutralized, if insoluble, filtered off and a water-immiscible solvent (e.g., ethyl acetate) is added. The organic layer is separated, and then washed with, for example, water, and the resulting compound is dried using, for example, anhydrous magnesium sulfate or anhydrous sodium sulfate. The solvent was then distilled off to give the desired compound.
The resulting compound may, if desired, be purified by one or more of the following methods: recrystallizing; then precipitating; or other methods commonly used for the separation and purification of organic compounds, for example, adsorption column chromatography using a carrier such as silica gel, alumina or magnesium-silica gel, Florisil; partition column chromatography using a synthetic adsorbent, for example, Sephadex (trademark) LH-20 (manufactured by Pharmacia Co., Ltd.), Amberlite (trademark) XAD-11 (manufactured by Rohm&Hass Co., Ltd.), Diaion (trademark) HP-20 (manufactured by Mitsubishi Kasei Co., Ltd.); using ion exchange chromatography; or normal/reverse phase liquid chromatography (preferably high performance liquid chromatography) using silica gel or alkylated silica gel. Reaction scheme D
In this reaction scheme, the compound of formula (I) wherein E represents methylene is prepared from the compound of formula (VIII), i.e. the compound of formula (Ia) and the compound of formula (VIII)Can be prepared from the above reaction scheme a.Step D1
In this step, paraformaldehyde is reacted with the amino group and DH group in the compound of formula (VIII) in the presence or absence of an acid catalyst and in the presence or absence of a solvent to form an oxazolidine or thiazolidine ring, to prepare the compound of formula (XIa).
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane, heptane, ligroin and petroleum ether; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, ethyl acetate, propyl acetate, butyl acetate and diethyl carbonate; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone and cyclohexanone; nitro compounds such as nitroethane and nitrobenzene; nitriles such as acetonitrile and isobutyl nitrile; amides such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrollidone) and hexamethylphosphoric triamide; and sulfoxides such as dimethyl sulfoxide and sulfolane. Among them, we prefer aromatic hydrocarbons, and particularly prefer benzene and toluene.
Likewise, there is no particular limitation on the nature of the acid catalyst used, and any acid catalyst commonly used in this type of reaction may be used here. Examples of such acid catalysts include: bronsted acids such as inorganic acids (e.g., hydrochloric acid, hydrobromic acid, sulfuric acid, perchloric acid or phosphoric acid) and organic acids (e.g., acetic acid, formic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, camphorsulfonic acid, trifluoroacetic acid or trifluoromethanesulfonic acid). Among them, we prefer organic acids, and particularly prefer p-toluenesulfonic acid.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 50 to 200 ℃ and preferably 80 to 150 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 48 hours, preferably 1 to 12 hours. Steps D2, D3 and D4
Corresponding to steps A8, a9 and a10, respectively, and using the same reagents and reaction conditions, the compound of formula (Ia) is finally obtained.
The resulting compound may, if desired, be purified by one or more of the following methods: recrystallizing; then precipitating; or other methods commonly used for separation and purification of organic compounds, for example, adsorption column chromatography using a carrier such as silica gel, alumina or magnesium-silica gel, Florisil, using a synthetic adsorbent, for example, partition column chromatography using Sephadex (trademark) LH-20 (manufactured by phamaoi co.), Amberlite (trademark) XAD-11 (manufactured by Rohm&Hass co.), Diaion (trademark) HP-20 (manufactured by Mitsubishi Kasei co., ltd.); using ion exchange chromatography; or normal/reverse phase liquid chromatography (preferably high performance liquid chromatography) using silica gel or alkylated silica gel. Reaction scheme E
In this reaction scheme, a particularly preferred compound of the general formula (I) wherein L represents a fused ring system having a sulfoxide group wherein the sulfur atom is in the S configuration, that is, an optically active sulfoxide compound of the general formula (Ib) is produced.
In the above formula, Ar, R1,R2A, B, D, E, J and Y are as defined above.
Represents a sulfoxide group in which the configuration of the sulfur atom is S configuration.
This reaction corresponds to step a10 and the same reagents and reaction conditions can be used to prepare compounds of general formula (Ib). Reaction scheme F
This reaction scheme provides an alternative method for preparing optically active sulfoxide compounds of the general formula (Ib).
In the above formula, R1,R2A, B, D, E, G, J, Ar andas defined above. Step F1
In this step, the aldehyde derivative of the formula (XXIII) is prepared by oxidation of the alcohol derivative of the formula (XIIif). This reaction is generally carried out in a solvent in the presence of an oxidizing agent.
There is no particular limitation on the nature of the oxidation reaction used, and any reaction commonly used to oxidize primary alcohols to form aldehydes may be used herein. Examples of such oxidation reactions include: collins oxidation using pyridine and chromic acid in dichloromethane; PCC oxidation reaction using pyridinium chlorochromate (PCC) in dichloromethane; oxidation of Pyridinium Dichromate (PDC) in dichloromethane using PDC; DMSO oxidation reactions such as the Swem oxidation reaction in dichloromethane using electrophiles (e.g., acetic anhydride, trifluoroacetic anhydride, thionyl chlorosulfonyl chloride, oxalyl chloride, but cyclohexyl carbodiimide, diphenylketene-p-tolylimine, N-diethylaminoacetylene, sulfur trioxide and pyridine complex) and dimethyl sulfoxide (DMSO); and manganese dioxide oxidation using manganese dioxide in dichloromethane or benzene.
Preference is given to using the Swem oxidation in dichloromethane using oxalyl chloride and DMSO.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carriedout at a temperature ranging from-100 ℃ to room temperature, preferably from-78 ℃ to-20 ℃. The reaction time may also vary over a wide range, depending on a number of factors, mainly reflecting the temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 2 days, preferably 10 minutes to 6 hours. Step F2
In this step, an optically active sulfoxide derivative of the general formula (Ib) is prepared by subjecting a compound of the general formula (XXIII) and a compound of the general formula (XXII) to reductive amination.
Likewise, there is no particular limitation on the nature of the solvent used, so long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants can be dissolved. Examples of suitable solvents include: alcohols, such as methanol, ethanol, propanol; ethers, such as diethyl ether, tetrahydrofuran and dioxane. Among these, we prefer alcohols, particularly methanol or ethanol.
Likewise, there is no particular limitation on the nature of the reducing agent used, and any reducing agent commonly used in this type of reaction may function here. Examples of such reducing agents include: hydride reagents such as alkali metal borohydrides, e.g., sodium cyanoborohydride, sodium borohydride and lithium borohydride, aluminum hydride compounds, e.g., lithium aluminum hydride and lithium tri-t-butoxyaluminum hydride, sodium tellurium hydride and organic aluminum hydride reducing agents, e.g., diisobutylaluminum hydride and sodium bis (methoxyethoxy) aluminum hydride. Among these, we prefer alkali metal borohydride, and particularly prefer sodium cyanoborohydride.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-10 to 100 ℃ and preferably at room temperature to 80 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 2 days, preferably 1 to 6 hours. Reaction scheme G
There is provided an alternative process for the preparation of compounds of formula (XI) which are useful in the preparation of the compounds of the invention.In the above formula:
R2,R11,R12,R13,R14d, E and G are as defined above; and this reaction scheme describes compounds of the general formula (XI) having 6-to 8-membered rings. Step G1
In this step, the primary hydroxyl group in the diol compound of the general formula (VI) is converted into an eliminated group (step G1a), and then substituted with an amino group in the amino alcohol compound of the general formula (XIX) to form a secondary amino group (step G1b), and then protected with an R14 group (step G1c), to prepare a compound of the general formula (XX). Step G1a
The primary hydroxyl group in the diol compound of formula (VI) may be converted to an eliminated group according to the first step in step A4. Step G1b
The substitution of the eliminated group in the resulting compound with the amino group in the aminoalcohol compound of the general formula (XIX) is usually carried out in a solvent using a metal salt.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone and cyclohexanone; nitriles such as acetonitrile, propionitrile, and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide. Among them, we prefer nitrile, and particularly prefer acetonitrile.
Likewise, there is no particular restriction on the nature of the metal salt used, and any metal salt commonly used in reactions of this type may function here. Examples of such metal salts include: metal perchlorates such as lithium perchlorate, magnesium perchlorate and sodium perchlorate; metal chlorides such as calcium chloride, zinc chloride and cobalt chloride; metal tetrafluoroborates such as lithium tetrafluoroborate, and potassium tetrafluoroborate; and zinc trifluoromethanesulfonate, preferably, a metal perchlorate, more preferably lithium perchlorate.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature isdetermined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 150 ℃ and preferably from room temperature to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 2 days, preferably 2 to 24 hours. Step G1c
The final use of R can be carried out according to the method described in step C2b14And (3) protecting an amino group. Step G2
In this step, the compound of the formula (XX) is subjected to a Mitsunobu reaction to dehydrate and ring-close it, to prepare a compound of the formula (XXI).
The reaction essentially uses the method described in step C3, and the same reagents and reaction conditions can be used.
It is to be noted that R11And R14Can be eliminated in this step. In this case, if necessary, R may be used in accordance with the method of step G1c14Protecting imino; and the hydroxyl group can be replaced with R according to the method of steps A2(i) to (iii)11And (4) protecting. Step G3
In this step, R in the compound of the formula (XXI) is removed12And R14Group (XI) preparation of the compound of formula (XI). This reaction may use essentially the method described in step C4, and the same reagents and reaction conditions may be used. Reaction scheme H
This reaction scheme illustrates a process for the preparation of compounds of formula (XXXII), which is a compound of formula (V) wherein G is two carbon atoms.
In the above formula, R2,R10And R11As defined above;
R15represents an alkyl group having 1 to 6 carbon atoms, such as R5Examples listed in (b) are preferably methyl, ethyl, propyl and isopropyl, or two R15The radicals together represent an alkylene radical having 1 to 6 carbon atoms, preferably a methylene, ethylene or 1, 3-propylene radical; and is
W represents a halogen atom, particularly preferably a chlorine atom. Step H1
In this step, β -ketoester derivatives of formula (XXIX) are prepared from compounds of formula (XXVIII.) this reaction may be carried out according to conventional methods, for example, as described in J.Wemple et al [ Synthesis, 290(1993)]. step H2
In this step, β -ketoester derivatives of the formula (XXIX) and of the formulaAlcohol (R) of15As defined above) of the general formulaAlkane diol of (2)(wherein R is15′Represents two R15Formed alkylene) or of the formulaOrthoformate of (R)15As defined above). The reaction can be carried out, for example, in an alcohol or an alkane diol with heating in the presence or absence of an acid catalyst.
General formula (VII)Examples of the alcohol of (b) include methanol, ethanol, propanol and isopropanol, with ethanol being preferred.
General formula (VII)Examples of the alkane diol of (2) include ethylene glycol, propylene glycol.
General formula (VII)Examples of the orthoformate of (b) include trimethoxymethane and triethoxymethane, preferably triethoxymethane.
This step can be carried out by heating in ethanol in the presence of ethyl orthoformate using p-toluenesulfonic acid as catalyst.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 40 to 150 ℃ and preferably 50 to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 2 days, preferably 2 to 12 hours. Step H3
In this step, the ester of formula (XXX) is reduced to form a primary hydroxyl group, the ketal group is deprotected and then treated with R11Protecting the primary hydroxyl group with a group to prepare a compound of formula (XXXI).
The reaction to reduce the orthoester is essentially the same as the first step in step a2, and the same reagents and reaction conditions can be used.
The deprotection of the ketal group is generally carried out in a solvent in the presence of an acid, preferably in the presence of trifluoroacetic acid in chloroform.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature of-20 to 100 ℃, preferably-10 ℃ to room temperature, and the reaction time can also be in a wide range, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 2 hours.
The reaction for protecting the primary hydroxyl group can be carried out according to the method of steps A2(i) to (iii), preferably according to the method of step A2 (i). Step H4
In this step, a compound of formula (XXXI) is subjected to a Wittig reaction in a solvent in the presence of a base to convert the carbonyl group therein to an exomethylene group to produce a compound of formula (XXXII). The reaction for this step is essentially the same as for step A1c, and the same reagents and reaction conditions can be used. Reaction scheme I
In the above formula, G, R2And R11As defined above.
This is another method for preparing the compound of formula (V), which can be used in reaction scheme A or C. Step I1
In this step, the compound of the general formula (XVI) is reacted with metallic magnesium using any conventional method to prepare a Grignard reagent, and then the above Grignard reagent is subjected to a cross-coupling reaction with thecompound of the general formula (XXXIII) and palladium or nickel is used as a catalyst to prepare the compound of the general formula (V).
There is no particular limitation on the nature of the palladium catalyst used, and any palladium catalyst commonly used in this type of reaction may be used here. Examples of such palladium catalysts include: tetrakis (diphenylphosphino) palladium (o) (tetrakis (triphenylphosphine) palladium (o)), bis (acetonitrile) palladium (II) chloride, bis (triphenylphosphine) palladium (II) chloride, [1, 1-bis (triphenylphosphine) -ferrocene]palladium (II) chloride, tris (dibenzylideneacetone) dipalladium (0), [1, 2-bis (diphenylphosphino) ethane]palladium (II) dichloride and palladium (II) acetate.
There is no particular limitation on the nature of the nickel catalyst used, and any nickel catalyst commonly used in this type of reaction may be used here. Examples of such nickel catalysts include: bis (triphenylphosphine) nickel (II) chloride, [1, 3-bis (diphenylphosphino) propane]nickel (II) chloride and palladium (II) acetoacetate.
The reaction is preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme, particular preference being given to diethyl ether and tetrahydrofuran.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at atemperature of 0 to 120 ℃ and preferably from room temperature to 80 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 30 minutes to 5 hours. Reaction scheme J
This reaction scheme illustrates a method for preparing an optically active sulfoxide compound of the general formula (XXII) as a starting material in reaction scheme E.
In the above formula:
R14j, ring Ar and formulaAs defined above.
Q represents a hydroxyl group or a halogen atom such as a chlorine, bromine, iodine or fluorine atom; and is
Q represents a halogen atom, preferably a bromine atom. Step J1
In this step, a compound of formula (XXXV) is prepared from a compound of formula (XXXIV). Step J1a
When Q is hydroxy, this step may be accomplished by converting the hydroxy group in the compound of formula (XXXIV) to an acetylthio group and then hydrolyzing the acetylthio group with a base to remove the acetyl group.
The first step of the reaction can be accomplished by:
(a) converting the hydroxy group in the compound of formula (XXXIV) to an eliminated group and then reacting the eliminated group with a thioacetate salt; or
(b) The mitussubu reaction was performed using thioacetic acid.
The conversion of the hydroxyl group into an eliminated group in the reaction (a) may be carried out according to the latter reaction of step A9; the thioacetyl substitution is generally accomplished by reaction with a thioacetate in a solvent.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone or cyclohexanone; nitriles such as acetonitrile, propionitrile, and isobutyl nitrile; and amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) or hexamethylphosphoric triamide. Among them, we prefer amides, and particularly prefer dimethylformamide.
Examples of thioates that can be used in this reaction include lithium thioacetate, sodium thioacetate and potassium thioacetate.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 150 ℃ and preferably from room temperature to 100 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 2 days, preferably 2 hours to 24 hours.
The Mitsunobu reaction of (b) can be carried out in the same manner as in step C3, except that a compound of formula (XXXIV) and thioacetic acid are used.
The reaction for eliminating the acetyl moiety in the acetylthio group can be accomplished by treatment with a base in a solvent.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: metal alcoholates, such as sodium methylate; alkali metal carbonates such as sodium carbonate, potassium carbonate and lithium carbonate; alkali metal and alkaline earth metal hydroxides, such as sodium hydroxide, potassium hydroxide and lithium hydroxide and barium hydroxide; and different forms of ammonia such as aqueous ammonia and concentrated methanolic ammonia.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, and any solvent that has been used in the hydrolysis reaction may be used as long as it does not adversely affect the reaction or the reagents used, and can dissolve at least some amount of the reactants. Examples of suitable solvents include: water; organic solvents, for example alcohols (such as methanol, ethanol and propanol), ethers (such as tetrahydrofuran or dioxane) or mixtures of water with any one or more of these organic solvents.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature in the range of 0 to 150 ℃. The reaction time can also vary over a wide range, depending on a number of factors. The main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 1 to 10 hours. Step J1b
When Q is a halogen atom, the compound of formula (XXXIV) and thiourea may be heated in a solvent to react them, followed by hydrolysis to complete the reaction.
This reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: alcohols such as methanol, ethanol or isopropanol.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature ranging from room temperature to 150 ℃, preferably from 50 ℃ to 100 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 4 days,preferably 12 hours to 24 hours.
The hydrolysis reaction of the latter step is generally carried out in a mixture of water and any one of the above formulae and several alcohols.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, the reaction is generally carried out at a temperature ranging from room temperature to 150 ℃, preferably from 50 ℃ to 100 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 30 minutes to 6 hours, preferably 30 minutes to 2 hours. Step J2
In this step, a compound of formula (XXXV) is reacted with a compound of formula (XXXVI) in the presence of a base in a solvent to produce a compound of formula (XXXVII).
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane and diglyme; nitriles such as acetonitrile and isobutyl nitrile;amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) and hexamethylphosphoric triamide. Among them, we prefer ethers, and particularly prefer tetrahydrofuran.
Likewise, there is no particular limitation on the nature of the base used, and any base commonly used in this type of reaction may be used here. Examples of such bases include: alkali metal hydrides such as lithium hydride, sodium hydride, potassium hydride; and organometallic bases such as butyllithium, sec-butyllithium, tert-butyllithium, lithium diisopropylamide and lithium bis (trimethylsilyl) amide. Among these, we prefer an organometallic base, particularly preferably butyl lithium.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-100 to 100 ℃, preferably-78 to 0 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 0.5 to 10 hours, preferably 1 to 6 hours. Step J3
In this step, the compound of formula (XXXVII) is dehydrated to ring closure in the presence of an acid with or without a solvent to prepare the compound of formula (XXXVIII).
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagentsused, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: alcohols such as methanol and ethanol; aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane or diglyme; ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone or cyclohexanone; nitriles such as acetonitrile and isobutyl nitrile; amides, such as formamide, dimethylformamide, dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidone (pyrrolidone) or hexamethylphosphoric triamide. Among them, methanol and ethanol are preferred.
Likewise, there is no particular limitation on the nature of the acid used, and any acid commonly used in this type of reaction may be used here. Examples of such acids include: bronsted acids such as inorganic acids (e.g., hydrochloric acid, hydrobromic acid, sulfuric acid, perchloric acid or phosphoric acid) and organic acids (e.g., acetic acid, formic acid, oxalic acid, methanesulfonic acid, p-toluenesulfonic acid, trifluoroacetic acid or trifluoromethanesulfonic acid); and Lewis acids such as boron trichloride, boron trifluoride, boron tribromide, or acid ion exchange resins. Among them, inorganic acids are preferable, and sulfuric acid is particularly preferable.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of from 0 to 150 ℃, preferably from 50 to 120 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 24 hours, preferably 5 hours to 24 hours. Step J4
In this step, optically active sulphoxide compounds of the general formula (XXXIX) are prepared from compounds of the general formula (XXXVIII)
(a) By direct asymmetric oxidation of compounds of the general formula (XXXVIII) or
(b) The compound of formula (XXXVIII) is oxidized and then optically resolved using a diastereomeric method.
(a) Wherein the asymmetric oxidation of the sulfoxide compound is prepared from a sulfide, is a method using an optically active oxidizing agent, is a chemical method using a combination of an optically active ligand and an oxidizing agent, or is a biological method using baker's yeast and microorganisms. Such asymmetric oxidations are described, for example, in the following references.
1)G.Solladie,Synthesis 185(1981);
2)K.K.Andersen,The Chemistry of Sulfones and Sulfoxides:S.Patai,Z.Rappoport,C.J.M.Stirling.,Eds.Wiley&Sons,Ltd.,Chichester,England,1988,Chapter 3,pp 55-94:G.H.Posner.,ibid,Chapter 16,pp 823-849;
3)H.B.Kagan et al.,Synlett 643(1990);
4)H.B.Kagan,Asymmetric Oxidation of Sulfides in CatalyticAsymmetric Synthesis 1,Ojima Ed.VCH,pp 203-226(1993);
5)F.A.Davis et al.,J.Am.Chem.Soc.,114,1428(1992)。
Among them, the asymmetric oxidation preferably uses (3S, 2R) - (-) -N-phenylsulfonyl) (3, 3-dichlorocamphoryl) oxazolidine or (+) - [ (8, 8-dimethoxycamphoryl) sulfonyl]oxazolidine reported by F.A. Davis et al.
The asymmetric oxidation method is used according to f.a. davis et al, and the reaction is preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and can dissolve at least some amount of the reactants. Examples of suitable solvents include: water; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, isobutanol and isoamyl alcohol; aliphatic hydrocarbons such as hexane and heptane; aromatic hydrocarbons such as benzene, toluene and xylene; halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, dichloroethane, chlorobenzene and dichlorobenzene; esters such as ethyl formate, propyl acetate, butyl acetate and diethyl carbonate; ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane or diglyme; ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophorone or cyclohexanone; nitriles such as acetonitrile and isobutyl nitrile; and pyridine.
The reaction can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-50 to 50 ℃ and preferably at a temperature of-20 ℃ to room temperature. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 10 minutes to 3 days, preferably 2 hours to 1 day.
(b) When the diastereomer method is used for optical resolution, first, the compound of the general formula (XXXVIII) is oxidized to synthesize a racemate of a sulfoxide derivative using a conventional method. Then, the protecting group is removed as described in step C4(i) to give an optically active sulfoxide derivative (XXXIX), which is then salified using an appropriate optically active carboxylic acid as an optical resolving agent and subjected to fractional recrystallization.
The oxidation in the preceding step is carried out with an oxidizing agent with or without a solvent.
Also, there is no particular limitation on the nature of the oxidizing agent used, and any oxidizing agent commonly used for oxidizing sulfides to prepare sulfoxide compounds can be used here. Examples of such oxidizing agents include: peracids, such as m-chloroperbenzoic acid, 2, 5-dinitroperbenzoic acid, o-carboxyperbenzoic acid, peracetic acid, pertrifluoroacetic acid and perphthalic acid; and succinimides such as, for example, N-bromosuccinimide and a base. Among them, peracids are preferable, and m-chloroperbenzoic acid is particularly preferable.
The reaction is generally and preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used, as long as it does not adversely affect the reaction or the reagents used, and at least some amount of the reactants may be dissolved. Examples of suitable solvents include: aromatic hydrocarbons such as benzene, toluene and xylene; a halogenated hydrocarbon; such as dichloromethane, chloroform; ethers such as diethyl ether, tetrahydrofuran, dioxane and dimethoxyethane; amides such as dimethylformamide, dimethylacetamide and hexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide; alcohols such as methanol, ethanol, propanol, isopropanol, butanol, isobutanol, and isoamyl alcohol; dilute acids, such as aqueous sulfuric acid; dilute bases such as aqueous sodium hydroxide; water; ketones such as acetone and methyl ethyl ketone; organic bases, such as pyridine, nitriles, such as acetonitrile; or a mixture of any two or more of the above solvents. Among them, halogenated hydrocarbons are preferable, and methylene chloride is particularly preferable.
The reaction is generally and can be carried out over a wide temperature range, and the precise reaction temperature is not particularly required for the present invention. The preferred reaction temperature is determined by the nature of the solvent, the starting materials or the reagents used, and the like. However, in general, the reaction is carried out at a temperature of-20 to 80 ℃, preferably-5 to 50 ℃. The reaction time can also vary within wide limits, depending on many factors, the main reaction temperature and the nature of the solvents and reagents used. However, assuming that the reaction is carried out under the above-mentioned preferred conditions, it is sufficient that the reaction is carried out for generally 1 to 24 hours, preferably 2 to 12 hours.
The optical resolving agent for carrying out optical resolution is not particularly limited, and examples thereof include tartaric acid, camphor-10-sulfonic acid and mandelic acid, and mandelic acid is particularly preferred.
The reaction is preferably carried out in a solvent. There is no particular limitation on the nature of the solvent used. Provided that it does not adversely affect the reaction or the reagents used and that at least some amount of the reactants may be dissolved. Examples of suitable solvents include: and (3) acetonitrile.
The resulting salt is resolved into the corresponding amine using an appropriate aqueous base such as aqueous sodium hydroxide, followed by extraction with a water-insoluble solvent (e.g., an aromatic hydrocarbon such as benzene, toluene, or xylene, a halogenated hydrocarbon such as dichloromethane or chloroform, or an ether such as diethyl ether), and isolation of the optically active sulfoxide derivative of formula (XXXIX). Step J5
In this step, the compound of formula (XXXIX) is prepared by removing the protecting group R14A compound of the formula (XXII) is prepared. This reaction can be carried out according to the method described in step C4 (i).
After completion of each of the above reactions, the desired compound can be isolated from the reaction mixture using conventional methods.
For example, in one suitable separation method, the reaction mixture is neutralized, if insoluble, filtered off and then a water-immiscible solvent (e.g., ethyl acetate) is added. The organic layer is separated, and then washed with, for example, water, and the resulting compound is dried using, for example, anhydrous magnesium sulfate or anhydrous sodium sulfate. The solvent was then distilled off to give the desired compound.
The resulting compound may, if desired, be purified by one or more of the following methods: recrystallizing and precipitating again; or other methods commonly used for separation and purification of organic compounds, for example, adsorption column chromatography using a carrier such as silica gel, alumina or magnesium-silica gel, Florisil; using a synthetic adsorbent, for example, partition column chromatography using Sephadex (trademark) LH-20 (manufactured by pharmacia Co., Ltd.), Amberlite (trademark) XAD-11 (manufactured by Rohm&Hass Co., Ltd.), Diaion (trademark) HP-20 (manufactured by Mitsubishi Kasei Co., Ltd.); using ion exchange chromatography; or normal/reverse phase liquid chromatography (preferably high performance liquid chromatography) using silica gel or alkylated silica gel.
The starting materials [ e.g., compounds of formula (XXXIV)]are commercially available or can be readily synthesized from known methods.
Biological activity
The novel compounds of the present invention have excellent antagonistic action against substance P and neurokinin A receptors, and further, due to their low toxicity, are useful for the prevention and treatment of diseases caused by the transfer of tachykinins, such as central nervous system diseases including anxiety, depression, psychosis and schizophrenia; neurodegenerative diseases including AIDS dementia, Alzheimer's senile dementia, Alzheimer's disease, Down's syndrome, demyelinating diseases, amyotrophic lateral sclerosis, neuropathy, peripheral neuropathy and neuralgia; respiratory diseases including chronic obstructive pulmonary disease, bronchitis, pneumonia, bronchoconstriction, asthma and cough; inflammatory diseases such as Inflammatory Bowel Disease (IBD), psoriasis, fibrosis, arthritis, osteoarthritis and rheumatoid arthritis; allergic diseases including eczema and rhinitis; allergic diseases, including allergy to vines; ophthalmic diseases including conjunctivitis, vernal mucositis, disruption of the aqueous blood barrier caused by various ocular inflammatory diseases, elevated intraocular pressure and miosis; skin diseases, including contact dermatitis, allergic dermatitis, urticaria and other eczematoid dermatitis; addiction, including alcohol addiction; physical illness caused by stress; sympathetic reflex type malnutrition, including hand and shoulder syndromes; dysthymia; undesirable immune responses, including transplant rejection; diseases associated with enhanced immunity including systemic lupus erythematosus or immunosuppression; digestive system diseases including diseases caused by abnormalities in the neuromodulatory apparatus, colitis, ulcerative colitis and Crohn'sdisease; emesis, including emesis caused by X-ray radiation and chemotherapy, poisons, toxins, pregnancy, vestibular disorders, post-operative disorders, gastrointestinal occlusion, gastrointestinal hypomotility, visceral pain disorders, migraine headaches, increased intracranial pressure, decreased intracranial pressure, or administration of various medications; disorders of bladder function including cystitis and urinary incontinence; eosinophilia caused by collagen disease, palpebral induration and Fasciola liver infection; diseases caused by abnormal blood flow due to vasodilation or vasoconstriction, including angina pectoris, migraine and Reynauds' disease; and nociceptive pain, including migraine, headache, and toothache.
The compounds of the invention may be formulated as oral preparations, for example as tablets, capsules, granules, powders and syrups, or as parenteral preparations, for example as injections or suppositories, these preparations being prepared in a manner known per se using additives such as excipients [ for example sugar derivatives such as lactose, sucrose, glucose, mannitol or sorbitol, starch derivatives such as corn starch, potato starch, α -starch, dextrin or carboxymethyl starch, cellulose derivatives such as crystalline cellulose, low-substituted hydroxypropylcellulose, hydroxypropylmethyl cellulose, carboxymethylcellulose calcium or internally crosslinked carboxymethylcellulose sodium, acacia, dextran, organic excipients such as pullulan, silicate derivatives such as light anhydrous silicic acid, synthetic aluminium or magnesium aluminates (maganesinuline metasiliciicalie), phosphates such as calcium phosphate, carbonates such as calcium carbonate, inorganic excipients such as sulfates (for example calcium sulfate), lubricants [ for example stearic acid and stearic acid metal salts, such as calcium stearate and magnesium stearate, talc, propolis, cetyl wax, and cetyl alcohol], or calcium phosphate, carbonates such ascalcium carbonate, inorganic excipients such as calcium carbonate, such as inorganic excipients such as sulfates (for example calcium sulfate), lubricants [ for example calcium sulfate, magnesium sulfate, sodium stearate, sodium lauryl sulfate, sodium stearate, sodium benzoate, sodium lauryl sulfate, sodium benzoate, sodium lauryl benzoate, sodium.
The dosage will vary depending on the severity of the disease, as well as the age and weight of the patient, and the route of administration. For example, when administered orally, the compound of the present invention is preferably administered once to several times daily at a dose of from 0.01mg/kg body weight (preferably 0.1mg/kg body weight, lower limit) to 100mg/kg body weight (preferably 50mg/kg body weight, upper limit), depending on the severity of the disease. When intravenous urea is administered, the dose is from 0.01mg/kg body weight (preferably 0.05mg/kg body weight, lower limit) to 100mg/kg body weight (preferably 50mg/kg body weight, upper limit) depending on the severity of the disease.
The biological activity of the compounds of the invention can be assessed by the following assay
NK1Receptor binding assay (a) preparation of native Lung Membrane fraction
The natural lung membrane fraction was prepared from the lungs of male guinea pigs of the species Hartley. The guinea pigs were abdominally dissected under chloroform anesthesia and lung airway tissue was rapidly removed.
The extracted buffer (1) (50 mM) for lungpH7.4) pouring into a pot, and cutting. Then, the buffer (2) [ buffer (1) containing 120mM sodium chloride and 5mM potassium chloride]was treated with a Polytro homogen]And (4) stirring and homogenizing. Large pieces of tissue were filtered from the homogenate using a nylon sieve (50μm) and the supernatant was centrifuged (30,000Xg, 30 min, 4 ℃). The resulting pellets were resuspended in ice-cooled buffer (3) [ containing 10 mM%EDTA and 300mM potassium chloride buffer (1)]After standing at 4 ℃ for 60 minutes, the mixture was washed twice by centrifugation (30,000Xg, 15 minutes, 4 ℃).
The native lung membrane fraction was stored at-80 ℃ prior to use. (b) Receptor binding assays
The natural lung membrane fraction solution (250. mu.l) was added to the test drug and3H]substance P (final concentration: 1nM) (50 mM)pH 7.4; 6mM manganese dichloride, 800. mu.g/ml BSA, 8. mu.g/ml chymostatin, 8. mu.g/ml leupeptin, 80. mu.g/ml bacitracin, 20. mu.g/ml phosphoramidon), followed by incubation at room temperature for 30 minutes.
At the end of the culture, the lung membrane fraction was recovered using an automatic filter (manufactured by Brandel co.) equipped with a GF/B glass fiber filter (manufactured by Whatman co).
The glass filter was pretreated with 0.1% polyethyleneimine solution for about 4 hours before use to suppress nonspecific binding as little as possible. The filter from which the membrane components were recovered was transferred to a small plastic tube-shaped vial containing picoflow (4ml) and the radioactivity was measured using a liquid scintillation counter (LSC 3000, manufactured by Beckman co. The results are shown in Table 4
TABLE 4
Test compounds IC50(ng/ml)
Example 75 Compounds 5.9
Compound A 38
Compound B >1000
Compound C 6.5
From the above results, it can be seen that the compounds of the present invention have antagonistic Nk1The activity of the receptor, which is at least equal to the activity of the closest compound with the strongest activity in the prior art, compound C.
NK2Receptor binding assay (a) preparation of native ileal membrane fraction
The native membrane fraction was prepared from the ileum of male guinea pigs of the species Hartley. The guinea pigs were abdominal incised under chloroform anesthesia and rapidly harvested to the ileum.
After scraping the contents, secretions and epithelium from the lumen using a glass slide, the ileum removed was buffered (1) (50 mM)pH7.4) and then in a buffer (2) [ buffer (1) containing 120mM sodium chloride and 5mM potassium chloride]And (4) homogenizing.
Large pieces of tissue were filtered from the homogenate using a nylon sieve (50 μm) and the supernatant was centrifuged (30,000Xg, 30 min, 4 ℃). The resulting pellet was resuspended in ice-cooled buffer (3) [ buffer (1) containing 10mM EDTA and 30mM potassium chloride], and left to stand at 4 ℃ for 60 minutes. Then washed twice by centrifugation (30,000Xg, 15 min, 4 ℃).
The natural membrane fraction was stored at-80 ℃ before use. (b) Receptor binding assays
The natural membrane portion solution (250. mu.l) was added to the test drug and [2]3H]SR-48968 (manufactured by Amasham Co., final concentration: 1nM) (50 mM)pH7.4; 4.6mM manganese dichloride, 800. mu.g/ml BSA, 8. mu.g/ml chymostatin, 8. mu.g/ml leupeptin, 80. mu.g/ml bacitracin, 20. mu.g/ml phosphoramidon), followed by incubation at room temperature for 30 minutes.
At the end of the culture, membrane fractions were recovered using an automatic transition apparatus (manufactured by Brandel Co.) equipped with GF/B glass fiber filters (manufactured by Whatman Co.). The glass filter was pretreated with 0.1% polyethyleneimine solution for about 4 hours before use to minimize inhibition of non-specific binding. The filter from which the membrane component was recovered was transferred to a small plastic tube-shaped bottle containing pico flow (4ml) and the radioactivity was measured using a liquid scintillation counter (LSC 3000, manufactured by beckmanco).
Comparison of the Compounds of the present invention to the NK1And NK2The receptor showed goodActivity of (2).
The results are shown in Table 5
TABLE 5
Test compounds IC50(ng/ml)
Example 75 Compounds 0.85
Compound A 18
Compound B 2.2
Compound C 31
As can be seen from the above results, NK antagonism to the compounds of the present invention2The activity of the receptor, which is greater than any of the closest compounds in the prior art. In addition, NK1The most active compound C was bound in this assay, which was very weak.
Inhibition of SP-induced elevated vascular permeability
Guinea pig (volume: about 400g, male Hartley guinea pig) was used as the test animal, and leakage of pigment was used as the test animalIndex evaluation pair consisting of Substance P (SP), an NK1Inhibition of the increase in vascular permeability induced by receptor agonists. SP (1mg/kg, i.v.) was used immediately after addition of pigment (Evans blue: 20mg/kg, i.v.) and test drug to the guinea pig femoral vein under pentobarbital anesthesia (25mg/kg, i.p.) to induce an increase in vascular permeability. Fifteen minutes later, the guinea pigs were sacrificed under chloroform anesthesia and the amount of pigment permeating into the main bronchi was measured according to the method of Harada (j.pharm. pharmacol., 23, 218, 1971). Inhibition was measured in terms of the amount of pigment penetration found in guinea pigs not treated with the test drug and is expressed in terms of percent inhibition (%) and the dose (ID50) that resulted in 50% inhibition.
The results are shown in Table 6
TABLE 6
Test compounds ID(mg/kg.iv)
Example 75 Compounds 0.025
Example 77 Compounds 0.047
Compound A 5.8
Compound B >10
Compound C 0.019
From the above results, it can be seen that the compounds of the invention have an inhibitory effect on the increase in vascular permeability induced by substance p, with an action strength at least equal to that of the closest compound of the prior art, compound C, which is the most active.
Inhibition of NKA-induced bronchiectasis
Guinea pigs (body weight: about 500g, male Hartley guinea pigs were used as test animals according to the modified method of Konzett-Rossler [ Nauyn-Schmiedeebergs Arch.Exp.Pathol.Pharmakol.195, 71, (1940)]Using airway pressure as index to specify the general formula [ Nle10]-NKA (4-10), an NK specific for neurokinin A (NKA) higher2Receptor agonists, inhibition of induced bronchodilation.
Pentobarbital anesthesia (30mg/kg, s.c.) followed by tracheal intubation in guinea pigs and treatment with Carlamine (20mg/kg, i.v.), at a frequency of 60 per minute and a tide of 8ml/kgVolume, experimental animals were artificially ventilated with a constant volume respiratory pump (Ugo Basile, 7025). Airway pressure during artificial ventilation was amplified by a pressure transducer (Nihon Koden. tp-200T) mounted on the endotracheal tube branch, measured (Nihon Koden, AP-610G), and recorded with a recorder (Nihon Koden, WT-685G). Test drugs were injected intravenously after pretreatment with atropine (1mg/kg, i.v.) and propranolol (1 mg/kg.i.v.). Five minutes later, [ Nle]at 4mg/kg.i.v10]-NKA[4-10]Bronchodilation was induced and airway pressure was then measured over a period of 10 minutes. The inhibition was determined from the intensity of bronchodilation in guinea pigs not treated with test drug, and the percent inhibition (%) and the dose (ID) resulting in 50% inhibition were used50) To indicate.
The results are shown in Table 7:
TABLE 7
Test compounds ID50(mg/kg.iv.)
Example 75 Compounds 0.074
Example 77 Compounds 0.047
Compound A >10
Compound B 0.37
Compound C 1.7
As can be seen from the above results, the compounds of the present invention have antagonistic NK activity2The activity of the receptor, which is greater than any of the closest compounds in the prior art.
As can be seen from the above data, the compounds of the present invention are directed to NK1And NK2All receptors have strong antagonismAnd (4) resisting activity. In addition, the compounds of the present invention are useful for NK1Antagonistic activity against receptors at least equal to that of the closest compounds of the prior art, and against NK2The antagonistic activity of the receptor is greater than that of the closest compounds in the prior art.
Preparation example 1
N, N-dimethyl-1-tert-butyloxycarbonyl-4-phenylpiperidine-4-carboxamide
1.0g (3.27mmole) of tert-butoxycarbonyl-4-phenylpiperidine-4-carboxylic acid are dissolved in 20ml of anhydrous dichloromethane, and 690mg (3.6mmole) of 1-ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride, 490mg (3.6mmol) of 1-hydroxybenzotriazole, 1.3ml (7.53mmole) of diisopropylethylamine and 295mg (3.93mmole) of diethylamine hydrochloride are added to the resulting solution, which is then stirred at room temperature under a nitrogen atmosphere for 15 hours. At the end of the stirring, the reaction mixture was diluted with dichloromethane, washed sequentially with water and saturated solution of sodium chloride, and then dried over anhydrous sodium sulfate.
The solvent was removed by distillation under the reduced pressure, and the residue was purified by silica gel column chromatography using a gradient elution method with a mixture of ethyl acetate and hexane in a volume of 10: 1 to 7: 1 as an eluent, to give 925mg (yield 85%) of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3) δ ppm: (the following and following preparations and examples have the following meanings in English words in nuclear magnetic data: double triplets for double doublets, multiplets for multiplets, broad singlets for broad Singlet, doublets for doublets, singlets for Singlet, triplets for doublets, doublets for doublets, and the like.
7.34(2H,doublet of triplets,J=6.7&1.9Hz);
7.26-7.21(3H,multiplet);
3.96(2H,broad singlet);
3.21(2H,broad singlet);
2.85(3H,broad singlet);
2.60(3H,broad singlet);
2.31(2H,doublet,J=12.05Hz);
1.87(2H,broad singlet);
1.45(9H, singlets). Mass Spectrometry (EI) m/z: 332 (M)+). "EI" means "electron impact ionization"
Preparation example 2
N, N-dimethyl-4-phenylpiperidine-4-carboxamide hydrochloride
900mg (2.7mmole) of N, N-dimethyl-1-tert-butoxycarbonyl-4-phenylpiperidine-4-carboxamide (prepared as described in preparation example 1) are dissolved in 10ml of ethyl acetate under ice cooling, and 5ml of a 4N hydrogen chloride solution in dioxane are added thereto. The mixture was then stirred at 0 ℃ for 1 hour. At the end of the stirring, the precipitated crystals were collected by filtration to yield 690mg (yield 95%) of the title compound as white crystals. Nuclear magnetic resonance spectrum (400MHz, hexadeuterium dimethyl sulfoxide (δ ppm):
9.02(1H,broad singlet);
7.43(2H,triplet,J=7.6Hz);
7.31(1H,doublet,J=7.2Hz);
7.23(2H,doublet,J=7.1Hz);
3.25(2H,doublet,J=13.1Hz);
3.03(2H,triplet,J=12.1Hz);
2.79(3H,broad singlet);
2.54(3H,broad singlet);
2.37(2H,doublet,J=12.9Hz);
2.11(2H,doublet of triplets,
J=13.4&3.3Hz) mass spectrometry (EI) m/z: 232 (free form, M)+)
Preparation example 3
Spiro (benzo [ C]thiophene-1 (3H), 4' -piperidine]hydrochloride
3(a)1 '-Cyanospiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]
2.34g (22.1mmol) of cyanogen bromide are dissolved in 20ml of anhydrous chloroform and 2.2g (10mmole) of an anhydrous chloroform solution of 1 '-methylspiro [ benzo [ c]thiophene-3 (H), 4'-piperidine][ synthesized as described in J.org.chem., Vol.41.page 2628(1976)]are added dropwise over a period of 20 minutes under nitrogen atmosphere under reflux. The mixture was then heated under reflux for 9 hours, after which the reaction mixture was cooled and poured into ice-cooled 1N aqueous hydrochloric acid solution. The chloroform layer was separated, washed with water and dried over anhydrous sodium sulfate.
The solvent was evaporated under reduced pressure and the residue was purified by column chromatography on silica gel using a 1: 9 by volume mixture of ethyl acetate and hexane as eluent to give 1.3g (56% yield) of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.38-7.27(3H,multiplet);
7.21(1H,doublet of doublets,
J=1.9&6.4Hz);
4.20(2H,singlet);
3.51(2H,multiplet);
3.37(2H,doublet,of triplets
J=2.2&12.9Hz);
2.29(2H,doublet of triplets,
J=4.6&12.9Hz);
1.91(2H, multiplex). Mass Spectrometry (FAB) m/z: 231(M + M)+) FAB is "fast atom bombardment" 3(b) 1' -tert-butyloxycarbonyl spiro [ benzo [ C]]Thiophene-1 (3H), 4' -piperidines]1.3g (5.64mmole) of 1' -cyanospiro [ benzo [ C]]Thiophene-1 (3H),4' -piperidines][ preparation according to the above step (a)]Dissolved in 20% w/v aqueous hydrochloric acid and the solution heated to reflux for 20 hours. At the end of the heating, the reaction mixture was cooled and washed with ethyl acetate. The aqueous layer was separated and basified with 10% w/v aqueous sodium hydroxide; it was then extracted three times with chloroform. The solvent of the combined extracts was removed by distillation under reduced pressure, and the residue was dissolved in anhydrous dichloromethane; under ice-cooling, 1.15ml (8.18mmol) of triethylamine and 1.45g (6.64mmol) of di-tert-butylcarbonate were added. The mixture was then stirred at room temperature for 2 hours. At the end of the stirring, the reaction mixture was diluted with dichloromethane and washed sequentially with water and saturated aqueous sodium chloride solution. The organic layer was separated and dried over anhydrous sodium sulfate, and then the solvent was removed under reduced pressure. The residue was purified by silica gel column chromatography using ethyl acetate and hexane in a volume ratio of 3: 97 as an eluent to give 1.65g (yield 96%) of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.28-7.24(3H,multiplet);
7.17-7.15(1H,multiplet);
4.23(2H,broad singlet);
4.19(2H,singlet);
3.02(2H,broad singlet);
2.07(2H,doublet,of triplets
J=4.4&13Hz);
1.88(2H,multiplet);
1.49(9H, singlet). Mass Spectrometry (EI) m/z: 305 (M)+)
3(C) spiro [ benzo [ C]]Thiophene-1 (3H), 41-piperidine (III)]Hydrochloride salt
150mg (0.49mmole) of 1 '-tert-butoxycarbonylspiro [ benzo [ C]thiophene 1(3H), 4' -piperidine][ prepared as in step (b) above]was dissolved in 3ml of anhydrous dichloromethane, and 1ml of 4N dioxane hydrochloride solution was added. The mixture was then stirred at room temperature for 1 hour. At the end of the stirring, the crystals deposited were collected by filtration to yield 108mg (yield 91%) of the title compound as white crystals. Nuclear magnetic resonance spectrum (400MHz, hexadeuterium dimethyl sulfoxide) δ ppm:
9.77(2H,broad singlet);
7.37-7.25(4H,multiplet);
4.24(2H,singlet);
3.67(2H,doublet,J=12.6Hz);
3.26(2H,doublet of triplets,
J=12.6&2.5Hz);
2.74(2H,doublet of triplets,
J=3.8&14.0Hz);
2.09(2H, doublet, J ═ 14.0 Hz). Mass Spectrometry (FAB) m/z: 206(M + H)+(free form)
Preparation example 4
Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2-oxide hydrochloride
4(a)1 '-tert-Butoxycarbonylspiro [ benzo [ C]thiophene-1 (3H), 4'
-piperidine]-2-oxide
485mg (1.59mmole) of 1' -tert-butoxycarbonylspiro [ benzo [ C]was added under ice-cooling]Thiophene-1 (3H), 4' -piperidines][ preparation according to the above preparation example 3(b)]]Dissolved in 5ml of anhydrous dichloromethane, 148mg (1.76mmole) of sodium hydrogencarbonate and subsequently 325mg (1.88mmole, content: 85%) of m-chloroperbenzoic acid were added. The reaction mixture was stirred for 30 minutes under ice-cooling, after which it was diluted with dichloromethane and washed sequentially with water and a saturated aqueous solution of sodium chloride. The solution was dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The resulting residue was purified by thin layer chromatography using ethyl acetate and hexane in a 2: 1volume ratio as developing solvent to give 498mg (98% yield) of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.37-7.32(3H,multiplet);
7.25-7.23(1H,multiplet);
4.37(1H,doublet,J=16.7Hz);
4.13(2H,broad singlet);
4.05(2H,doublet,J=16.7Hz);
3.21(2H,broad singlet);
2.43(1H,multiplet);
2.21(1H,multiplet);
1.70(1H,multiplet);
1.61(1H,multiplet);
1.50(9H, single); mass Spectrometry (FAB) m/z: 322(M + H)+
4(b) spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2-
Hydrochloride of an oxide
295mg (0.92mmol) of 1 '-tert-butoxycarbonylspiro [ benzo [ C]]thiophene 1(3H), 4' -piperidine]-2-oxide (prepared as in the above step (a)) was dissolved in 3ml of dichloromethane, and 1ml of 4N hydrogen chloride dioxane solution was added under ice-cooling, the mixture was stirred for 1 hour, and then the deposited crystals were collected by filtration to give 173mg (yield 75%) of the title compound as white crystals under ice-cooling, nuclear magnetic resonance spectroscopy (400MHz, deuterium dimethyl sulfoxide) δ ppm:
9.13(2H,broad singlet);
7.44-7.36(3H,multiplet);
7.33-7.31(1H,multiplet);
4.66(1H,doublet,J=17Hz);
4.08(1H,doublet,J=17Hz);
3.49-3.37(2H,multiplet);
3.15-3.00(2H,multiplet);
2.66-2.57(1H,multiplet);
2.27-2.23(1H,multiplet);
2.18-2.10(1H,multiplet);
1.97-1.93(1H, multiplex); mass Spectrometry (FAB) m/z: 222(M + H)+(free form)
Preparation example 5
Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2, 2-dioxide hydrochloride
5(a) 1' -tert-butoxycarbonylspiro [ benzo [ C]thiophene-1 (3H),
4' -piperidine]-2, 2-dioxide
190mg (0.59mmole) of 1' -tert-butoxycarbonylspiro [ benzo [ C]]Thiophene 1(3H), 4' -piperidines]-2-oxide [ prepared as in preparation 4(a) above]Dissolved in 30ml of methanol, and then dissolved in the solvent,and 10ml of an aqueous solution containing 270mg (1.77mmole) of Oxone (trade mark) were added. The reaction mixture was stirred at room temperature for 5 days, after which it was poured into water and extracted twice with chloroform. The organic extract was separated, dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure. The resulting residue was purified by thin layer chromatography using a 1: 1 volume ratio mixture of ethyl acetate and hexane as a developing solvent to give 175mg (88% yield) of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.52-7.27(3H,multiplet);
7.23-7.20(1H,multiplet);
4.36(2H,singlet);
4.10(2H,broad singlet);
3.44(2H,broad singlet);
2.38(2H,multiplet);
2.00(2H,multiplet);
1.50(9H, singlets). Mass Spectrometry (FAB) m/z: 337 (M)+)
5(b) spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2, 2-
Dioxide hydrochloride
170mg (0.5mmole) of 1 '-tert-butoxycarbonylspiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2, 2-dioxide [ prepared as in step (a) above]was dissolved in 3ml of dichloromethane under ice-cooling, and 1ml of 4N hydrogen chloride dioxane solution was added. The mixture was then stirred under ice-cooling for 1 hour, after which the deposited crystals were collected by filtration to give 131mg (yield 95%) of the title compound as white crystals. Nuclear magnetic resonance spectrum (400MHz, hexadeuterium dimethyl sulfoxide) δ ppm:
9.32(2H,broad singlet).
7.51-7.35(4H,multiplet).
4.74(2H,singlet).
3.45-3.67(2H,multiplet).
3.24-3.12(2H,multiplet).
2.47-2.43(4H, multiplex). Mass Spectrometry (FAB) m/z: 238(M + H)+(Game)From type)
Preparation example 6
Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]- (2S) -oxidations
Substance hydrochloride
6(a) Spiro 1 '-Boc-Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]
81.0g (0.40mole) of 2-bromobenzylthiol are dissolved in 800ml of tetrahydrofuran and 0.84mole of butyllithium (solution in 1.6M hexane) is added dropwise at a temperature of-78 ℃ over a period of 6 hours. Then, the mixture was stirred at this temperature for 1.5 hours, after which 800ml of a tetrahydrofuran solution containing 79.5g (0.40mole) of 1-t-butoxycarbonyl-4-piperidone was added dropwise over a period of 3 hours. The solution was stirred for another 1 hour, and then a saturated aqueous solution of ammonium chloride was added. And the mixture was extracted with ethyl acetate. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. To the residue was added 2 liters of a 4N aqueous sulfuric acid solution, and the mixture was heated under reflux for 14 hours. At the end of heating, 350g (8.75mole) of sodium hydroxide was added under ice cooling to basify the solution, and then 102g (0.47mole) of di-t-butyl carbonate (di-t-butyl carbonate) was added.The mixture was stirred for 1 hour. At the end of the stirring, it is extracted with dichloromethane and the organic extract is washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure and the residue was purified by column chromatography on silica gel using a 97: 3 volume ratio mixture of hexane and ethyl acetate as eluent to give 56g of the title compound as white crystals with a melting point of 131.0-132.5 deg.C (after crystallization from hexane/ethyl acetate). Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.28-7.24(3H,multiplet);
7.17-7.15(1H,multiplet);
4.23(2H,broad singlet);
4.19(2H,singlet);
3.02(2H,broad singlet);
2.07(2H,doublet of triplets,
J=4.4&13Hz);
1.88(2H,multiplet);
1.49(9H, singlets.) Infrared absorption Spectrum vmaxcm-1(KBr): 2970, 1680, 1428, 1234, 1163. Mass Spectrometry (FAB) m/z: 306(M + H)+
6(b) 1' -Boc-Spiro [ benzo [ C]thiophene-1 (3H)
4' -piperidine]-2-oxide
42.0g (0.14mole) of 1' -tert-butoxycarbonylspiro [ benzo [ C]]Thiophene-1 (3H), 4' -piperidines][ preparation according to the above step (a)]Dissolved in 420ml chloroform and added with 12.7g (0.15mole) sodium bicarbonate. Under ice-cooling, 28.0g (0.14mole) of m-chloroperbenzoic acid (purity 95%) was added little by little. Then, the mixture was stirred for 30 minutes under ice-cooling, after which 10g of potassium iodide was added, and the mixture was stirred for another 30 minutes at room temperature. The reaction mixture was washed with water and then saturated aqueous solution of sodium chloride, and anhydrous magnesium sulfateAnd (5) drying. Thereafter, the solvent was distilled off under reduced pressure, and the resulting residue was purified by silica gel column chromatography using a 1: 1 volume ratio mixture of hexane and ethyl acetate as an eluent to give 42g of the title compound as white crystals having a melting point of 103 ℃ and 107 ℃ (crystallization from diisopropyl ether). Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.37-7.32(3H,multiplet);
7.25-7.23(1H,multiplet);
4.37(1H,doublet,J=16.7Hz);
4.13(2H,broab singlet);
4.05(2H,doublet,J=16.7Hz);
3.21(2H,broad singlet);
2.43(1H,multiplet);
2.21(1H,multiplet);
1.70(1H,multiplet);
1.61(1H,multiplet);
1.50(9H, singlets.) Infrared absorption Spectrum vmaxcm-1(KBr): 2985, 1686, 1429, 1368, 1286, 1167. Mass spectrometric analysis(FAB)m/z:322(M+H)+
6(C) spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2-oxide
42.0g (0.13mole) of 1 '-tert-butoxycarbonylspiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2-oxide [ prepared as in step (b) above]was dissolved in 420ml of 2-propanol under ice-cooling, and 150ml of a 4N hydrogen chloride dioxane solution was added. The mixture was then stirred for 4 hours. At the end of the stirring, 200ml of ether was added to the mixture under ice-cooling, and it was left for l hours. The precipitated crystals were collected by filtration. The crystals were dissolved in 200ml of 5% w/v aqueous sodium hydroxide solution. The resulting product was extracted with dichloromethane and the organic extracts were dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain 21.7g of the title compound in the form of a white amorphous.
6(d) Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]- (2S)
(S) - (+) -mandelate salt as monoxide
33.51g (0.15mole) of spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2-oxide [ prepared as described in step (C) above]were dissolved in 3350ml of acetonitrile with heating. 11.52g (75.7mmole) (S) - (+) -mandelic acid was then dissolved in the solution obtained. The mixture was allowed to stand at room temperature overnight, and the precipitated crystals were collected by filtration to give 19.62g of the title compound as white crystals. The mother liquor was concentrated by evaporation under reduced pressure and the residue obtained was dissolved in 5% w/v aqueous sodium hydroxide solution; it was then extracted with dichloromethane. The organic extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain 22.01g (99.5mmole) of a residue. The residue was dissolved in 2200ml of acetonitrile by heating, and then 7.22g (47.5mmole) (R) - (-) -mandelic acid was dissolved therein. The mixture was allowed to stand at room temperature overnight, and the precipitated crystals were collected by filtration to give 15.91g of spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]- (2R) -oxide (R) - (-) -mandelate as white crystals. The mother liquor was concentrated by evaporation under reduced pressure, and the resulting residue was dissolved in 5% w/v aqueous sodium hydroxide solution and extracted with dichloromethane. The organic extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain 11.51g (52.0mmole) of a residue. The residue was dissolved in 1100ml of acetonitrile by heating, and 3.95g (26.0mmole) (S) - (+) -mandelic acid was dissolved therein. The mixture was left at room temperature overnight. The precipitated crystals were collected by filtration to obtain 4.73g of the title compound as white crystals.
All the resulting title compounds were combined, heated to redissolve 24.00g of the compound in 9.6 liters of acetonitrile, and the solution was allowed to stand overnight at room temperature. 20.13g of precipitated crystals were obtained, having a melting point of 197-. Converting it into a 1' -tert-butoxycarbonylspiro [ benzo [ C]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide, HPLC (high Performance liquid chromatography) analysis showed 99.8% ee in optical purity [ α]]D 24+ 78.3 (C1, methanol) infrared absorption spectrum vmaxcm-1(KBr): 3388, 3029, 1629, 1332, 1017. Mass Spectrometry (EI) m/z: 221(free form, M)+)
6- (e) 1' -tert-butoxyspiro [ benzo [ C]thiophene-1 (3H),
4' -piperidine]- (2S) -oxide
19.88g (53.2mmole) of spiro [ benzo (C)]Thiophene-1 (3H) 4' -piperidines]- (2S) -oxide (S) - (+) -mandelate salt prepared according to step (d) above]Dissolving in 200ml of 5% w/v aqueous sodium hydroxide solution and extracting three times with 200ml of dichloromethane each time, drying the combined organic extracts over anhydrous magnesium sulfate, then evaporating off the solvent under reduced pressure, dissolving 11.80g of the residue in 300ml of dichloromethane under ice cooling, and adding 11.2ml (79.8mmole) of triethylamine and 17.4g (79.8mmole) of di-tert-butyl carbonate in succession, stirring the mixture at room temperature overnight, at the end of the stirring, diluting the reaction mixture with 200ml of dichloromethane, washing it with 10% w/v aqueous citric acid and then with saturated aqueous sodium bicarbonate, drying it over anhydrous magnesium sulfate, evaporating off the solvent under reduced pressure, eluting with a mixture of hexane and ethyl acetate in a volume ratio of 4: 6 to 3: 7, purifying the residue by column chromatography using gradient elution, then recrystallizing it with diisopropyl ether to give 13.1g of the title compound in the form of white crystals, m.p. 129.0-130.5 ℃ [ α]]D 24+ 57.1(C ═ 1, methanol) HPLC analysis
Column: chiral Cel OD (250X 4.6mm phi)
Eluent: hexane: 2-propanol 80: 20 by volume
Flow rate: 0.8 ml/min
Retention time: 18.1 minutes
The NMR spectrum, IR absorption spectrum and mass spectrum analysis data of this isomer were in agreement with those of the racemate described in preparation example6 (b).
6(f) Spiro [ benzo [ C]thiophene-1 (3H), 4' -piperidine]-2(S)
-oxide hydrochloride
Under ice-cooling, 13.0g (40.4mmole) of 1' -tert-butoxycarbonylspiro [ benzo [ C]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide [ prepared as in step (e) above]Dissolved in 130ml of 2-propanol and 50ml of 4N hydrogen chloride in dioxane were added. The mixture was stirred at the same temperature for 1 hour, and then at room temperature for another 6 hours. The reaction mixture was concentrated by evaporation under reduced pressure. 200ml of diethyl ether are added to the residue and the solvent is distilled off under reduced pressure;this procedure was repeated three times and the residue was recrystallized from 300ml of a 1: 2 by volume mixture of methanol and diethyl ether to give 9.10g of the title compound as white crystals having a melting point of 209.5-210.5 ℃ [ α]]D 24+63.8(C ═ 1, methanol) nuclear magnetic resonance spectrum (400MHz, CD)3OD)δppm:
7.38-7.46(4H,multiplet);
4.69(1H,doublet,J=17.2Hz);
4.17(1H,doublet,J=17.2Hz);
3.52-3.63(2H,multiplet);
3.25-3.40(2H,multiplet);
2.62(1H,multiplet);
2.51(1H,multiplet);
2.22(1H,multiplet);
2.06(1H,multiplet).
6(g) 1' -tert-butoxycarbonylspiro [ benzo [ C]thiophene-1 (3H).
4' -piperidine]-2(S) -oxide
250mg (0.82mmole) of 1 ' -tert-butoxycarbonylspiro [ benziso [ C]thiophene-1 (3H), 4 ' -piperidine]was dissolved in 5ml of methylene chloride, and 308mg (0.82mmole) of (3 ' S, 2R) - (-) -N- (benzenesulfonyl) (3, 3-dichlorocamphoryl) oxaziridine synthesized by the procedure of F.A.Davis et al [ J.Am.chem.Soc., 114.1428(1992)]was added to the resulting solution. The resulting mixture was then stirred at room temperature overnight. 500mg of potassium iodide was added to the mixture, and the mixture was stirred for 30 minutes. Then, it was washed with water and a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography using a 1: 2 volume ratio mixture of hexane and ethyl acetate as an eluent to give 245mg of the title compound.
Optical purity: 94% ee
Preparation example 7
3- (3, 4-dichlorophenyl) -3-butenol tert-butyl dimethyl
Silyl ethers
7(a)3- (3, 4-dichlorophenyl) -3-oxo-1-propanol
L19g (0.46mole) ethyl 3- (3, 4-dichlorophenyl) -3-oxopropanoate was dissolved in 2.4 l ethanol and 115ml (0.68mole) ethyl orthoformate and 4.4g (22.8mmole) p-toluenesulphonic acid were added. The mixture was heated to reflux for 8 hours. At the end of the reflux, the reaction solution was poured into 1 l of saturated aqueous sodium bicarbonate solution and extracted three times with 700ml of ethyl acetate each time. The combined organic extracts were washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 800ml of tetrahydrofuran, and then 4 liters of a tetrahydrofuran suspension containing 25.9g (0.68mole) of lithium aluminum hydride was added dropwise thereto under ice-cooling over a period of 1 hour. The mixture was stirred at 0 ℃ for 2 hours, then 250ml of water and 125ml of 10% w/sodium hydroxide aqueous solution were added and the mixture was stirred at room temperature for a further 1 hour. It was filtered through a Celite (trade name) filter, and the filtrate was poured into 1L of a saturated aqueous solution of sodium chloride and extracted with ethyl acetate. The organic extracts were dried over anhydrous sodium sulfate and concentrated by evaporation under reduced pressure. The residue obtained is dissolved in 500ml of chloroform. 500ml of 50% v/v trifluoro were added over a period of 30 minutes under ice coolingAn aqueous acetic acid solution was added to the resulting solution. And the mixture was stirred at the same temperature for another 30 minutes. At the end of the stirring, the reaction solution was diluted with 300ml of chloroform, and the organic layer was washed with water and then with an aqueous solution of sodium hydrogencarbonate, followed by drying over anhydrous sodium sulfate. The solvent was removed under reduced pressure and the resulting residue was purified by column chromatography on silica gel using a 9: 1 by volume mixture of hexane and ethyl acetate as eluent to give 46g of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (270MHz, CDCl)3)δppm:
8.05(1H,doublet,J=2.0Hz);
7.79(1H,doublet of doublets,
J=2.0&8.1Hz);
7.57(1H,doublet,J=8.1Hz);
4.04(2H,multiplet);
3.19(2H,triplet,J=5.3Hz);
2.44(1H, triplet, J ═ 6.6Hz), this peak was spiked with D2ODisappear when necessary)
7(b)3- (3, 4-dichlorophenyl) -3-oxo-1-propanol
Tert-butyldimethylsilyl ether
46.0g (0.21mole) of 3- (3, 4-dichlorophenyl) -3-oxo-1-propanol [ prepared according to step (a) above]Dissolved in 460ml of methylformamide and added with 35ml (0.25mole) of triethylamine and 38.0g (0.25mole) of tert-butyldimethylsilyl chloride. The mixture was then stirred at 0 ℃ for 2 hours. At the end of stirring, the reaction mixture was poured into water and extracted with ethyl acetate. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure and the residue was purified by silica gel column chromatography using hexane and ethyl acetate in a 96: 4 volume ratio as an eluent to give 66.1g of the title compound as white crystals. Nuclear magnetic resonance spectroscopy (270MHz, CDCl)3)δppm:
8.06(1H,doublet,J=2.0Hz);
7.80(1H,doublet of doublets,
J=2.0&8.3Hz);
7.55(1H,doublet,J=8.3Hz);
4.04(2H,triplet,J=6.3Hz);
3.13(2H,triplet,J=6.3Hz);
0.85(9H,singlet);
0.04(6H,singlet).
7(C)3- (3, 4-dichlorophenyl) -3-butenol tert-butyl bis
Methyl silyl ethers
215g (0.60mole) of methyltriphenyl bromide and 54g (0.48mole) of potassium tert-butoxide were added to 2 liters of anhydrous benzene, and the mixture was stirred at room temperature for 9 hours. At the end of the stirring, a solution of 40g (0.12mole) of 3- (3, 4-dichlorophenyl) -3-oxo-1-propanol tert-butyldimethylsilyl ether [ prepared according to the above step (b)]dissolved in 800ml of benzene was slowly dropped into the mixture over a period of 2.5 hours. Then, 1 liter of water was added to the reaction mixture, and the reaction mixture was stirred for 30 minutes under ice-cooling. The organic phase was separated, washed with water and saturated aqueous solution of sodium chloride, and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure and the resulting residue was purified by silica gel column chromatography using hexane as an eluent to give 23.5g of the title compound. The physicochemical properties of this product were the same as the product prepared in example 1 (b).
Preparation example 8
3- (3, 4-dichlorophenyl) -3-butenol tert-butyl dimethyl
Silyl ethers
129mg (5.31mmole) of magnesium flakes are added to 2ml of diethyl ether and a small amount of iodine is added to the mixture. A solution of 1.01g (4.47 mmoles) of 3, 4-dichlorobromobenzene in 1ml of diethyl ether was then added dropwise to the mixture, and the mixture was stirred at room temperature for 1 hour under a nitrogen atmosphere to give the Grignard reagent.
500mg (1.60mmole) of 3-iodo-3-butanol tert-butyldimethylsilyl ether and 34mg (0.048mmole) of dichlorobis (triphenylphosphine) palladium (II) were dissolved in 5ml of tetrahydrofuran and the Grignard reagent previously prepared was added dropwise at room temperature under nitrogen. As the reaction temperature rose, diethyl ether was distilled off and the reaction mixture was heated at 60 ℃ for 1 hour. At the end of the heating, the reaction mixture was poured into aqueous ammonium chloride solution and extracted with ethyl acetate. The organic layer was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified by silica gel column chromatographyusing hexane as an eluent to give 422mg of the title compound. The physicochemical properties of this product are identical to those of the product of example 1 (b).
Example 11- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide 1(a) methyl 3- (3, 4-dichlorophenyl) -3-butanoate
To 300ml of diethyl ether was added 11.31g (0.47mole) of magnesium flakes followed by a small amount of iodine. The mixture was then left to stand for 1 hour, after which a solution of 102.87g (0.46mole) of 1-bromo-3, 4-dichlorobenzene in 150ml of diethyl ether was slowly added dropwise. 150ml of diethyl ether are additionally added, then 60.33g (44.3mmole) of anhydrous zinc chloride are slowly added and the mixture is stirred for 1 hour. Then 3.10g (4.42mmole) are addedDichlorobis (triphenylphosphine) palladium (II) and a solution of 34.15ml (42.8mmole) of diketene in 600ml of diethyl ether is added dropwise. The reaction mixture is stirred at room temperature for 30 minutes, then poured into 1 l of ice-cooled 1N aqueous hydrochloric acid and extracted three times with 500ml of diethyl ether each time. The combined organic extracts were extracted three times with 700ml of 1N aqueous sodium hydroxide solution each time. The combined aqueous extracts were acidified with concentrated aqueous hydrochloric acid and extracted three times with 500ml of ether each time under ice cooling, and the combined organic extracts were dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 350ml of methanol. 10ml of concentrated sulfuric acid aqueous solution was added, and the solution was heated under reflux for 30 minutes. At the end of the reflux, the reaction mixture was cooled in air and neutralized with a saturated aqueous solution of sodium bicarbonate. Methanol was distilled off under reduced pressure and the residue was extracted three times with 200ml of dichloromethane each time. The combined organic extracts were dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The resulting residue was distilled under reduced pressure to give 69.13g (yield 62%) of the title compound as a pale yellow oil having a boiling point of 144 ℃ and 146 ℃ (5 mmHg). CoreMagnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.51(1H,doublet,J=2.2Hz);
7.40(1H,doublet,J=8.2Hz);
7.25(1H,doublet,of doublets,
J=8.2&2.2Hz);
5.55(1H,singlet);
5.30(1H,singlet);
3.67(3H,singlet);
3.49(2H, singlet). 1(b)3- (3, 4-dichlorophenyl) -3-butenol tert-butyldimethylsilyl ether
11.76g (0.28mole) of lithium aluminum hydride was suspended in 500ml of anhydrous tetrahydrofuran, and 69.06g (0.28mole) of methyl 3- (3, 4-dichlorophenyl) -3-butanoate [ prepared according to step (a) above]was slowly added dropwise at 0 ℃ under a nitrogen atmosphere over 15 minutes]Solution in 500ml of anhydrous tetrahydrofuran. The reaction mixture was stirred at the same temperature for 30 minutes, then 500ml of water and 500ml of 10% w/v hydrogen were slowly addedAn aqueous sodium oxide solution. The mixture was stirred at room temperature for 1 hour. It is then filtered through Celite (trade mark) filter aid and the filtrate is extracted three times with 500ml of ethyl acetate each time. The combined organic extracts were dried over anhydrous magnesium sulfate. The solvent in the extract was distilled off under reduced pressure, and the resulting residue was dried under reduced pressure. The residuewas dissolved in 250ml of anhydrous dimethylformamide, and then 47.12ml (0.34mole) of triethylamine, 6.88g (0.06mole) of 4-dimethylaminopyridine and 50.96g (0.34mole) of t-butyldimethylsilyl chloride were sequentially added under ice-cooling. The mixture was then stirred under ice-cooling for 2 hours. At the end of the stirring, 1 l of ethyl acetate was added to the reaction mixture and the mixture was washed successively with ice-cooled 10% w/v aqueous hydrochloric acid and saturated aqueous sodium chloride solution. It was then dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified by flash column chromatography on silica gel using a gradient elution method with a mixture of hexane and ethyl acetate in a volume ratio of 50: 1 to 20: 1 as an eluent, to give 43.52g (yield 47%) of the title compound as a colorless oil. Nuclear magnetic resonance spectroscopy (400MHz,CDCl3)δppm:
7.50(1H,doublet,J=2.1Hz);
7.38(1H,doublet,J=8.1Hz);
7.24(1H,doublet of doublets,
J=8.1&2.1Hz);
5.35(1H,singlet);
5.16(1H,singlet);
3.70(2H,triplet,J=6.9Hz);
2.67(2H,triplet,J=6.9Hz);
0.86(9H,singlet);
0.00(6H, singlet).1(C) 4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) butane-1, 2-diol
790mg (1.01mmole) of hydroquinidine 1, 4-naphthyridinediyldiether (hydroquinidine 1, 4-phthalazinediyldiether), 100.19g (0.30mole) of potassium ferricyanide (III),42.06g (0.30mole) potassium carbonate and 0.516ml (0.20mmole) osmium tetroxide (solution in 0.393M toluene) are dissolved in 500ml of tert-butanol and 500ml of water, and 33.61g (0.10mole) of 3- (3, 4-dichlorophenyl) -3-butenol tert-butyldimethylsilyl ether [ prepared according to step (b) above]are added while cooling at 0 deg.C]The mixture was stirred at 0 ℃ for 5 hours, at the end of the stirring 150g of sodium sulfite were added and the reaction mixture was stirred at room temperature for 1 hour, then it was extracted three times with 800ml of ethyl acetate each time, and the combined organic extracts were dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, and the resulting residue was purified by flash column chromatography on silica gel using a gradient elution method with a 5: 1 to 1: 1 volume ratio mixture of hexane and ethyl acetate as eluent to give 32.3g (yield 87%) of the title compound as a colorless oil with an optical purity of 97% ee [ α]]D 24+ 11.39(C ═ 1.01, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.57(1H,doublet,J=2.1Hz);
7.43(1H,doublet,J=8.1Hz);
7.24(1H,doublet of doublets,
J=8.1&2.1Hz);
5.00(1H,singlet);
3.80(1H,doubled doublet of
doublets,J=10.4,3.8&3.8Hz);
3.5-3.7(3H,multiplet);
2.51(1H,doublet of doublets,
J=8.0&5.2Hz);
2.37(1H,doubled doublet of
doublets,J=15.0,11.1&4.0Hz);
1.86(1H,doubled doublet of
doublets,J=15.0,2.9&2.9Hz);
0.89(9H,singlet);
0.04(3H,singlet);
-0.01(3H, singlet).1(d) 1-azido-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol
32.07g (87.8 mmoles) of 4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) butane-1, 2-diol [ prepared as in step (C) above]And 1.07g (8.76mmole) of 4-dimethylaminopyridine were dissolved in 320ml of pyridine, and 10.19ml (0.132mole) of methanesulfonyl chloride was slowly dropped under ice-cooling. The mixture was stirred at the same temperature under nitrogen atmosphere for 2 hours. The reaction mixture is then poured into 1500ml of ice-cooled 10% w/v aqueous hydrochloric acid and extracted three times with 200ml of ethyl acetate each time. The combined organic extracts were washed with saturated aqueous sodium chloride solution and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dried under reduced pressure. It is then dissolved in 300ml of anhydrous dimethylformamide and 11.41g (0.18mole) of sodium azide are added. The mixture was heated at 120 ℃ for 4 hours under nitrogen atmosphere. At the end of the heating. The reaction mixture was cooled to room temperature, poured into 1000ml of saturated aqueous sodium chloride solution and then extracted three times with 500ml of ethyl acetate each time. Drying the combined organic extracts with anhydrous magnesium sulfate, and removing solvent by evaporation under reduced pressure at a ratio of 10: 1 to 5: 1The residue was purified by flash column chromatography on silica gel using a gradient elution method using a 1 volume ratio mixture of hexane and ethyl acetate as an eluent to give 29.3g (yield 85%) of the title compound as a colorless oil [ α]]D 24-48.56 (C ═ 1.04, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.59(1H,doublet,J=2.2Hz);
7.44(1H,doublet,J=8.3Hz);
7.24(1H,doublet of doublets,
J=8.3&2.2Hz);
5.12(1H,singlet);
3.81(1H,doubled doublet of
doublets,J=10.6,4.1&3.0Hz);
3.51(1H,doubled doublet of
doublets,J=10.6,10.6&2.8Hz);
3.40(1H,doublet,J=12.5Hz);
3.31(1H,doublet,J=12.5Hz);
2.35(1H,doublet,of doublets,
J=15.8,10.6&4.1Hz);
1.91(1H,doublet of doublets,
J=15.8,3.0&2.8Hz);
0.88(9H,singlet);
0.02(3H,singlet);
-0.04(3H, singlet).1(e) 1-amino-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol
10.00g (25.6 mmoles) of 1-azido-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol [ prepared according to step (d) above]Dissolved in 100ml of tetrahydrofuran and 0.6ml of water, and 7.39g (28.2mmole) of triphenylphosphine was added to the resulting solution. The mixture was then stirred at 80 ℃ under nitrogen for 4 hours. After the stirring, the solvent was distilled off under reduced pressure, and hexane was added to the residueThe precipitated crystals were filtered off, the filtrate was concentrated by evaporation under reduced pressure, and the resulting residue was purified by flash column chromatography on silica gel using a gradient elution method using a mixture of dichloromethaneand methanol in a volume ratio of 30: 1 to 10: 1 as an eluent to give 3.83g (yield 41%) of the title compound [ α]as a colorless oil]D 24+ 3.94(C ═ 0.71, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.56(1H,doublet,J=2.2Hz);
7.42(1H,doublet,J=8.6Hz);
7.22(1H,doublet of doublets,
J=8.6&2.2Hz);
4.91(1H,broad singlet);
3.73(1H,doubled doublet of
doublets,J=10.3,4.6&3.7Hz);
3.53(1H,doubled doublet of
doublets,J=10.3,10.2&3.7Hz);
2.91(1H,doublet,J=13.1Hz);
2.86(1H,doublet,J=13.1Hz);
2.16(1H,doublet,of doublets,
J=14.6,10.2&4.6Hz);
1.88(1H,doublet of doublets,
J=14.6,3.7&3.7Hz);
1.44(2H,broad singlet);
0.87(9H,singlet);
0.01(3H,singlet);
0.04(3H, singlets). 1(f)2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethanol tert-butyldimethylsilyl ether
1.35g (3.71mmole) of 1-amino-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol [ prepared as in step (e) above]Dissolved in 50ml of benzene and in the resulting solutionTo this mixture were added 167mg (5.57mmole) of paraformaldehyde and 13mg of p-toluenesulfonyl chloride. The mixture was heated to reflux for 3 hours at 100 ℃ under nitrogen using a Dean-Stark instrument. At the end of the heating reflux, the solvent was distilled off under reduced pressure, and 100ml of ethyl acetate was added to the residue. The resulting solution was washed with a saturated aqueous solution of sodium hydrogencarbonate and dried over anhydrous magnesium sulfate. Distilling under reduced pressure to remove solvent to obtain 2- [ (5R) - (3, 4-dichlorophenyl) oxazolidin-5-yl]Ethyl tert-butyl dimethyl silyl ether. This compound was dissolved in 50ml of dichloromethane, and 0.62ml (4.45mmole) of triethylamine and 45mg (0.37mmole) of 4-dimethylaminopyridine were added to the resulting solution. Then, under ice-cooling, 1.03g (4.47mmole) of 3, 4, 5-trimethoxybenzoyl chloride was added, and the mixture was stirred at 0 ℃ for 1 hour. 100ml of methylene chloride was added to the reaction mixture, and the mixture was washed successively with a 10% w/v aqueous hydrochloric acid solution, a saturated aqueous solution of sodium hydrogencarbonate and saturated aqueous solution of sodium chloride. It was dried over anhydrous magnesium sulfate. The solvent is distilled off under reduced pressure and the ratio of the solvent to the solvent is from 1: 5 to 2: 1The residue was purified by flash column chromatography on silica gel using a gradient elution method using a mixture of ethyl acetate and hexane in volume ratio as eluent to give 1.27g (60% yield) of the title compound as a white amorphous substance [ α]]D 24+ 61.73(C ═ 1.39, methanol) 1(g)2[ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethanol methanesulfonate
3.95g (6.92mmole) of 2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethanol tert-butyldimethylsilyl ether [ prepared according to step (f) above]Dissolved in 70ml of a mixture of acetic acid, tetrahydrofuran and water in a volume ratio of 3: 1. Themixture was heated at 80 ℃ for 8 hours under nitrogen atmosphere. At the end of the heating, the solution was neutralized with a saturated aqueous solution of sodium hydrogencarbonate and extracted with ethyl acetate. The organic layer was then dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 30ml of pyridine. To the resulting solution were added 70mg (0.57mmole) of 4-dimethylaminopyridine and 0.66ml (8.53mmole) of methanesulfonyl chloride under ice-cooling, and the mixture was stirred at 0 ℃ for 2 hours under nitrogen atmosphere. At the end of the stirring, the reaction mixture is poured into 200ml of iceThe combined organic extracts were washed with saturated aqueous sodium chloride solution and dried over anhydrous magnesium sulphate, the solvent was evaporated off under reduced pressure and the residue was purified by flash column chromatography on silica gel using a gradient eluent with a mixture of hexane and ethyl acetate in a volume ratio of 5: 1 to 1: 1 to give 3.02g (82% yield) of the title compound as a white amorphous substance [ α]]D 24+ 53.1(C-1.0, methanol) 1(h)1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethyl } -4-phenylpiperidine-4-carboxamide
150mg (0.28mmole) of 2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethanol ASulfonate [ prepared according to the above step (g)]]And 75mg (0.31mmole) of 4-phenylpiperidine-4-carboxamide hydrochloride in 3ml of anhydrous dimethylformamide, to the solution 71mg (0.85mmole) of sodium hydrogencarbonate and 70mg (0.42mmole) of potassium iodide were added, the mixture was heated at 80 ℃ for 6 hours under a nitrogen atmosphere, at the end of the heating, 50m of 1 saturated aqueous solution of sodium chloride was added to the reaction mixture, which was then extracted three times with 50ml of ethyl acetate eachtime, the organic extracts were combined and dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, a mixture of dichloromethane and methanol in a volume ratio of 10: 1 was used as a developing agent, and the resultant residue was subjected to silica gel thin layer chromatography to obtain 127mg (yield: 71%) of the title compound as a white amorphous substance [ α]]D 24+ 25.2(C ═ 0.48, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.50-7.10(8H,multiplet);
6.67(2H,singlet);
5.30-4.85(2H,multiplet);
5.18(2H,singlet);
4.13-3.70(2H,multiplet);
3.87(3H,Singlet);
3.85(6H,singlet);
2.67-1.93(12H, multiplex). Infrared absorption Spectrum vmax(KBr)cm-1: 2940, 1678, 1640, 1584, 1456, 1416, 1236, 1128. Elemental analysis:
calculated value:
:60.77%;:5.83%;:6.45%;:
10.89%;
Actually measuring::60.63%;:5.94%;:6.39%;:
10.93% Mass Spectrometry (FAB) m/z: 642(M +)+
The following compounds of examples 2-4 were prepared in the same manner as in example 1 above.
Example 21- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide) in 76% yield [ α]]D 24+ 19.2(c 1.05, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.60-7.10(8H,multiplet);
6.71(2H,broad singlet);
5.50-4.90(2H,multiplet);
3.88(9H,singlet);
3.40-1.40(20H, multiplex). Infrared absorption spectrum vmax(KBr)cm-1
2938, 1633, 1584, 1464, 1416, 1236, 1128. Elemental analysis:
calculated value:
:61.05%;:6.29%;:6.10%;:
10.30%;
Actually measuring::60.66%;:6.25%;:5.80%;:
10.65%。
example 3
1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethyl
Oxybenzoyl) oxazolidin-5-yl ethyl } -4- (pyrrolidin-1-ylcarbonyl)
Yield of 4-phenylpiperidine 82% [ α]]D 24+ 23.2(c 0.49 methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.52-7.40(2H,multiplet);
7.33-7.00(6H,multiplet);
6.68(2H,singlet);
5.30-4.85(2H,multiplet);
4.09-3.65(2H,multiplet);
3.87(3H,singlet);
3.86(6H,singlet);
3.56-3.41(2H,broad singlet);
2.89-2.60(4H,multiplet);
2.48-2.29(4H,multiplet);
2.20-1.98(10H, multiplex). Infrared absorption spectrum vmax(KBr)cm-1
2948, 1625, 1584, 1464, 1415, 1235, 1128. Elemental analysis:
calculated value:
:62.98%;:6.28%;:5.95%;:
10.04%;
Actually measuring::63.01%;:6.43%;:5.97%;:
9.71 percent. Mass Spectrometry (FAB) m/z: 696(M + H)+
Example 41- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) -oxazolidin-5-yl]Ethyl } -4-morpholinocarbonyl-4-phenylpiperidine in 63% yield [ α]]D 24+ 20.5(c ═ 1.04, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.60-7.10(8H,multiplet);
6.70(2H,singlet);
5.40-4.90(2H,multiplet);
3.87(9H,singlet);
4.10-1.40(2H, multiplex); infrared absorption spectrum vmax(KBr)cm-1
2966, 1637, 1584, 1455, 1416, 1233, 1128. Elemental analysis:
calculated value:
:61.58%;:6.15%;:5.82%;:
9.83%;
Actually measuring::61.47%;:6.62%;:5.45%;:
9.67 percent. Mass Spectrometry (FAB) m/z: 712(M + H)+
Examples 5 to 40
The compounds represented by the following formulas (A-1) and (A-2) can also be prepared in the same manner as described above. The meanings of the substituents shown in these formulae are summarized in tables A-1 and A-2. For convenience, the products of examples 1 to 4 are also listed in these tables.
TABLE A-1
TABLE A-1 (continuation)
TABLE A-1 (continuation)
TABLE A-1 (continuation)
TABLE A-1 (continuation)
TABLE A-2
TABLE A-2 (continuation)
TABLE A-2 (continuation)
TABLEA-2 (continuation)
Example 411{3- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) -oxazolidin-5-yl]propyl } -4-phenylpiperidine-4-carboxamide 41(a) methyl 4- (3, 4-dichlorophenyl) -4-chlorobutanoate
1.00g (6.80mmole) of dichlorobenzene and 0.72g (7.14mmole) of succinic anhydride are suspended in 3ml of dichloroethane and 1.36g (10.2mmole) of aluminum chloride powder are added. The mixture was stirred at 60 ℃ for 3 hours. At the end of the stirring, the reaction mixture was cooled with ice and 1N aqueous hydrochloric acid was added. And then extracted with dichloromethane. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue obtained is dissolved in 30ml of methanol and 0.20ml of aqueous sulfuric acid solution is added. The solution was then heated to reflux for 2 hours, after which the reaction mixture was cooled to room temperature, poured into water and extracted with ether. The organic extract was washed successively with a saturated aqueous solution of sodium hydrogencarbonate and saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using a gradient elution method using a mixture of hexane and diethyl ether at a volume ratio of 17: 3 to 7: 3 as an eluent to give 0.25g (yield 14%) of the title compound as light orange crystals. Nuclear magnetismResonance spectra (400MHz, CDCl)3)δppm:
8.07(1H,doublet,J=2Hz);
7.81(1H,doublet of doublets,
J=2&8Hz);
7.56(1H,doublet,J=8Hz);
3.71(3H,singlet);
3.27(2H,triplet,J=7Hz);
2.78(2H, triplet, J ═ 7 Hz). 41(b) methyl 4- (3, 4-dichlorophenyl) -4-pentenoate
330mg (0.92mmole) of methyltriphenylbromide and 105mg (0.94mmole) of potassium tert-butoxide are suspended in 4ml of anhydrous benzene and the mixture is stirred under a stream of nitrogen at room temperature for 4 hours. 200mg of 4- (3, 4-dichlorophenyl) -4-oxobutyric acid methyl ester [ prepared according to the above step (a)]]A solution prepared by dissolving in 1ml of benzene was added to the reactionThe mixture was then stirred for 18 hours. At the end of the stirring, the reaction mixture was filtered through Celite (trade mark) filter aid and washed with diethyl ether. The filtrate was concentrated by evaporation under reduced pressure. The resulting residue was purified by silica gel column chromatography using a 23: 2 volume ratio mixture of hexane and diethyl ether as an eluent to give 95mg (64% yield) of the title compound as a pale yellow oil. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.48(1H,doublet,J=2Hz);
7.40(1H,doublet,J=8Hz);
7.23(1H,doublet of doublets,
J=2&8Hz);
5.32(1H,singlet);
5.14(1H,singlet);
3.67(3H,singlet);
2.79(2H,triplet,J=8Hz);
2.48(2H, triplet, J ═ 8 Hz). 41(C)4- (3, 4-dichlorophenyl) -4-penten-1-ol tert-butyldimethylsilyl ether
Except that methyl 4- (3, 4-dichlorophenyl) -4-pentenoate [ was used as in step (b) above) Preparation of]In addition, the title compound was obtained in 93% yield by operating in a similar manner to the procedure described in example 1 (b). Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.49(1H,doublet,J=2Hz);
7.38(1H,doublet,J=9Hz);
7.24(1H,doublet of doublets,
J=2&9Hz);
5.30(1H,singlet);
5.13(1H,doublet,J=1Hz);
3.62(2H,triplet,J=6Hz);
2.52(2H,triplet,J=8Hz);
1.60-1.68(2H,multiplet);
0.90(9H,singlet);
0.04(6H, singlets). 41(d) (2R) -5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) pentane-1, 2-diol
Except that 4- (3, 4-dichlorophenyl) -4-penten-1-ol tert-butyldimethylsilyl ether [ prepared by the above step (C)]]In addition, by operating in a similar manner to the procedure described in example 1(C), the title compound was obtained in 90% yield with an optical purity of 98% ee [ α]]D 24-2.08(C ═ 0.48, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.56(1H,doublet,J=2Hz);
7.41(1H,doublet,J=8Hz);
7.23(1H,doublet of doublets,
J=2&8Hz);
4.96(1H,singlet);
3.53-3.70(4H,multiplet):
1.98-2.14(3H,multiplet):
1.35-1.57(2H,multiplet);
0.91(9H,singlet):
0.082(3H,singlet);
0.078(3H, singlet). 41(e) (2R) -1-azido-5- (tert-butyldisilyloxy) -2- (3, 4-dichlorophenyl) -2-pentanol
Except that (2R) -5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) pentane-1, 2-diol [ prepared as in step (d) above]is used]Otherwise, the same procedure as in example 1(d)) Similar procedure, the title compound was obtained in 86% yield [ α]]D 24-48.2(C ═ 0.61, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.58(1H,doublet,J=2Hz);
7.42(1H,doublet,J=9Hz);
7.23(1H,doublet of doublets,
J=2&9Hz);
4.93(1H,singlet);
3.67(1H,multiplet);
3.58(1H,multiplet);
3.43(1H,doublet,J=12Hz);
3.31(1H,doublet,J=12Hz);
2.13(1H,multiplet);
2.04(1H,multiplet);
1.54(1H,multiplet);
1.40(1H,multiplet);
0.91(9H,singlet)
0.09(3H,singlet)
0.08(3H, singlets). 41(f) (2R) -1-amino-5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) -2-pentanol
Prepared as described in step (e) above, except that (2R) -1-azido-5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) -2-pentanol [ is used]The title compound was obtained in 76% yield by operating in a similar manner to the procedure described in example 1(e) [ α]D 24-8.13 (C ═ 0.48, methanol)Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.54(1H,doublet,J=2Hz);
7.40(1H,doublet,J=9Hz);
7.21(1H,doublet of doublets,
J=2&9Hz);
4.57(1H,broad singlet);
3.50-3.62(2H,multiplet);
2.96(1H,doublet,J=13Hz);
2.82(1H,doublet,J=13Hz);
1.93(1H,multiplet);
1.80(1H,multiplet);
1.33-1.60(2H,multiplet);
0.89(9H,singlet);
0.04(6H, singlets). 41(g)3- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]-1-propanol tert-butyldimethylsilyl ether
Except that (2R) -1-amino-5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) -2-pentanol [ is used, the preparation is carried out in the above step (f)]In addition, the title compound was obtained in 48% yield by operating in a similar manner to the procedure described in example 1(f) [ α]D 24+ 37.73(C ═ 0.44, methanol) 41(h)3- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]-1-propanol methanesulfonate
Except using 3- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]-1-propanol tert-butyldimethylsilyl ether [ prepared according to step (g) above]In addition, the title compound was obtained in 93% yield by operating in a similar manner to the procedure described in example 1 (g).[α]D 24+ 52.90(C ═ 0.62, methanol) 41(i)1- {3- (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Propyl } -4-phenylpiperidine-4-carboxamide
Except using 3- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]-1-propanol methanesulfonate [ prepared as described in step (h) above]In addition, in a similar manner to that described in example 1(h), a yield of 66% was obtainedRate preparation of the title compound [ α]]D 24+ 35.9(C ═ 0.48, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.60-7.10(8H,multiplet);
6.68(2H,broad singlet);
5.40-4.90(4H,multiplet);
3.88(9H,singlet);
3.87(9H,singlet)
4.10-1.10(16H, multiplex). Infrared absorption Spectrum vmax(KBr)cm-1
3440, 3353, 2940, 1676, 1641, 1585 element analysis:
calculated value:
:61.35%;:6.06%;:6.31%;:
10.65%;
Actually measuring::61.81%;:6.22%;:6.50%;:
10.26 percent. Mass Spectrometry (FAB) m/z: 656(M + H)+
Examples 42 to 50
A compound represented by the following formula (A-3) was prepared in the same manner as in example 41 above. The various substituents shown in the formula are summarized in Table A-3. For convenience, the products of example 41 are also listed in the table.
TABLE A-3
TABLE A-3 (continuation)
TABLE A-3 (continuation)
Example 51
1- {2- (2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide (Compound 2-1969)51(a)3- (3, 4-dichlorophenyl) -3, 4-epoxy-1-butanol tert-butyldimethylsilyl ether
3.00g (9.05mmole) of 3- (3, 4-dichlorophenyl) -3-butenol tert-butyldimethylsilyl ether prepared as described in example 1(b)]Dissolved in 60ml of methylene chloride, and to the solution were added 2.52g (30.0mmole) of sodium hydrogencarbonate and 3.88g (15.7mmole) of 3-chloroperbenzoic acid (content: 70%). The mixture was stirred at room temperature for 3 hours. At the end of the stirring, the reaction mixture was diluted with dichloromethane and washed with 1N aqueous sodium hydroxide solution and saturated aqueous sodium chloride solution. The organic layer was thendried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using gradient elution with hexane and ether at a volume ratio of 24: 1 to 19: 1 as an eluent to give 2.70g of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.47(1H,doublet,J=2Hz);
7.38(1H,doublet,J=8Hz);
7.21(1H,doublet of doublets,
J=2&8Hz);
3.57-3.72(2H,multiplet);
3.01(1H,doublet,J=5Hz);
2.68(1H,doublet,J=5Hz);
2.27(1H,multiplet);
2.01(1H,multiplet);
0.84(9H,singlet);
-0.016(3H,singlet);
-0.024(3H, singlet). 51(b)4- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl-1- [ N- (tert-butoxycarbonyl) -N- (2-hydroxyethyl) amino]-2-butanol
1.50g (4.32mmole) of 3- (3, 4-dichlorophenyl) -3, 4-epoxy-1-butanol tert-butyldimethylsilyl ether [ prepared according to step (a) above]and 1.84g (17.3mmole) of lithium perchlorate are dissolved in 30ml of nitrile. The mixture was stirred at room temperature for 10 minutes under nitrogen atmosphere. 2.11g (34.5mmole) of 2-aminoethanol are added to the reaction mixture and the mixture is heated under reflux for 5 hours. At the end of stirring, the reaction mixture was cooled to room temperature, diluted with ethyl acetate and washed with saturated aqueous solution of sodium chloride. The organic layer was partitioned and dried over anhydrous sodium sulfate, and then the solvent was distilled off under reduced pressure.
The resulting residue was dissolved in 30ml of methylene chloride, and 0.89ml (6.42mmole) of triethylamine and 943mg (4.32mmole) of di-tert-butyl dicarbonate were added to the resulting solution. The mixture was stirred at room temperature for 16 hours. At the end of the stirring, the reaction mixture was poured into water and extracted with dichloromethane. The extract was then washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using a mixture of hexane and ethyl acetate in a volume ratio of 3: 2 as an eluent to give 1.94g of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.30-7.75(3H,multiplet);
5.30 and 5.57 (total 1H, each wide singlet);
3.05-4.00(9H,multiplet);
2.00-2.40(2H,multiplet);
1.53(9H,singlet);
0.94(9H,singlet);
0.09(3H,singlet);
0.07(3H, singlet); infrared absorption spectrum vmax(KBr)cm-1: 3298, 2955, 2936, 2885, 2857, 1659. Mass spectrometry analysis: (FAB) m/z: 508(M + H)+51(c)2- [ 4-tert-Butoxycarbonyl-2- (3, 4-dichlorophenyl) morpholin-2-yl]Ethanol tert-butyl dimethyl silyl ether
10.4g (20.5 mmoles) of 4- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl-N- (2-hydroxyethyl) amino group]-2-Butanol [ prepared according to step (b) above]And 8.03g (30.6mmole) of triphenylphosphine were dissolved in 180ml of anhydrous toluene and a solution of 5.33g (30.6mmole) of diethyl azodicarboxylate in 20ml of toluene was added dropwise under a nitrogen atmosphere at room temperature. The mixture was stirred for 2 hours. At the end of the stirring, the reaction mixture was poured into aqueous ammonium chloride solution and extracted with ethyl acetate. The mixture was then washed with a saturated aqueous solution of sodium chloride. The organic extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using a gradient elution method using a mixture of hexane and ethyl acetate in a volume ratio of 23: 2 to 9: 1 as an eluent to give 8.85g of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.56(1H,broad singlet);
7.43(1H,doublet,J=9Hz);
7.28(1H,doublet of doublets,
J=2&9Hz);
4.20-4.55(1H,borad singlet);
3.00-3.80(8H,multiplet);
1.80-2.10(2H,multiplet);
1.35-1.60(9H,broad singlet);
0.85(9H,multiplet);
0.01(6H, singlets). Infrared absorption spectrum vmaxcm-1():
2957, 2931, 2859, 1730, 1687. Mass spectrometry analysis: (FAB) m/z: 490(M + H)+51(d)2- [2- (3, 4-dichlorophenyl) morpholin-2-yl]Ethanol
7.80g (15.9mmole) of 2- [ 4-tert-butoxycarbonyl-2- (3, 4, dichlorophenyl) -morpholin-2-yl]Ethanol t-butyldimethylsilyl ether [ prepared according to the above step (C)]]Dissolved in 150ml of dichloromethane and 7.05g (35.5mmole) of B-bromocatechol borane were added. The mixture was stirred at room temperature for 2 hours under a nitrogen stream. At the end of the stirring, 150ml of water were added to the reaction mixture, which was then stirred for a further 2 hours. The reaction mixture was basified by the addition of 1N aqueous sodium hydroxide solution. It was extracted with dichloromethane and the extract was washed with saturated aqueous solution of sodium chloride, the solvent was distilled off under reduced pressure, and the resulting residue was purified by silica gel column chromatography using a mixture of dichloromethane and methanol at a volume ratio of 19: 1 to 17: 3 as an eluent to give 4.40g of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.51(1H,doublet,J=2Hz);
7.48(1H,doublet,J=8Hz);
7.24(1H,doublet of doublets,
J=2&8Hz);
3.76(1H,doublet of triplets,
J=3&12Hz);
3.66(1H,multiplet);
3.58(2H,triplet,J=6Hz);
3.36(1H,doublet,J=13Hz);
3.11(1H,doublet,J=13Hz);
2.97(1H,multiplet);
2.79(1H,doublet of triplets,
J=3&13Hz);
2.14(1H,doublet of triplets,
J=6&15Hz);
1.79(1H,doublet of triplets,
J ═ 6&15Hz)51(e)2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethanol
1.28g (4.63mmole) of 2- (2- (3,4-dichlorophenyl) morpholin-2-yl]Ethanol [ prepared according to step (d) above)]Dissolved in 30ml of methylene chloride, and to the resulting solution were added 2.66g (26.3mmole) of triethylamine, 1.28g (5.55mmole) of 3, 4, 5-trimethoxybenzoyl chloride and 5mg of 4-dimethylaminopyridine. The mixture was stirred at room temperature for 6 hours. At the end of the stirring, the reaction mixture was poured into aqueous sodium bicarbonate and extracted with dichloromethane. The extract was washed with a saturated aqueous solution of sodium chloride. The organic extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was subjected to silica gel column chromatography using a gradient elution method using a mixture of dichloromethane and acetone in a volume ratio of 4: 1 to 7: 3 as an eluent to give 1.72g of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
6.80-7.80(3H,multiplet);
6.47(2H,singlet);
3.40-4.80(8H,multiplet);
3.84 and 3.86 (total 9H, each singlet);
1.75-2.25(2H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr)3429,2940,2838,
1630, 1585. Mass spectrometry analysis: (EI) m/z: 469(M)+51(f)2- [2-3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl) ethanol methanesulfonate]
388mg (0.83mmole) of 2- [2- (3, 4-dichlorophenyl) -4-3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol [ prepared according to the above step (e)]]Dissolved in 5ml of dichloromethane, and to the resulting solution 126mg (1.25mmole) of triethylamine and 0.078ml (1.01mmole) of methanesulfonyl chloride were added. Mixing the mixtureStirred at room temperature for 2 hours. The reactionmixture was diluted with dichloromethane and then washed sequentially with a 1N aqueous hydrochloric acid solution and a saturated aqueous solution of sodium chloride. The organic extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. Purifying the residue by silica gel column chromatography using a gradient elution method using a mixture of hexane and ethyl acetate at a volume ratio of 1: 4 to 0: 1 as an eluentThis gave 424mg of the title compound. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
6.90-7.80(3H,multiplet);
6.52(2H,singlet);
3.40-4.35(8H,multiplet);
3.86 and 3.87 (total 9H, each singlet);
2.93(3H,singlet);
2.10-2.55(2H, multiplex). Infrared absorption spectrum vmaxcm-1(RBv):
2999, 2966, 2939, 2875, 1634, 1585. Mass Spectrometry (FAB) m/z: 548(M + H)+51(g)1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide
200mg (0.36mmole) of 2- [2-3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol methanesulfonate [ prepared as described in step (f) above]105mg (0.44mmole) of 4-phenylpiperidine-4-carboxamide hydrochloride, 100mg (1.19mmole) of sodium hydrogen carbonate and 100mg (0.60mmole) of potassium iodide are suspended in 2ml of dimethylformamide and the mixture is stirred at 80 ℃ for 6 hours under a nitrogen stream. The reaction mixture was poured into water and extracted with ethyl acetate. The extract was washed successively with an aqueous solution of sodium thiosulfate, water and a saturated aqueous solution of sodium chloride. The organic extract was then evaporated with anhydrous sodium sulfate and the solvent was removed under reduced pressure. The resulting residue was subjected to thin layer chromatography using a 9: 1 mixture of dichloromethane and methanol as a developing solvent, followed by crystallization from hexane to give 205mg (yield 86%) of the titled compound.Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
6.80-7.75(8H,multiplet);
6.48(2H,singlet);
5.18(2H,singlet);
1.80-4.70(18H,multiplet);
3.83 and 3.85 (total 9H, each singlet). Infrared absorption spectrum vmaxcm-1(KBr):
3440,3356,2937,2831,1679,1631,
1584. Mass Spectrometry (FAB) m/z: 656(M + H)+Elemental analysis:
calculated value:
:62.02%;:6.00%;:6.38%;:
10.76%;
Actually measuring::61.54%;:6.07%;:6.25%;:
11.35%。
the following compounds of examples 52 to 69 were prepared in the same manner as in example 1 above.
Example 52
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide) (compound No.2-1971) yield: 84% Mass Spectrometry (FAB) m/z: 684(M + H)+Elemental analysis:
calculated value:
:63.16%;:6.33%;:6.14%;:
10.36%;
Actually measuring::63.28%;:6.64%;:5.79%;:
9.96%。
example 53
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenyl-4- (pyrrolidin-1-ylcarbonyl) piperazine (compound No.2-1972) yield: 76% Mass Spectrometry (FAB) m/z: 710(M + H)+Elemental analysis:
calculated value:
:64.06%;:6.39%;:5.90%;:
9.95%;
Actually measuring::63.62%;:6.37%;:5.75%;:
9.96%。
example 54
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-morpholinocarbonyl-4-phenylpiperidine (compound No. 2-1973)) Yield: 68% Mass Spectrometry (FAB) m/z: 726(M + H)+Elemental analysis:
calculated value:
:62.65%;:6.25%;:5.77%;:
9.73%;
Actually measuring::62.26%;:6.18%;:5.66%;:
9.87%。
example 55
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ isobenzofuran-1 (3H), 4' -piperidine](Compound No.2-2006) yield: 63% Mass Spectrometry (FAB) m/z: 641(M + H)+Elemental analysis:
calculated value:
:63.47%;:5.98%;:4.35%;:
11.02%;
Actually measuring::63.04%;:6.10%;:4.24%;:
11.10%。
example 56
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -1-methanesulfonylspiro (indoline-3, 4' -piperidine) (compound No.2-2014) yield: 85% Mass Spectrometry (FAB) m/z: 718(M + H)+)Elemental analysis:
calculated value:
:58.49%;:5.75%;:5.85%;:
9.87%;:4.46%。
Actually measuring::58.26%;:5.8O%;:5.74%;:
10.02%;:4.33%。
example 57
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ C]]Thiophene-1 (3H),4' -piperidines](Compound No.2-2008) yield: 78% Mass Spectrometry (FAB) m/z: 657(M + H)+Elemental analysis:
calculated value:
:60.44%;:5.97%;:4.15%;:
10.49%;:4.74%;
Actually measuring::60.68%;:5.95%;:3.92%;:
10.60%;:4.85%。
example 58
1{2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ C]]Thiophene-1 (3H), 4' -piperidines]2-oxide (compound 2-2010) yield: 60% Mass Spectrometry (FAB) m/z: 673(M + H)+Elemental analysis:
calculated values::
:60.62%;:5.69%;:4.16%;:10.53%;:4.76%;
actually measuring::60.50%;:5.94%;:4.09%;:10.35%;:4.71%。
example 59
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidine]-3(4H) -one (compound No.2-2015) yield: 80% Mass Spectrometry (FAB) m/z: 668(M + H)+Elemental analysis:
calculated values::
:62.87%;:5.88%;:6.29%;:10.61%;
actually measuring::62.95%;:5.98%;:6.07%;:10.77%。
example 60
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-pyridinecarbonyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide (compound No.2-2353) yield: 73% Mass Spectrometry (FAB) m/z: 567(M + H)+Elemental analysis:
Calculated values::
:62.50%;:5.77%;:9.72%;:12.30%;
actually measuring::62.19%;:5.88%;:9.39%;:13.12%。
example 61
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-pyridinecarbonyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide) (compound No.2-2355) yield: 70% Mass Spectrometry (FAB) m/z: 595(M + H)+Elemental analysis:
calculated values::
:63.57%;:6.17%;:9.27%;:11.73%;
actually measuring::63.34%;:6.26%;:9.23%;:11.97%。
example 62
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-methoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide (compound No.2-1585) yield: 75% Mass Spectrometry (FAB) m/z: 596(M + H)+Elemental analysis:
calculated values::
:63.47%;:5.99%;:6.94%;:11.71%;
actually measuring::63.02%;:6.12%;:6.74%;:12.97%。
example 63
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-methoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine- (N, N-dimethylformamide) (compound No.2586) yield: 77% Mass Spectrometry (FAB) m/z: 624(M + H)+Elemental analysis:
calculated values::
:64.45%;:6.36%;:6.63%;:11.19%;
actually measuring::64.29%;:6.42%;:6.68%;:11.57%。
example 64
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide (compound No.2-1633) yield: 80% Mass Spectrometry (FAB) m/z: 596(M + H)+Elemental analysis
Calculated values::
:63.47%;:5.99%;:6.94%;:11.71%;
actually measuring::63.44%;:5.79%;:6.79%;:11.47%。
example 65
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide) (compound No.2-1635) yield: 80% Mass Spectrometry (FAB) m/z: 624(M + H)+Elemental analysis:
calculated values::
:65.01%;:6.32%;:6.69%;:11.29%;
actually measuring::64.79%;:6.47%;:6.42%;:10.93%。
example 66
1- {2- [2- (3, 4-dichlorophenyl) -4- (4-methoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide (compound No.2-1681) yield: 94% Mass Spectrometry (FAB) m/z: 596(M + H)+Elemental analysis:
calculated values::
:64.04%;:5.95%;:7.00%;:11.82%;
actually measuring::63.67%;:5.97%;:6.70%;:12.20%。
example 67
1- {2- [2- (3, 4-dichlorophenyl) -4- (4-methoxybenzoyl)Morpholin-2-yl]Ethyl } -4-phenylpyridine-4- (N, N-di)Methylformamide (compound No.2-1683) yield: 78% Mass Spectrometry (FAB) m/z: 624(M + H)+Elemental analysis:
calculated values::
:65.38%;:6.29%;:6.73%;:11.35%;
actually measuring::65.32%;:6.94%;:6.61%;:10.97%。
example 68
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-pyrazinylcarbonyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide (compound No.2-2497) yield: 31% Mass Spectrometry (FAB) m/z: 568(M + H)+Elemental analysis:
calculated values::
:59.39%;:5.67%;:11.87%;:12.09%;
actually measuring::59.58%;:5.82%;:11.30%;:12.56%。
example 69
1- {2- [2- (3, 4-dichlorophenyl) -4- (2-pyrazinylcarbonyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide) (Compound No.2-2499)Yield: 33% Mass Spectrometry (FAB) m/z: 596(M + H)+Elemental analysis:
calculated values::
:60.58%;:6.07%;:11.40%;:11.54%;
actually measuring::60.57%;:5.95%;:9.97%;:12.88%。
example 70
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl) -4-phenylpiperidine-4-carboxamide (Compound No.2-1969)70(a)1- (chloroacetyl) amino-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol
3.60g (9.88mmole) of 1-amino-4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -2-butanol [ prepared as described in example 1(e)]]1.64ml (11.8mmole) of triethylamine and 121mg (0.99mmole) of 4-dimethylaminopyridine are dissolved in 100ml of dichloromethane and 0.94(11.8mmole) of chloroacetyl chloride is added dropwise under ice cooling. The mixture was stirred at the same temperature for 2 hours. At the end of the stirring, 100ml of dichloromethane are added to the reaction mixture and the reaction mixture is filteredThe mixture was washed with ice-cooled 10% w/v aqueous hydrochloric acid, saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution in this order. It was then dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was subjected to flash silica gel column chromatography using a gradient elution method using a mixture of ethyl acetate and hexane in a volume ratio of 1: 5 to 1: 2 as an eluent, to give 3.32g (yield 76%) of the title compound as a colorless oil. Nuclear magnetic resonance spectroscopy (270MHz, CDCl)3)δppm:
7.64(1H,doublet,J=2.1Hz);
7.47(1H,doublet,J=8.4Hz);
7.28(1H,doublet of doublets,J=8.4&2.1Hz);
7.03(1H,broad triplet),
5.27(1H,singlet);
4.04(2H, AB-quartet, J15.1 Hz, Δ δ 0.08 ppm);
3.81(1H,doublet of triplets,J=10.5&3.7Hz);
3.72(1H,doublet of doublets,J=13.5&6.2Hz);
3.53(1H,doublet of doublets,J=10.9&2.3Hz);
3.45(1H,doublet of doublets,J=13.5&5.4Hz);
2.24(1H,doublet of doublets,J=14.8,10.9&4.1Hz);
1.93(1H,doublet of triplets,J=14.8&2.8Hz);
0.92(9H,singlet);
0.06(3H,singlet);
0.00(3H, singlets). 70(b)2- [ (2R) - (3, 4-dichlorophenyl) -5-oxomorpholin-2-yl]ethanol tert-butyldimethylsilyl ether
219mg (5.48mmole) of sodium hydride (suspension in 60% w/v mineral oil) are suspended in 30ml of anhydrous tetrahydrofuran and, under ice-cooling, 1.61g (3.65mmole) of 1- (chloroacetyl) amino-4-tert-butyldimethylsilyloxy- (2R- (3, 4-dichlorophenyl) -2-butanol [ as described above]are slowly added dropwise over a period of 30 minutes
(a) Prepared]dissolved in 30ml of anhydrous tetrahydrofuran. The mixture was stirred at the same temperature for 4 hours. At the end of the stirring, the reaction mixture was poured into ice-cooled 10% w/v aqueous hydrochloric acid and extracted three times with 100ml of ethyl acetate each time. The combined organic extracts were washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was subjected to flash silica gel column chromatography using a mixture of ethyl acetate and hexane in a volume of 1: 4 to 2: 1 as an eluent to obtain 700mg (yield 47%) of the title compound.
[α]D 24Nuclear magnetic resonance spectrum (270MHz, CDCl) of +67.65(c 0.81 methanol)3)δppm:
7.532(1H,doublet,J=2.2Hz);
7.526(1H,doublet,J=8.1Hz);
7.27(1H,doublet of doublets,J=8.1&2.2Hz);
6.76(1H,broad singlet);
4.17(2H, AB-quartet, J17.3 Hz, Δ δ 0.24 ppm);
3.98(1H,doublet of doublets,J=13.0&3.9Hz);
3.76(1H,doublet of doublets,J=13.0&2.0Hz);
3.63(1H,multiplet);
3.29(1H,multiplet);
2.12(2H,multiplet);
0.91(9H,singlet);
0.04(3H,singlet);
0.03(3H, singlets). 70(c)2- [ (2R) - (3, 4-dichlorophenyl) morpholin-2-yl]ethanol
580mg (1.43mmole) of 2- [ (2R) - (3, 4-dichlorophenyl) -5-oxomorpholin-2-yl]ethanol tert-butyldimethylsilyl ether [ prepared as in step (b) above]was dissolved in 6ml of anhydrous tetrahydrofuran. The solution is heated to reflux under a stream of nitrogen and 0.60ml (6.0mmole) of 10M borane-dimethyl sulfite complex are added dropwise. The mixture was stirred for 2 hours. At the end of the stirring, the solvent was distilled off under reduced pressure and 5ml of a 1N aqueous hydrochloric acid solution were added. The mixture was then stirred at 100 ℃ for 1 hour. The reaction mixture was air-cooled, basified by addition of a 1N aqueous solution of sodium hydroxide, diluted with a saturated aqueous solution of sodium chloride, and extracted with ethyl acetate. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using a gradient elution method using a mixture of dichloromethane and methanol in a volume ratio of 9: 1 to 17: 3 as an eluent to yield 360mg of the title compound.
[α]D 24= 16.22(c ═ 0.45, methanol)
NMR spectroscopy, IR spectroscopy and mass spectroscopy were consistent with those for the racemic product described in example 51 (d). 70(d)2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethanol
The title compound was obtained in 92% yield by the same procedures as described in example 51(e) except for using 2- [ (2R) - (3, 4-dichlorophenyl) morpholin-2-yl]ethanol [ prepared as in step (c) above].
[α]D 2430.65(c is 0.56 methanol)
NMR spectroscopy, IR spectroscopy and mass spectroscopy were consistent with those for the racemic product described in example 51 (e). 70(e)2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethanol methanesulfonate
30.0g (63.8mmole) of 2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol [ prepared according to step (d) above)]Dissolved in 500ml of dichloromethane. To the mixture were added 11.5ml (83.0mmole) of triethylamine and 5.93ml (76.6 ml) in this order under ice-coolingmmole) methanesulfonyl chloride, the mixture was stirred at room temperature for 2 hours under an ammonia atmosphere. The reaction mixture was diluted with dichloromethane and washed with a 1N aqueous hydrochloric acid solution, a saturated aqueous solution of sodium chloride, and then dried over anhydrous sodium sulfate. The solvent is distilled off under reduced pressure andthe product is distilled off at a ratio of 1: 4 to 1: 9The residue was purified by column chromatography on silica gel using a mixture of an alkane and ethyl acetate as eluent to give 34.8g of the title compound [ α]]D 24+26.36(c ═ 0.66, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
6.90-7.80(3H,multiplet);
6.52(2H,singlet);
3.40-4.35(8H,multiplet);
3.86&3.87 (9H total, each unimodal);
2.93(3H,singlet);
2.10-2.55(2H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
2999, 2966, 2939, 2875, 1634, 1585 mass spectrometry (FAB) m/z: 548(M + H)+70(f)1- {2- [ (2R- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4-carboxamide
Except using 2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol methanesulfonate [ prepared as described in step (e) above]In addition, the title compound was obtained in 79% yield by operating in a similar manner to example 51(g) [ α]D 24= 7.53(c ═ 0.50, methanol)Elemental analysis:
calculated values::
:61.85%;:6.01%;:6.36%;:10.74%;
actually measuring::61.51%;:6.18%;:6.13%;:10.72%。
NMR, IR, and mass spectral analyses were consistent with the racemic product described in example 51 (g).
The following compounds of examples 71-74 were prepared by the same procedure as in example 70 above.
Example 71
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide (Compound No. 2-1971)) yield 84% [ α]]D 24Elemental analysis of +7.04(c 0.45, methanol):
calculated values::
:62.69%;:7.02%;:6.09%;:10.28%;
actually measuring::62.37%;:6.42%;:5.94%;:10.72%。
example 72
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1- (3H),4' -piperidines]Yield of-2-oxide (Compound No.2-2010) 66% [ α%]D 24Elemental analysis (2.50 (c 0.50, methanol):
calculated values::
:60.62%;:5.69%;:4.16%;:10.53%;:4.76%;
actually measuring::60.17%;:5.68%;:4.00%;:10.47%;:4.55%。
example 73
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidine]Yield of (E) -3(4H) -one (Compound No.2-2015) 75% [ α]]D 24Elemental analysis +2.58(c ═ 0.40, methanol):
calculated values::
:62.87%;:5.88%;:6.29%;:10.61%;
actually measuring::62.46%;:6.01%;:6.08%;:9.63%。
example 74
78% yield of 1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl } -4-phenylpiperidine-4- (N, N-dimethylformamide) (compound No.2-1635) [ α%]D 24Elemental analysis +9.67(c 0.50, methanol):
calculated values::
:65.01%;:6.32%;:6.69%;:11.29%;
actually measuring::64.84%;:6.46%;:6.52%;:11.58%。
example 75
1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-10)
600mg of (1.12mmole)2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]Ethanol methanesulfonate [ prepared as described in example 1(g)]]318mg (1.23mmole) of spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide hydrochloride [ prepared as described in preparation 6]283mg (3.37mmole) of sodium bicarbonate, and 280mg (169mmole) of sodium iodide are suspended in 10ml of anhydrous dimethylformamide, and the mixture is heated at 80 ℃ for 8 hours under a nitrogen atmosphere. Then will beThe reaction mixture was poured into 100ml of a saturated aqueous solution of sodium chloride and extracted with ethyl acetate. The organic extract was dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by column chromatography on silica gel using a gradient elution method using a mixture of dichloromethane and methanol in a volume ratio of 40: 1 to 20: 1 as an eluent, and then crystallized from diisopropyl ether to give 496mg of the title compound as white crystals.[α]D 24+41.0(c ═ 1, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent::=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 28.6min NMR spectra (400MHz, CDCl)3)δppm:
7.1-7.6(7H,multiplet);
6.70(2H,singlet);
4.9-5.3 (total 2H, broad singlet);
4.32(1H,doublet,J=16.7Hz);
4.00(1H,doublet,J=16.7Hz);
3.7-4.2(2H,multiplet);
3.87&3.89 (total 9H, each unimodal);
1.5-3.1(12H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
2940, 1642, 1584, 1416, 1237, 1128. Mass Spectrometry (FAB) M/z659(M + H)+Elemental analysis
Calculated values::
:59.28%;:5.58%;:4.19%;:4.79%;:10.60%;
actually measuring::59.36%;:5.58%;:4.12%;:4.73%;:10.60%。
example 76
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-42)76(a)4- (tert-butyldimethylsilyloxy) - (2R) - (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (2-hydroxyethyl) amino]-2-butanol
39.9g (109mmole) of 4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) butane-1, 2-diol [ prepared as described in example 1(c)]]Dissolved in 80ml of pyridine, and 31.3g (164mmole) of p-toluenesulfonyl chloride was added to the resulting solution. The mixture was stirred at room temperature under nitrogen atmosphere for 2 days. At the end of the stirring, the reaction mixture was diluted with water and extracted with ethyl acetate. The organic extract was washed successively with water and saturated aqueous solution of sodium chloride, and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue obtained is dissolved in 600ml of acetonitrile and 35.0g (329mmole) of lithium perchlorate and 33.4g (547mmole) of 2-aminoethanol are added to the solution obtained. The mixture was heated to reflux for 16 hours. At the end of the heating, the reaction mixture was cooled to room temperature, diluted with ethyl acetate and washed with saturated aqueous solution of sodium chloride. The organic phase was separated and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 700ml of dichloromethane. To the resulting solution were added 22.8ml (164mmole) of triethylamine and 26.3g (120mmole)Di-tert-butyl dicarbonate, and the mixture is stirred at room temperature for 12 hours, then the reaction mixture is poured into water and extracted with dichloromethane, the organic extract is washed with saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate, the solvent is distilled off under reduced pressure, the residue obtained is subjected to silica gel column chromatography using a mixture of hexane and ethyl hexanoate in a volume ratio of 4: 1 to 7: 3 as eluent, using gradient elution to give 49.9g of the title compound [ α]]D 24+3.92(c ═ 0.72, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.30-7.75(3H,multiplet);
5.30&5.57 (total 1H, each wide singlet);
3.05-4.00(9H,multiplet);
2.00-2.40(2H,multiplet);
1.53(9H,singlet);
0.94(9H,singlet);
0.09(3H,singlet);
0.07(3H, singlet). Infrared absorption spectrum vmaxcm-1(KBr):
3420, 2957, 2933, 2885, 2861, 1687. Mass Spectrometry (FAB) m/z: 508(M + H)+76(b)2- [ 4-tert-Butoxycarbonyl- (2R) - (3, 4-dichlorophenyl) morpholin-2-yl]Ethanol tert-butyl dimethyl silyl ether
49.9g (98.1mmole) of 4-tert-butyldimethylsilyloxy- (2R) - (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (2-hydroxyethyl) amino]-2-Butanol [ prepared according to step (a) above]And 30.9g (118mmole) of triphenylphosphine in 600ml of anhydrous toluene, 51.3g of a 40% w/v toluene solution containing 118mmole of diethyl azodicarboxylate was added dropwise to the resulting solution at room temperature under a nitrogen atmosphere, and the mixture was stirred for 2 hours, at the end of the stirring, the solvent was distilled off under reduced pressure, and the resulting residue was subjected to silica gel column chromatography purification using a gradient elution method with a mixture of hexane and ethyl acetate in a volume ratio of 47: 3 to 23: 2 as an eluent, to give 43.2g of the title compound [ α]]D 24+32.67(c ═ 0.60, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.56(1H,broad singlet);
7.43(1H,doublet,J=9Hz);
7.28(1H,doublet of doublets,J=2&9Hz);
3.00-4.55(8H,multiplet);
1.80-2.10(2H,multiplet);
1.35-1.60(9H,broad singlet);
0.85(9H,singlet);
0.01(6H, singlets). Infrared absorption spectrum vmaxcm-1():
2957, 2931, 2859, 1687. Mass Spectrometry (FAB) m/z: 490(M + H)+76(c) (2R- (3, 4-dichlorophenyl) -2- (2-hydroxyethyl) morpholine hydrochloride
43.1g (87.9mmole) of 2- [ 4-tert-butoxycarbonyl- (2R) - (3, 4-dichlorophenyl) morpholin-2-yl]Ethanol tert-butyldimethylsilyl ether [ prepared according to step (b) above]Dissolving in 600ml of 4N hydrogen chloride in dioxane, stirring the mixture at 60 ℃ for 4 hours, distilling off the solvent under reduced pressure at the end of the stirring, adding diethyl ether to the residue, distilling off the solvent under reduced pressure, recrystallizing the residue from ethanol/ethyl acetate to give 24.1g of the title compound [ α]]D 24+48.07(c ═ 0.57, methanol) nuclear magnetic resonance spectrum (400MHz, hexafluorodimethyl sulfoxide) δ ppm:
8.60-9.80(2H,broad singlet);
7.72(1H,singlet);
7.70(1H,doublet,J=9Hz);
7.44(1H,doublet of doublets,J=2&9Hz);
4.53(1H,broad singlet);
3.89(1H,doublet of triplets,J=4&
13Hz);
3.75(1H,doublet,J=14Hz);
3.68(1H,multiplet);
3.30-3.45(2H,multiplet);
2.93-3.13(3H,multiplet);
2.09(1H,multiplet);
1.90(1H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
3378, 2966, 2893, 2812, 2783, 2724, 2656, 2530, 1598. MassSpectrometry (FAB) m/z: 276(M + H)+76(d)2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl (free form)]Ethanol
22.9g (82.9mmole) (2R- (3, 4-dichlorophenyl) -2- (2-hydroxyethyl) morpholine hydrochloride [ prepared as described in step (c) above]]Suspending in 500ml of dichloromethane, adding 27.6ml (199mmole) of triethylamine, 21.0g (91.0mmole) of 3, 4, 5-trimethoxybenzoyl chloride and 100mg of 4-dimethylaminopyridine to the suspension, and stirring the mixture at room temperature for 12 hours, pouring the reaction mixture into water and extracting with dichloromethane at the end of the stirring, washing the organic extract with a saturated aqueous solution of sodium chloride, drying it with anhydrous sodium sulfate, evaporating the solvent under reduced pressure, and purifying the residue by column chromatography on silica gel using a gradient elution method using a mixture of dichloromethane and acetone in a volume ratio of 4: 1 to 7: 3 as an eluent to obtain 30.0g of the title compound [ α]]D 24+30.65(c ═ 0.56, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
6.80-7.80(3H,multiplet);
6.47(2H,singlet);
3.40-4.80(8H,multiplet);
3.84&3.86 (total 9H, each singlet);
1.75-2.25(2H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
3429, 2940, 2838, 1630, 1585. Mass Spectrometry (EI) m/z: 469(M)+76(e) [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Acetaldehyde
0.88ml (10.1mmole) of oxalyl chloride was dissolved in 10ml of dichloromethane, and 5ml of a dichloromethane solution containing 0.79ml (11.1mmole) ofdimethyl sulfoxide was added dropwise to the above-obtained solution at-78 ℃ under a nitrogen atmosphere. The mixture was stirred for 30 minutes. To the resulting mixture was added dropwise 10ml of a mixture containing 950mg (2.02mmole) of 2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol [ prepared according to step (d) above)]And the mixture was stirred for 4 hours, when stirring was completed, 2.24ml (16.2mmole) of triethylamine was further added, and the mixture was stirred at room temperature for 2 hours, then the reaction mixture was poured into water and extracted with dichloromethane, the organic phase was washed successively with water and a saturated solution of sodium chloride, then dried over anhydrous sodium sulfate, the solvent was distilled off under reduced pressure, and the resulting residue was subjected to silica gel column chromatography purification using a gradient elution method with a mixture of dichloromethane and acetone in a volume ratio of 23: 2 to 21: 4 as an eluent, to give 878mg of the title compound [ α]]D 24+36.15(c ═ 0.65, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
9.56(1H,singlet);
6.90-7.80(3H,multiplet);
6.50(2H,singlet);
3.40-4.60(6H,multiplet);
3.85-3.87 (9H total, each unimodal);
2.70-3.05(2H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
2962, 2930, 2838, 1723, 1636, 1585. Mass Spectrometry (FAB) m/z: 468(M + H)+76(f)1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H) 4' -piperidines]- (2S) -oxides
15.00g (274mmole) of 2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethanol methanesulfonate [ prepared as described in example 70(e)]]7.76(30.1mmole) spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) oxide hydrochloride [ prepared as described in preparation example 6],6.89g(82.0mmole) Sodium bicarbonate, and 6.81g (41.0mmole) of potassium iodide suspended in 150ml of anhydrous dimethylformamide, the mixture was heated at 80 ℃ for 8 hours under nitrogen, then the reaction mixture was poured into 400ml of saturated aqueous solution of sodium chloride and extracted with ethyl acetate, the organic extract was dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, the resulting residue was subjected to silica gel column chromatography purification using a mixture of dichloromethane and methanol in a volume ratio of 40: 1 to 20: 1 as an eluent, and crystallized with hexane to give 15.5g of the title compound [ α]as white crystals]D 24+14.0(c ═ 1, methanol)HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 23.7min Nuclear magnetic resonance Spectroscopy (400MHz, CDCl)3)δppm:
7.1-7.8(7H,multiplet);
6.49(2H,broad singlet);
4.31(1H,doublet,J=16.8Hz);
3.99(1H,doublet,J=16.8Hz);
3.86&3.84 (total 9H, each singlet);
3.3-4.0(6H,multiplet)
1.5-3.1(12H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
2939, 1636, 1584, 1464, 1426, 1329, 1237, 1128. Mass Spectrometry (FAB) m/z: 673(M + H)+Elemental analysis:
calculated values::
:59.82%;:5.76%;:4.10%;:4.7%;,10.39%;
actually measuring::60.20%;:6.14%;:4.04%;:4.54%;10.38 percent. 76(g)1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4,5-Trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxides
150mg (0.32mmole) [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]acetaldehyde [ prepared as in step (e) above]and 99mg (0.38mmole) of spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide hydrochloride [ prepared as in preparation 6]were dissolved in 1ml of methanol. To the resulting solution were added 100mg of molecular sieve 3A (powder) and 209mg (3.33mmole) of sodium cyanoborohydride, and the mixture was heated under reflux for 8 hours under a nitrogen atmosphere. The reaction mixture was filtered through Celire (trade mark) filter aid. The filtrate was poured into water and extracted with ethyl acetate. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified by column chromatography on silica gel using a mixture of methylene chloride and methanol in a volume ratio of 97: 3 to 19: 1 as an eluent to give 184mg of the title compound. The physico-chemical properties of this product are in accordance with those of the product described in example 76 (f).
Example 771- {2- [ (2R) - (3, 4-dichlorophenyl) -4- [ (3-isopropoxyphenyl) acetyl]morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-811)77(a)2- { (2R) - (3, 4-dichlorophenyl) -4- [ (3-isopropoxyphenyl) acetyl]morpholin-2-yl } ethanol
1.03g (5.28mmole) of 3-isopropoxyphenylacetic acid was dissolved in 50ml of methylene chloride, and 1.10g (5.76mmole) of WSC-(Water-soluble carbodiimide-) 780mg (5.76mmole) of 1-hydroxybenzotriazole-1.61ml (11.5mmole) of triethylamine and 1.50g (4.80mmole) of (2R) - (3, 4-dichlorophenyl) -2- (2-hydroxyethyl) morpholine hydrochloride are prepared as described in example 76(c)]. The mixture was then stirred at room temperature under nitrogen for 15 hours. At the end of the stirring, a saturated aqueous solution of ammonium chloride was added to the reaction mixture, which was then extracted with ethyl acetate. The organic extract was washed with a saturated aqueous solution of sodium hydrogencarbonate and saturated aqueous solution of sodium chloride in this order, and then dried over anhydrous magnesium sulfate. The solvent is distilled off under reduced pressure,and subjecting the residue to silica gel column chromatography using a mixture of hexane and ethyl acetate in a volume ratio of 3: 1 to 2: 1 as an eluent to obtain 1.81g of the title compound [ α]]D 24-8.2(c ═ 0.60, methanol) nuclear magnetic resonance spectrum (270MHz, CDCl)3)δppm:
6.45-7.57(7H,multiplet);
4.74(1H,doublet,J=13.9Hz);
4.37-4.52(1H,multiplet);
3.22-3.90(9H,multiplet);
2.10-2.21(1H,broad singlet);
1.87-2.09(2H,multiplet);
1.30(3H,singlet);
1.28(3H, singlet). Infrared absorption spectrum vmaxcm-1(KBr):
3693, 3622, 3589, 2981, 2934, 1645, 1608, 1583. Mass Spectrometry (FAB) m/z: 452(M + H)+77(b)2- { (2R) - (3, 4-dichloro-N-methyl-N-ethyl-N-methyl-N-ethyl-N-methyl-N-Phenyl) -4- [ (3-isopropoxyphenyl) acetyl]Morpholin-2-yl } ethanol methanesulfonate
1.81g (4.00mmole) of 2- { (2R) - (3, 4-dichlorophenyl) -4- [ (3-isopropoxyphenyl) acetyl]Morpholin-2-yl } ethanol [ prepared as described in step (a) above]Dissolved in 5ml of pyridine, and 45mg (0.40mmole) of 4-dimethylaminopyridine and 0.46ml (6.00mmole) of methanesulfonyl chloride were added to the resulting solution under ice-cooling. The mixture was stirred at 0 ℃ for 2 hours under nitrogen and at the end of stirring, the reaction mixture was poured into ice-cooled 10% w/v aqueous hydrochloric acid and extracted with ethyl acetate. Organic extractThe extract was washed with saturated aqueous solution of sodium chloride and dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, and the obtained residue was purified by silica gel column chromatography using a mixture of hexane and ethyl acetate in a volume ratio of 1: 1 to 1: 2 as an eluent to give 2.00g of the title compound as a colorless oil [ α]]D 24-6.3(c ═ 0.70, methanol) nuclear magnetic resonance spectrum (270MHz, CDCl)3)δppm:
6.51-7.59(7H,multiplet);
4.40-4.63(2H,multiplet);
3.17-4.26(9H,multiplet);
2.93(3H,singlet);
2.08-2.32(2H,multiplet);
1.31(3H,singlet);
1.29(3H, singlet). Infrared absorption spectrum vmaxcm-1(KBr):
2981, 2934, 1645, 1608, 1583. Mass Spectrometry (FAB) m/z: 530(M + H)+77(c)1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- [ (3-isopropoxyphenyl) acetyl]Morpholin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxides
630mg of (1.19mmole)2- { (2R) - (3, 4-dichlorophenyl) -4- [ (3-isopropoxyphenyl) acetyl]Morpholin-2-yl]Ethanol methanesulfonate [ prepared according to the above step (b)]]367mg (1.43mmole) of spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide hydrochloride [ prepared as described in preparation 6]299mg (3.56mmole) of sodium bicarbonate and 296mg (1.78mmole) of potassium iodide were suspended in 6ml of ethanolIn aqueous dimethylformamide under nitrogen atmosphereThis suspension was heated at 80 ℃ for 6 hours, at the end of the heating, the reaction mixture was poured into saturated aqueous sodium chloride solution and extracted with ethyl acetate, the organic extract was dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, the residue obtained was purified by column chromatography on silica gel using a mixture of dichloromethane and methanol in a volume ratio of 25: 1 as eluent and then crystallized from hexane to give 400mg of the title compound in the form of white crystals having an alkane point of 85-88 ℃ [ α]]D 24+2.5(c ═ 0.51, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=60∶40,0.1%
flow rate: 1.0ml/min
Retention time: 23.7min Nuclear magnetic resonance Spectroscopy (400MHz, CDCl)3)δppm:
6.55-7.61(11H,multiplet);
4.71(1H,doublet,J=13.8Hz);
4.40-4.51(1H,multiplet);
4.31(1H,doublet,J=16.8Hz);
3.99(1H,doublet,J=16.8Hz);
3.25-3.85(8H,multiplet);
2.56-2.97(2H,multiplet);
2.01-2.45(6H,multiplet);
1.88-2.45(2H,multiplet);
1.48-1.59(1H,multiplet);
1.30(3H,singlet);
1.29(3H, singlet). Infrared absorption spectrum vmaxcm-1(KBr):
2975, 2923, 1645, 1607, 1582, 1047. Mass Spectrometry (FAB) m/z: 655(M + H)+Elemental analysis
Calculated values::
:63.25%;:6.22%;:4.21%;:4.82%;:10.67%;
actually measuring::62.96%;:6.38%;:4.08%;:4.71%;:10.41%。
example 781- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl]hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-74)78(a)4- (tert-butyldimethylsilyloxy) - (2R) - (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (3-hydroxypropyl) amino-2-butanol
Except that 5.00g (13.7mmole) of 4-tert-butyldimethylsilyloxy) - (2R) - (3, 4-dichlorophenyl) -butane-1, 2-diol [ prepared as in example 1(c)]]And 5.15g (68.6mmole) of 3-amino-1-propanol as starting material, in a manner similar to example 76(a), to give 6.00g of the title compound [ α]]D 24-1.31(c ═ 1.22, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.20-7.70(3H,multiplet);
5.04&5.32 (total 1H, each unimodal);
3.15-3.85(9H,multiplet);
1.95-2.30(2H,multiplet);
1.65-1.85(2H,multiplet);
1.45(9H,singlet);
0.86(9H,singlet);
-0.08&0.01 (total 6H, each singlet). Infrared absorption spectrum vmaxcm-1():
3432, 2957, 2885, 2861, 1675. Mass Spectrometry (FAB) m/z: 522(M + H)+78(b)2- [ 4-tert-Butoxycarbonyl- (2R) - (3, 4-dichlorophenyl) hexahydro-1, 4-oxazepin-2-yl]Ethanol tert-butyl dimethyl silyl ether
300mg (0.57mmole) of 4- (tert-butyldimethylsilyloxy) - (2R) - (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (3-hydroxypropyl) amino]-2-Butanol [ prepared according to step (a) above]Dissolving in 2ml pyridine, adding 196mg (1.03mmole) of p-toluenesulfonyl chloride to the resulting solution, stirring the mixture at room temperature under nitrogen for 16 hours, at the end of the stirring, pouring the reaction mixture into water and extracting with ethyl acetate, washing the organic extracts with water and saturated aqueous sodium chloride solution in that order, drying with anhydrous sodium sulfate, evaporating the solvent under reduced pressure, dissolving the residue in 3ml 2-methyl-2-propanol, adding 67mg (0.58mmole) of potassium tert-butoxide to the solution, heating the mixture at 80 ℃ for 8 hours under nitrogen, at the end of the heating, cooling the reaction mixture to room temperature, pouring into water and extracting with ethyl acetate, washing the organic extracts with saturated aqueous sodium chloride solution and drying with anhydrous sodium sulfate, evaporating the solvent under reduced pressure, eluting with a mixture of hexane and ethyl acetate in a volume ratio of 47: 3 to 23: 2, and purifying the residue by gradient elution to obtain 56mg of the title compound [ α]]D 24+14.19(c ═ 0.74, methanol) nuclear magnetic resonance spectrum (270MHz, CDCl)3)δppm:
7.17-7.65(3H,multiplet);
3.10-4.10(8H,multiplet);
1.75-2.30(4H,multiplet);
1.37&1.44 (total 9H, each singlet);
0.82(9H,singlet);
-0.07&0.05 (total 6H, each singlet). Mass Spectrometry (FAB) m/z: 504(M + H)+78(c)2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]Ethanol methanesulfonate
Except using 2- [ 4-tert-butoxycarbonyl- (2R) - (3, 4-dichlorophenyl) hexahydro-1, 4-oxazepin-2-yl]Ethanol tert-butyldimethylsilyl ether [ prepared according to step (b) above]In addition, the title compound was obtained in 65% yield by operating in a similar manner to the procedures described in examples 76(c), 76(d) and 70(e) [ α]]D 24+19.41(c ═ 0.45, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.20-7.65(3H,multiplet);
6.62(2H,singlet);
0.75-4.90(12H,multiplet);
3.87&3.89 (9H total, each unimodal);
2.86(3H, singlet). Infrared absorption spectrum vmaxcm-1(KBr):
2935, 1637, 1585. Mass Spectrometry (FAB) m/z: 562(M + H)+78(d)1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxides
Except using 2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]Ethanol methanesulfonate [ prepared as described in step (c) above]In addition, the title compound was obtained in 59% yield by operating in a similar manner to the procedure described in example 76(f) [ α]D 24+19.33(c ═ 0.1, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 17.7min Nuclear magnetic resonance Spectroscopy (400MHz, CDCl)3)δppm:
7.15-7.75(7H,multiplet);
6.62(2H,broad singlet);
0.75-4.80(29H,multiplet);
4.29(1H,doublet,J=17Hz);
3.97(1H, doublet, J ═ 17 Hz); infrared absorption spectrum vmaxcm-1(KBr):
2928, 2855, 2836, 1637, 1584. Mass Spectrometry (FAB) m/z: 687(M + H)+
Example 791 methyl- {3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl]morpholin-2-yl]propyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-42)79(a)4- (3, 4-dichlorophenyl) -4-oxobutanoate
8.50g (84.9mmole) of succinic anhydride and 24.8g (93.0mmole) of aluminum bromide are added successively to 150ml of 1, 2-dichlorobenzene, and the mixture is stirred at room temperature for 5 hours. At the end of stirring, the reaction mixture was poured into ice-cooled water and extracted with dichloromethane. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 100ml of methanol. To the resulting solution was added 1.0ml of sulfuric acid, and the mixture was heated under reflux for 4 hours. At the end of heating, the reaction mixture was cooled to room temperature, poured into water and extracted with ethyl acetate. The organic extract was washed successively with a saturated aqueous solution of sodium hydrogencarbonate and saturated aqueous solution of sodium chloride, and then dried over anhydrous sodium sulfate. Evaporating under reduced pressure to remove solvent, eluting with mixture of hexane and diethyl ether at volume ratio of 17: 3 to 7: 3, and purifying the residue by silica gel column chromatography to obtain 9.10g light orangeThe title compound was in the form of a colored crystal. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
8.07(1H,doublet,J=2Hz);
7.81(1H,doublet of doublets,J=2&8Hz);
7.56(1H,doublet,J=8Hz);
3.71(3H,singlet);
3.27(2H,triplet,J=7Hz);
2.78(2H, triplet, J ═ 7 Hz). Infrared absorption spectrum vmaxcm-1(KBr):
3093, 3061, 2954, 1746, 1678, 1583. Mass Spectrometry (EI) m/z: 260(M)+79(b) methyl 4- (3, 4-dichlorophenyl) -4-pentenoate
1.75g (49.0mmole) of methyltriphenyl bromide and 5.50g (49.0mmole) of potassium tert-butoxide are suspended in 200 g of anhydrous benzene, and the mixture is stirred at room temperature for 6 hours under a nitrogen atmosphere. At the end of the stirring, 8.50g of methyl 4- (3, 4-dichlorophenyl) -4-oxobutanoate [ prepared according to step (a) above]were added to the reaction mixture]Dissolved in 40ml of benzene. The mixture was stirred for 1 hour. The reaction mixture was then poured into water and extracted with ethyl acetate. The organic extract was dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The residue was subjected to a silica gel column using a gradient elution method using a mixture of hexane and ethyl acetate at a volume ratio of 19: 1 to 23: 2 as an eluent, to give 4.20g of the title compound as a pale orange oil. Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.48(1H,doublet,J=2Hz);
7.40(1H,doublet,J=8Hz);
7.23(1H,doublet of doublets,J=2&8Hz);
5.32(1H,singlet);
5.14(1H,singlet);
3.67(3H,singlet);
2.79(2H,triplet,J=8Hz);
2.48(2H, triplet, J ═ 8 Hz). Infrared absorption spectrum vmaxcm-1(film):
2952, 1740, 1630, 1550. Mass Spectrometry (EI) m/z: 258 (M)+)79(c)4- (3, 4-dichlorophenyl) -4-penten-1-ol tert-butyldimethylsilyl ether
Except that 4- (3, 4-dichlorophenyl) -4-pentenoate [ prepared by the above step (b)]Prepare for]In addition, the title compound was obtained in 93% yield by operating in a similar manner to the procedure described in example 1 (b). Nuclear magnetic resonance spectroscopy (400MHz, CDCl)3)δppm:
7.49(1H,doublet,J=2Hz);
7.38(1H,doublet,J=9Hz);
7.24(1H,doublet of doublets,J=2&9Hz);
5.30(1H,singlet);
5.13(1H,doublet,J=1Hz);
3.62(2H,triplet,J=6Hz);
2.52(2H,triplet,J=8Hz);
1.60-1.68(2H,multiplet);
0.90(9H,singlet);
0.04(6H, singlets). Infrared absorption spectrum vmaxcm-1(film):
2954, 2929, 2887, 2858, 1627, 1550. Mass Spectrometry (FAB) m/z: 345(M + H)+79(d) (2R) -5-tert-butyldimethylsilyloxy-2- (3, 4-dichlorophenyl) pentane-1, 2-diol
Except that 4- (3, 4-dichlorophenyl) -4-penten-1-ol tert-butylsilyl ether [ prepared as in step (c) above]is used]In addition, by operating in a similar manner to example 1(c), the title compound was obtained in 94% yield. Optical purity: 98% ee[α]D 24-2.08(c ═ 0.48, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.56(1H,doublet,J=2Hz);
7.41(1H,doublet,J=8Hz);
7.23(1H,doublet of doublets,J=2&8Hz);
4.96(1H,singlet);
3.53-3.70(4H,multiplet);
1.98-2.14(3H,multiplet);
1.35-1.57(2H,multiplet);
0.91(9H,singlet);
0.082(3H,singlet);
0.078(3H, singlet). Infrared absorption spectrum vmaxcm-1():
3584, 3311, 2956, 2932, 2861. Mass Spectrometry (FAB) m/z: 379 (M)+)79(e) (2R) -5- (tert-butyldimethylsilyloxy) -2- (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (2-hydroxyethyl) amino]-2-pentanol
Except that (2R) -5-tert-butyldimethylsilyloxy-2- (3, 4-dichlorophenyl) pentane-1, 2-diol [ prepared as in step (d) above]is used]In addition, the title compound was obtained in 95% yield by operating in a similar manner to the procedure described in example 76(a) [ α]D 24-14.75(c ═ 0.61, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.15-7.65(3H,multiplet);
5.30&5.79 (total 1H, each unimodal);
2.50-3.95(9H,multiplet);
1.85-2.25(2H,multiplet);
1.30-1.60(2H,multiplet);
1.43(9H,singlet);
0.89(9H,singlet);
0.04&0.05 (total 6H, each singlet). Infrared absorption spectrum vmaxcm-1(KBr):
3355, 2955, 2931, 2894, 2858, 1668. Mass Spectrometry (FAB) m/z: 522(M + H)+79(f) (2R) -3- [ 4-tert-butoxycarbonyl-2- (3, 4-dichlorophenyl) morpholin-2-yl]-1-propanol tert-butyldimethylsilyl ether
Except that (2R) -5-, (Tert-butyldimethylsiloxy group]-2- (3, 4-dichlorophenyl) -1- [ N- (tert-butoxycarbonyl) -N- (2-hydroxyethyl) amino]-2-pentanol [ prepared according to step (e) above]In addition, the title compound was obtained in 92% yield by operating in a similar manner to that described in example 76(b) [ α]D 24+58.15(c ═ 0.54, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.40-7.65(3H,multiplet);
4.14(1H,doublet,J=14Hz);
3.42-3.75(5H,multiplet);
3.23(2H,doublet,J=14Hz);
1.15-2.00(4H,multiplet);
1.44&1.52 (total 9H, each wide singlet);
0.85(9H,singlet);
0.00&0.01 (total 6H, each singlet). Infrared absorption spectrum vmaxcm-1():
2957, 2931, 2860, 1668. Mass Spectrometry (FAB) m/z: 504(M + H)+79(g)3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]-1-propanol
3.43g (6.80mmole) of (2R) -3- [ 4-tert-butoxycarbonyl-2- (3, 4-dichlorophenyl) morpholin-2-yl]-1-propanol tert-butyldimethylsilyl ether [ prepared according to step (f) above]Dissolved in 60ml of methylene chloride, and 2.98g (15.0mmole) of B-bromocatechol borane was added to the resulting solution. The mixture was stirred at room temperature for 2 hours under nitrogen atmosphere. At the end of the stirring, 60ml of water were poured into it, which was then stirred for a further 2 hours. The mixture was basified by the addition of 1N aqueous sodium hydroxide solution and then extracted with dichloromethane. The organic extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure. The resulting residue was dissolved in 40ml of methylene chloride, and to the resulting solution were added 1.23ml (8.87mmole) of triethylamine, 1.65g (7.15mmole) of 3, 4, 5-trimethoxybenzoyl chloride and 10mg of 4-dimethylaminopyridine. The resulting mixture was stirred at room temperature 12 hours at the end of the stirring, the reaction mixturewas poured into water and extracted with dichloromethane, the organic extract was washed with saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate, the solvent was distilled off under reduced pressure, the resulting residue was purified by column chromatography on silica gel using a mixture of dichloromethane and acetone in a volume ratio of 7: 3 as an eluent to give 2.13g of the title compound [ α]]D 24+30.78(c ═ 0.51, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
6.80-7.80(3H,multiplet);
6.48(2H,broad singlet);
3.30-4.80(8H,multiplet);
3.84&3.86 (total 9H, each singlet);
1.10-2.35(4H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
3426, 2942, 2872, 1632, 1584. Mass Spectrometry (FAB) m/z: 484(M + H)+79(h)3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]-1-propanol methanesulfonate
Except using 3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]-1-propanol [ prepared according to step (g) above)]In addition, the title compound was obtained in 84% yield by operating in a similar manner to the procedure described in example 70(e) [ α]D 24+27.87(c ═ 0.54, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
6.80-7.80(3H,multiplet);
6.50(2H,singlet);
3.20-4.50(8H,multiplet);
3.85&3.86 (total 9H, each singlet);
2.97(3H,singlet);
1.35-2.35(4H, multiplex). Infrared absorption spectrum vmaxcm-1(KBr):
3001, 2939, 2875, 2839, 1634, 1585. Mass Spectrometry (FAB) m/z: 562(M + H)+79(i)1{3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Propyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxides
Except using 3- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]-1-propanol methanesulfonate [ prepared as in step (h) above]In addition, the title compound was obtained in 68% yield by operating in a similar manner to the procedure described in example 76(g) [ α]]D 24+26.97(c ═ 0.55, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 23.4min Nuclear magnetic resonance Spectroscopy (400MHz, CDCl)3)δppm:
6.80-7.80(7H,multiplet);
6.48(2H,broad singlet);
0.80-4.70(20H,multiplet);
4.32(1H,doublet,J=17Hz);
4.00(1H,doublet,J=17Hz);
3.84&3.86 (9H in total, each singlet); infrared absorption spectrum vmaxcm-1(KBr):
2940, 2872, 2834, 2771, 1636, 1584. Mass Spectrometry (FAB) m/z: 687(M + H)+
EXAMPLE 801- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl l oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide (Compound No.3-2055)80(a)2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl) oxazolidin-5-yl]ethanol tert-butyldimethylsilyl ether
1.00g (2.72mmole) of 2- [ (5R) - (3, 4-dichlorophenyl) are added) Oxazolidin-5-yl]Ethanol tert-butyldimethylsilyl ether [ prepared as in example 1(f) first part]Dissolving in 10ml of pyridine, adding 773mg (3.27mmole) of 3, 4-dimethoxybenzenesulfonyl chloride to the resulting solution under ice-cooling, stirring the mixture under nitrogen for 2 hours, pouring the reaction mixture into 100ml of ice-cooled 10% w/v aqueous hydrochloric acid solution and extracting with ethyl acetate, washing the organic extract with saturated aqueous sodium chloride solution and then drying over anhydrous magnesium sulfate, evaporating the solvent under reduced pressure, eluting with a mixture of hexane and ethyl acetate in a volume ratio of 10: 1 to 2: 1, and purifying the resulting residue by silica gel column chromatography using a gradient elution method to obtain 1.27g of the title compound [ α]as a white crystal]D 24-5.74(c ═ 1.29, methanol) infrared absorption spectrum νmaxcm-1(KBr):
1588, 1510, 1468, 1264, 1155, 1140. 80(b)2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl) oxazolidin-5-yl]ethanol methanesulfonate
1.19g (2.06mmole) of 2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl) oxazolidin-5-yl]Ethanol tert-butyl dimethylBasilyl ethers [ prepared according to step (a) above]Dissolved in 20ml of a 3: 1 by volume mixture of acetic acid, tetrahydrofuran and water and the mixture heated at 80 ℃ for 2 hours under nitrogen. At the end of the heating, the reaction mixture wasneutralized with a saturated aqueous solution of sodium hydrogencarbonate and extracted with ethyl acetate. The organic extract was dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was dissolved in 10ml of pyridine. To the resulting solution, 23mg (0.19mmole) of 4-dimethylaminopyridine and 0.22ml (2.84mmole) of methanesulfonyl chloride were added under ice-cooling. The mixture was stirred at 0 ℃ for 2 hours under nitrogen atmosphere. At the end of the stirring, the reaction mixture was poured into 200ml of ice-cooled 10% w/v aqueous hydrochloric acid solution and extracted with ethyl acetate. The organic phase was washed with a saturated solution of sodium chloride and dried over anhydrous magnesium sulfate. Evaporating under reduced pressure to remove solvent, eluting with 2: 1 to 1: 2 volume ratio mixture of hexane and ethyl acetate, and purifying the residue by silica gel column chromatography to obtain 992mg of white crystalThe title compound [ α]]D 24-3.80(c ═ 0.5, methanol) nuclear magnetic resonance spectrum (400MHz, CDCl)3)δppm:
7.33(1H,doublet,J=8.6Hz);
7.30(1H,doublet of doublets,J=8.6&2.1Hz);
7.14(1H,doublet,J=2.2Hz);
7.11(1H,doublet,J=2.1Hz);
6.92(1H,doublet of doublets,J=8.7&2.2Hz);
6.80(1H,doublet,J=8.7Hz);
5.08(1H,doublet,J=5.7Hz);
4.98(1H,doublet,J=5.7Hz);
4.11(1H,multiplet);
3.94(3H,singlet);
3.86(3H,singlet);
3.82(1H,multiplet);
3.70(2H, AB-quartet, J11.3 Hz, Δ δ 0.08 ppm);
2.88(3H,singlet);
2.16(2H, multiplex). Mass Spectrometry (FAB) m/z: 540(M + H)+80(c)1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl) oxazolidin-5-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxides
105mg (0.19mmole) of 2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4-dimethoxybenzenesulfonyl) oxazolidin-5-yl group]Ethanol methanesulfonate [ prepared according to the above step (b)]]55mg (0.21mmole) of spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide hydrochloride (prepared as described in preparation 6), 49mg (0.58mmole) of sodium hydrogencarbonate, and 48mg (0.29mmole) of potassium iodide were suspended in 2ml of anhydrous dimethylformamide. The resulting mixture was heated at 80 ℃ for 8 hours under nitrogen atmosphere. At the end of the heating, the reaction mixture was poured into 10ml of saturated aqueous solution of sodium chloride and extracted with ethyl acetate. The organic extract was dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. Dichloro in a volume ratio of 40: 1 to 20: 1The residue was purified by column chromatography on silica gel using a mixture of methane and methanol as eluent to give 82mg of the title compound as white crystals [ α]]D 24+2.5(c ═ 0.52, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 21.4min infrared absorption spectrum vmaxcm-1(KBr):
1674, 1587, 1509, 1469, 1350, 1264, 1155, 1140, 1039. Mass Spectrometry (FAB) m/z: 665(M + H)+
Example 811- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl]morpholin-2-yl]ethyl } -1-methylspiro [ benzo [ c]thiophene-1 (3H), 4' -piperidinium]- (2S) -oxide iodide (methyl iodide salt of Compounds No.3-42)
300mg (0.45mmole) of 1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]Ethyl } spiro [ benzo [ c]]Thiophene-1 (3H), 4' -piperidines]- (2S) -oxide [ prepared as described in example 76]Dissolved in 3ml of acetonitrile, 30. mu.l (0.48mmole) of methyl iodide were added to the resulting solution, the mixture was stirred at room temperature overnight under nitrogen atmosphere, at the end of the stirring, the solvent was distilled off under reduced pressure, and the resulting residue was crystallized from diisopropyl ether to give 312mg of the title compound as pale yellow crystals [ α]]D 24+42.0(c ═ 1.0, methanol) HPLC analysis
Column: YMC-Pack ODS-A (250X 4.6 mm. RTM.)
Eluent:∶=40∶60,0.1%
flow rate: 1.0ml/min
Retention time: 9.9min Infrared absorption Spectrum vmaxcm-1(KBr):
3444,1632,1584,1464,1126。Mass Spectrometry (FAB) m/z: 687 (free form, M)+) Elemental analysis:
calculated values::
:51.54%;:5.07%;:3.44%;:3.93%;:8.69%;:15.56%。
actually measuring::51.14%;:5.39%;:3.42%;:4.01%;:8.50%;:15.96%。

Claims (56)

1. a compound of formula (I) and its quaternary ammonium derivatives of formula (Ia):wherein R is1And R2Which may be the same or different, each represents a carbocyclic aryl or an aromatic heterocyclic group, the aryl and heterocyclic groups being unsubstituted or substituted by at least one substituent preferably selected from the group consisting of α, A represents a methylene group, a carbonyl group or a sulfonyl group, B represents the groups A and R1An alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 4 carbon atoms; d represents an oxygen or sulfur atom; e represents an alkylene group having 1 to 6 carbon atoms, a haloalkylene group having 1 to 6 carbon atoms, a cycloalkane-1, 1-diyl group having 3 to 6 carbon atoms, a cycloalkane-1, 1-diyl methyl group having 3 to 6 carbon atoms in the cycloalkane moiety or a cycloalkane-1, 1-di (C) group having 3 to 6 carbon atoms in the cycloalkane moietyAn oxymethyl group); g represents an alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 4 carbon atoms; l representsGroup or formulaGroup wherein R3Denotes a carbocyclic aryl or aromatic heterocyclic radical, which aryl and aromatic heterocyclic radicals are unsubstituted or substituted by at least one substituent preferably selected from the group of substituents α4Represents a hydrogen atom, a carbocyclic aryl or aromatic heterocyclic group which is unsubstituted or substituted by at least one substituent preferably selected from the group consisting of α5Expression formula (I)A group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an amino group, an amido group, an amino group, anAn alkyl group having 1 to 6 carbon atoms and substituted with an amido group, an amido group having a nitrogen atom substituted with an alkyl group having 1 to 6 carbon atoms, a hydroxyl group, a hydroxyalkyl group having 1 to 6 carbon atoms, an alkoxyalkyl group having both an alkoxy moiety and an alkyl group each having 1 to 6 carbon atoms, or an aralkyloxyalkyl group wherein an oxyalkyl moiety has 1 to 6 carbon atoms, an alkyl moiety of an aralkyl moiety has 1 to 4 carbon atoms and is substituted with 1 to 3 carbocyclic aryl groups which are unsubstituted or substituted with at least one substituent preferably defined by α below,
wherein R is6Represents an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, formulaA group, a carbocyclic aryl or heterocyclic group, the aryl and heterocyclic groups being unsubstituted or substituted by at least one substituent preferably customized to the substituent α,
wherein R isaRepresents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxylic acid group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, a carbocyclic aryl group which is unsubstituted or substituted by at least one substituent preferably defined as α below, or an aralkyl group in which the alkyl moiety has 1 to 4 carbon atoms and is substituted by 1 to 3 carbocyclic aryl groups defined as below, and
Rbrepresents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxylic acid group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, a carbocyclic aryl group or an aromatic heterocyclic group which are unsubstituted or substituted by at least one substituent preferably defined as α below, or an aralkyl group in which the alkyl moiety has 1 to 4 carbon atoms and is substituted by 1 to 3 carbocyclic aryl groups as defined above, or
RaAnd RbTogether with the nitrogen atom to which they are attachedNitrogen-containing heterocyclic group, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent selected from the group consisting of substituents β as defined below, and which has one heteroatom selected from nitrogen, oxygen and sulfur atoms, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above and fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl or aromatic heterocyclyl group is unsubstituted or substituted by at least one substituent preferably defined as substituent α7Represents an alkyl group having 1 to 6 carbon atoms, and the above-mentioned substituent α is selected from the group consisting of a halogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxylic acid group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 carbon atoms, a hydroxyl group, a carboxyl group, an alkoxycarbonyl group having 1 to 6 carbon atoms in the alkoxy moiety, an acylamino group having 1 to 6 carbon atoms, an alkylsulfonylamino group having 1 to 6 carbon atoms, an haloalkylsulfonyl group having 1 to 6 atoms, an amino group, a cyano group, and an alkylene group having 1 to 8 carbonatoms (forming a cycloalkyl group fused with an aryl group or a heterocyclic group), the above-mentioned substituent β is:
when substituting carbon atoms, oxo
When a nitrogen atom is substituted, it is selected from the group consisting of an alkylsulfonyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms which is unsubstituted or substituted with at least one substituent preferably self-defined as the substituent γ, an aliphatic acyl group, a carbocyclic aryl group which is unsubstituted or substituted with at least one substituent preferably self-defined as the substituent α above, an aralkyl group in which the alkyl moiety has 1 to 4 carbon atoms and is substituted with 1 to 3 carbocyclic aryl groups as defined above, and when a sulfur atom is substituted, one or two oxygen atoms to form a sulfoxide or sulfone group, and the above-mentioned substituent γ is selected from the group consisting of a halogen atom, an alkoxy group having 1 to 6 carbon atoms, an aliphatic carboxyacyl group having 1 to 6 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a haloalkylsulfonyl group having 1 to 6 carbon atoms, a hydroxyl group, a carboxyl group, an alkoxycarbonyl group having 1 to 6 carbon atoms in the alkoxy moiety, an aliphatic acylamino group having 1 to 6 carbon atoms, an amino group, and a cyano group.
2. A compound according to claim 1, wherein E represents methylene.
3. The compound of claim 2, wherein R1And R2May be the same or different and each represents a carbocyclic aromatic groupAn aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
4. The compound of claim 2, wherein R2Represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
5. A compound according to claim 2, wherein a represents a carbonyl group.
6. A compound according to claim 2, wherein B represents a single bond.
7. A compound according to claim 2, wherein D represents an oxygen atom.
8. The compound of claim 2, wherein G is alkylene having 1 to 4 carbon atoms.
9. The compound of claim 2, wherein G is alkylene having 2 or 3 carbon atoms.
10. The compound of claim 2, wherein R3Represents an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
11. A compound according to claim 2 wherein L represents formula (la)A group.
12. The compound of claim 2, wherein R4Represents a carbocyclic aryl or aromatic heterocyclic radical。
13. The compound of claim 2, wherein R5Expression formula (I)Group, wherein R6Represents an alkyl group having 1 to 6 carbon atoms or formulaA group.
14. The compound of claim 2, wherein R5Represents amino, amido or hydroxyl.
15. The compound of claim 2, wherein R4To R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent β, or a heterocyclyl group having a single heteroatom selected from nitrogen, oxygen and sulfur atoms4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl or aromatic heterocyclyl group is unsubstituted or substituted by at least one substituent preferably selected from substituent α.
16. The compound of claim 2, wherein:
R1and R2The same or different each represents a carbocyclic aryl group, an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α;
a represents a carbonyl group;
b represents a single bond;
d represents an oxygen atom;
g represents an alkylene group having 1 to 4 carbon atoms;
l representsA group;
R4represents a carbocyclic aryl or aromatic heterocyclic group, and
R5expression formula (I)The radical(s) is (are),wherein R is6Represents an alkyl group having 1 to 6 carbon atoms or formulaA group.
17. The compound of claim 2, wherein:
R1and R2The same or different, each represents a carbocyclic aryl group, an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α;
a represents a carbonyl group;
b represents a single bond;
d represents an oxygen atom;
g represents an alkylene group having 1 to 4 carbon atoms;
l representsA group; and
R4and R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent β, and which has a single heteroatom selected from nitrogen, oxygen and sulfur, or R4And R5Together with the carbon atom to which they are attached represent the above cycloalkyl or heterocyclyl group fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl and aromatic heterocyclyl group are unsubstituted or substituted by at least one substituent selected from the group consisting of substituents α.
18. A compound according to claim 1 wherein E represents formula (la)A group wherein n is an integer from 2 to 4.
19. The compound of claim 18, wherein R1And R2The same or different, each represents a carbocyclic aryl group, an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
20. The compound of claim 18, wherein R2Represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents.
21. A compound according to claim 18, wherein a represents carbonyl.
22. A compound according to claim 18, wherein B represents a single bond.
23. A compound according to claim 18, wherein D represents an oxygen atom.
24. A compound according to claim 18, wherein G represents an alkylene group having from 1 to 4 carbon atoms.
25. A compound according to claim 18, wherein G represents an alkylene group having 2 or 3 carbon atoms.
26. The compound of claim 18, wherein R3Represents an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
27. A compound according to claim 18 wherein L represents formula (la)A group.
28. The compound of claim 18, wherein R4Represents a carbocyclic aryl or aromatic heterocyclic group.
29. The compound of claim 18, wherein R5Expression formula (I)Group, wherein R6Represents an alkyl group having1 to 6 carbon atoms or formulaA group.
30. The compound of claim 18, wherein R5Represents amino, amido or hydroxyl.
31. The compound of claim 18, wherein R4And R5Together with the carbon atom to which they are attached, represent a group having 5 to 10Cycloalkyl or heterocyclyl of a ring atom, which group is unsubstituted or substituted by at least one substituent β, so as to have a single heteroatom in the heterocyclyl selected from nitrogen, oxygen and sulphur, or R4And R3Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl or aromatic heterocyclyl group is unsubstituted or substituted by at least one substituent preferably selected from substituent α.
32. The compound of claim 18, wherein n is 2 or 3.
33. The compound of claim 18, wherein n is 2.
34. The compound of claim 18, wherein:
R1and R2The same or different, each represents a carbocyclic aryl group, an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α;
a represents a carbonyl group;
b represents a single bond;
d represents an oxygen atom;
g represents an alkylene group having 1 to 4 carbon atoms;
l represents a group of the formulaA group;
R4represents an aryl group or an aromatic heterocyclic group;
R5expression formula (I)Group, wherein R6Represents an alkyl group having 1 to 6 carbon atoms or formulaA group; and
n is 2 or 3.
35. The compound of claim 18, wherein:
R1and R2The same or different, each represents a carbocyclic aryl group, an aromatic heterocyclic group or a carbocyclic aryl group substituted with 1 to 3 substituents α;
a represents a carbonyl group;
r represents a single bond;
d represents an oxygen atom;
g represents an alkylene group having 1 to 4 carbon atoms;
l represents a group of the formulaA group of (a);
R4and R5Together with the carbon atom to which they are attached represent a cycloalkyl group having 5 to 10 ring atoms, which is unsubstituted or substituted by at least one substituent β, and which has a single heteroatom selected from nitrogen, oxygen and sulfur, or R4And R5Together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclyl group as defined above fused to a carbocyclic aryl or aromatic heterocyclyl group, which aryl and aromatic heterocyclyl group are unsubstituted or substituted by at least one substituent preferably selected from the group consisting of substituent α,and
n is 2 or 3.
36. The compound of claim 1, wherein R4And R5Together with the carbon atom to which they are attached represent a group of the formula
J represents an alkylene group having 1 to 6 carbon atoms;
ar represents a carbocyclic aromatic group or aromatic heterocyclic group fused to a ring containing J and S, the aromatic group or aromatic heterocyclic group being unsubstituted or substituted with at least one substituent preferably defined as the above substituent α, and
is shown in whichThe sulfur atom is a sulfoxide group of S-configuration.
37. The compound of claim 36, wherein R1Represents a carbocyclic aryl group, an aromatic heterocyclic group, or a carbocyclic aryl group substituted with 1 to 3 substituents α.
38. RightsThe compound of claim 36, wherein R1Represents a carbocyclic aryl group or from 1 to 3 substituents α1Substituted carbocyclic aryl, and substituent α1Selected from alkyl groups having 1 to 6 carbon atoms, havingHaloalkyl of 1 to 6 carbon atoms, and alkoxy of 1 to 6 carbon atoms.
39. The compound of claim 36, wherein R2Represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
40. The compound of claim 36, wherein R2Represents a carbocyclic aryl group or a carbocyclic aryl group substituted by 1 to 3 halogen atoms.
41. A compound according to claim 36, wherein a represents carbonyl.
42. A compound according to claim 36, wherein B represents a single bond.
43. A compound according to claim 36, wherein D represents an oxygen atom.
44. A compound according to claim 36, wherein E represents C1-4Alkylene or containing C therein3-6C of cycloalkane-1, 1-diyl group3-8An alkylene group.
45. A compound according to claim 36, wherein E represents methylene, ethylene, dimethylmethylene, 1, 1-dimethylethylene, 2, 2-dimethylethylene, cyclopropane-1, 1-diyl, cyclobutane-1, 1-diyl, cyclopentane-1, 1-diyl, cyclohexane-1, 1-diyl, cyclopropane-1, 1-diyl methyl, cyclobutane-1, 1-diyl methyl, cyclopentane-1, 1-diyl methyl or cyclohexane-1, 1-diyl methyl.
46. A compound according to claim 36, wherein G represents C1-4An alkylene group;
47. the process of claim 36A compound wherein G represents C2-3An alkylene group.
48. A compound according to claim 36, wherein J represents C1-4An alkylene group.
49. A compound according to claim 36, wherein J represents methylene or ethylene.
50. The compound of claim 36, wherein ring Ar represents an aryl group, an aryl group substituted with 1 to 3 substituents α, or an aromatic heterocyclic group.
51. The compound of claim 36, wherein ring Ar represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
52. The compound of claim 36, wherein:
R1represents aryl, aromatic heterocyclic group, or carbocyclic aryl substituted with 1 to 3 substituents α;
R2represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents α;
a represents a carbonyl group;
b represents a single bond;
d represents an oxygen atom;
e represents C1-4Alkylene or containing C therein3-6Of cycloalkane-1, 1-diyl groupsC3-8An alkylene group;
g represents C1-4An alkylene group;
j represents C1-4An alkylene group; and
ring Ar represents a carbocyclic aryl group, a carbocyclic aryl group substituted with 1 to 3 substituents α, or an aromatic heterocyclic group.
53. The compound of claim 36, wherein:
R1represents a carbocyclic aryl group or from 1 to 3 substituents α1Substituted carbocyclic aryl, and substituent α1Selected from alkyl groups having 1 to 6 carbon atoms, halogen having 1 to 6 carbon atomsAlkyl substituents, and alkoxy groups having 1 to 6 carbon atoms;
R2represents a carbocyclic aryl group or a carbocyclic aryl group substituted by 1 to 3 halogen atoms;
a represents a carbonyl group;
b represents a single bond;
d represents an oxygen atom;
e represents methylene, ethylene, dimethylmethylene, 1, 1-dimethylethylene, 2, 2-dimethylethylene, cyclopropane-1, 1-diyl, cyclobutane-1, 1-diyl, cyclopentane-1, 1-diyl, cyclohexane-1, 1-diyl, cyclopropane-1, 1-diyl methyl, cyclobutane-1, 1-diyl methyl, cyclopentane-1, 1-diyl methyl or cyclohexane-1, 1-diyl methyl;
g represents C2-3An alkylene group;
j represents a methylene group or an ethylene group; and
ring Ar represents a carbocyclic aryl group or a carbocyclic aryl group substituted with 1 to 3 substituents α.
54. The following compound of claim 1;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1{2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl) -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (2-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (3-pyridyl) piperidine-4-carboxamide;
1- {2- [5- (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } -4- (4-pyridyl) piperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4- (pyrrolidin-1-ylcarbonyl) piperidine;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-morpholinocarbonyl-4-phenylpiperidine;
1- {2- [2- (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4-carboxamide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } -4-phenylpiperidine-4- (N, N-dimethylformamide);
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzofuran-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isobenzo [ c]thiophene-1 (3H), 4' -piperidine]-2-oxide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidin]-3(4H) -one;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isobenzofuran-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine];
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]-2-oxide;
1- {2- [2- (3, 4-dichlorophenyl) -4- (3-methoxybenzoyl) morpholin-2-yl]ethyl } spiro [ isoquinoline-1 (2H), 4' -piperidin]-3(4H) -one;
1- {2- [ (5R) - (3, 4-dichlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H) 4' -piperidine]- (2S) -oxide;
1- {2- [ (5R) - (4-chlorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (5R) - (4-fluorophenyl) -3- (3, 4, 5-trimethoxybenzoyl) oxazolidin-5-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexahydro-1, 4-oxazepin-2-yl]ethyl } spiro[ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-fluorophenyl) -4- (3, 4, 5-trimethoxybenzoyl) hexaoxy-1, 4-oxazepin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine 1- (2S) -oxide;
1- {2- [ (2R) - (4-chlorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (4-fluorophenyl) -4- (3-isopropoxyphenylacetyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide;
1- {2- [ (2R) - (3, 4-dichlorophenyl) -5, 5-dimethyl-4- (3, 4, 5-trimethoxybenzoyl) morpholin-2-yl]ethyl } spiro [ benzo [ c]thiophene-1 (3H), 4' -piperidine]- (2S) -oxide; and salts and esters thereof.
55. A composition for the treatment or prophylaxis of central nervous system disorders, neurodegenerative disorders, respiratory disorders, inflammatory disorders, allergy, allergic disorders, ophthalmic disorders, dermatological disorders, drug addiction, physical disorders due to stress, sympatholytic dystrophy, dysthymia, unwanted immune responses, disorders associated with increased immunity, digestive disorders, emesis, bladder dysfunction, eosinophilia, disorders due to abnormal blood flow, and pain, which comprises an active compound of formula (I) or (Ia), or a pharmaceutically acceptable salt or ester thereof, in admixture with a pharmaceutically acceptable carrier or diluent.
56. Use of a compound of formula (I) or (Ia) as defined in any one of claims 1 to 54, or a pharmaceutically acceptable salt or ester thereof, for the manufacture of a medicament for the treatment or prophylaxis of: central nervous system diseases, neurodegenerative diseases, respiratory diseases, inflammatory diseases, allergies, allergic diseases, ophthalmic diseases, skin diseases, drug addiction, physical diseases caused by stress, sympathoreflex dystrophy, dysthymia, undesired immune reactions, diseases associated with intensified immunity, digestive system diseases, emesis, bladder functional diseases, eosinophilia, diseases caused by abnormal blood flow, and pain.
HK98101290.8A 1995-12-01 1998-02-19 Heterocyclic compounds having tachykinin receptor antagonist activity, their preparation and their use HK1002279A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP313828/95 1995-12-01
JP336369/95 1995-12-25
JP296869/96 1996-11-08

Publications (1)

Publication Number Publication Date
HK1002279A true HK1002279A (en) 1998-08-14

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