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CN1429199A - Insecticidal 1,8-naphthalenedicarboxamides - Google Patents

Insecticidal 1,8-naphthalenedicarboxamides Download PDF

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Publication number
CN1429199A
CN1429199A CN01805190A CN01805190A CN1429199A CN 1429199 A CN1429199 A CN 1429199A CN 01805190 A CN01805190 A CN 01805190A CN 01805190 A CN01805190 A CN 01805190A CN 1429199 A CN1429199 A CN 1429199A
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pyridyl
chf
ocf
clme
alkyl
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CN01805190A
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T·P·塞尔比
孙经武
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EIDP Inc
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EI Du Pont de Nemours and Co
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Publication of CN1429199A publication Critical patent/CN1429199A/en
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/18—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
    • A01N37/22—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof the nitrogen atom being directly attached to an aromatic ring system, e.g. anilides
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/18—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
    • A01N37/22—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof the nitrogen atom being directly attached to an aromatic ring system, e.g. anilides
    • A01N37/24—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof the nitrogen atom being directly attached to an aromatic ring system, e.g. anilides containing at least one oxygen or sulfur atom being directly attached to the same aromatic ring system
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    • C07C233/00—Carboxylic acid amides
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    • C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
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    • C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/75—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40—Y being a hydrogen or a carbon atom
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

本发明公开了式I和式II的化合物及其N－氧化物和农业适用盐，其用于防治无脊椎害虫，式I和式II中，A、B、J、R1、R2、R3、R4和n如说明书中所定义。本发明还公开了包含式I或式II化合物的组合物以及防治无脊椎害虫的方法，该方法包括使无脊椎害虫或其环境与有效量的式I或式II化合物相接触。The present invention discloses compounds of formula I and formula II and their N-oxides and agriculturally applicable salts, which are used to control invertebrate pests. In formula I and formula II, A, B, J, R1, R2, R3, R4 and n are as defined in the specification. The present invention also discloses a composition comprising the compound of formula I or formula II and a method of controlling invertebrate pests, the method comprising contacting the invertebrate pest or its environment with an effective amount of the compound of formula I or formula II.

Description

杀虫剂1，8-萘二甲酰胺Insecticide 1,8-naphthalene dicarboxamide

               发明背景 Background of the invention

本发明涉及特定的1，8-萘二甲酰胺、其农业适用盐和组合物，以及其在农学和非农学环境中在防治无脊椎害虫上的使用方法。The present invention relates to specific 1,8-naphthalene dicarboxamides, agriculturally acceptable salts and compositions thereof, and methods of use thereof for controlling invertebrate pests in both agronomic and non-agronomic settings.

为了获得作物的高收益，控制无脊椎害虫非常重要。无脊椎害虫对于正在生长以及储存的农作物造成的危害能使产量显著降低，并从而导致消费者花费增加。在林业、温室作物、观赏性植物、苗圃作物、储存的食物和纤维产品、牲畜、家用品、以及公共和动物健康等方面，控制无脊椎害虫也很重要。已有许多商业产品用于这些目的，但是仍不断需要更有效、更廉价、毒性低、无害于环境或具有不同施用模式的新化合物。In order to obtain high crop yields, it is very important to control invertebrate pests. Invertebrate pest damage to growing and stored crops can significantly reduce yields and thus increase costs to consumers. Control of invertebrate pests is also important in forestry, greenhouse crops, ornamental plants, nursery crops, stored food and fiber products, livestock, household products, and public and animal health. There are many commercial products for these purposes, but there is a constant need for new compounds that are more effective, cheaper, less toxic, environmentally friendly or have different modes of administration.

EP919542公开了作为杀虫剂的式i的邻苯二甲酰胺其中，除其它之外，Z1和Z2是O和S；而R1、R2和R3特别是H、烷基或取代烷基。EP919542 discloses phthalamides of formula i as insecticides wherein Z 1 and Z 2 are, inter alia, O and S; and R 1 , R 2 and R 3 are in particular H, alkyl or substituted alkyl.

                        发明概述 Summary of the invention

本发明涉及式I和式II的化合物，包括其所有几何和立体异构体、N-氧化物和农业适用盐：其中每一J独立地是苯基环、萘基环体系、5或6元杂芳环或芳香8、9或10元杂双环稠环体系，其中，每一环或环体系任选地是用1-5个R5取代的；A和B独立地是O或S；n为0-4；R1是H；或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基和C3-C6环烷基氨基；或者R1是C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基或C3-C8二烷基氨基羰基；R2是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C4烷氧基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷氧基羰基或C2-C6烷基羰基；R3是H；或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基和C1-C4烷基磺酰基；或者R2和R3可通过与它们相连的氮而在一起形成环，该环含2-6个碳原子并任选地含有一个另外的氮、硫或氧原子，该环可任选地被选自C1-C2烷基、卤素、CN、NO2和C1-C2烷氧基的1-4个取代基取代；和每一R4和每一R5独立地是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C6卤代烷基、C2-C6卤代链烯基、C2-C6卤代炔基、C3-C6卤代环烷基、卤素、CN、CO2H、CONH2、NO2、羟基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基、或C3-C6三烷基甲硅烷基；或者每一R4和每一R5独立地是苯基、苄基、苯氧基、5或6元杂芳环或芳香8、9或10元杂双环稠环体系，每一环任选地为1或3个独立地选自下列的取代基取代：C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C2-C4卤代链烯基、C2-C4卤代炔基、C3-C6卤代环烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C3-C6(烷基)环烷基氨基、C2-C4烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基、或C3-C6三烷基甲硅烷基；或者(R5)2当连在相邻碳原予上时可以合在一起成为-OCF2O-、-CF2CF2O-或-OCF2CF2O-。The present invention relates to compounds of formula I and II, including all geometric and stereoisomers, N-oxides and agriculturally suitable salts thereof: wherein each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring, or an aromatic 8-, 9-, or 10-membered heterobicyclic fused ring system, wherein each ring or ring system is optionally 1-5 R 5 substituted; A and B are independently O or S; n is 0-4; R 1 is H; or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, each optionally substituted by one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino and C 3 -C 6 cycloalkylamino; or R 1 is C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkyl Aminocarbonyl or C 3 -C 8 dialkylaminocarbonyl; R 2 is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 ring Alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkoxycarbonyl or C 2 -C 6 alkylcarbonyl; R 3 is H; or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, Each is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 Alkylsulfinyl and C 1 -C 4 alkylsulfonyl; or R 2 and R 3 may be joined together through the nitrogen attached to them to form a ring containing 2 to 6 carbon atoms and optionally containing a Another nitrogen, sulfur or oxygen atom, the ring may be optionally substituted by 1-4 substituents selected from C 1 -C 2 alkyl, halogen, CN, NO 2 and C 1 -C 2 alkoxy; and each R 4 and each R 5 is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 6 haloalkenyl, C 2 -C 6 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, CO 2 H, CONH 2 , NO 2 , hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkane Sulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 Alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkyl Aminocarbonyl, C 3 -C 8 dialkylaminocarbonyl, or C 3 -C 6 trialkylsilyl; or each R 4 and each R 5 are independently phenyl, benzyl, phenoxy, 5 or 6-membered heteroaryl ring or aromatic 8-, 9- or 10-membered heterobicyclic condensed ring system, each ring is optionally substituted by 1 or 3 substituents independently selected from the following: C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 2 -C 4 haloalkenyl, C 2 -C 4 Haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio , C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino , C 3 -C 6 (alkyl)cycloalkylamino, C 2 -C 4 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylaminocarbonyl, C 3 -C 8 di Alkylaminocarbonyl, or C 3 -C 6 trialkylsilyl; or (R 5 ) 2 can be combined into -OCF 2 O-, -CF 2 CF 2 when connected to adjacent carbon atoms O- or -OCF 2 CF 2 O-.

本发明还涉及用于控制无脊椎害虫的组合物，包含生物有效量的式I或式II化合物以及至少一种选自表面活性剂、固体稀释剂和液体稀释剂的附加组分。本发明还涉及一种组合物，其包含生物有效量的式I或式II化合物以及有效量的至少一种附加生物活性化合物或试剂。The present invention also relates to compositions for controlling invertebrate pests comprising a biologically effective amount of a compound of formula I or formula II and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. The present invention also relates to a composition comprising a biologically effective amount of a compound of formula I or formula II and an effective amount of at least one additional biologically active compound or agent.

本发明还涉及控制无脊椎害虫的方法，包括使无脊椎害虫或其环境与生物有效量的式I或式II化合物(例如作为在此描述的组合物)接触。本发明还涉及这样的方法，其中，使无脊椎害虫或其环境与用于控制无脊椎害虫、含有生物有效量的式I或式II化合物的组合物接触，或与含有式I或式II化合物及生物有效量的至少一种附加化合物或试剂的组合物接触，以防治无脊椎害虫。The invention also relates to a method of controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of formula I or formula II (eg, as a composition described herein). The present invention also relates to a method wherein the invertebrate pest or its environment is contacted with a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of formula I or II, or with a compound of formula I or II and a biologically effective amount of at least one additional compound or agent to control invertebrate pests.

                     发明详述 Detailed description of the invention

在上文中，单独使用或在诸如“烷基硫代”或“卤代烷基”等复合词中使用的术语“烷基”包括直链或支链烷基，如甲基、乙基、正丙基、异丙基，或不同的丁基、戊基或己基异构体。“链烯基”包括直链或支链烯类，如1-丙烯基、2-丙烯基，以及丁烯基、戊烯基和己烯基的不同异构体。“链烯基”还包括多烯类，如1，2-丙二烯和2，4-己二烯。“炔基”包括直链或支链炔类，如1-丙炔基、2-丙炔基，以及丁炔基、戊炔基和己炔基的不同异构体。“炔基”还可包括由多重三键组成的部分，如2，5-己二炔。“烷氧基”包括例如甲氧基、乙氧基、正丙氧基、异丙氧基以及丁氧基、戊氧基和己氧基的不同异构体。“烷基硫代”包括支链或直链烷基硫代部分，如甲基硫代、乙基硫代、以及丙基硫代、丁基硫代、戊基硫代和己基硫代的不同异构体。“环烷基”包括例如环丙基、环丁基、环戊基和环己基。“烷基氨基”、“链烯基硫代”、“链烯基亚硫酰基”、“链烯基磺酰基”、“炔基硫代”、“炔基亚硫酰基”、“炔基磺酰基”等等的定义与以上例子相似。“烷氧基羰基”的例子包括CH3OC(＝O)，CH3CH2OC(＝O)，CH3CH2CH2OC(＝O)，(CH3)2CHOC(＝O)，以及丁氧基羧基或戊氧基羧基的不同异构体。“烷基氨基羧基”的例子包括CH3NHC(＝O)，CH3CH2NHC(＝O)，CH3CH2CH2NHC(＝O)，(CH3)2CHNHC(＝O)，以及丁基氨基羧基或戊基氨基羧基的不同异构体。术语“二烷基氨基”包括用可以相同或不同的两个烷基基团取代的氨基官能团。“二烷基氨基羧基”定义类似，其例包括(CH3)2NC(＝O)和CH3CH2NCH3C(＝O)。In the above, the term "alkyl" used alone or in compound words such as "alkylthio" or "haloalkyl" includes straight or branched chain alkyl groups such as methyl, ethyl, n-propyl, Isopropyl, or the different butyl, pentyl, or hexyl isomers. "Alkenyl" includes straight or branched chain alkenes such as 1-propenyl, 2-propenyl, and the different isomers of butenyl, pentenyl and hexenyl. "Alkenyl" also includes polyenes such as 1,2-propadiene and 2,4-hexadiene. "Alkynyl" includes straight or branched alkynes such as 1-propynyl, 2-propynyl, and the different isomers of butynyl, pentynyl and hexynyl. "Alkynyl" may also include moieties composed of multiple triple bonds, such as 2,5-hexadiyne. "Alkoxy" includes, for example, methoxy, ethoxy, n-propoxy, isopropoxy and the different isomers of butoxy, pentyloxy and hexyloxy. "Alkylthio" includes branched or straight-chain alkylthio moieties such as methylthio, ethylthio, and variations of propylthio, butylthio, pentylthio, and hexylthio isomer. "Cycloalkyl" includes, for example, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. "Alkylamino", "Alkenylthio", "Alkenylsulfinyl", "Alkenylsulfonyl", "Alkynylthio", "Alkynylsulfinyl", "Alkynylsulfonyl""Acyl", etc. are defined similarly to the above examples. Examples of "alkoxycarbonyl" include CH 3 OC(=O), CH 3 CH 2 OC(=O), CH 3 CH 2 CH 2 OC(=O), (CH 3 ) 2 CHOC(=O), And the different isomers of butoxycarboxyl or pentyloxycarboxyl. Examples of "alkylaminocarboxy" include CH 3 NHC(=O), CH 3 CH 2 NHC(=O), CH 3 CH 2 CH 2 NHC( = O), (CH 3 ) 2 CHNHC(=O), and the different isomers of butylaminocarboxy or pentylaminocarboxy. The term "dialkylamino" includes an amino function substituted with two alkyl groups which may be the same or different. "Dialkylaminocarboxy" is defined similarly, examples of which include (CH 3 ) 2 NC(=O) and CH 3 CH 2 NCH 3 C(=O).

术语“杂环”或“杂环体系”表示其中的至少一个环原子不是碳并包含1-4个杂原子的环或环体系，所述杂原子独立地选自氮、氧或硫，前提是每一杂环含有不多于4个的氮、不多于2个的氧，和不多于2个的硫。可以通过任何可用的碳或氮、通过取代该碳或氮上的氢而与杂环进行连接。术语“芳环体系”表示完全未饱和的碳环和杂环，其中多核环体系是芳族的(其中芳族表示所述环体系满足休克尔规则)。术语“杂芳环”表示具完全芳香性的环，其中至少一个环原子不是碳并包含1-4个杂原子，所述杂原子独立地选自氮、氧或硫，前提是每一杂环含有不多于4个的氮、不多于2个的氧，和不多于2个的硫(其中芳香表示所述环体系满足休克尔规则)。可以通过任何可用的碳或氮、通过取代该碳或氮上的氢而与所述杂环进行连接。术语“芳香杂环体系”包括完全芳香杂环和其中的多核环体系获的至少一个环是芳香的(其中芳香表示所述环体系满足休克尔规则)杂环。术语“杂双环稠环体系”包括由两个稠环组成的环体系，其中，至少一个环原子不是碳，并且是芳香的或非芳香的(如上所定义)。The term "heterocycle" or "heterocycle system" means a ring or ring system in which at least one ring atom is other than carbon and contains 1 to 4 heteroatoms independently selected from nitrogen, oxygen or sulfur, provided that Each heterocycle contains no more than 4 nitrogens, no more than 2 oxygens, and no more than 2 sulfurs. Attachment to the heterocycle can be through any available carbon or nitrogen, by substitution of a hydrogen on the carbon or nitrogen. The term "aromatic ring system" denotes fully unsaturated carbocyclic and heterocyclic rings, wherein the polynuclear ring system is aromatic (where aromatic means that the ring system satisfies Huckel's rule). The term "heteroaromatic ring" means a fully aromatic ring in which at least one ring atom is not carbon and contains 1 to 4 heteroatoms independently selected from nitrogen, oxygen or sulfur, provided that each heterocyclic Contains no more than 4 nitrogens, no more than 2 oxygens, and no more than 2 sulfurs (where aromatic means that the ring system satisfies Huckel's rule). Attachment to the heterocycle can be through any available carbon or nitrogen, by substitution of a hydrogen on the carbon or nitrogen. The term "aromatic heterocyclic ring system" includes entirely aromatic heterocyclic rings and heterocyclic rings in which at least one ring of a polynuclear ring system is aromatic (where aromatic means that the ring system satisfies Huckel's rule). The term "heterobicyclic fused ring system" includes ring systems consisting of two fused rings wherein at least one ring atom is other than carbon and is aromatic or non-aromatic (as defined above).

单独的或在诸如“卤代烷基”等复合词中的术语“卤素”包括氟、氯、溴或碘。另外，当用于诸如“卤代烷基”等复合词中时，所述烷基可以用相同或不同的卤原子部分或全部取代。“卤代烷基”的例子包括F3C，ClCH2，CF3CH2和CF3CCl2。术语“卤代链烯基”、“卤代炔基”、“卤代烷氧基”等的定义与术语“卤代烷基”类似。“卤代链烯基”的例子包括(Cl2)C＝CHCH2和CF3CH2CH＝CHCH2。“卤代炔基”的例子包括HC≡CCHCl，CF3C≡C，CCl3C≡C和FCH2C≡CCH2。“卤代烷氧基”的例子包括CF3O，CCl3CH2O，HCF2CH2CH2O和CF3CH2O。The term "halogen" alone or in compound words such as "haloalkyl" includes fluorine, chlorine, bromine or iodine. In addition, when used in compound words such as "haloalkyl", the alkyl group may be partially or fully substituted with the same or different halogen atoms. Examples of "haloalkyl" include F 3 C, ClCH 2 , CF 3 CH 2 and CF 3 CCl 2 . The terms "haloalkenyl", "haloalkynyl", "haloalkoxy", etc. are defined similarly to the term "haloalkyl". Examples of "haloalkenyl" include ( Cl2 )C= CHCH2 and CF3CH2CH = CHCH2 . Examples of "haloalkynyl" include HC≡CCHCl, CF3C≡C , CCl3C≡C and FCH2C≡CCH2 . Examples of " haloalkoxy" include CF3O , CCl3CH2O , HCF2CH2CH2O and CF3CH2O .

取代基团中的碳原子总数由“Ci-Cj”前缀表示，其中，i和j为1-6的数。例如，C1-C3烷基磺酰基表示甲基磺酰基直至丙基磺酰基；C2烷氧基烷基表示CH3OCH2；C3烷氧基烷基表示例如CH3CH(OCH3)，CH3OCH2CH2或CH3CH2OCH2；而C4烷氧基烷基表示用烷氧基基团取代的烷基基团的各种异构体，含有总共4个碳原子，例子包括CH3CH2CH2OCH2和CH3CH2OCH2CH2。在上面所列举的当中，当式1的化合物含有杂环时，所有的取代基均通过任何可用的碳或氮、通过取代该碳或氮上的氢而与该环进行连接。The total number of carbon atoms in a substituent group is indicated by the "C i -C j " prefix, where i and j are numbers from 1-6. For example, C 1 -C 3 alkylsulfonyl represents methylsulfonyl up to propylsulfonyl; C 2 alkoxyalkyl represents CH 3 OCH 2 ; C 3 alkoxyalkyl represents for example CH 3 CH(OCH 3 ), CH 3 OCH 2 CH 2 or CH 3 CH 2 OCH 2 ; and C 4 alkoxyalkyl denotes the various isomers of alkyl groups substituted with alkoxy groups, containing a total of 4 carbon atoms , examples include CH 3 CH 2 CH 2 OCH 2 and CH 3 CH 2 OCH 2 CH 2 . Among the above enumerated, when the compound of Formula 1 contains a heterocyclic ring, all substituents are attached to the ring through any available carbon or nitrogen, by substituting a hydrogen on the carbon or nitrogen.

当基团含有可为氢的取代基时，例如R3，则当该取代基为氢时，即认为相当于该基团未被取代。当基团上任选取代基的数目为0时，例如当n为0时，则认为相当于该基团未被取代。当键被标示为不固定时，则取代基可通过氢的取代而与环上的任何可用碳原子连接；对于双环体系，一个或多个取代基可与双环体系中的任何一环连接，或与两环均连接。例如当n为1时，单一的R4取代基可在所表明的2、3、4、5、6或7位的任何位置上连接式I或式II；而当n为2时，2个独立的R4取代基可在2，3；2，4；2，5；2，6或2，7位或在两位的任何其它组合上连接。当R2和R3与它们所连接的氮合起形成环时，则该环可在其中任何可用的碳或任选地在任何可用的氮上被任选地取代。When a group contains a substituent which may be hydrogen, eg R3 , then the group is considered unsubstituted when the substituent is hydrogen. When the number of optional substituents on a group is 0, for example when n is 0, it is considered that the group is unsubstituted. When a bond is indicated as not fixed, the substituents may be attached to any available carbon atom on the ring by substitution of hydrogen; for bicyclic systems, one or more substituents may be attached to either ring in the bicyclic system, or Connect to both rings. For example, when n is 1, a single R 4 substituent can be connected to formula I or formula II at any position of the indicated 2, 3, 4, 5, 6 or 7 positions; and when n is 2, 2 Independent R4 substituents may be attached at positions 2,3; 2,4; 2,5; 2,6 or 2,7 or at any other combination of two positions. When R2 and R3 are joined with the nitrogen to which they are attached to form a ring, then the ring may be optionally substituted on any available carbon or optionally on any available nitrogen.

本发明的化合物可作为一种或多种立体异构体存在。所述各种立体异构体包括对映异构物、非对映异构体、阻转异构体和几何异构体。本领域技术人员将理解的是，当一种异构体相对于其它异构体为富集时或当与其它异构体分离时，其可以更为活泼和/或可以具有有利作用。另外，本领域技术人员知道如何对所述异构体进行分离、富化和/或选择性制备。本发明的化合物可以以异构体混合物、个体异构体、或以旋光形式体存在。The compounds of the invention may exist as one or more stereoisomers. The various stereoisomers include enantiomers, diastereomers, atropisomers and geometric isomers. Those skilled in the art will appreciate that one isomer may be more reactive and/or may have beneficial effects when it is enriched relative to the other isomer or when isolated from the other isomer. In addition, those skilled in the art know how to separate, enrich and/or selectively prepare said isomers. The compounds of the present invention may exist as mixtures of isomers, individual isomers, or in optically active forms.

本发明包括的化合物选自式I或式II、其N-氧化物和农业适用盐。本领域技术人员将理解的是，不是所有含氮杂环可以形成N-氧化物，这是因为氮需要可以利用的孤对电子来氧化成氧化物；本领域技术人员应能识别那些能形成N-氧化物的含氮杂环。本领域技术人员还应认识到叔胺可以形成N-氧化物。制备杂环和叔胺的氮氧化物的合成方法为本领域技术人员所熟知，包括用过氧酸(如过乙酸和间氯过苯甲酸(MCPBA))、过氧化氢、烷基过氧化氢(如过氧化氢叔丁基)、过硼酸钠和双环氧乙烷类(如二甲基双环氧乙烷)对杂环和叔胺进行氧化作用。在文献中对N-氧化物的这些制备方法已作了广泛描述和评论，参见例如：T.L.Gilchrist在Comprehensive Organic Synthesis(综合有机合成)第7卷第748-750页，S.V.Ley编辑，Pergamon出版社；M.Tisler和B.Stanovnik在Comprehensive Heterocyclic Chemistry(综合杂环化学)第3卷第18-19页，A.J.Boulton和A.McKillop编辑，Pergamon出版社；M.R.Grimmett和B.R.T.Keene在Advances inHeterocyclic Chemistry(杂环化学进展)第43卷第139-151页，A.R.Katritzky编辑，Academic出版社；M.Tisler和B.Stanovnik在Advancesin Heterocyclic Chemistry第9卷第285-291页，A.R.Katritzky和A.J.Boulton编辑，Academic出版社；以及G.W.H.Cheeseman和E.S.G.Werstiuk在Advances in Heterocyclic Chemistry第22卷第390-392页，A.R.Katritzky和A.J.Boulton编辑，Academic出版社。Compounds encompassed by the present invention are selected from formula I or formula II, N-oxides and agriculturally suitable salts thereof. Those skilled in the art will understand that not all nitrogen-containing heterocyclic rings can form N-oxides because nitrogen requires available lone pairs of electrons to oxidize to oxides; those skilled in the art should be able to identify those that can form N-oxides. - Nitrogen-containing heterocycles of oxides. Those skilled in the art will also recognize that tertiary amines can form N-oxides. Synthetic methods for the preparation of nitrogen oxides of heterocycles and tertiary amines are well known to those skilled in the art and include the use of peroxyacids such as peracetic acid and m-chloroperbenzoic acid (MCPBA), hydrogen peroxide, alkyl hydroperoxides (such as tert-butyl hydroperoxide), sodium perborate and dioxiranes (such as dimethyldioxirane) for the oxidation of heterocycles and tertiary amines. These preparations of N-oxides have been described and reviewed extensively in the literature, see for example: T.L. Gilchrist in Comprehensive Organic Synthesis (Comprehensive Organic Synthesis) Vol. 7 pp. 748-750, edited by S.V. Ley, Pergamon Press ; M.Tisler and B.Stanovnik in Comprehensive Heterocyclic Chemistry (Comprehensive Heterocyclic Chemistry) Volume 3 pp. 18-19, edited by A.J.Boulton and A.McKillop, Pergamon Press; Advances in Heterocyclic Chemistry) Vol. 43, pp. 139-151, edited by A.R. Katritzky, Academic Press; M. Tisler and B. Stanovnik in Advances in Heterocyclic Chemistry, Vol. 9, pp. 285-291, edited by A.R. Katritzky and A.J. Boulton, Academic Press and G.W.H. Cheeseman and E.S.G. Werstiuk in Advances in Heterocyclic Chemistry Vol. 22 pp. 390-392, edited by A.R. Katritzky and A.J. Boulton, Academic Press.

本发明化合物的盐包括与诸如氢溴酸、盐酸、硝酸、磷酸、硫酸、醋酸、丁酸、富马酸、乳酸、马来酸、丙二酸、草酸、丙酸、水杨酸、酒石酸、4-甲苯磺酸或戊酸的无机或有机酸的酸加成盐。Salts of compounds of the present invention include compounds such as hydrobromic acid, hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid, acetic acid, butyric acid, fumaric acid, lactic acid, maleic acid, malonic acid, oxalic acid, propionic acid, salicylic acid, tartaric acid, Acid addition salts of inorganic or organic acids of 4-toluenesulfonic acid or pentanoic acid.

为了包括使合成容易进行和/或更高的节足害虫沙虫效力的缘故，优选的是：优选1.式I化合物，其中For reasons including ease of synthesis and/or higher efficacy of arthropod sandworms, preferred are: Preferred 1. Compounds of formula I, wherein

  A和B均为0；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和n为0-2。优选2.式II化合物，其中Both A and B are 0; R 1 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and n is 0-2. Preferred 2. Compounds of formula II, wherein

    A和B均为0；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和n为0-2。优选3.优选1或优选2的化合物，其中J是苯基环或选自如下J-1、J-2、J-3和J-4的5元或6元杂芳环，每-J环任选地用1-3个R5取代

Figure A0180519000141
Q是O、S或NR5；W、X、Y和Z独立地是N或CR5，前提是在J-3和J-4中W、X、Y或Z至少之一是N；R2是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；R3是C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、C1-C2烷氧基、C1-C2烷基硫代、C1-C2烷基亚硫酰基和C1-C2烷基磺酰基；一个R4基团在2位或7位连接萘基环体系，且该R4是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基或C1-C4卤代烷基磺酰基；每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基，C3-C8二烷基氨基羰基；或每一R5独立地是苯基、苄基或5元或6元杂芳环，每一环任选地为下列的取代基取代：C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C2-C4卤代链烯基、C2-C4卤代炔基、C3-C6卤代环烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C3-C6(烷基)环烷基氨基、C2-C4烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基或C3-C6三烷基甲硅烷基；或(R5)2当与相邻碳原子连接时可以合在一起成为-OCF2O-、-CF2CF2O-或-OCF2CF2O-；和n为1-2。优选4.优选3的式I化合物，其中R2是H；R3是C1-C4烷基；和至少一个R5取代基与NR1C(＝B)部分邻位。优选5.优选4的化合物，其中R3是甲基。优选6.优选3的式II化合物，其中Both A and B are 0; R 1 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and n is 0-2. Preferred 3. The compound of preferred 1 or preferred 2, wherein J is a phenyl ring or a 5-membered or 6-membered heteroaromatic ring selected from the following J-1, J-2, J-3 and J-4, each -J ring Optionally substituted with 1-3 R 5
Figure A0180519000141
Q is O, S or NR 5 ; W, X, Y and Z are independently N or CR 5 , provided that at least one of W, X, Y or Z in J-3 and J-4 is N; R 2 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; R 3 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, each optionally one or A plurality of substituents selected from the group consisting of halogen, CN, C 1 -C 2 alkoxy, C 1 -C 2 alkylthio, C 1 -C 2 alkylsulfinyl and C 1 -C 2 alkane Sulfonyl; one R 4 group is connected to the naphthyl ring system at the 2-position or 7-position, and the R 4 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl or C 1 -C 4 haloalkylsulfonyl; each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl , C 3 -C 8 dialkylaminocarbonyl; or each R 5 is independently phenyl, benzyl, or a 5-membered or 6-membered heteroaryl ring, each ring optionally substituted by the following substituents: C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 2 -C 4 haloalkenyl , C 2 -C 4 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 - C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 - C 6 cycloalkylamino, C 3 -C 6 (alkyl) cycloalkylamino, C 2 -C 4 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylaminocarbonyl, C 3 -C 8 dialkylaminocarbonyl or C 3 -C 6 trialkylsilyl; or (R 5 ) 2 can be combined into -OCF 2 O-, -CF when connected to adjacent carbon atoms 2 CF 2 O- or -OCF 2 CF 2 O-; and n is 1-2. Preferred 4. Compounds of formula I according to Preferred 3, wherein R 2 is H; R 3 is C 1 -C 4 alkyl; and at least one R 5 substituent is ortho to the NR 1 C(=B) moiety. Preferred 5. The compound of Preferred 4, wherein R3 is methyl. Preferred 6. The compound of formula II of preferred 3, wherein

R1是H或C1-C4烷基；R 1 is H or C 1 -C 4 alkyl;

R2是H或C1-C4烷基；R 2 is H or C 1 -C 4 alkyl;

R3是任选地用卤素、CN、OCH3或S(O)pCH3取代的C1-C4烷基；一个R5基团在与C(＝B)NR1部分邻位的位置上与J相连，且该R5是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；C3-C8二烷基氨基羰基或苯基、苄基，或5元或6元杂芳环，每一环任选地为下列的取代基取代：卤素、CN、NO2、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C1-C4烷氧基或C1-C4卤代烷氧基；而任选的第二R5基团独立地是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；C3-C8二烷基氨基羰基或苯基、苄基，或5元或6元杂芳环，每一环任选地为下列的取代基取代：卤素、CN、NO2、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C1-C4烷氧基或C1-C4卤代烷氧基。优选7.优选6的化合物，其中J是苯基、吡唑、吡咯、吡啶或嘧啶，每一个均被在与C(＝B)NR1部分邻位的位置上与J相连的一个R5和第二个任选的R5取代。优选8.优选7的化合物，其中R1和R2均是H；一个R4在与NR1C(＝X)J部分邻位的7位上连接，并选自C1-C3烷基、CF3、OCF3、OCHF2、S(O)pCF3、S(O)pCHF2和卤素，而任选的第二R4在与NR1C(＝X)J部分对位的5位上连接，并选自卤素、C1-C3烷基和C1-C3卤代烷基。优选9.优选8的化合物，其中J是J-1；Q是NR5a；X是N或CH；Y是CH；Z是CR5b；R5a是用一个或两个选自卤素、C1-C4烷基、C1-C4卤代烷基或C1-C4卤代烷氧基所取代的苯基或2-吡啶基；和R5b是卤素或CF3。 R3 is C1 - C4alkyl optionally substituted with halogen, CN, OCH3 or S(O) pCH3 ; one R5 group is in a position ortho to the C(=B) NR1 moiety is connected to J, and the R 5 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy , C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylene Sulfonyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl; C 3 -C 8 dialkylaminocarbonyl or phenyl, benzyl, or a 5-membered or 6-membered heteroaromatic ring, Each ring is optionally substituted with the following substituents: halogen, CN, NO 2 , C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, or C 1 -C 4 haloalkoxy; and the optional second R 5 group is independently C 1 -C 4 alkyl , C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkane sulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl; C 3 -C 8 dialkylaminocarbonyl or phenyl, benzyl, or 5-membered or 6-membered heteroaromatic ring, each ring is optionally substituted by the following substituents: halogen, CN, NO 2 , C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 1 -C 4 Alkoxy or C 1 -C 4 haloalkoxy. Preferred 7. The compound of Preferred 6, wherein J is phenyl, pyrazole, pyrrole, pyridine or pyrimidine, each of which is connected to J in a position ortho to the C(=B)NR moiety and the second Two optional R 5 substitutions. Preferred 8. The compound of Preferred 7, wherein R 1 and R 2 are both H; one R 4 is attached at the 7-position ortho to the NR 1 C(=X)J moiety and is selected from C 1 -C 3 alkyl , CF 3 , OCF 3 , OCHF 2 , S(O) p CF 3 , S(O) p CHF 2 and halogen, while the optional second R 4 is in the para position to the NR 1 C(=X)J moiety 5-position, and selected from halogen, C 1 -C 3 alkyl and C 1 -C 3 haloalkyl. Preferred 9. The compound of Preferred 8, wherein J is J-1; Q is NR 5a ; X is N or CH; Y is CH; Z is CR 5b ; C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 haloalkoxy substituted phenyl or 2-pyridyl; and R 5b is halogen or CF 3 .

特别优选的化合物选自N-甲基-N′-(2-溴-4-氟苯基)-1，8-萘-二甲酰、N-甲基8-[(3，4-二氟苯基)羰基氨基]-1-萘甲酰和N-甲基8-[(2-噻吩基)羰基氨基]-1-萘甲酰。Particularly preferred compounds are selected from N-methyl-N'-(2-bromo-4-fluorophenyl)-1,8-naphthalene-diformyl, N-methyl 8-[(3,4-difluoro phenyl)carbonylamino]-1-naphthoyl and N-methyl 8-[(2-thienyl)carbonylamino]-1-naphthoyl.

本发明还涉及一种防治无脊椎动物的组合物，包含生物有效量的式I或式II化合物和至少一种选自表面活性剂、固体稀释剂和液体稀释剂的组分。本发明还涉及一种组合物，包含生物有效量的式I或式II化合物和有效量的至少一种附加生物活性化合物或试剂。优选的组合物含有优选1-9中优选的式I或式II化合物以及上述特别优选的化合物。The present invention also relates to a composition for controlling invertebrates, comprising a biologically effective amount of a compound of formula I or formula II and at least one component selected from surfactants, solid diluents and liquid diluents. The present invention also relates to a composition comprising a biologically effective amount of a compound of formula I or formula II and an effective amount of at least one additional biologically active compound or agent. Preferred compositions contain preferred compounds of formula I or formula II among preferred 1 to 9 as well as the abovementioned particularly preferred compounds.

本发明还涉及防治节肢动物的方法，包括使节肢动物或其环境与对于杀灭节肢动物有效的量的式I或式II化合物、其N-氧化物或农业适用盐(例如以含式I或式II化合物的组合物的形式)进行接触。本发明还涉及这样一种方法，其中，使无脊椎害虫或其环境与生物有效量的式I或式II化合物或含式I或式II化合物及生物有效量的至少一种附加化合物或试剂的组合物进行接触，以防治无脊椎害虫。优选的方法包括优选1-9中优选的式I或式II化合物以及上述特别优选的化合物。The present invention also relates to a method for preventing and controlling arthropods, comprising making the arthropods or their environment with the compound of formula I or formula II, its N-oxide or an agriculturally suitable salt (for example, in a compound containing formula I or in the form of a composition of a compound of formula II). The present invention also relates to a method wherein the invertebrate pest or its environment is mixed with a biologically effective amount of a compound of formula I or formula II or a compound containing a compound of formula I or formula II and a biologically effective amount of at least one additional compound or agent The composition is contacted to control invertebrate pests. Preferred methods include the preferred compounds of formula I or formula II among preferred 1-9 as well as the particularly preferred compounds mentioned above.

重要的是某些下列的式Ih和式IIc化合物，包括其所有的几何和立体异构体及农业适用盐：其中：A和B独立地是O或S；m为1-5；n为0-4；R1是H；或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基和C3-C6环烷基氨基；或者R1是C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基或C3-C8二烷基氨基羰基；R2是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C4烷氧基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷氧基羰基或C2-C6烷基羰基；R3是H；或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基和C1-C4烷基磺酰基；或者R2和R3可通过与它们相连的氮而在一起形成环，该环含2-6个碳原子并任选地含有一个另外的氮、硫或氧原子，该环可任选地被选自C1-C2烷基、卤素、CN、NO2和C1-C2烷氧基的1-4个取代基取代；和每一R4和每一R5独立地是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C6卤代烷基、C2-C6卤代链烯基、C2-C6卤代炔基、C3-C6卤代环烷基、卤素、CN、CO2H、CONH2、NO2、羟基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基、或C3-C6三烷基甲硅烷基；或者每一R4和每一R5独立地是任选地为下列取代基取代的苯基：C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C2-C4卤代链烯基、C2-C4卤代炔基、C3-C6卤代环烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C3-C6(烷基)环烷基氨基、C2-C4烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基或C3-C6三烷基甲硅烷基。Important are certain of the following compounds of formula Ih and formula IIc, including all geometric and stereoisomers and agriculturally suitable salts thereof: Wherein: A and B are independently O or S; m is 1-5; n is 0-4; R 1 is H; or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 - C 6 alkynyl or C 3 -C 6 cycloalkyl, each optionally substituted by one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino and C 3 -C 6 cycloalkylamino; or R 1 is C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylamino Carbonyl or C 3 -C 8 dialkylaminocarbonyl; R 2 is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkane radical, C 1 -C 4 alkoxy, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkoxycarbonyl or C 2 -C 6 alkylcarbonyl; R 3 is H; or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, each Optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkane sulfinyl and C 1 -C 4 alkylsulfonyl; or R 2 and R 3 may be joined together through the nitrogen to which they are attached to form a ring containing 2 to 6 carbon atoms and optionally containing an additional Nitrogen, sulfur or oxygen atom, the ring can be optionally substituted by 1-4 substituents selected from C 1 -C 2 alkyl, halogen, CN, NO 2 and C 1 -C 2 alkoxy; and Each R 4 and each R 5 is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 6 haloalkenyl, C 2 -C 6 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, CO 2 H, CONH 2 , NO 2. Hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkyl Sulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 alkane C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylamino carbonyl, C 3 -C 8 dialkylaminocarbonyl, or C 3 -C 6 trialkylsilyl; or each R 4 and each R 5 is independently phenyl optionally substituted with the following substituents : C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 2 -C 4 halo Alkenyl, C 2 -C 4 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 3 -C 6 (alkyl) cycloalkylamino, C 2 -C 4 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkyl Aminocarbonyl, C 3 -C 8 dialkylaminocarbonyl or C 3 -C 6 trialkylsilyl.

同样重要的是杀灭节肢害虫的组合物，包含对于杀灭节肢害虫有效的量的上述式Ih或式IIc化合物及至少一种选自表面活性剂、固体稀释剂或液体稀释剂的组分。Equally important is a composition for killing arthropod pests, comprising the above-mentioned compound of formula Ih or formula IIc in an effective amount for killing arthropod pests and at least one component selected from surfactants, solid diluents or liquid diluents.

本发明还涉及防治节肢动物的方法，包括使节肢动物或其环境与对于杀灭节肢动物有效的量的上述式Ih或式IIc化合物进行接触。The present invention also relates to a method for controlling arthropods, comprising contacting the arthropods or their environment with the above-mentioned compound of formula Ih or IIc in an amount effective for killing arthropods.

部分1.重要的是式Ih的经选择的化合物，其中Part 1. Importantly are selected compounds of formula Ih, wherein

A和B均为0；Both A and B are 0;

m为1-3；m is 1-3;

n为0-2；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和每一R4和每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基。n is 0-2; R 1 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 Alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and each R 4 and each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 Haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 Haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl.

部分2.重要的是部分1的经选择的化合物，其中Part 2. Importantly, selected compounds of part 1, wherein

R2是H； R2 is H;

R3是C1-C4烷基；每一R4和每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；和至少一个R5取代基是在酰胺键的邻位；部分3.重要的是部分2的经选择的化合物，其中R3是甲基。部分4.重要的是式IIc的经选择的化合物，其中R 3 is C 1 -C 4 alkyl; each R 4 and each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 - C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl, or C 2 -C 4 alkoxycarbonyl; and at least one R substituent is on the amide bond ortho position; part 3. Importantly are selected compounds of part 2, wherein R 3 is methyl. Part 4. Importantly are selected compounds of formula IIc, wherein

A和B均未0；Neither A nor B is 0;

m为1-3；m is 1-3;

n为0-2；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和每一R4和每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基。部分5.重要的是部分4的经选择的化合物，其中n is 0-2; R 1 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 Alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and each R 4 and each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2. C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl , C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl. Part 5. Importantly, selected compounds of part 4, wherein

R2是H； R2 is H;

R6是任选地为C1-C4烷氧基或C1-C4烷基硫代取代的C1-C6烷基；每一R4和每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；和至少一个R5取代基是在酰胺键的邻位。R 6 is C 1 -C 6 alkyl optionally substituted by C 1 -C 4 alkoxy or C 1 -C 4 alkylthio; each R 4 and each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 Alkylsulfinyl, C 1 -C 4 Alkylsulfonyl, C 1 -C 4 Haloalkylthio, C 1 -C 4 Haloalkylsulfinyl, C 1 -C 4 Haloalkylsulfonyl acyl or C 2 -C 4 alkoxycarbonyl; and at least one R 5 substituent is in the ortho position to the amide bond.

如上所指出的，每一J独立地是苯基环、萘基环体系、5或6元杂芳环或芳香8、9或10元杂双环稠环体系，其中，每一环或环体系任选地是用1-5个R5取代的。与这些J基团相关联的术语“任选地取代”是指未被取代的基团或具有至少一个非氢取代基，其不使未取代的类似物所具有的杀灭节肢害虫的活性消失。任选地用1-5个R5取代的苯基的例子是在陈列1中以U-1表示的环，其中Rv是R5，而r为1-5的整数。任选地用1-5个R5取代的萘基的例子是在陈列1中以U-85表示的环，其中Rv是R5，而r为1-5的整数。任选地用1-5个R5取代的5元或6元杂芳环的例子包括在陈列1中U-2至U-53表示的环，其中Rv是R5，而r为1-5的整数。注意下述J-1至J-4也表示5元或6元杂芳环。注意U-2至U-20是J-1的例子，U-21至U-35以及U-40是J-2的例子，U-41至U-48是J-3的例子，而U-49至U-53是J-4的例子。任选地以1-4个R3取代的芳香8、9或10元杂双环稠环体系的例子包括陈列1中图示的U-54至U-84，其中Rv是R5，而r为1-5的整数。As noted above, each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring, or an aromatic 8-, 9-, or 10-membered heterobicyclic fused ring system, wherein each ring or ring system is either is optionally substituted with 1-5 R5. The term "optionally substituted" associated with these J groups refers to an unsubstituted group or having at least one non-hydrogen substituent which does not abolish the arthropodicidal activity of the unsubstituted analog . An example of phenyl optionally substituted with 1-5 R5 is the ring represented by U-1 in Scheme 1, wherein Rv is R5 and r is an integer of 1-5. An example of naphthyl optionally substituted with 1-5 R5 is the ring represented by U-85 in Scheme 1, wherein Rv is R5 and r is an integer of 1-5. Examples of 5-membered or 6-membered heteroaryl rings optionally substituted with 1-5 R5 include rings represented by U-2 to U-53 in Listing 1, wherein Rv is R5 , and r is 1- Integer of 5. Note that the following J-1 to J-4 also represent a 5-membered or 6-membered heteroaromatic ring. Note that U-2 through U-20 are examples of J-1, U-21 through U-35 and U-40 are examples of J-2, U-41 through U-48 are examples of J-3, and U- 49 through U-53 are examples of J-4. Examples of aromatic 8-, 9- or 10-membered heterobicyclic fused ring systems optionally substituted with 1-4 R 3 include U-54 to U-84 illustrated in Scheme 1, wherein R v is R 5 , and r It is an integer of 1-5.

尽管Rv基团出现在U-1至U-85的结构中，但应注意的是它们不是必须存在，这是因为它们是任选的取代基。应注意的是，当与原子相连时Rv是H时，其等同于好像该原子未被取代。需要通过取代来填充其化合价的氮原子用H或Rv进行取代。应注意的是，一些U基团只能用少于5个的Rv基团进行取代(例如U-14、U-15、U-18至U-21和U-32至U-34只能用一个Rv进行取代)。应注意的是，当(Rv)r和U基团间的连接点被表示为不固定时，(Rv)r可与U基团上任何可以使用的碳原子连接。应注意的是，当U基团上的连接点被表示为不固定时，U基团可通过取代氢原子而与式I的其余部分通过U基团上任何可供使用的碳进行连接。Although R v groups occur in the structures U-1 to U-85, it should be noted that they do not have to be present as they are optional substituents. It should be noted that when R v is H when attached to an atom, it is equivalent as if the atom were unsubstituted. Nitrogen atoms that require substitution to fill their valences are substituted with H or R v . It should be noted that some U groups can only be substituted with fewer than 5 R groups (e.g. U-14, U-15, U-18 to U-21 and U-32 to U-34 can only Substitution with an Rv ). It should be noted that when the point of attachment between (R v ) r and the U group is indicated as not fixed, (R v ) r may be attached to any available carbon atom on the U group. It should be noted that when the point of attachment on the U group is indicated as not fixed, the U group can be linked to the remainder of Formula I by substituting a hydrogen atom through any available carbon on the U group.

                      陈列1

Figure A0180519000231
Figure A0180519000241
display 1
Figure A0180519000231
Figure A0180519000241

式I和式II的化合物可通过如反应方案1-21所描述的下述一种或多种方法或变更方法进行制备。在下述反应方案中所述的R1、R2、R3、R4、A、B、m和n的定义如在上述发明概述或其附属部分中所定义。Compounds of Formula I and Formula II can be prepared by one or more of the following methods or variations thereof as depicted in Reaction Schemes 1-21. The definitions of R 1 , R 2 , R 3 , R 4 , A, B, m and n described in the following reaction schemes are as defined in the above Summary of the Invention or its subsections.

式I的化合物可通过反应方案1-9所概述的程序进行制备。式Ia-h的化合物为式I化合物的各种子集。Compounds of formula I can be prepared by the procedures outlined in Reaction Schemes 1-9. Compounds of formula la-h are various subsets of compounds of formula I.

典型程序描述于反应方案1中，并涉及在碱存在或不存在的情况下式2的异萘亚甲基酰亚胺(isonaphthalimide)与式3的胺的连接或式4的化合物与式5的胺的连接。典型的碱包括胺碱，如三乙胺、二异丙基乙胺和吡啶。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。式3和式5的胺类是市售的、在化学文献中已充分描述的，或是由已确立的文献步骤易于得到的。利用各种的标准硫代转移剂包括五硫化磷和Lawesson试剂，可将式Ia的酰胺转化为式Ib的硫代酰胺。A typical procedure is described in Reaction Scheme 1 and involves the attachment of an isonaphthalimide of formula 2 to an amine of formula 3 or a compound of formula 4 to an amine of formula 5 in the presence or absence of a base. Amine linkage. Typical bases include amine bases such as triethylamine, diisopropylethylamine and pyridine. In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Amines of Formula 3 and Formula 5 are either commercially available, well described in the chemical literature, or readily available from established literature procedures. Amides of formula Ia can be converted to thioamides of formula Ib using a variety of standard thiotransfer reagents including phosphorus pentasulfide and Lawesson's reagent.

                     反应方案1

Figure A0180519000251
Reaction Scheme 1
Figure A0180519000251

式2和式4的化合物通常是通过将式6的1，8-萘酰氯(1，8-naphthaloyl chloride)分别与式7的胺或式8的胺连接而制备的(反应方案2)。典型的除酸剂包括胺碱，如三乙胺、二异丙基乙胺和吡啶。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。在一些情况下，式7的胺当过量使用时可用作除酸剂。式6的1，8-萘酰氯化合物已在化学文献中进行了充分描述，并通常是由相应的1，8-萘二甲酸或酸酐、使用通常用于羧酸到羧酰氯(carboxylic acid chloride)的转换的氯化试剂制备的。这些通常使用的氯化试剂包括氯氧化磷和五氯化磷。Compounds of formula 2 and formula 4 are generally prepared by linking 1,8-naphthaloyl chloride of formula 6 with an amine of formula 7 or amine of formula 8, respectively (reaction scheme 2). Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. In some cases, the amines of formula 7 can be used as acid scavengers when used in excess. The 1,8-naphthoyl chloride compounds of formula 6 are well described in the chemical literature and are generally prepared from the corresponding 1,8-naphthalene dicarboxylic acid or anhydride, using the compounds commonly used for carboxylic acids to carboxylic acid chlorides. The conversion of the chlorination reagent prepared. These commonly used chlorinating agents include phosphorus oxychloride and phosphorus pentachloride.

                   反应方案2

Figure A0180519000261
Reaction scheme 2
Figure A0180519000261

一个供选择的制备式2和式4化合物的程序分别涉及式9和式10的8-氨基羰基-1-萘甲酸的环化作用(反应方案3)，它是利用脱水试剂、在惰性溶剂中、-30至30℃的温度范围内、除酸剂存在或不存在的情况下进行的。典型的脱水试剂包括二环己基碳二亚胺和三氟醋酸酐。聚合物支持的试剂如聚合物结合的二环己基碳二亚胺是有用的。典型的除酸剂包括胺碱，如三乙胺、二异丙基乙胺和吡啶。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。典型的惰性试剂包括非质子溶剂，如二氯甲烷和1-氯丁烷。典型反应稳定范围为-5至25℃。An alternative procedure for the preparation of compounds of formula 2 and formula 4 involves the cyclization (Scheme 3) of 8-aminocarbonyl-1-naphthoic acids of formula 9 and formula 10, respectively, by utilizing a dehydrating reagent in an inert solvent , in the temperature range of -30 to 30°C, in the presence or absence of acid scavengers. Typical dehydrating agents include dicyclohexylcarbodiimide and trifluoroacetic anhydride. Polymer supported reagents such as polymer bound dicyclohexylcarbodiimide are useful. Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Typical inert reagents include aprotic solvents such as dichloromethane and 1-chlorobutane. Typical reaction stability ranges from -5 to 25°C.

                   反应方案3

Figure A0180519000271
Reaction Scheme 3
Figure A0180519000271

式9和式10的8-氨基羰基-1-萘甲酸的制备涉及在惰性溶剂中、0-30℃的温度范围内，使式11的1，8-萘二甲酸酐分别与式7的胺或式8的胺连接(反应方案4)。典型的惰性试剂是二甲基甲酰胺。反应通常是在5-10℃的稳定范围内进行。The preparation of 8-aminocarbonyl-1-naphthoic acid of formula 9 and formula 10 involves in an inert solvent, in the temperature range of 0-30 ℃, makes the 1,8-naphthalene dicarboxylic anhydride of formula 11 and the amine of formula 7 respectively or amine linkage of formula 8 (Scheme 4). A typical inert reagent is dimethylformamide. The reaction is usually carried out in a stable range of 5-10°C.

                 反应方案4 Reaction scheme 4

一个供选择的制备式9和式10的8-氨基羰基-1-萘甲酸的程序分别涉及式12和式13的1，8-萘亚甲基酰亚胺的水解(反应方案5)，该水解利用氢氧化物如氢氧化钠或氢氧化钾，在质子溶剂体系如水-甲醇或水-二恶烷中、在高温下进行。该反应通常是在反应混合物的回流温度下进行。式12和式13的1，8-萘亚甲基酰亚胺化合物通常是如下制备的：即通常在酸的存在下，在高温下使式11的1，8-萘二甲酸酐分别与式7或式8的胺缩合。典型反应涉及使式11的1，8-萘二甲酸酐和式7或式8的胺在醋酸中进行回流。An alternative procedure for the preparation of 8-aminocarbonyl-1-naphthoic acids of formulas 9 and 10 involves the hydrolysis of 1,8-naphthylidene imides of formulas 12 and 13, respectively (Scheme 5), which The hydrolysis is carried out using hydroxides such as sodium hydroxide or potassium hydroxide in protic solvent systems such as water-methanol or water-dioxane at elevated temperature. The reaction is usually carried out at the reflux temperature of the reaction mixture. 1,8-naphthalene imide compounds of formula 12 and formula 13 are usually prepared as follows: that is, usually in the presence of an acid, 1,8-naphthalene dicarboxylic anhydride of formula 11 is respectively mixed with formula 7 or the amine condensation of formula 8. A typical reaction involves refluxing 1,8-naphthalic anhydride of formula 11 and an amine of formula 7 or 8 in acetic acid.

                    反应方案5 Reaction scheme 5

一个供选择的制备式I化合物的程序涉及在除酸剂的存在下使式14和式15的8-氨基羰基-1-萘甲酰氯分别与式3的胺或式5的胺连接(反应方案6)。典型的除酸剂包括胺碱，如三乙胺、二异丙基乙胺和吡啶。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。通常反应温度范围为0-25℃。An alternative procedure for the preparation of compounds of formula I involves linking 8-aminocarbonyl-1-naphthoyl chlorides of formulas 14 and 15 to amines of formula 3 or 5, respectively, in the presence of acid scavengers (Reaction Scheme 6). Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Usually the reaction temperature ranges from 0 to 25°C.

由在除酸剂的存在下使相应的式6的1，8-萘甲酰二氯(1，8-naphthaloyl dichloride)分别与式5或式3的胺进行连接，可以得到式14和式15的8-氨基羰基-1-萘甲酰氯(反应方案7)。典型的除酸剂包括胺碱，如三乙胺、二异丙基乙胺和吡啶。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。By making corresponding formula 6 1,8-naphthaloyl dichloride (1,8-naphthaloyl dichloride) connect with the amine of formula 5 or formula 3 in the presence of acid scavenger, formula 14 and formula 15 can be obtained 8-Aminocarbonyl-1-naphthoyl chloride (Scheme 7). Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine. In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine.

                     反应方案6 Reaction scheme 6

                  反应方案7 制备式I化合物的另一程序涉及式20的萘的分步进行的甲氨酰化或硫代甲氨酰化(反应方案8和9)。在弗瑞德-克来福特反应的条件下用路易斯酸进行处理时，式16或式17的1-萘甲酰胺或1-萘硫代甲酰胺(1-naphthalenethiocarboxamide)与式18或式19的氨基甲酰氯或硫代氨基甲酰氯连接，提供式I的化合物(反应方案8)。常用的路易斯酸包括氯化氯和氯化锡。 Reaction Scheme 7 Another procedure for the preparation of compounds of formula I involves the stepwise carbamylation or thiocarbamylation of naphthalenes of formula 20 (Schemes 8 and 9). When treating with Lewis acid under the conditions of Friedel-Crafts reaction, 1-naphthalenecarboxamide or 1-naphthalenethiocarboxamide of formula 16 or formula 17 and 1-naphthalenethiocarboxamide of formula 18 or formula 19 Carbamoyl chloride or thiocarbamoyl chloride linkage provides compounds of formula I (Scheme 8). Commonly used Lewis acids include chlorine chloride and tin chloride.

式16或式17的1-萘甲酰胺或1-萘硫代甲酰胺的制备(反应方案9)涉及在弗瑞德-克来福特反应的条件下、在路易斯酸如氯化氯和氯化锡存在下，使式20的萘分别与式19或式18的氨基甲酰氯或硫代氨基甲酰氯进行连接。式20的萘、式18和式19的氨基甲酰氯或硫代氨基甲酰氯均为市售可得，在化学文献中已充分进行了描述，或者遵照已确立的文献程序进行制备。The preparation of 1-naphthylcarboxamide or 1-naphthalenethiocarboxamide of formula 16 or formula 17 (reaction scheme 9) involves under the conditions of the Friedel-Crafts reaction, in Lewis acids such as chlorine chloride and chlorination Naphthalene of formula 20 is linked to carbamoyl chloride or thiocarbamoyl chloride of formula 19 or 18, respectively, in the presence of tin. Naphthalene of formula 20, carbamoyl chlorides or thiocarbamoyl chlorides of formula 18 and 19 are all commercially available, well described in the chemical literature, or prepared following established literature procedures.

                      反应方案8

Figure A0180519000301
Reaction Scheme 8
Figure A0180519000301

                      反应方案9 Reaction scheme 9

式II的化合物可通过下述反应方案10-13中所描述的方法或改变方案中的一种或多种制备。式IIa-b的化合物是式II化合物的子集。Compounds of formula II can be prepared by one or more of the methods described in Reaction Schemes 10-13 below, or modifications thereof. Compounds of formula Ila-b are a subset of compounds of formula II.

典型程序描述于反应方案10中并涉及使式21的8-氨基-萘-1-氨甲酰在除酸剂的存在下与式22的碳酰氯进行连接，以提供式IIa的化合物，或者在芳烃硒醇盐(areneselenolate)的存在下与式22的硫代碳酰氯进行连接，以提供式IIb的化合物。典型的除酸剂包括胺碱，如三乙胺、二异丙基乙胺和吡啶，其它除酸剂包括氢氧化物如氢氧化钠和氢氧化钾，以及碳酸盐如碳酸钠和碳酸钾。在某些情况下，使用聚合物支持的除酸剂如聚合物结合的二异丙基乙胺和聚合物结合的二甲基氨基吡啶是有用的。典型的芳烃硒醇盐包括芳烃硒醇钠。式22的碳酰氯和硫代碳酰氯为市售可得，在化学文献中已充分进行了描述，或者遵照已确立的文献程序易于进行制备。利用标准硫代转移剂如五硫化磷和Lawesson试剂可将式IIa的酰胺转化为IIb的硫代酰胺。A typical procedure is depicted in Reaction Scheme 10 and involves coupling 8-amino-naphthalene-1-carbamoyl of formula 21 with phosgene of formula 22 in the presence of an acid scavenger to provide a compound of formula Ha, or Ligation with thiocarbonyl chloride of formula 22 in the presence of areneselenolate provides compounds of formula lib. Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine, and pyridine, others include hydroxides such as sodium hydroxide and potassium hydroxide, and carbonates such as sodium carbonate and potassium carbonate . In some cases, it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine. Typical arene selenides include sodium arene selenides. The phosgene and thiocarbonyl chlorides of formula 22 are commercially available, well described in the chemical literature, or readily prepared following established literature procedures. Amides of formula IIa can be converted to thioamides of lib using standard thiotransfer reagents such as phosphorus pentasulfide and Lawesson's reagent.

                   反应方案10 Reaction scheme 10

制备式IIa化合物的另一程序涉及在脱水试剂如二环己基碳二亚胺(DCC)的存在下使式21的1-氨基-萘-8-氨甲酰或1-氨基-萘-8-硫代氨甲酰与式23的羧酸进行连接。聚合物支持的试剂如聚合物结合的二环己基碳二亚胺是有用的。式23的苯甲酸为市售可得，在化学文献中已充分进行了描述，或者遵照已确立的文献程序易于进行制备。因为用于制备氨甲酰的文献很广泛，所以反应方案10和反应方案11的程序仅为制备式II化合物的有用方法的代表性例子。Another procedure for the preparation of compounds of formula IIa involves reacting 1-amino-naphthalene-8-carbamoyl or 1-amino-naphthalene-8-carbamoyl of formula 21 in the presence of a dehydrating reagent such as dicyclohexylcarbodiimide (DCC). Thiocarbamyl is linked to the carboxylic acid of formula 23. Polymer supported reagents such as polymer bound dicyclohexylcarbodiimide are useful. Benzoic acids of formula 23 are commercially available, well described in the chemical literature, or readily prepared following established literature procedures. Because the literature for the preparation of carboxamides is extensive, the procedures in Reaction Scheme 10 and Reaction Scheme 11 are only representative examples of useful methods for preparing compounds of formula II.

                   反应方案11

Figure A0180519000321
Reaction Scheme 11
Figure A0180519000321

式21a的8-氨基-萘-1-氨甲酰或8-氨基-萘-1-硫代氨甲酰通常是通过还原硝基基团而分别由式24的相应的8-硝基-萘-1-氨甲酰和8-硝基-萘-1-硫代氨甲酰得到的。典型程序涉及在碳或氧化铂上的金属催化剂如钯的存在下、在羟基溶剂如乙醇和异丙醇中用氢进行的还原作用。这些方法已在化学文献中作了充分记载。通过已知的方法，包括直接烷基化或通过通常优选的胺的还原烷基化，可通常在这一阶段引入R1取代基如烷基、取代烷基等。通常使用的方法是在还原剂如氰基氢硼化钠的存在下，使氨基萘21a与醛结合，以产生式21的化合物，其中R1不是H。8-Amino-naphthalene-1-carbamoyl or 8-amino-naphthalene-1-thiocarbamoyl of formula 21a is usually prepared from the corresponding 8-nitro-naphthalene of formula 24 by reducing the nitro group -1-carbamoyl and 8-nitro-naphthalene-1-thiocarbamoyl. Typical procedures involve reductions with hydrogen in hydroxylic solvents such as ethanol and isopropanol in the presence of metal catalysts such as palladium on carbon or platinum oxide. These methods are well documented in the chemical literature. R1 substituents such as alkyl, substituted alkyl, etc. can typically be introduced at this stage by known methods including direct alkylation or by reductive alkylation of amines which is often preferred. A commonly used approach is to combine aminonaphthalene 21a with an aldehyde in the presence of a reducing agent such as sodium cyanoborohydride to yield compounds of formula 21, where R is other than H.

                    反应方案12

Figure A0180519000322
Reaction scheme 12
Figure A0180519000322

由8-硝基-萘-1-甲酸易于制备式24的中间酰胺，8-硝基-萘-1-甲酸为市售、文献中已知，或通过已在文献中确立的、用于萘或通用于芳组的衍生作用而制备。形成酰胺的典型方法在此可以使用。这些包括式25的酸和式5的胺利用例如DCC进行的脱水连接，以及使酸转化为活性形式如酰基氯或酸酐，随后与胺连接，形成式24a的酰胺。另外，氰基膦酸二乙酯是用于这类涉及酸活化作用的有用试剂。对于这类反应，化学文献很充分。利用市售硫代转移剂如五硫化磷和Lawesson试剂，式24a的酰胺易于转化为式24b的硫代酰胺。Intermediate amides of formula 24 are readily prepared from 8-nitro-naphthalene-1-carboxylic acid, which is commercially available, known in the literature, or through established literature for naphthalene Or it can be prepared by the derivatization of aromatic groups. Typical methods of amide formation can be used here. These include the dehydrative linkage of an acid of formula 25 and an amine of formula 5 using, for example, DCC, and conversion of the acid to a reactive form such as an acid chloride or anhydride, followed by coupling with the amine to form an amide of formula 24a. Additionally, diethyl cyanophosphonate is a useful reagent for such activations involving acids. The chemical literature is plentiful for such reactions. Amides of formula 24a are readily converted to thioamides of formula 24b using commercially available thiotransfer reagents such as phosphorus pentasulfide and Lawesson's reagent.

                   反应方案13

Figure A0180519000331
Reaction Scheme 13
Figure A0180519000331

式23a的苯甲酸(式23的化合物，其中J任选地被取代的苯基环)在本领域中是众所周知的。式4的某些杂环酸的制备描述于反应方案14-21中。各种杂环酸及其通常合成方法可见于WO 98/57397中。Benzoic acids of formula 23a (compounds of formula 23 wherein J is an optionally substituted phenyl ring) are well known in the art. The preparation of certain heterocyclic acids of Formula 4 is described in Reaction Schemes 14-21. Various heterocyclic acids and their general synthesis can be found in WO 98/57397.

反应方案14描述了具有代表性的吡啶酸(23b)的合成。所述方法涉及已知的由β-酮酸酯和4-氨基丁烯酮(29)合成吡啶。取代基R5(c)和R5(d)包括例如烷基和卤代烷基。Reaction Scheme 14 describes the synthesis of a representative picolinic acid (23b). The method involves the known synthesis of pyridines from β-ketoesters and 4-aminobutenone (29). Substituents R 5 (c) and R 5 (d) include, for example, alkyl and haloalkyl.

                   反应方案14 Reaction Scheme 14

反应方案15描述了具有代表性的嘧啶酸(23c)的合成。所述方法涉及已知的由亚乙烯基-β-酮酸酯(33)和脒(34)合成嘧啶。取代基R5(c)和R5(d)包括例如烷基和卤代烷基。Reaction Scheme 15 describes the synthesis of a representative pyrimidine acid (23c). The method involves the known synthesis of pyrimidines from vinylidene-β-ketoesters (33) and amidines (34). Substituents R 5 (c) and R 5 (d) include, for example, alkyl and haloalkyl.

                   反应方案15

Figure A0180519000341
Reaction Scheme 15
Figure A0180519000341

反应方案16-21描述了具有代表性的吡唑酸(23d)的合成。反应方案16中23d的合成的关键步骤涉及通过吡唑的芳基化或烷基化引入R5(c)取代基。芳基化剂或烷基化剂R5(c)-Lg(其中Lg是离去基团，如Cl、Br、I，磺酸根如对甲苯磺酸根或甲磺酸根，或硫酸根如-SO2OR5(c))包括R5(c)基团，如C1-C6烷基、C2-C6链烯基、C2-C6炔基、C2-C6烷基羰基、C2-C6烷氧基羰基、C3-C8二烷基氨基羰基、C3-C6三烷基甲硅烷基；或苯基、苄基、苯甲酰基、每一环或环体系被任选地取代的5元或6元杂芳环。甲基基团的氧化作用产生吡唑羧酸。一些更优选的R5(d)基团包括硫代烷基。Reaction Schemes 16-21 describe the synthesis of representative pyrazole acids (23d). A key step in the synthesis of 23d in Scheme 16 involves the introduction of the R5 (c) substituent by arylation or alkylation of the pyrazole. Arylating agent or alkylating agent R 5 (c)-Lg (where Lg is a leaving group such as Cl, Br, I, a sulfonate such as p-toluenesulfonate or methanesulfonate, or a sulfate such as -SO 2 OR 5 (c)) includes R 5 (c) groups such as C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 2 -C 6 alkylcarbonyl , C 2 -C 6 alkoxycarbonyl, C 3 -C 8 dialkylaminocarbonyl, C 3 -C 6 trialkylsilyl; or phenyl, benzyl, benzoyl, each ring or ring The system is an optionally substituted 5-membered or 6-membered heteroaromatic ring. Oxidation of the methyl group yields pyrazole carboxylic acid. Some more preferred R5 (d) groups include thioalkyl groups.

                   反应方案16 Reaction Scheme 16

反应方案17描述了式23d的吡唑的合成。这些酸可以如下合成：通过利用二异丙基酰胺锂(LDA)使式40的化合物金属化，然后通过用二氧化碳使锂盐骤冷，产生了利用二异丙基酰胺锂(LDA)的金属化作用，式40化合物的羧化作用是关键步骤。R5(c)基团的引入类似于反应方案16中的方式，即通过用式37的化合物进行烷基化或芳基化。具代表性的R5(d)基团包括例如氰基、硫代烷基和卤素。Reaction Scheme 17 describes the synthesis of pyrazoles of formula 23d. These acids can be synthesized by metallation of the compound of formula 40 with lithium diisopropylamide (LDA), followed by quenching of the lithium salt with carbon dioxide, resulting in metallation with lithium diisopropylamide (LDA). The carboxylation of the compound of formula 40 is a key step. The introduction of the R5 (c) group is similar to that in Reaction Scheme 16, ie by alkylation or arylation with compounds of formula 37. Representative R5 (d) groups include, for example, cyano, thioalkyl and halo.

                   反应方案17 Reaction Scheme 17

如反应方案18所示，所述方法对于制备式23e的1-(2-吡啶基)吡唑羧酸尤其有用。式39的吡唑与式37a的2，3-二卤代吡啶反应，产生具有良好产率的式40a的1-吡啶基吡唑，其具有良好的所需区域化学特性。如上所述的式40a化合物的金属化和羧化产生式23e的1-(2-吡啶基)吡唑羧酸。As shown in Reaction Scheme 18, the method is particularly useful for the preparation of 1-(2-pyridyl)pyrazolecarboxylic acids of formula 23e. Reaction of pyrazoles of formula 39 with 2,3-dihalopyridines of formula 37a gives good yields of 1-pyridylpyrazoles of formula 40a with good desired regiochemistry. Metallation and carboxylation of compounds of formula 40a as described above yields 1-(2-pyridyl)pyrazolecarboxylic acids of formula 23e.

                  反应方案18 Reaction Scheme 18

反应方案19描述了式4c的吡唑的合成。它们可通过式41的任选被取代的苯基肼与式42的酮基丙酮酸盐反应生成式43的吡唑酯而制备。所述酯的水解产生式23d的吡唑酸。此方法对于制备其中的R5(c)是任选被取代的苯基而R5(d)是卤代烷基的化合物尤其有用。Reaction Scheme 19 describes the synthesis of pyrazoles of formula 4c. They can be prepared by reacting optionally substituted phenylhydrazines of formula 41 with ketopyruvates of formula 42 to give pyrazole esters of formula 43. Hydrolysis of the ester yields pyrazole acids of formula 23d. This method is especially useful for preparing compounds wherein R5 (c) is optionally substituted phenyl and R5 (d) is haloalkyl.

                     反应方案19

Figure A0180519000362
Reaction Scheme 19
Figure A0180519000362

反应方案20描述了式23d的吡唑酸的另一供选择的合成方法。它们可通过适当取代的ntrilimine与式45的取代丙炔酸酯或式47的丙烯酸酯的3+2环加成而制备。与丙烯酸酯的环加成需要附加的氧化作用，使中间体安替吡啉氧化为吡唑。酯水解产生式23d的吡唑酸。用于此反应的优选偕卤代亚胺包括式48的三氟甲基偕氯代亚胺和式49的偕二溴代亚胺(iminodibromide)。化合物如48是已知的(J.Heterocycl.Chem.1985，22(2)，565-8)。化合物如49可通过已知方法获得(TetrahedronLetters 1999，40，2605)。此方法对于制备其中的R5(c)是任选被取代的苯基而R5(d)是卤代烷基或溴的化合物尤其有用。Reaction Scheme 20 depicts an alternative synthesis of pyrazole acids of formula 23d. They can be prepared by 3+2 cycloaddition of appropriately substituted ntrilimines to substituted propiolates of formula 45 or acrylates of formula 47. Cycloaddition to acrylates requires additional oxidation to oxidize the intermediate antipyridine to pyrazole. Ester hydrolysis yields pyrazole acids of formula 23d. Preferred gem-haloimides for this reaction include trifluoromethyl gem-chloroimines of formula 48 and gem-iminodibromides of formula 49. Compounds such as 48 are known (J. Heterocycl. Chem. 1985, 22(2), 565-8). Compounds such as 49 can be obtained by known methods (Tetrahedron Letters 1999, 40, 2605). This method is especially useful for preparing compounds wherein R5 (c) is optionally substituted phenyl and R5 (d) is haloalkyl or bromo.

                     反应方案20 式39的起始吡唑是已知的化合物。式39a的吡唑(式39的化合物，其中R5(d)是CF3)为市售。式39c的吡唑(式39的化合物，其中R5(d)是Cl或Br)可通过文献方法制备(Chem.Ber.1966，99(10)，3350-7)。在反应方案21中描述了制备化合物39c的另一供选择的有用方法。用正丁基锂使氨磺酰吡唑金属化，随后用六氯乙烷(R5(d)为Cl)或1，2-二溴四氯乙烷(R5(d)为Br)进行直接卤化，即产生式51的卤化衍生物。用三氟醋酸(TFA)在室温下除去氨磺酰基团进行得很完全，产率良好，从而产生式39c的吡唑。本领域的技术人员将知道，式39c是式39b的互变异构体。 Reaction Scheme 20 The starting pyrazoles of formula 39 are known compounds. Pyrazoles of formula 39a (compounds of formula 39 wherein R5 (d) is CF3 ) are commercially available. Pyrazoles of formula 39c (compounds of formula 39 wherein R 5 (d) is Cl or Br) can be prepared by literature methods (Chem. Ber. 1966, 99(10), 3350-7). Another useful alternative method for the preparation of compound 39c is depicted in Reaction Scheme 21. Metallation of sulfamoylpyrazole with n-butyllithium followed by hexachloroethane ( R5 (d) is Cl) or 1,2-dibromotetrachloroethane ( R5 (d) is Br) Direct halogenation, ie, produces halogenated derivatives of formula 51. Removal of the sulfamoyl group with trifluoroacetic acid (TFA) at room temperature goes to completion in good yields to give pyrazoles of formula 39c. Those skilled in the art will appreciate that Formula 39c is a tautomer of Formula 39b.

                     反应方案21

Figure A0180519000381
Reaction Scheme 21
Figure A0180519000381

应认识到的是，上述用于制备式I和式II化合物的一些试剂和反应条件可能与中间体中存在的某些官能基团并不相容。在这些情况下，在合成过程中引入保护/脱保护程序或官能基团相互转换将有助于获得所需产物。保护基团的使用和选择对于化学合成的技术人员而言是显而易见的(参见例如Greene，T.W.；Wuts，P.G.M所著《Protective Groupsin Organic Synthesis》(有机合成中的保护基团)第二版；Wiley：NewYork，1991)。本领域的技术人员将知道，在某些情况下，在引入特定试剂之后(如在任何单独的反应方案中所描述的)，可能需要进行另外的为加以详细描述的常规合成步骤，以完成式I和II的化合物的合成。本领域的技术人员还应认识到，为了制备式I和II的化合物，可能需要将上述反应方案中所描述的步骤结合进行，而其顺序可与所述的具体顺序不同。It will be recognized that some of the reagents and reaction conditions described above for the preparation of compounds of formula I and formula II may not be compatible with certain functional groups present in the intermediates. In these cases, introducing protection/deprotection procedures or interconversion of functional groups during the synthesis will help to obtain the desired products. The use and choice of protecting groups will be apparent to those skilled in chemical synthesis (see, e.g., Greene, T.W.; Wuts, P.G.M, Protective Groups in Organic Synthesis, 2nd ed.; Wiley : NewYork, 1991). Those skilled in the art will appreciate that, in some cases, after the introduction of specific reagents (as described in any individual reaction scheme), it may be necessary to perform additional, not detailed, conventional synthetic steps to complete the formula Synthesis of compounds of I and II. Those skilled in the art will also recognize that in order to prepare compounds of formulas I and II, it may be necessary to combine the steps described in the above reaction schemes, and the order may be different from the specific order described.

本领域的技术人员还应认识到，在此所述的式I和II的化合物及中间体可进行各种亲电、亲核、自由基、金属有机、氧化和还原反应，以加成取代基或对现有取代基进行改性。Those skilled in the art will also recognize that compounds of Formulas I and II and intermediates described herein can undergo a variety of electrophilic, nucleophilic, free radical, metalorganic, oxidation and reduction reactions to add substituents Or modify existing substituents.

无需进一步详述，具信利用上述描述的本领域的技术人员能够在其最完全的范围内应用本发明。因此，以下的实施例只应视为例示性的，并不以任何方式对发明内容进行限制。1H NMR光谱以ppm由四甲基硅烷的低磁场记录得到：s为单一态，d为双重态，t为三重态，q为四重态，m为多重态，dd为双重态的双重态，dt为三重态的双重态，br为宽单一态，m.p.熔点。Without further elaboration, it is believed that one skilled in the art, using the preceding description, can utilize the present invention in its fullest scope. Therefore, the following embodiments should only be regarded as illustrative, and not limiting the content of the invention in any way. 1 H NMR spectra in ppm from downfield recordings of tetramethylsilane: s for singlet, d for doublet, t for triplet, q for quartet, m for multiplet, dd for doublet of doublet , dt is the doublet state of the triplet state, br is the wide single state, and mp is the melting point.

                    实施例1 制备N-甲基-N’-(2-溴-4-氟苯基)-1，8-萘-二甲酰胺 步骤A：制备8-[甲基氨基)羰基]-1-萘甲酸 Example 1 Preparation of N-methyl-N'-(2-bromo-4-fluorophenyl)-1,8-naphthalene-dicarboxamide Step A: Preparation of 8-[methylamino)carbonyl]-1-naphthalene formic acid

在室温下，向经搅拌的1，8-萘二甲酸酐(5g，25.3mmol)的N，N-二甲基甲酰胺(50mL)溶液中加入甲胺(0.82g，26.5mmol)的N，N-二甲基甲酰胺(5mL)溶液。将反应混合物搅拌2.5小时。在减压下除去溶剂。用小量的二乙醚洗涤由此而得到的粗固体，并进行空气干燥，以生成产物(5g)，其经NMR分析确定含8-[(甲氨基)羰基]-1-萘甲酸和1，8-萘二甲酸酐，比例为约7∶1。此物质不经进一步纯化而用于随后的反应中。1H NMR(DMSO-d6)δ：2.77(双重态，3H)，7.55-7.65(多重态，3H)，7.83(双重态，1H)，8.03-8.12(多重态，2H)，8.39(四重态，1H)。步骤B：制备N-甲基-N’-(2-溴-4-氟苯基)-1，8-萘-二甲酰 胺 To a stirred solution of 1,8-naphthalic anhydride (5 g, 25.3 mmol) in N,N-dimethylformamide (50 mL) was added methylamine (0.82 g, 26.5 mmol) in N at room temperature, N-Dimethylformamide (5 mL) solution. The reaction mixture was stirred for 2.5 hours. The solvent was removed under reduced pressure. The crude solid thus obtained was washed with a small amount of diethyl ether and air dried to give a product (5 g) which was determined by NMR analysis to contain 8-[(methylamino)carbonyl]-1-naphthoic acid and 1, 8-Naphthalic anhydride in a ratio of about 7:1. This material was used in subsequent reactions without further purification. 1 H NMR (DMSO-d6) δ: 2.77 (doublet, 3H), 7.55-7.65 (multiplet, 3H), 7.83 (doublet, 1H), 8.03-8.12 (multiplet, 2H), 8.39 (quadruple state, 1H). Step B: Preparation of N-methyl-N'-(2-bromo-4-fluorophenyl)-1,8-naphthalene- dicarboxamide

向经搅拌的、在氮气氛下冷却至约5℃的按步骤A所述制备的8-[(甲氨基)羰基]-1-萘甲酸(22.3g，97.4mmol)和吡啶(15.4g，0.195mol)的二氯甲烷(300ml)溶液中，滴加在二氯甲烷(50ml)中稀释的三氟醋酸酐(22.5g，0.107mol)。滴加后，在常温下将反应混合物进一步搅拌半小时。滤除小量的固体。在减压下将滤液浓缩为固体，用热己烷(3×250ml)对该固体进行萃取。将己烷萃取液合并，并在减压下进行浓缩，产生3-(甲基亚氨基)-1H，3H-萘并[1，8-cd]比喃-1-酮粗品(15g)。To stirred 8-[(methylamino)carbonyl]-1-naphthoic acid (22.3 g, 97.4 mmol) and pyridine (15.4 g, 0.195 mol) in dichloromethane (300ml), was added dropwise trifluoroacetic anhydride (22.5g, 0.107mol) diluted in dichloromethane (50ml). After the dropwise addition, the reaction mixture was further stirred at normal temperature for half an hour. A small amount of solid was filtered off. The filtrate was concentrated under reduced pressure to a solid which was extracted with hot hexane (3 x 250ml). The hexane extracts were combined and concentrated under reduced pressure to give crude 3-(methylimino)-1H,3H-naphtho[1,8-cd]pyran-1-one (15 g).

将由此获得的3-(甲基亚氨基)-1H，3H-萘并[1，8-cd]吡喃-1-酮(0.25g，1.19mmol)溶解于二氯甲烷(3ml)中，并加入2-溴-4-氟苯胺(0.17g，1.45mmol)。在室温下搅拌反应混合物48小时。对固体进行过滤、收集，并用小量甲醇在二氯甲烷中进行洗涤和进行空气干燥，以产生N-甲基N’-(2-甲基-4-氟苯基)-1，8-萘-二甲酰胺(0.12g，熔点为249℃)。1H NMR(DMSO-d6)δ：2.37(单一态，3H)，2.72(双重态，3H)，7.05-7.12(多重态，2H)，7.54-7.64(多重态，3H)，7.75-7.83(多重态，2H)，8.05-8.10(多重态，2H)，8.33(四重态，1H)，9.84(单一态，1H)。The 3-(methylimino)-1H,3H-naphtho[1,8-cd]pyran-1-one (0.25 g, 1.19 mmol) thus obtained was dissolved in dichloromethane (3 ml), and 2-Bromo-4-fluoroaniline (0.17 g, 1.45 mmol) was added. The reaction mixture was stirred at room temperature for 48 hours. The solid was filtered, collected, washed with a small amount of methanol in dichloromethane and air dried to yield N-methyl N'-(2-methyl-4-fluorophenyl)-1,8-naphthalene - Diformamide (0.12 g, melting point 249° C.). 1 H NMR (DMSO-d6) δ: 2.37 (single state, 3H), 2.72 (double state, 3H), 7.05-7.12 (multiple state, 2H), 7.54-7.64 (multiple state, 3H), 7.75-7.83 ( multiplet, 2H), 8.05-8.10 (multiplet, 2H), 8.33 (quartet, 1H), 9.84 (singlet, 1H).

                     实施例2 制备N-甲基8-[(3，4-二氟苯基)羰基氨基]-1-萘甲酰胺 步骤A：制备N-甲基8-硝基 1-萘甲酰胺 Example 2 Preparation of N-methyl 8-[(3,4-difluorophenyl)carbonylamino]-1-naphthylcarboxamide Step A: Preparation of N-methyl 8-nitro 1-naphthylcarboxamide

向经搅拌的室温下的8-硝基-1-萘甲酸(1.5g，6.9mmol)、甲胺(0.22g，7.3mmol)和咪唑(0.68g，8.3mmol)的N，N-二甲基甲酰胺(12mL)溶液中，加入氰基膦酸二乙酯(1.24g，7.6mmol)。将反应混合物彻夜搅拌，倒入水(100mL)中，和用醋酸乙酯(3×100mL)萃取。合并醋酸乙酯萃取液，在无水硫酸镁上干燥，过滤，和在减压下进行浓缩，以产生固体，该固体用小量甲醇洗涤，生成产物(0.64g)，该产物不经进一步纯化而被利用。1H NMR(DMSO-d6)δ：2.76(双重态，3H)，7.72-8.37(多重态，6H)，8.66(宽四重态，1H)。步骤B：制备N-甲基8-胺基  1-萘甲酰胺 To 8-nitro-1-naphthoic acid (1.5g, 6.9mmol), methylamine (0.22g, 7.3mmol) and imidazole (0.68g, 8.3mmol) N,N-dimethyl To a solution of formamide (12 mL), diethyl cyanophosphonate (1.24 g, 7.6 mmol) was added. The reaction mixture was stirred overnight, poured into water (100 mL), and extracted with ethyl acetate (3 x 100 mL). The ethyl acetate extracts were combined, dried over anhydrous magnesium sulfate, filtered, and concentrated under reduced pressure to give a solid which was washed with a small amount of methanol to give the product (0.64 g) which was used without further purification And be used. 1 H NMR (DMSO-d6) δ: 2.76 (doublet, 3H), 7.72-8.37 (multiplet, 6H), 8.66 (broad quartet, 1H). Step B: Preparation of N-methyl 8-amino-1-naphthylcarboxamide

在30psi氢压下，用催化量的钯(10％，在活性炭上)氢化N-甲基8-硝基-1-萘甲酰胺(0.5g，2.17mmol)1小时。通过C盐对反应混合物进行吸滤，并在减压下进行浓缩，以生成产物(0.42g)，该产物不经进一步纯化而被利用。1H NMR(DMSO-d6)δ：2.82(双重态，3H)，5.46(单一态，2H)，6.81-7.85(多重态，6H)，8.59(宽四重态，1H)。步骤C：制备N-甲基8-[(3，4-二氟苯基)羰基氨基]-1-萘甲酰胺 N-methyl 8-nitro-1-naphthylcarboxamide (0.5 g, 2.17 mmol) was hydrogenated with a catalytic amount of palladium (10% on charcoal) under 30 psi hydrogen pressure for 1 hour. The reaction mixture was suction filtered through Celite and concentrated under reduced pressure to give the product (0.42g) which was used without further purification. 1 H NMR (DMSO-d6) δ: 2.82 (doublet, 3H), 5.46 (singlet, 2H), 6.81-7.85 (multiplet, 6H), 8.59 (broad quartet, 1H). Step C: Preparation of N-methyl 8-[(3,4-difluorophenyl)carbonylamino]-1-naphthylcarboxamide

向经搅拌的N-甲基8-胺基  1-萘甲酰胺(0.2g，1mmol)和吡啶(0.24g，3mmol)的二氯甲烷(10mL)溶液中，分批加入在二氯甲烷(2mL)中的actyl chloride(94.2mg，1.2mmol)。混合物搅拌3小时。用吸滤收集固体(110mg，熔点高于250℃)。1H NMR(DMSO-d6)δ：2.43(双重态，3H)，7.46-8.10(多重态，9H)，8.51(宽四重态，1H)，10.13(单一态，1H)。To a stirred solution of N-methyl 8-amino-1-naphthylcarboxamide (0.2 g, 1 mmol) and pyridine (0.24 g, 3 mmol) in dichloromethane (10 mL), add dichloromethane (2 mL) in portions ) in actyl chloride (94.2mg, 1.2mmol). The mixture was stirred for 3 hours. The solid (110 mg, melting point above 250°C) was collected by suction filtration. 1 H NMR (DMSO-d6) δ: 2.43 (doublet, 3H), 7.46-8.10 (multiplet, 9H), 8.51 (broad quartet, 1H), 10.13 (singlet, 1H).

                    实施例3 制备N-甲基8-[(2-噻吩基)羰基氨基]-1-萘甲酰胺 Example 3 Preparation of N-methyl 8-[(2-thienyl) carbonylamino]-1-naphthylcarboxamide

向经搅拌的N-甲基8-胺基  1-萘甲酰胺(0.2g，1mmol)和吡啶(0.24g，3mmol)的二氯甲烷(10mL)溶液中，分批加入在二氯甲烷(2mL)中的2-噻吩羧酰氯(176mg，1.2mmol)。混合物搅拌3小时。用稀盐酸、饱和碳酸氢钠水溶液和水顺序洗涤反应混合物。在减压下部分除去溶剂。用吸滤收集由此而形成的固体(36mg，熔点为210℃)。1H NMR(DMSO-d6)δ：2.53(双重态，3H)，7.26-8.10(多重态，9H)，8.66(宽四重态，1H)，10.07(单一态，1H)，。To a stirred solution of N-methyl 8-amino-1-naphthylcarboxamide (0.2 g, 1 mmol) and pyridine (0.24 g, 3 mmol) in dichloromethane (10 mL), add dichloromethane (2 mL) in portions ) in 2-thiophenecarboxylic acid chloride (176mg, 1.2mmol). The mixture was stirred for 3 hours. The reaction mixture was washed sequentially with dilute hydrochloric acid, saturated aqueous sodium bicarbonate and water. The solvent was partially removed under reduced pressure. The solid thus formed (36 mg, melting point 210° C.) was collected by suction filtration. 1 H NMR (DMSO-d6) δ: 2.53 (doublet, 3H), 7.26-8.10 (multiplet, 9H), 8.66 (broad quartet, 1H), 10.07 (singlet, 1H).

通过在此所述的程序和本领域中已知的方法，可制备出以下的表1-10的化合物。在各表中使用了下列缩写：t为叔，s为仲，n为正，i为异，c为环，Me为甲基，Et为乙基，Pr为丙基，i-Pr为异丙基，t-Bu为叔丁基，Ph为苯基，OMe为甲氧基，OEt为乙氧基，SMe为甲基硫代，SEt为乙基硫代，CN为氰基，NO2为硝基，TMS为三甲基甲硅烷基，S(O)Me为甲基亚硫酰基，而S(O)2Me为甲基磺酰基。The compounds of Tables 1-10 below can be prepared by the procedures described herein and methods known in the art. The following abbreviations are used in the tables: t for tertiary, s for secondary, n for positive, i for iso, c for ring, Me for methyl, Et for ethyl, Pr for propyl, i-Pr for isopropyl t-Bu is tert-butyl, Ph is phenyl, OMe is methoxy, OEt is ethoxy, SMe is methylthio, SEt is ethylthio, CN is cyano, NO2 is nitrate group, TMS is trimethylsilyl, S(O)Me is methylsulfinyl, and S(O) 2 Me is methylsulfonyl.

                       表1

Figure A0180519000411
R 3   R 4  R 4b  R 5a  R 5bMe   H     Me    H     CF3Me   H     Me    H     OCF3Et   H     Me    H     OCF3Me   H     Me    Me    BrMe   H     Me    Et    BrMe   H     Me    Me    ClMe   H     Me    Et    ClMe   H     Me    Me    IMe   H     Me    Me    CF3Me   H     Me    Me    OCF3Et   H     Me    Me    CF3 R 3    R 4a  R 4b  R 5a  R 5bMe    H     H     H     CF3Me    H     H     H     OCF3Et    H     H     H     OCF3Me    H     H     Me    BrMe    H     H     Et    BrMe    H     H     Me    ClMe    H     H     Er    CtMe    H     H     Me    IMe    H     H     Me    CF3Me    H     H     Me    OCF3Et    H     H     Me    CF3 R 3   R 4a  R 4b  R 5a   R 5bMe    H    Me    Me     SCF3Me    H    Me    Me     SCHF2Me    H    Me    Me     OCHF2n-Pr  H    Me    Me     CF3Me    H    Me    Me     C2F5Et    H    Me    Me     C2F5Me    H    Me    Et     CF3Me    H    Me    n-Pr   CF3Me    H    Me    i-Pr   CF3Me    H    Me    Cl     CF3Me    H    Me    F      CF3Me    H    Me    Me     SMeMe    H    Me    Me     OMeMe    H    Me    Me     OEtMe    H    Me    Me     n-C3F7Me    H    Me    Me     i-C3F7Me    H    Me    Me     EtMe    H    Me    Me     OCF2CHF2Me    H    Me    Me     SCF2CHF2Me    H    Me    Me     SO2MeMe    H    Me    Me     SO2CF3Me    H    Me    CF3   CF3Me    H    Me    CF3   MeMe    H    Me    OMe    CF3Me    H    Me    H      CF3Me    H    Me    H      OCHF2Me    H    Me    H      C2F5Et    H    Me    H      C2F5Me    H    Me    H      OCF3Me    H    Me    H      OCF2CHF2Me    H    Me    H      SCF2CHF2Me    H    Me    H      n-C3F7Me    H    Me    H      i-C3F7Me    H    Me    H      BrMe    H    Me    H      ClMe    H    Me    H      SCF3Me    H    Me    Ph     CF3 R 3   R 4a  R 4b R 5a  R 5bMe    H    H    Me    SCF3Me    H    H    Me    SCHF2Me    H    H    Me    OCHF2n-Pr  H    H    Me    CF3Me    H    H    Me    C2F5Et    H    H    Me    C2F5Me    H    H    Et    CF3Me    H    H    n-Pr  CF3Me    H    H    i-Pr  CF3Me    H    H    Cl    CF3Me    H    H    F     CF3Me    H    H    Me    SMeMe    H    H    Me    OMeMe    H    H    Me    CEtMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    EtMe    H    H    Me    OCF2CHF2Me    H    H    Me    SCF2CHF2Me    H    H    Me    SO2MeMe    H    H    Me    SO2CF3Me    H    H    CF3  CF3Me    H    H    CF3  MeMe    H    H    OMe   CF3Me    H    H    H     CF3Me    H    H    H     OCHF2Me    H    H    H     C2F5Et    H    H    H     C2F5Me    H    H    H     OCF3Me    H    H    H     OCF2CHF2Me    H    H    H     SCF2CHF2Me    H    H    H     n-C3F7Me    H    H    H     i-C3F7Me    H    H    H     BrMe    H    H    H     ClMe    H    H    H     SCF3Me    H    H    Ph    CF3     R 3  R 4a  R 4b  R 5a          R 5bMe    H    Me    Ph            ClMe    H    Me    Ph            BrMe    H    Me    2-吡啶基      CF3Me    H    Me    2-吡啶基      ClMe    H    Me    2-ClPh        CF3Me    H    Me    2-ClPh        OCF3Me    H    Me    2-ClPh        BrMe    H    Me    2-ClPh        ClMe    H    Me    2-ClPh        SCHF2Me    H    Me    2-BrPh        CF3Me    H    Me    2-MePh        CF3Me    H    Me    2-CNPh        CF3Me    H    Me    2-FPh         CF3Me    H    Me    2,6-F2Ph     CF3Me    H    Me    2,4-F2Ph     CF3Me    H    Me    2,5-F2Ph     CF3Me    H    Me    2-MeOPh       CF3Me    H    Me    3-Cl-2-吡啶基 CF3Me    H    Me    3-Cl-2-吡啶基 OCF3Me    H    Me    3-Cl-2-吡啶基 BrMe    H    Me    3-Cl-2-吡啶基 ClMe    H    Me    3-Cl-2-吡啶基 SCHF2Me    H    Me    3-F-2-吡啶基  CF3Me    H    Me    3-CF3-2-     CF3吡啶基Me    H    Me    3-Me-2-       CF3吡啶基Me    H    Me    3-Br-2-吡啶基 CF3Me    H    Me    3-Br-2-吡啶基 OCF3Me    H    Me    3-Br-2-吡啶基 BrMe    H    Me    3-Br-2-吡啶基 ClMe    Me   H     H             CF3Me    Me   H     H             OCF3Et    Me   H     H             OCF3Me    Me   H     Me            BrMe    Me   H     Et            BrMe    Me   H     Me            Cl R 3  R 4a  R 4b   R 5a             R 5bMe    H    H     Ph               ClMe    H    H     Ph               BrMe    H    H     2-吡啶基         CF3Me    H    H     2-吡啶基         ClMe    H    H     2-ClPh           CF3Me    H    H     2-ClPh           OCF3Me    H    H     2-ClPh           BrMe    H    H     2-ClPh           ClMe    H    H     2-ClPh           SCHF2Me    H    H     2-BrPh           CF3Me    H    H     2-MePh           CF3Me    H    H     2-CNPh           CF3Me    H    H     2-FPh            CF3Me    H    H     2,6-F2Ph        CF3Me    H    H     2,4-F2Ph        CF3Me    H    H     2,5-F2Ph        CF3Me    H    H     2-MeOPh          CF3Me    H    H     3-Cl-2-吡啶基    CF3Me    H    H     3-Cl-2-吡啶基    OCF3Me    H    H     3-Cl-2-吡啶基    BrMe    H    H     3-Cl-2-吡啶基    ClMe    H    H     3-Cl-2-吡啶基    SCHF2Me    H    H     3-F-2-吡啶基     CF3Me    H    H     3-CF3-2-        CF3吡啶基Me    H    H     3-Me-2-          CF3吡啶基Me    H    H     3-Br-2-吡啶基    CF3Me    H    H     3-Br-2-吡啶基    OCF3Me    H    H     3-Br-2-吡啶基    BrMe    H    H     3-Br-2-吡啶基    ClMe    H    Cl    Et               BrMe    H    Cl    Me               ClMe    H    Cl    Et               ClMe    H    Cl    Me               IMe    H    Cl    Me               CF3Me    H    Cl    Me               OCF3     R 3   R 4a  R 4b R 5a   R 5bMe    Me    H    Et     ClMe    Me    H    Me     IMe    Me    H    Me     CF3Me    Me    H    Me     OCF3Et    Me    H    Me     CF3Me    Me    H    Me     SCF3Me    Me    H    Me     SCHF2Me    Me    H    Me     OCHF2n-Pr  Me    H    Me     CF3Me    Me    H    Me     C2F5Et    Me    H    Me     C2F5Me    Me    H    Et     CF3Me    Me    H    n-Pr   CF3Me    Me    H    i-Pr   CF3Me    Me    H    Cl     CF3Me    Me    H    F      CF3Me    Me    H    Me     SMeMe    Me    H    Me     OMeMe    Me    H    Me     OEtMe    Me    H    Me     n-C3F7Me    Me    H    Me     i-C3F7Me    Me    H    Me     EtMe    Me    H    Me     OCF2CHF2Me    Me    H    Me     SCF2CHF2Me    Me    H    Me     SO2MeMe    Me    H    Me     SO2CF3Me    Me    H    CF3   CF3Me    Me    H    CF3   MeMe    Me    H    OMe    CF3Me    Me    H    H      CF3Me    Me    H    H      OCHF2Me    Me    H    H      C2F5Et    Me    H    H      C2F5Me    Me    H    H      OCF3Me    Me    H    H      OCF2CHF2Me    Me    H    H      SCF2CHF2Me    Me    H    H      n-C3F7 R 3   R 4a  R 4b  R 5a    R 5bEt    H    Cl    Me      CF3Me    H    Cl    Me      SCF3Me    H    Cl    Me      SCHF2Me    H    Cl    Me      OCHF2n-Pr  H    Cl    Me      CF3Me    H    Cl    Me      C2F5Et    H    Cl    Me      C2F5Me    H    Cl    Et      CF3Me    H    Cl    n-Pr    CF3Me    H    Cl    i-Pr    CF3Me    H    Cl    Cl      CF3Me    H    Cl    F       CF3Me    H    Cl    Me      SMeMe    H    Cl    Me      OMeMe    H    Cl    Me      OEtMe    H    Cl    Me      n-C3F7Me    H    Cl    Me      i-C3F7Me    H    Cl    Me      EtMe    H    Cl    Me      OCF2CHF2Me    H    Cl    Me      SCF2CHF2Me    H    Cl    Me      SO2MeMe    H    Cl    Me      SO2CF3Me    H    Cl    CF3    CF3Me    H    Cl    CF3    MeMe    H    Cl    OMe     CF3Me    H    Cl    H       CF3Me    H    Cl    H       OCHF2Me    H    Cl    H       C2F5Et    H    Cl    H       C2F5Me    H    Cl    H       OCF3Me    H    Cl    H       OCF2CHF2Me    H    Cl    H       SCF2CHF2Me    H    Cl    H       n-C3F7Me    H    Cl    H       i-C3F7Me    H    Cl    H       BrMe    H    Cl    H       ClMe    H    Cl    H       SCF3 R 3  R 4a  R 4b R 5a              R 5bMe  Me    H    H                i-C3F7Me  Me    H    H                BrMe  Me    H    H                ClMe  Me    H    H                SCF3Me  Me    H    Ph               CF3Me  Me    H    Ph               ClMe  Me    H    Ph               BrMe  Me    H    2-吡啶基         CF3Me  Me    H    2-吡啶基         ClMe  Me    H    2-ClPh           CF3Me  Me    H    2-ClPh           OCF3Me  Me    H    2-ClPh           BrMe  Me    H    2-ClPh           ClMe  Me    H    2-ClPh           SCHF2Me  Me    H    2-BrPh           CF3Me  Me    H    2-MePh           CF3Me  Me    H    2-CNPh           CF3Me  Me    H    2-FPh            CF3Me  Me    H    2,6-F2Ph        CF3Me  Me    H    2,4-F2Ph        CF3Me  Me    H    2,5-F2Ph        CF3Me  Me    H    2-MeOPh          CF3Me  Me    H    3-Cl-2-吡啶基    CF3Me  Me    H    3-Cl-2-吡啶基    OCF3Me  Me    H    3-CF3-2-        CF3吡啶基Me  Me    H    3-Me-2-          CF3吡啶基Me  Me    H    3-Cl-2-吡啶基    SCHF2Me  Me    H    3-F-2-吡啶基     CF3Me  Me    H    3-Cl-2-吡啶基    BrMe  Me    H    3-Cl-2-吡啶基    ClMe  Me    H    3-Br-2-吡啶基    CF3Me  Me    H    3-Br-2-吡啶基    OCF3Me  Me    h    3-Br-2-吡啶基    BrMe  Me    H    3-Br-2-吡啶基    ClMe  Cl    H    Me               Br R 3   R 4a  R 4b  R 5a             R 5bMe    H    Cl    Ph               CF3Me    H    Cl    Ph               ClMe    H    Cl    Ph               BrMe    H    Cl    2-吡啶基         CF3Me    H    Cl    2-吡啶基         ClMe    H    Cl    2-ClPh           CF3Me    H    Cl    2-ClPh           OCF3Me    H    Cl    2-ClPh           BrMe    H    Cl    2-ClPh           ClMe    H    Cl    2-ClPh           SCHF2Me    H    Cl    2-BrPh           CF3Me    H    Cl    2-MePh           CF3Me    H    Cl    2-CNPh           CF3Me    H    Cl    2-FPh            CF3Me    H    Cl    2,6-F2Ph        CF3Me    H    Cl    2,4-F2Ph        CF3Me    H    Cl    2,5-F2Ph        CF3Me    H    Cl    2-MeOPh          CF3Me    H    Cl    3-Cl-2-吡啶基    CF3Me    H    Cl    3-Cl-2-吡啶基    OCF3Me    H    Cl    3-Cl-2-吡啶基    BrMe    H    Cl    3-Cl-2-吡啶基    ClMe    H    Cl    3-Cl-2-吡啶基    SCHF2Me    H    Cl    3-F-2-吡啶基     CF3Me    H    Cl    3-CF3-2-        CF3吡啶基Me    H    Cl    3-Me-2-          CF3吡啶基Me    H    Cl    3-Br-2-吡啶基    CF3Me    H    Cl    3-Br-2-吡啶基    OCF3Me    H    Cl    3-Br-2-吡啶基    BrMe    H    Cl    3-Br-2-吡啶基    ClMe    Cl   H     Ph               CF3Me    Cl   H     Ph               ClMe    Cl   H     Ph               BrMe    Cl   H     2-吡啶基         CF3Me    Cl   H     2-吡啶基         Cl R 3   R 4a  R 4b  R 5a     R 5bMe    Cl    H    Et       BrMe    Cl    H    Me       ClMe    Cl    H    Et       ClMe    Cl    H    Me       IMe    Cl    H    Me       CF3Me    Cl    H    Me       OCF3Et    Cl    H    Me       CF3Me    Cl    H    Me       SCF3Me    Cl    H    Me       SCHF2Me    Cl    H    Me       OCHF2n-Pr  Cl    H    Me       CF3Me    Cl    H    Me       C2F5Et    Cl    H    Me       C2F5Me    Cl    H    Et       CF3Me    Cl    H    n-Pr     CF3Me    Cl    H    i-Pr     CF3Me    Cl    H    Cl       CF3Me    Cl    H    F        CF3Me    Cl    H    Me       SMeMe    Cl    H    3-Me-2-  CF3吡啶基Me    Cl    H    Me       OEtMe    Cl    H    Me       n-C3F7Me    Cl    H    Me       i-C3F7Me    Cl    H    Me       EtMe    Cl    H    Me       OCF2CHF2Me    Cl    H    Me       SCF2CHF2Me    Cl    H    Me       SO2MeMe    Cl    H    Me       SO2CF3Me    Cl    H    CF3     CF3Me    Cl    H    CF3     MeMe    Cl    H    OMe      CF3Me    Cl    H    H        CF3Me    Cl    H    H        OCHF2Me    Cl    H    H        C2F5Et    Cl    H    H        C2F5 R 3   R 4a  R 4b  R 5a           R 5bMe    Cl    H    2-ClPh         CF3Me    Cl    H    2-ClPh         OCF3Me    Cl    H    2-ClPh         BrMe    Cl    H    2-ClPh         ClMe    Cl    H    2-ClPh         SCHF2Me    Cl    H    2-BrPh         CF3Me    Cl    H    2-MePh         CF3Me    Cl    H    2-CNPh         CF3Me    Cl    H    2-FPh          CF3Me    Cl    H    2,6-F2Ph      CF3Me    Cl  H      2,4-F2Ph      CF3Me    Cl    H    2,5-F2Ph      CF3Me    Cl    H    2-MeOPh        CF3Me    Cl    H    3-Cl-2-吡啶基  CF3Me    Cl    H    3-Cl-2-吡啶基  OCF3Me    Cl    H    3-Cl-2-吡啶基  BrMe    Cl    H    3-Cl-2-吡啶基  ClMe    Cl    H    3-Cl-2-吡啶基  SCHF2Me    Cl    H    3-F-2-吡啶基   CF3Me    Cl    H    3-CF3-2-      CF3吡啶基Me    Cl    H    3-Br-2-吡啶基  CF3Me    Cl    H    3-Br-2-吡啶基  OCF3Me    Cl    H    3-Br-2-吡啶基  BrMe    Cl    H    3-Br-2-吡啶基  ClMe    Cl    H    H              OCF3Me    Cl    H    H              OCF2CHF2Me    Cl    H    H              SCF2CHF2Me    Cl    H    H              n-C3F7Me    Cl    H    H              i-C3F7Me    Cl    H    H              BrMe    Cl    H    H              ClMe    Cl    H    H              SCF3Me    Cl    H    Ph             CF3Me    Cl    H    Me             OMe Table 1
Figure A0180519000411
R 3 R 4 R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 Me H Me Me OCF 3 Et H Me Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Er CtMe H H Me IMe H H Me CF 3 Me H H Me OCF 3 Et H H Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me EtMe H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H ClMe H Me H SCF 3 Me H Me Ph CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me CEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me EtMe H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H OCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H ClMe H H H SCF 3 Me H H Ph CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 Me H Me 3 -Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridyl ClMe H Me 3-Cl -2-pyridyl SCHF 2 Me H Me 3-F-2-pyridyl CF 3 Me H Me 3-CF 3 -2- CF 3 pyridyl Me H Me 3-Me-2- CF 3 pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridyl ClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me BrMe Me H Et BrMe Me H Me Cl R 3 R 4a R 4b R 5a R 5b Me H H Ph ClMe H H Ph BrMe H H 2-Pyridyl CF 3 Me H H 2-Pyridyl ClMe H H 2 - ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridine OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2-pyridyl ClMe H H 3-Cl-2-pyridyl SCHF 2 Me H H 3-F-2-pyridyl CF 3 Me H H 3 -CF 3 -2- CF 3 pyridyl Me H H 3-Me-2- CF 3 pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3- Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me OCF 3 R 3 R 4a R 4b R 5a R 5b Me Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMeMe Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 R 3 R 4a R 4b R 5a R 5b Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe HCl Me OEtMe HCl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H BrMe H Cl H ClMe H Cl H SCF 3 R 3 R 4a R 4b R 5a R 5b Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3 -CF 3 -2- CF 3 pyridyl Me Me H 3-Me-2- CF 3 pyridyl Me Me H 3-Cl-2-pyridyl SCHF 2 Me H 3-F-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-Br-2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl OCF 3 Me Me h 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridyl ClMe Cl H Me Br R 3 R 4a R 4b R 5a R 5b Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me HCl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me H Cl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2-pyridyl BrMe H Cl 3-Cl-2-pyridyl ClMe H Cl 3-Cl-2-pyridyl SCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me H Cl 3-CF 3 -2- CF 3 pyridyl Me H Cl 3-Me-2- CF 3 pyridine Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me H Cl 3-Br-2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-pyridyl CF 3 Me Cl H 2-pyridyl Cl R 3 R 4a R 4b R 5a R 5b Me Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 Me Cl H F CF 3 Me Cl H Me SMeMe Cl H 3-Me-2- CF 3 Pyridyl Me Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H CF 3 CF 3 Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 Et Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 Me Cl H 2 -BrPh CF 3 Me Cl H 2-MePh CF 3 Me Cl H 2-CNPh CF 3 Me Cl H 2-FPh CF 3 Me Cl H 2,6-F 2 Ph CF 3 Me Cl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2-MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl-2-pyridylBrMeCl H 3-Cl-2-pyridylClMeCl H 3-Cl-2-pyridylSCHF 2 MeCl H 3-F-2-pyridylCF 3 MeCl H 3 -CF 3 -2- CF 3 Pyridyl Me Cl H 3-Br-2-Pyridyl CF 3 Me Cl H 3-Br-2-Pyridyl OCF 3 Me Cl H 3-Br-2-Pyridyl BrMe Cl H 3-Br-2-PyridylClMe Cl H H OCF 3 Me Cl H H OCF 2 CHF 2 Me Cl H H SCF 2 CHF 2 Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Me OMe

                                  表2 R 3  R 4a  R 4b   R 5a  R 5bMe    H    Me    H     CF3Me    H    Me    H     OCF3Et    H    Me    H     OCF3Me    H    Me    Me    BrMe    H    Me    Et    BrMe    H    Me    Me    ClMe    H    Me    Et    ClMe    H    Me    Me    IMe    H    Me    Me    CF3Me    H    Me    Me    OCF3Et    H    Me    Me    CF3Me    H    Me    Me    SCF3Me    H    Me    Me    SCHF2Me    H    Me    Me    OCHF2n-Pr  H    Me    Me    CF3Me    H    Me    Me    C2F5Et    H    Me    Me    C2F5Me    H    Me    Et    CF3Me    H    Me    n-Pr  CF3Me    H    Me    i-Pr  CF3Me    H    Me    Cl    CF3Me    H    Me    F     CF3Me    H    Me    Me    SMeMe    H    Me    Me    OMeMe    H    Me    Me    OEtMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    Et R 3   R 4a  R 4b R 5a  R 5bMe    H    H    H     CF3Me    H    H    H     OCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3Me    H    H    Me    OCF3Et    H    H    Me    CF3Me    H    H    Me    SCF3Me    H    H    Me    SCHF2Me    H    H    Me    OCHF2n-Pr  H    H    Me    CF3Me    H    H    Me    C2F5Et    H    H    Me    C2F5Me    H    H    Et    CF3Me    H    H    n-Pr  CF3Me    H    H    i-Pr  CF3Me    H    H    Cl    CF3Me    H    H    F     CF3Me    H    H    Me    SMeMe    H    H    Me    OMeMe    H    H    Me    OEtMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    Et   R 3   R 4a R 4b  R 5a         R 5bMe    H    Me    Me          OCF2CHF2Me    H    Me    Me          SCF2CHF2Me    H    Me    Me          SO2MeMe    H    Me    Me          SO2CF3Me    H    Me    CF3        CF3Me    H    Me    CF3        MeMe    H    Me    OMe         CF3Me    H    Me    H           CF3Me    H    Me    H           OCHF2Me    H    Me    H           C2F5Et    H    Me    H           C2F5Me    H    Me    H           OCF3Me    H    Me    H           OCF2CHF2Me    H    Me    H           SCF2CHF2Me    H    Me    H           n-C3F7Me    H    Me    H           i-C3F7Me    H    Me    H           BrMe    H    Me    H           ClMe    H    Me    H           SCF3Me    H    Me    Ph          CF3Me    H    Me    Ph          ClMe    H    Me    Ph          BrMe    H    Me    2-吡啶基    CF3Me    H    Me    2-吡啶基    ClMe    H    Me    2-ClPh      CF3Me    H    Me    2-ClPh      OCF3Me    H    Me    2-ClPh      BrMe    H    Me    2-ClPh      ClMe    H    Me    2-ClPh      SCHF2Me    H    Me    2-BrPh      CF3Me    H    Me    2-MePh      CF3Me    H    Me    2-CNPh      CF3Me    H    Me    2-FPh       CF3Me    H    Me    2,6-F2Ph   CF3Me    H    Me    2,4-F2Ph   CF3Me    H    Me    2,5-F2Ph   CF3Me    H    Me    2-MeOPh     CF3   R 3  R 4a  R 4b R 5a        R 5bMe    H    H    Me         OCF2CHF2Me    H    H    Me         SCF2CHF2Me    H    H    Me         SO2MeMe    H    H    Me         SO2CF3Me    H    H    CF3       CF3Me    H    H    CF3       MeMe    H    H    OMe        CF3Me    H    H    H          CF3Me    H    H    H          OCHF2Me    H    H    H          C2F5Et    H    H    H          C2F5Me    H    H    H          OCF3Me    H    H    H          OCF2CHF2Me    H    H    H          SCF2CHF2Me    H    H    H          n-C3F7Me    H    H    H          i-C3F7Me    H    H    H          BrMe    H    H    H          ClMe    H    H    H          SCF3Me    H    H    Ph         CF3Me    H    H    Ph         ClMe    H    H    Ph         BrMe    H    H    2-吡啶基   CF3Me    H    H    2-吡啶基   ClMe    H    H    2-ClPh     CF3Me    H    H    2-ClPh     OCF3Me    H    H    2-ClPh     BrMe    H    H    2-ClPh     ClMe    H    H    2-ClPh     SCHF2Me    H    H    2-BrPh     CF3Me    H    H    2-MePh     CF3Me    H    H    2-CNPh     CF3Me    H    H    2-FPh      CF3Me    H    H    2,6-F2Ph  CF3Me    H    H    2,4-F2Ph  CF3Me    H    H    2,5-F2Ph  CF3Me    H    H    2-MeOPh    CF3 R 3   R 4a  R 4b   R 5a          R 5bMe    H    Me  3-Cl-2-吡啶基    CF3Me    H    Me  3-Cl-2-吡啶基    OCF3Me    H    Me  3-Cl-2-吡啶基    BrMe    H    Me  3-Cl-2-吡啶基    ClMe    H    Me  3-Cl-2-吡啶基    SCHF2Me    H    Me  3-F-2-吡啶基     CF3Me    H    Me  3-CF3-2-        CF3吡啶基Me    H    Me  3-Me-2-          CF3吡啶基Me    H    Me  3-Br-2-吡啶基    CF3Me    H    Me  3-Br-2-吡啶基    OCF3Me    H    Me  3-Br-2-吡啶基    BrMe    H    Me  3-Br-2-吡啶基    ClMe    Me   H   H                CF3Me    Me   H   H                OCF3Et    Me   H   H                OCF3Me    Me   H   Me               BrMe    Me   H   Et               BrMe    Me   H   Me               ClMe    Me   H   Et               ClMe    Me   H   Me               IMe    Me   H   Me               CF3Me    Me   H   Me               OCF3Et    Me   H   Me               CF3Me    Me   H   Me               SCF3Me    Me   H   Me               SCHF2Me    Me   H   Me               OCHF2n-Pr  Me   H   Me               CF3Me    Me   H   Me               C2F5Et    Me   H   Me               C2F5Me    Me   H   Et               CF3Me    Me   H   n-Pr             CF3Me    Me   H   i-Pr             CF3Me    Me   H   Cl               CF3Me    Me   H   F                CF3Me    Me   H   Me               SMe R 3   R 4a  R 4b      R 5a         R 5bMe    H    H     3-Cl-吡啶基      CF3Me    H    H     3-Cl-2-吡啶基    OCF3Me    H    H     3-Cl-2-吡啶基    BrMe    H    H     3-Cl-2-吡啶基    ClMe    H    H     3-Cl-2-吡啶基    SCHF2Me    H    H     3-F-2-吡啶基     CF3Me    H    H     3-CF3-2-        CF3吡啶基Me    H    H     3-Me-2-          CF3吡啶基Me    H    H     3-Br-2-吡啶基    CF3Me    H    H     3-Br-2-吡啶基    OCF3Me    H    H     3-Br-2-吡啶基    BrMe    H    H     3-Br-2-吡啶基    ClMe    H    Cl    Et               BrMe    H    Cl    Me               ClMe    H    Cl    Et               ClMe    H    Cl    Me               IMe    H    Cl    Me               CF3Me    H    Cl    Me               OCF3Et    H    Cl    Me               CF3Me    H    Cl    Me               SCF3Me    H    Cl    Me               SCHF2Me    H    Cl    Me               OCHF2n-Pr  H    Cl    Me               CF3Me    H    Cl    Me               C2F5Et    H    Cl    Me               C2F5Me    H    Cl    Et               CF3Me    H    Cl    n-Pr             CF3Me    H    Cl    i-Pr             CF3Me    H    Cl    Cl               CF3Me    H    Cl    F                CF3Me    H    Cl    Me               SMeMe    H    Cl    Me               OMeMe    H    Cl    Me               OEtMe    H    Cl    Me               n-C3F7Me    H    Cl    Me               i-C3F7 R 3  R 4a  R 4b R 5a      R 5bMe  Me    H    Me        OMeMe  Me    H    Me        OEtMe  Me    H    Me        n-C3F7Me  Me    H    Me        i-C3F7Me  Me    H    Me        EtMe  Me    H    Me        OCF2CHF2Me  Me    H    Me        SCF2CHF2Me  Me    H    Me        SO2MeMe  Me    H    Me        SO2CF3Me  Me    H    CF3      CF3Me  Me    H    CF3      MeMe  Me    H    OMe       CF3Me  Me    H    H         CF3Me  Me    H    H         OCHF2Me  Me    H    H         C2F5Et  Me    H    H         C2F5Me  Me    H    H         OCF3Me  Me    H    H         OCF2CHF2Me  Me    H    H         SCF2CHF2Me  Me    H    H         n-C3F7Me  Me    H    H         i-C3F7Me  Me    H    H         BrMe  Me    H    H         ClMe  Me    H    H         SCF3Me  Me    H    Ph        CF3Me  Me    H    Ph        ClMe  Me    H    Ph        BrMe  Me    H    2-吡啶基  CF3Me  Me    H    2-吡啶基  ClMe  Me    H    2-ClPh    CF3Me  Me    H    2-ClPh    OCF3Me  Me    H    2-ClPh    BrMe  Me    H    2-ClPh    ClMe  Me    H    2-ClPh    SCHF2Me  Me    H    2-BrPh    CF3Me  Me    H    2-MePh    CF3Me  Me    H    2-CNPh    CF3 R 3 R 4a  R 4b  R 5a         R 5bMe  H    Cl    Me          EtMe  H    Cl    Me          OCF2CHF2Me  H    Cl    Me          SCF2CHF2Me  H    Cl    Me          SO2MeMe  H    Cl    Me          SO2CF3Me  H    Cl    CF3        CF3Me  H    Cl    CF3        MeMe  H    Cl    OMe         CF3Me  H    Cl    H           CF3Me  H    Cl    H           OCHF2Me  H    Cl    H           C2F5Et  H    Cl    H           C2F5Me  H    Cl    H           OCF3Me  H    Cl    H           OCF2CHF2Me  H    Cl    H           SCF2CHF2Me  H    Cl    H           n-C3F7Me  H    Cl    H           i-C3F7Me  H    Cl    H           BrMe  H    Cl    H           ClMe  H    Cl    H           SCF3Me  H    Cl    Ph          CF3Me  H    Cl    Ph          ClMe  H    Cl    Ph          BrMe  H    Cl    2-吡啶基    CF3Me  H    Cl    2-吡啶基    ClMe  H    Cl    2-ClPh      CF3Me  H    Cl    2-ClPh      OCF3Me  H    Cl    2-ClPh      BrMe  H    Cl    2-ClPh      ClMe  H    Cl    2-ClPh      SCHF2Me  H    Cl    2-BrPh      CF3Me  H    Cl    2-MePh      CF3Me  H    Cl    2-CNPh      CF3Me  H    Cl    2-FPh       CF3Me  H    Cl    2,6-F2Ph   CF3Me  H    Cl    2,4-F2Ph   CF3Me  H    Cl    2,5-F2Ph   CF3 R 3   R 4a  R 4b   R 5a            R 5bMe    Me    H    2-FPh            CF3Me    Me    H    2,6-F2Ph        CF3Me    Me    H    2,4-F2Ph        CF3Me    Me    H    2,5-F2Ph        CF3Me    Me    H    2-MeOPh          CF3Me    Me    H    3-Cl-2-吡啶基    CF3Me    Me    H    3-Cl-2-吡啶基    OCF3Me    Me    H    3-CF3-2-        CF3吡啶基Me    Me    H    3-Me-2-          CF3吡啶基Me    Me    H    3-Cl-2-吡啶基    SCHF2Me    Me    H    3-F-2-吡啶基     CF3Me    Me    H    3-Cl-2-吡啶基    BrMe    Me    H    3-Cl-2-吡啶基    ClMe    Me    H    3-Br-2-吡啶基    CF3Me    Me    H    3-Br-2-吡啶基    OCF3Me    Me    H    3-Br-2-吡啶基    BrMe    Me    H    3-Br-2-吡啶基    ClMe    Cl    H    Me               BrMe    Cl    H    Et               BrMe    Cl    H    Me               ClMe    Cl    H    Et               ClMe    Cl    H    Me               IMe    Cl    H    Me               CF3Me    Cl    H    Me               OCF3Et    Cl    H    Me               CF3Me    Cl    H    Me               SCF3Me    Cl    H    Me               SCHF2Me    Cl    H    Me               OCHF2n-Pr  Cl    H    Me               CF3Me    Cl    H    Me               C2F5Et    Cl    H    Me               C2F5Me    Cl    H    Et               CF3Me    Cl    H    n-Pr             CF3Me    Cl    H    i-Pr             CF3Me    Cl    H    Cl               CF3 R 3   R 4a  R 4b    R 5a           R 5bMe    H    Cl    2-MeOPh          CF3Me    H    Cl    3-Cl-2-吡啶基    CF3Me    H    Cl    3-Cl-2-吡啶基    OCF3Me    H    Cl    3-Cl-2-吡啶基    BrMe    H    Cl    3-Cl-2-吡啶基    ClMe    H    Cl    3-Cl-2-吡啶基    SCHF2Me    H    Cl    3-F-2-吡啶基     CF3Me    H    Cl    3-CF3-2-        CF3吡啶基Me    H    Cl    3-Me-2-          CF3吡啶基Me    H    Cl    3-Br-2-吡啶基    CF3Me    H    Cl    3-Br-2-吡啶基    OCF3Me    H    Cl    3-Br-2-吡啶基    BrMe    H    Cl    3-Br-2-吡啶基    ClMe    Cl   H     H                OCF3Me    Cl   H     H                OCF2CHF2Me    Cl   H     H                SCF2CHF2Me    Cl   H     H                n-C3F7Me    Cl   H     H                i-C3F7Me    Cl   H     H                BrMe    Cl   H     H                ClMe    Cl   H     H                SCF3Me    Cl   H     Ph               CF3Me    Cl   H     Ph               ClMe    Cl   H     Ph               BrMe    Cl   H     2-吡啶基         CF3Me    Cl   H     2-吡啶基         ClMe    Cl   H     2-ClPh           CF3Me    Cl   H     2-ClPh           OCF3Me    Cl   H     2-ClPh           BrMe    Cl   H     2-ClPh           ClMe    Cl   H     2-ClPh           SCHF2Me    Cl   H     2-BrPh           CF3Me    Cl   H     2-MePh           CF3Me    Cl   H     2-CNPh           CF3Me    Cl   H     2-FPh            CF3   R 3   R 4a  R 4b R 5a     R 5bMe    Cl    H    F        CF3Me    Cl    H    Me       SMeMe    Cl    H    Me       OMeMe    Cl    H    Me       OEtMe    Cl    H    Me       n-C3F7Me    Cl    H    Me       i-C3F7Me    Cl    H    Me       EtMe    Cl    H    Me       OCF2CHF2Me    Cl    H    Me       SCF2CHF2Me    Cl    H    Me       SO2MeMe    Cl    H    Me       SO2CF3Me    Cl    H    3-CF3-2-CF3吡啶基Me    Cl    H    CF3     MeMe    Cl    H    OMe      CF3Me    Cl    H    H        CF3Me    Cl    H    H        OCHF2Me    Cl    H    H        C2F5 R 3   R 4a  R 4b   R 5a            R 5bMe    Cl    H    2,6-F2Ph        CF3Me    Cl    H    2,4-F2Ph        CF3Me    Cl    H    2,5-F2Ph        CF3Me    Cl    H    2-MeOPh          CF3Me    Cl    H    3-Cl-2-吡啶基    CF3Me    Cl    H    3-Cl-2-吡啶基    OCF3Me    Cl    H    3-Cl-2-吡啶基    BrMe    Cl    H    3-Cl-2-吡啶基    ClMe    Cl    H    3-Cl-2-吡啶基    SCHF2Me    Cl    H    3-F-2-吡啶基     CF3Me    Cl    H    CF3             CF3Me    Cl    H    3-Me-2-          CF3吡啶基Me    Cl    H    3-Br-2-吡啶基    CF3Me    Cl    H    3-Br-2-吡啶基    OCF3Me    Cl    H    3-Br-2-吡啶基    BrMe    Cl    H    3-Br-2-吡啶基    ClEt    Cl    H    H                C2F5 Table 2 R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me Et R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me Et R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H ClMe H Me H SCF 3 Me H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2 ,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H OCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H ClMe H H H SCF 3 Me H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-Pyridyl CF 3 Me H H 2-Pyridyl ClMe H H 2-ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridylClMeH Me 3-Cl- 2 -pyridylSCHF2MeHMe3-F- 2 -pyridylCF3MeHMe3- CF3-2 - CF3pyridylMeH Me 3-Me-2-CF 3- pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridylClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me BrMe Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMe R 3 R 4a R 4b R 5a R 5b Me H H 3-Cl-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2- PyridylClMeHH 3-Cl- 2 -pyridylSCHF2MeHH3-F - 2-pyridylCF3MeHH3- CF3-2 - CF3pyridylMeHH3-Me-2- CF3pyridine Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me OCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr HCl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 R 3 R 4a R 4b R 5a R 5b Me Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H BrMe H Cl H ClMe H Cl H SCF 3 Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me HCl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-CF 3 -2- CF 3 Pyridyl Me Me H 3-Me-2- CF 3 Pyridyl Me Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me Me H 3-Cl-2- Pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-Br-2-pyridyl CF 3 Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridylClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2 -PyridylBrMeHCl 3-Cl-2-PyridylClMeHCl 3-Cl-2-PyridylSCHF 2 Me H Cl 3-F-2-PyridylCF 3 Me HCl 3-CF 3 -2- CF 3 Pyridyl Me H Cl 3-Me-2- CF 3 Pyridyl Me H Cl 3-Br-2-Pyridyl CF 3 Me H Cl 3-Br-2-Pyridyl OCF 3 Me H Cl 3-Br- 2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe Cl H H OCF 3 Me Cl H H OCF 2 CHF 2 Me Cl H H SCF 2 CHF 2 Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-Pyridyl CF 3 Me Cl H 2-Pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 Me Cl H 2-BrPh CF 3 Me Cl H 2-MePh CF 3 Me Cl H 2-CNPh CF 3 Me ClH2- FPhCF3 R 3 R 4a R 4b R 5a R 5b Me Cl H F CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H 3-CF 3 -2-CF 3 Pyridyl Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H 2,6-F 2 Ph CF 3 Me Cl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2 -MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2- Pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H CF 3 CF 3 Me Cl H 3-Me-2-CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br-2-pyridyl ClEt Cl H H C 2 F 5

                           表3

Figure A0180519000521
R 3   R 4a  R 4b  R 5a R 5bMe    H    Me    H    CF3Me    H    Me    H    OCF3Et    H    Me    H    OCF3Me    H    Me    Me   BrMe    H    Me    Et   BrMe    H    Me    Me   ClMe    H    Me    Et   ClMe    H    Me    Me   IMe    H    Me    Me   CF3   R 3   R 4a R 4b  R 5a  R 5bMe    H    H    H     CF3Me    H    H    H     OCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Me    Me    OCF3Et    H    Me    Me    CF3Me    H    Me    Me    SCF3Me    H    Me    Me    SCHF2Me    H    Me    Me    OCHF2n-Pr  H    Me    Me    CF3Me    H    Me    Me    C2F5Et    H    Me    Me    C2F5Me    H    Me    Et    CF3Me    H    Me    n-Pr  CF3Me    H    Me    i-Pr  CF3Me    H    Me    Cl    CF3Me    H    Me    F     CF3Me    H    Me    Me    SMeMe    H    Me    Me    OMeMe    H    Me    Me    OEtMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    EtMe    H    Me    Me    OCF2CHF2Me    H    Me    Me    SCF2CHF2Me    H    Me    Me    SO2MeMe    H    Me    Me    SO2CF3Me    H    Me    CF3   CF3Me    H    Me    CF3   MeMe    H    Me    OMe   CF3Me    H    Me    H     CF3Me    H    Me    H     OCHF2Me    H    Me    H     C2F5Et    H    Me    H     C2F5Me    H    Me    H     OCF3Me    H    Me    H     OCF2CHF2Me    H    Me    H     SCF2CHF2Me    H    Me    H     n-C3F7Me    H    Me    H     i-C3F7Me    H    Me    H     BrMe    H    Me    H     Cl R 3   R 4a  R 4b R 5a  R 5bMe    H    H    Me    OCF3Et    H    H    Me    CF3Me    H    H    Me    SCF3Me    H    H    Me    SCHF2Me    H    H    Me    OCHF3n-Pr  H    H    Me    CF3Me    H    H    Me    C2F5Et    H    H    Me    C2F5Me    H    H    Et    CF3Me    H    H    n-Pr  CF3Me    H    H    i-Pr  CF3Me    H    H    Cl    CF3Me    H    H    F     CF3Me    H    H    Me    SMeMe    H    H    Me    OMeMe    H    H    Me    OEtMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    EtMe    H    H    Me    OCF2CHF2Me    H    H    Me    SCF2CHF2Me    H    H    Me    SO2MeMe    H    H    Me    SO2CF3Me    H    H    CF3  CF3Me    H    H    CF3  MeMe    H    H    OMe   CF3Me    H    H    H     CF3Me    H    H    H     OCHF2Me    H    H    H     C2F5Et    H    H    H     C2F5Me    H    H    H     CCF3Me    H    H    H     OCF2CHF2Me    H    H    H     SCF2CHF2Me    H    H    H     n-C3F7Me    H    H    H     i-C3F7Me    H    H    H     BrMe    H    H    H     Cl   R 3   R 4a R 4b  R 5a             R 5bMe    H    Me    H                SCF3Me    H    Me    Ph               CF3Me    H    Me    Ph               ClMe    H    Me    Ph               BrMe    H    Me    2-吡啶基         CF3Me    H    Me    2-吡啶基         ClMe    H    Me    2-ClPh           CF3Me    H    Me    2-ClPh           OCF3Me    H    Me    2-ClPh           BrMe    H    Me    2-ClPh           ClMe    H    Me    2-ClPh           SCHF2Me    H    Me    2-BrPh           CF3Me    H    Me    2-MePh           CF3Me    H    Me    2-CNPh           CF3Me    H    Me    2-FPh            CF3Me    H    Me    2,6-F2Ph        CF3Me    H    Me    2,4-F2Ph        CF3Me    H    Me    2,5-F2Ph        CF3Me    H    Me    2-MeOPh          CF3Me    H    Me    3-Cl-2-吡啶基    CF3Me    H    Me    3-Cl-2-吡啶基    OCF3Me    H    Me    3-Cl-2-吡啶基    BrMe    H    Me    3-Cl-2-吡啶基    ClMe    H    Me    3Cl-2-吡啶基     SCHF2Me    H    Me    3-F-2-吡啶基     CF3Me    H    Me    3-CF3-2-        CF3吡啶基Me    H    Me    3-Me-2-          CF3吡啶基Me    H    Me    3-Br-2-吡啶基    CF3Me    H    Me    3-Br-2-吡啶基    OCF3Me    H    Me    3-Br-2-吡啶基    BrMe    H    Me    3-Br-2-吡啶基    ClMe    Me   H     H                CF3Me    Me   H     H                OCF3Et    Me   H     H                OCF3Me    Me   H     Me               Br R 3   R 4a  R 4b R 5a             R 5bMe    H    H    H                SCF3Me    H    H    Ph               CF3Me    H    H    Ph               ClMe    H    H    Ph               BrMe    H    H    2-吡啶基         CF3Me    H    H    2-吡啶基         ClMe    H    H    2-ClPh           CF3Me    H    H    2-ClPh           OCF3Me    H    H    2-ClPh           BrMe    H    H    2-ClPh           ClMe    H    H    2-ClPh           SCHF2Me    H    H    2-BrPh           CF3Me    H    H    2-MePh           CF3Me    H    H    2-CNPh           CF3Me    H    H    2-FPh            CF3Me    H    H    2,6-F2Ph        CF3Me    H    H    2,4-F2Ph        CF3Me    H    H    2,5-F2Ph        CF3Me    H    H    2-MeOPh          CF3Me    H    H    3-Cl-2-吡啶基    CF3Me    H    H    3-Cl-2-吡啶基    OCF3Me    H    H    3-Cl-2-吡啶基    BrMe    H    H    3-Cl-2-吡啶基    ClMe    H    H    3-Cl-2-吡啶基    SCHF2Me    H    H    3-F-2-吡啶基     CF3Me    H    H    3-CF3-2-        CF3吡啶基Me    H    H    3-Me-2-          CF3吡啶基Me    H    H    3-Br-2-吡啶基    CF3Me    H    H    3-Br-2-吡啶基    OCF3Me    H    H    3-Br-2-吡啶基    BrMe    H    H    3-Br-2-吡啶基    ClMe    H    Cl   Et               BrMe    H    Cl   Me               ClMe    H    Cl   Et               ClMe    H    Cl   Me               I R 3   R 4a  R 4b  R 5a  R 5bMe    Me    H    Et    BrMe    Me    H    Me    ClMe    Me    H    Et    ClMe    Me    H    Me    IMe    Me    H    Me    CF3Me    Me    H    Me    OCF3Et    Me    H    Me    CF3Me    Me    H    Me    SCF3Me    Me    H    Me    SCHF2Me    Me    H    Me    OCHF2n-Pr  Me    H    Me    CF3Me    Me    H    Me    C2F5Et    Me    H    Me    C2F5Me    Me    H    Et    CF3Me    Me    H    n-Pr  CF3Me    Me    H    i-Pr  CF3Me    Me    H    Cl    CF3Me    Me    H    F     CF3Me    Me    H    Me    SMeMe    Me    H    Me    OMeMe    Me    H    Me    OEtMe    Me    H    Me    n-C3F7Me    Me    H    Me    i-C3F7Me    Me    H    Me    EtMe    Me    H    Me    OCF2CHF2Me    Me    H    Me    SCF2CHF2Me    Me    H    Me    SO2MeMe    Me    H    Me    SO2CF3Me    Me    H    CF3  CF3Me    Me    H    CF3  MeMe    Me    H    OMe   CF3Me    Me    H    H     CF3Me    Me    H    H     OCHF2Me    Me    H    H     C2F5Et    Me    H    H     C2F5Me    Me    H    H     OCF3Me    Me    H    H     OCF2CHF2 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Cl    Me    CF3Me    H    Cl    Me    OCF3Et    H    Cl    Me    CF3Me    H    Cl    Me    SCF3Me    H    Cl    Me    SCHF2Me    H    Cl    Me    OCHF2n-Pr  H    Cl    Me    CF3Me    H    Cl    Me    C2F5Et    H    Cl    Me    C2F5Me    H    Cl    Et    CF3Me    H    Cl    n-Pr  CF3Me    H    Cl    i-Pr  CF3Me    H    Cl    Cl    CF3Me    H    Cl    F     CF3Me    H    Cl    Me    SMeMe    H    Cl    Me    OMeMe    H    Cl    Me    OEtMe    H    Cl    Me    n-C3F7Me    H    Cl    Me    i-C3F7Me    H    Cl    Me    EtMe    H    Cl    Me    OCF2CHF2Me    H    Cl    Me    SCF2CHF2Me    H    Cl    Me    SO2MeMe    H    Cl    Me    SO2CF3Me    H    Cl    CF3  CF3Me    H    Cl    CF3  MeMe    H    Cl    OMe   CF3Me    H    Cl    H     CF3Me    H    Cl    H     OCHF2Me    H    Cl    H     C2F5Et    H    Cl    H     C2F5Me    H    Cl    H     OCF3Me    H    Cl    H     OCF2CHF2Me    H    Cl    H     SCF2CHF2Me    H    Cl    H     n-C3F7Me    H    Cl    H     i-C3F7Me    H    Cl    H     Br R 3  R 4a  R 4b R 5a                R 5bMe  Me    H    H                SCF2CHF2Me  Me    H    H                n-C3F7Me  Me    H    H                i-C3F7Me  Me    H    H                BrMe  Me    H    H                ClMe  Me    H    H                SCF3Me  Me    H    Ph               CF3Me  Me    H    Ph               ClMe  Me    H    Ph               BrMe  Me    H    2-吡啶基         CF3Me  Me    H    2-吡啶基         ClMe  Me    H    2-ClPh           CF3Me  Me    H    2-ClPh           OCF3Me  Me    H    2-ClPh           BrMe  Me    H    2-ClPh           ClMe  Me    H    2-ClPh           SCHF2Me  Me    H    2-BrPh           CF3Me  Me    H    2-MePh           CF3Me  Me    H    2-CNPh           CF3Me  Me    H    2-FPh            CF3Me  Me    H    2,6-F2Ph        CF3Me  Me    H    2,4-F2Ph        CF3Me  Me    H    2,5-F2Ph        CF3Me  Me    H    2-MeOPh          CF3Me  Me    H    3-Cl-2-吡啶基    CF3Me  Me    H    3-Cl-2-吡啶基    OCF3Me  Me    H    3-CF3-2-        CF3吡啶基Me  Me    H    3-Me-2-          CF3吡啶基Me  Me    H    3-Cl-2-吡啶基    SCHF2Me  Me    H    3-F-2-吡啶基     CF3Me  Me    H    3-Cl-2-吡啶基    BrMe  Me    H    3-Cl-2-吡啶基    ClMe  Me    H    3-Br-2-吡啶基    CF3Me  Me    H    3-Br-2-吡啶基    OCF3Me  Me    H    3-Br-2-吡啶基    Br R 3   R 4a  R 4b  R 5a             R 5bMe    H    Cl    H                ClMe    H    Cl    H                SCF3Me    H    Cl    Ph               CF3Me    H    Cl    Ph               ClMe    H    Cl    Ph               BrMe    H    Cl    2-吡啶基         CF3Me    H    Cl    2-吡啶基         ClMe    H    Cl    2-ClPh           CF3Me    H    Cl    2-ClPh           OCF3Me    H    Cl    2-ClPh           BrMe    H    Cl    2-ClPh           ClMe    H    Cl    2-ClPh           SCHF2Me    H    Cl    2-BrPh           CF3Me    H    Cl    2-MePh           CF3Me    H    Cl    2-CNPh           CF3Me    H    Cl    2-FPh            CF3Me    H    Cl    2,6-F2Ph        CF3Me    H    Cl    2,4-F2Ph        CF3Me    H    Cl    2,5-F2Ph        CF3Me    H    Cl    2-MeOPh          CF3Me    H    Cl    3-Cl-2-吡啶基    CF3Me    H    Cl    3-Cl-2-吡啶基    OCF3Me    H    Cl    3-Cl-2-吡啶基    BrMe    H    Cl    3-Cl-2-吡啶基    ClMe    H    Cl    3-Cl-2-吡啶基    SCHF2Me    H    Cl    3-F-2-吡啶基     CF3Me    H    Cl    3-CF3-2-        CF3吡啶基Me    H    Cl    3-Me-2-          CF3吡啶基Me    H    Cl    3-Br-2-吡啶基    CF3Me    H    Cl    3-Br-2-吡啶基    OCF3Me    H    Cl    3-Br-2-吡啶基    BrMe    H    Cl    3-Br-2-吡啶基    ClMe    Cl   H     H                OCF3Me    Cl   H     H                OCF2CHF2Me    Cl   H     H                SCF2CHF2 R 3   R 4a  R 4b R 5a          R 5bMe    Me    H  3-Br-2-吡啶基 ClMe    Cl    H  Me            BrMe    Cl    H  Et            BrMe    Cl    H  Me            ClMe    Cl    H  Et            ClMe    Cl    H  Me            IMe    Cl    H  Me            CF3Me    Cl    H  Me            OCF3Et    Cl    H  Me            CF3Me    Cl    H  Me            SCF3Me    Cl    H  Me            SCHF2Me    Cl    H  Me            OCHF2n-Pr  Cl    H  Me            CF3Me    Cl    H  Me            C2F5Et    Cl    H  Me            C2F5Me    Cl    H  Et            CF3Me    Cl    H  n-Pr          CF3Me    Cl    H  i-Pr          CF3Me    Cl    H  Cl            CF3Me    Cl    H  F             CF3Me    Cl    H  Me            SMeMe    Cl    H  Me            OMeMe    Cl    H  Me            OEtMe    Cl    H  Me            n-C3F7Me    Cl    H  Me            i-C3F7Me    Cl    H  Me            EtMe    Cl    H  Me            OCF2CHF2Me    Cl    H  Me            SCF2CHF2Me    Cl    H  Me            SO2MeMe    Cl    H  Me            SO2CF3Me    Cl    H  3-CF3-2-     CF3吡啶基Me    Cl    H  CF3          MeMe    Cl    H  OMe           CF3Me    Cl    H  H             CF3Me    Cl    H  H             OCHF2Me    Cl    H  H             C2F5 R 3   R 4a  R 4b  R 5a              R 5bMe    Cl    H    H                n-C3F7Me    Cl    H    H                i-C3F7Me    Cl    H    H                BrMe    Cl    H    H                ClMe    Cl    H    H                SCF3Me    Cl    H    Ph               CF3Me    Cl    H    Ph               ClMe    Cl    H    Ph               BrMe    Cl    H    2-吡啶基         CF3Me    Cl    H    2-吡啶基         ClMe    Cl    H    2-ClPh           CF3Me    Cl    H    2-ClPh           OCF3Me    Cl    H    2-ClPh           BrMe    Cl    H    2-ClPh           ClMe    Cl    H    2-ClPh           SCHF2Me    Cl    H    2-BrPh           CF3Me    Cl    H    2-MePh           CF3Me    Cl    H    2-CNPh           CF3Me    Cl    H    2-FPh            CF3Me    Cl    H    2,6-F2Ph        CF3Me    Cl    H    2,4-F2Ph        CF3Me    Cl    H    2,5-F2Ph        CF3Me    Cl    H    2-MeOPh          CF3Me    Cl    H    3-Cl-2-吡啶基    CF3Me    Cl    H    3-Cl-2-吡啶基    OCF3Me    Cl    H    3-Cl-2-吡啶基    BrMe    Cl    H    3-Cl-2-吡啶基    ClMe    Cl    H    3-Cl-2-吡啶基    SCHF2Me    Cl    H    3-F-2-吡啶基     CF3Me    Cl    H    CF3             CF3Me    Cl    H    3-Me-2-          CF3吡啶基Me    Cl    H    3-Br-2-吡啶基    CF3Me    Cl    H    3-Br-2-吡啶基    OCF3Me    Cl    H    3-Br-2-吡啶基    BrMe    Cl    H    3-Br-2-吡啶基    ClEt    Cl    H    H                C2F5 table 3
Figure A0180519000521
R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me EtMe H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H Cl R 3 R 4a R 4b R 5a R 5b Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 3 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me EtMe H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H CCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H Cl R 3 R 4a R 4b R 5a R 5b Me H Me H SCF 3 Me H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2 -ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3- Cl-2-pyridylClMe H Me 3Cl-2-pyridyl SCHF 2 Me H Me 3-F-2-pyridyl CF 3 Me H Me 3-CF 3 -2 -CF 3pyridyl Me H Me 3-Me -2- CF 3 pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br -2-PyridylClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me Br R 3 R 4a R 4b R 5a R 5b Me H H H SCF 3 Me H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-pyridyl CF 3 Me H H 2-pyridyl ClMe H H 2-ClPh CF 3 Me H H 2- ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2 -FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2-pyridyl ClMe H H 3-Cl-2-pyridyl SCHF 2 Me H H 3-F- 2-pyridyl CF 3 Me H H 3-CF 3 -2- CF 3 pyridyl Me H H 3-Me-2- CF 3 pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2 -pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me I R 3 R 4a R 4b R 5a R 5b Me Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMeMe Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 R 3 R 4a R 4b R 5a R 5b Me H Cl Me CF 3 Me H Cl Me OCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H Br R 3 R 4a R 4b R 5a R 5b Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-CF 3 -2- CF 3 pyridyl Me Me H 3-Me-2- CF 3 pyridyl Me Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-Br-2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl Br R 3 R 4a R 4b R 5a R 5b Me H Cl H ClMe H Cl H SCF 3 Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe HCl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me H Cl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2-pyridyl BrMe H Cl 3-Cl-2-pyridylClMe H Cl 3-Cl-2-pyridylSCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me H Cl 3-CF 3 -2 -CF 3pyridylMeH Cl 3-Me-2-CF 3- pyridyl Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me H Cl 3-Br-2-pyridyl BrMe H Cl 3-Br-2-pyridylClMe Cl H H OCF 3 Me Cl H H OCF 2 CHF 2 Me Cl H H SCF 2 CHF 2 R 3 R 4a R 4b R 5a R 5b Me Me H 3-Br-2-pyridyl ClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 Me Cl H F CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H 3 -CF 3 -2- CF 3 pyridyl Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-pyridyl CF 3 Me Cl H 2-pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 MeClH 2-BrPh CF 3 MeClH 2-MePh CF 3 MeClH 2-CNPh CF 3 MeClH 2-FPh CF 3 MeClH 2,6-F 2 PhCF 3 MeClH 2, 4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2-MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridine OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2-pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H CF 3 CF 3 Me Cl H 3-Me-2- CF 3 Pyridyl Me Cl H 3-Br-2-Pyridyl CF 3 Me Cl H 3-Br-2-Pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMeCl H 3-Br-2-pyridyl ClEt Cl H H C 2 F 5

                                      表4

Figure A0180519000581
R 3   R 4a  R 4b  R 5a  R 5bMe    H    Me    H     CF3Me    H    Me    H     OCF3Et    H    Me    H     OCF3Me    H    Me    Me    BrMe    H    Me    E     BrMe    H    Me    Me    ClMe    H    Me    Et    ClMe    H    Me    Me    IMe    H    Me    Me    CF3Me    H    Me    Me    OCF3Et    H    Me    Me    CF3Me    H    Me    Me    SCF3Me    H    Me    Me    SCHF2Me    H    Me    Me    OCHF2n-Pr  H    Me    Me    CF3Me    H    Me    Me    C2F5Et    H    Me    Me    C2F5Me    H    Me    El    CF3Me    H    Me    B-Pr  CF3Me    H    Me    i-Pr  CF3Me    H    Me    i-Pr  OCF3Me    H    Me    Me    SMeMe    H    Me    Me    OMeMe    H    Me    Me    OEtMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    EtMe    H    Me    Me    OCF2CHF2 R 3   R 4a  R 4b  R 5a  R 5bMe    H    H     H     CF3Me    H    H     H     OCF3Et    H    H     H     OCF3Me    H    H     Me    BrMe    H    H     Et    BrMe    H    H     Me    ClMe    H    H     Et    ClMe    H    H     Me    IMe    H    H     Me    CF3Me    H    H     Me    OCF3Et    H    H     Me    CF3Me    H    H     Me    SCF3Me    H    H     Me    SCHF2Me    H    H     Me    OCHF2n-Pr  H    H     Me    CF3Me    H    H     Me    C2F5Et    H    H     Me    C2F5Me    H    H     Et    CF3Me    H    H     n-Pr  CF3Me    H    H     i-Pr  CF3Me    H    H     Me    SMeMe    H    H     Me    OMeMe    H    H     Me    OEtMe    H    H     Me    n-C3F7Me    H    H     Me    i-C3F7Me    H    H     Me    EtMe    H    tH    Me    OCF2CHF2Me    H    H     Me    SCF2CHF2 R 3   R 4a  R 4b  R 5a             R 5bMe    H    Me    Me               SCF2CHF2Me    H    Me    Me               SO2MeMe    H    Me    Me               SO2CF3Me    H    Me    CHF2            CF3Me    H    Me    CHF2            MeMe    H    Me    Ph               CF3Me    H    Me    Ph               ClMe    H    Me    Ph               BrMe    H    Me    2-吡啶基         CF3Me    H    Me    2-吡啶基         ClMe    H    Me    2-ClPh           CF3Me    H    Me    2-ClPh           OCF3Me    H    Me    2-ClPh           BrMe    H    Me    2-ClPh           ClMe    H    Me    2-ClPh           SCHF2Me    H    Me    2-BrPh           CF3Me    H    Me    2-MePh           CF3Me    H    Me    2-CNPh           CF3Me    H    Me    2-FPh            CF3Me    H    Me    2,6-F2Ph        CF3Me    H    Me    2,4-F2Ph        CF3Me    H    Me    2,5-F2Ph        CF3Me    H    Me    2-MeOPh          CF3Me    H    Me    3-Cl-2-吡啶基    CF3Me    H    Me    3-Cl-2-吡啶基    OCF3Me    H    Me    3-Cl-2-吡啶基    BrMe    H    Me    3-Cl-2-吡啶基    ClMe    H    Me    3-Cl-2-吡啶基    SCHF2Me    H    Me    3-CF3-2-        CF3吡啶基Me    H    Me    3-Me-2-          CF3吡啶基Me    H    Me    3-F-2-吡啶基     CF3Me    H    Me    3-Br-2-吡啶基    CF3Me    H    Me    3-Br-2-吡啶基    OCF3Me    H    Me    3-Br-2-吡啶基    BrMe    H    Me    3-Br-2-吡啶基    Cl R 3   R 4a  R 4b R 5a             R 5bMe    H    H    Me               SC2MeMe    H    H    Me               SO2CF3Me    H    H    CF3             CF3Me    H    H    CF3             MeMe    H    H    Ph               CF3Me    H    H    Ph               ClMe    H    H    Ph               BrMe    H    H    2-吡啶基         CF3Me    H    H    2-吡啶基         ClMe    H    H    2-ClPh           CF3Me    H    H    2-ClPh           OCF3Me    H    H    2-ClPh           BrMe    H    H    2-ClPh           ClMe    H    H    2-ClPh           SCHF2Me    H    H    2-BrPh           CF3Me    H    H    2-MePh           CF3Me    H    H    2-CNPh           CF3Me    H    H    2-FPh            CF3Me    H    H    2,6-F2Ph        CF3Me    H    H    2,4-F2Ph        CF3Me    H    H    2,5-F2Ph        CF3Me    H    H    2-MeOPh          CF3Me    H    H    3-Cl-2-吡啶基    CF3Me    H    H    3-Cl-2-吡啶基    OCF3Me    H    H    3-Cl-2-吡啶基    BrMe    H    H    3-Cl-2-吡啶基    ClMe    H    H    3-Cl-2-吡啶基    SCHF2Me    H    H    3-F-2-吡啶基     CF3Me    H    H    3-CF3-2-        CF3吡啶基Me    H    H    3-Me-2-          CF3吡啶基Me    H    H    3-Br-2-吡啶基    CF3Me    H    H    3-Br-2-吡啶基    OCF3Me    H    H    3-Br-2-吡啶基    BrMe    H    H    3-Br-2-吡啶基    ClMe    H    Cl   Et               Br R 3   R 4a  R 4b  R 5a    R 5bMe    Me    H    Me      BrMe    Me    H    E       BrMe    Me    H    Me      ClMe    Me    H    Et      ClMe    Me    H    Me      IMe    Me    H    Me      CF3Me    Me    H    Me      OCF3Et    Me    H    Me      CF3Me    Me    H    Me      SCF3Me    Me    H    Me      SCHF2Me    Me    H    Me      OCHF2n-Pr  Me    H    Me      CF3Me    Me    H    Me      C2F5Et    Me    H    Me      C2F5Me    Me    H    Et      CF3Me    Me    H    n-Pr    CF3Me    Me    H    i-Pr    CF3Me    Me    H    Me      SMeMe    Me    H    Me      OMeMe    Me    H    Me      OEtMe    Me    H    Me      n-C3F7Me    Me    H    Me      i-C3F7Me    Me    H    Me      EtMe    Me    H    Me      OCF2CHF2Me    Me    H    Me      SCF2CHF2Me    Me    H    Me      SO2MeMe    Me    H    Me      SO2CF3Me    Me    H    CF3    CF3Me    Me    H    CF3    MeMe    Me    H    Ph      CF3Me    Me    H    Ph      ClMe    Me    H    Ph      BrMe    Me    H    2-吡啶基CF3Me    Me    H    2-吡啶基ClMe    Me    H    2-ClPh  CF3Me    Me    H    2-ClPh  OCF3Me    Me    H    2-ClPh  Br R 3   R 4a  R 4b  R 5a      R 5bMe    H    Cl    Me        ClMe    H    Cl    Et        ClMe    H    Cl    Me        IMe    H    Cl    Me        CF3Me    H    Cl    Me        OCF3Et    H    Cl    Me        CF3Me    H    Cl    Me        SCF3Me    H    Cl    Me        SCHF2Me    H    Cl    Me        OCHF2n-Pr  H    Cl    Me        CF3Me    H    Cl    Me        C2F5Et    H    Cl    Me        C2F5Me    H    Cl    Et        CF3Me    H    Cl    n-Pr      CF3Me    H    Cl    i-Pr      CF3Me    H    Cl    Me        SMeMe    H    Cl    Me        OMeMe    H    Cl    Me        OEtMe    H    Cl    Me        n-C3F7Me    H    Cl    Me        i-C3F7Me    H    Cl    Me        EtMe    H    Cl    Me        OCF2CHF2Me    H    Cl    Me        SCF2CHF2Me    H    Cl    Me        SO2MeMe    H    Cl    Me        SO2CF3Me    H    Cl    CF3      CF3Me    H    Cl    CF3      MeMe    H    Cl    Ph        CF3Me    H    Cl    Ph        ClMe    H    Cl    Ph        BrMe    H    Cl    2-吡啶基  CF3Me    H    Cl    2-吡啶基  ClMe    H    Cl    2-ClPh    CF3Me    H    Cl    2-ClPh    OCF3Me    H    Cl    2-ClPh    BrMe    H    Cl    2-ClPh    ClMe    H    Cl    2-ClPh    SCHF2   R 3   R 4a  R 4b  R 5a            R 5bMe    Me    H    2-ClPh           ClMe    Me    H    2-ClPh           SCHF2Me    Me    H    2-BrPh           CF3Me    Me    H    2-MePh           CF3Me    Me    H    2-CNPh           CF3Me    Me    H    2-FPh            CF3Me    Me    H    2,6-F2Ph        CF3Me    Me    H    2,4-F2Ph        CF3Me    Me    H    2,5-F2Ph        CF3Me    Me    H    2-MeOPh          CF3Me    Me    H    3-Cl-2-吡啶基    CF3Me    Me    H    3-Cl-2-吡啶基    OCF3Me    Me    H    3-Cl-2-吡啶基    BrMe    Me    H    3-Cl-2-吡啶基    ClMe    Me    H    3-CF3-2-        CF3吡啶基Me    Me    H    3-Me-2-          CF3吡啶基Me    Me    H    3-Cl-2-吡啶基    SCHF2Me    Me    H    3-F-2-吡啶基     CF3Me    Me    H    3-Br-2-吡啶基    CF3Me    Me    H    3-Br-2-吡啶基    OCF3Me    Me    H    3-Br-2-吡啶基    BrMe    Me    H    3-Br-2-吡啶基    ClMe    Cl    H    Me               BrMe    Cl    H    Et               BrMe    Cl    H    Me               ClMe    Cl    H    Et               ClMe    Cl    H    Me               IMe    Cl    H    Me               CF3Me    Cl    H    Me               OCF3Et    Cl    H    Me               CF3Me    Cl    H    Me               SCF3Me    Cl    H    Me               SCHF2Me    Cl    H    Me               OCHF2n-Pr  Cl    H    Me               CF3Me    Cl    H    Me               C2F5   R 3  R 4a   R 4b   R 5a        R 5bMe    H     Cl   2-BrPh        CF3Me    H     Cl   2-MePh        CF3Me    H     Cl   2-CNPh        CF3Me    H     Cl   2-FPh         CF3Me    H     Cl   2,6-F2Ph     CF3Me    H     Cl   2,4-F2Ph     CF3Me    H     Cl   2,5-F2Ph     CF3Me    H     Cl   2-OMe         CF3Me    H     Cl   3-Cl-2-吡啶基 CF3Me    H     Cl   3-Cl-2-吡啶基 OCF3Me    H     Cl   3-Cl-2-吡啶基 BrMe    H     Cl   3-Cl-2-吡啶基 ClMe    H     Cl   3-Cl-2-吡啶基 SCHF2Me    H     Cl   3-F-2-吡啶基  CF3Me    H     Cl   3-CF3-2-     CF3吡啶基Me    H     Cl   3-Me-2-       CF3吡啶基Me    H     Cl   3-Br-2-吡啶基 CF3Me    H     Cl   3-Br-2-吡啶基 OCF3Me    H     Cl   3-Br-2-吡啶基 BrMe    H     Cl   3-Br-2-吡啶基 ClMe    Cl    H    Et            CF3Me    Cl    H    n-Pr          CF3Me    Cl    H    i-Pr          CF3Me    Cl    H    Me            SMeMe    Cl    H    Me            OMeMe    Cl    H    Me            OEtMe    Cl    H    Me            n-C3F7Me    Cl    H    Me            i-C3F7Me    Cl    H    Me            EtMe    Cl    H    Me            OCF2CHF2Me    Cl    H    Me            SCF2CHF2Me    Cl    H    Me            SO2MeMe    Cl    H    Me            SO2CF3Me    Cl    H    CF3          CF3Me    Cl    H    CF3          Me R 3   R 4a  R 4b  R 5a             R 5bEt    Cl    H    Me               C2F5Me    Cl    H    3-Cl-2-吡啶基    CF3Me    Cl    H    3-Cl-2-吡啶基    OCF3Me    Cl    H    3-Cl-2-吡啶基    BrMe    Cl    H    3-Cl-2-吡啶基    ClMe    Cl    H    3-Cl-2-吡啶基    SCHF2Me    Cl    H    3-F-2-吡啶基     CF3Me    Cl    H    3-CF3-2-        CF3吡啶基Me    Cl    H    3-Br-2-吡啶基    CF3Me    Cl    H    3-Br-2-吡啶基    OCF3Me    Cl    H    3-Br-2-吡啶基    BrMe    Cl    H    3-Br-2-吡啶基    ClMe    Cl    H    2,4-F2Ph        CF3Me    Cl    H    2,5-F2Ph        CF3Me    Cl    H    2-OMe            CF3Me    Cl    H    2-ClPh           Br   R 3   R 4a  R 4b R 5a         R 5bMe    Cl    H    OMe         CF3Me    Cl    H    Ph          CF3Me    Cl    H    Ph          ClMe    Cl    H    Ph          BrMe    Cl    H    2-吡啶基    CF3Me    Cl    H    2-吡啶基    ClMe    Cl    H    2-ClPh      CF3Me    Cl    H    3-Me-2-     CF3吡啶基Me    Cl    H    2-ClPh      ClMe    Cl    H    2-ClPh      SCHF2Me    Cl    H    2-BrPh      CF3Me    Cl    H    2-MePh      CF3Me    Cl    H    2-CNPh      CF3Me    Cl    H    2-FPh       CF3Me    Cl    H    2,6-F2Ph   CF3Me    Cl    H    2-ClPh      OCF3 Table 4
Figure A0180519000581
R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me E BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me El CF 3 Me H Me B-Pr CF 3 Me H Me i-Pr CF 3 Me H Me i-Pr OCF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me EtMe H Me Me OCF 2 CHF 2 R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me EtMe H tH Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 R 3 R 4a R 4b R 5a R 5b Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CHF 2 CF 3 Me H Me CHF 2 MeMe H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2 -ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridyl ClMe H Me 3-Cl-2-pyridyl SCHF 2 Me H Me 3-CF 3 -2- CF 3 pyridyl Me H Me 3-Me-2- CF 3 pyridyl Me H Me 3-F-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridyl Cl R 3 R 4a R 4b R 5a R 5b Me H H Me SC 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-pyridyl CF 3 Me H H 2-pyridyl ClMe H H 2-ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2-pyridyl ClMe H H 3-Cl-2-pyridyl SCHF 2 Me H H 3-F-2-pyridyl CF 3 Me H H 3-CF 3 -2- CF 3 pyridyl Me H H 3-Me-2- CF 3 pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et Br R 3 R 4a R 4b R 5a R 5b Me Me H Me BrMe Me H E BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n- Pr CF 3 Me Me H i-Pr CF 3 Me Me H Me SMeMe Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh Br R 3 R 4a R 4b R 5a R 5b Me H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me OCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i -Pr CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 R 3 R 4a R 4b R 5a R 5b Me Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-Cl-2-pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-CF 3 -2- CF 3 Pyridyl Me Me H 3-Me-2- CF 3 Pyridyl Me Me H 3-Cl-2-Pyridyl SCHF 2 Me Me H 3-F-2-Pyridyl CF 3 Me Me H 3-Br-2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridyl ClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me H Cl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 Me H Cl 2-OMe CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me HCl 3-Cl-2-pyridyl OCF 3 Me H Cl 3-Cl-2-pyridyl BrMe H Cl 3-Cl-2-pyridyl ClMe H Cl 3-Cl-2-pyridyl SCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me H Cl 3-CF 3 -2- CF 3 pyridyl Me H Cl 3-Me-2- CF 3 pyridyl Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me H Cl 3-Br-2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H CF 3 CF 3 Me Cl H CF 3 Me R 3 R 4a R 4b R 5a R 5b Et Cl H Me C 2 F 5 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl -2-pyridylBrMeCl H 3-Cl-2-pyridylClMeCl H 3-Cl-2-pyridylSCHF 2 MeClH 3-F-2-pyridyl CF 3 MeCl H 3-CF 3 - 2- CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br- 2-PyridylClMeCl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2-OMe CF 3 Me Cl H 2-ClPh Br R 3 R 4a R 4b R 5a R 5b Me Cl H OMe CF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-pyridyl CF 3 Me Cl H 2-pyridyl ClMe Cl H 2 -ClPh CF 3 Me Cl H 3-Me-2- CF 3 pyridyl Me Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 Me Cl H 2-BrPh CF 3 Me Cl H 2-MePh CF 3 Me Cl H 2-CNPh CF 3 Me Cl H 2-FPh CF 3 Me Cl H 2,6-F 2 Ph CF 3 Me Cl H 2-ClPh OCF 3

                                表5 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Me    H     CHF2Me    H    Me    H     CH2CF3Et    H    Me    H     CH2CF3Me    H    Me    Me    CH2CF3Me    H    Me    Et    CH2CF3Me    H    Me    Me    CF2CHF2Me    H    Me    Et    CHF2Me    H    Me    Me    CHF2Me    H    Me    Me    CBrF2Me    H    Me    Me    CH2   R 3   R 4a R 4b  R 5a  R 5bMe    H    H    H     CHF2Me    H    H    H     CH2CF3Et    H    H    H     CH2CF3Me    H    H    Me    CH2CF3Me    H    H    Et    CH2CF3Me    H    H    Me    CF2CHF2Me    H    H    Et    CHF2Me    H    H    Me    CHF2Me    H    H    Me    CBrF2Me    H    H    Me    CHF2   R 3  R 4a  R 4b  R 5a  R 5bEt    H    Me    Me    CH2CF3Me    H    Me    Me    EtMe    H    Me    Me    n-PrMe    H    Me    Me    CH2C2F5n-Pr  H    Me    Me    CH2CF3Me    H    Me    Me    CF3Et    H    Me    Me    C2F5Me    H    Me    Et    CHF2Me    H    Me    n-Pr  CH2CF3Me    H    Me    i-Pr  CHF2Me    H    Me    Cl    CH2CF3Me    H    Me    F     CH2CF3Me    H    Me    Me    CH2ClMe    H    Me    Me    CClF2Me    H    Me    Me    CH2CH2ClMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    AllylMe    H    Me    Et    CF2CHF2Me    H    Me    Et    i-C3F7Me    H    Me    i-Pr  CF2CHF2Me    H    Me    n-Pr  CF2CHF2Me    H    Me    CF3  CF2CHF2Me    H    Me    CF3  MeMe    H    Me    OMe   CH2CF3Me    H    Me    H     CH2CF3Me    H    Me    H     CH2CF3Me    H    Me    H     C2F5Et    H    Me    H     C2F5Me    H    Me    H     C2F5Me    H    Me    H     CF2CHF2Me    H    Me    i-Pr  CH2CF3Me    H    Me    H     n-C3F7Me    H    Me    H     i-C3F7Me    H    Me    Ph    CH2CF3Me    H    Me    Ph    CF2CHF2Me    H    Me    Ph    CF3 R 3   R 4a  R 4b R 5a  R 5bEt    H    H    Me    CH2CF3Me    H    H    Me    EtMe    H    H    Me    n-PrMe    H    H    Me    CH2C2F5n-Pr  H    H    Me    CH2CF3Me    H    H    Me    CF3Et    H    H    Me    C2F5Me    H    H    Et    CHF2Me    H    H    n-Pr  CH2CF3Me    H    H    i-Pr  CHF2Me    H    H    Cl    CH2CF3Me    H    H    F     CH2CF3Me    H    H    Me    CH2ClMe    H    H    Me    CClF2Me    H    H    Me    CH2CH2ClMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    AllylMe    H    H    Me    CF2CHF2Me    H    H    Me    i-C3F7Me    H    H    Me    CF2CHF2Me    H    H    Me    CF2CHF2Me    H    H    CF3  CF2CHF2Me    H    H    CF3  MeMe    H    H    OMe   CH2CF3Me    H    H    H     CH2CF3Me    H    H    H     CH2CF3Me    H    H    H     C2F5Et    H    H    H     C2F5Me    H    H    H     C2F5Me    H    H    H     CF2CHF2Me    H    H    H     CH2CF3Me    H    H    H     n-C3F7Me    H    H    H     i-C3F7Me    H    H    H     CH2CF3Me    H    H    H     CF2CHF2Me    H    H    H     CHF2 R 3   R 4a  R 4b  R 5a           R 5bMe    H    Me    2-吡啶基       CH2CF3Me    H    Me    2-吡啶基       CF2CHF2Me    H    Me    2-ClPh         CH2CF3Me    H    Me    2-ClPh         CF2CHF2Me    H    Me    2-ClPh         CHF2Me    H    Me    2-ClPh         EtMe    H    Me    2-ClPh         CBrF2Me    H    Me    2-BrPh         CH2CF3Me    H    Me    2-MePh         CH2CF3Me    H    Me    2-CNPh         CH2CF3Me    H    Me    2-FPh          CH2CF3Me    H    Me    2,6-F2Ph      CH2CF3Me    H    Me    2,4-F2Ph      CH2CF3Me    H    Me    2,5-F2Ph      CH2CF3Me    H    Me    2-MeOPh        CH2CF3Me    H    Me    3-Cl-2-吡啶基  CH2CF3Me    H    Me    3-Cl-2-吡啶基  CF2CHF2Me    H    Me    3-Cl-2-吡啶基  CF3Me    H    Me    3-Cl-2-吡啶基  CHF2Me    H    Me    3-Cl-2-吡啶基  CBrF2Me    H    Me    3-F-2-吡啶基   CH2CF3Me    H    Me    3-CF3-2-      CH2CF3吡啶基Me    H    Me    3-Me-2-        CH2CF3吡啶基Me    H    Me    3-Br-2-吡啶基  CF3Me    H    Me    3-Br-2-吡啶基  CH2CF3Me    H    Me    3-Br-2-吡啶基  CF2CHF2Me    H    Me    3-Br-2-吡啶基  CClF2Me    Me   H     H              CHF2Me    Me   H     H              CH2CF3Et    Me   H     H              CH2CF3Me    Me   H     Me             CH2CF3Me    Me   H     Et             CH2CF3Me    Me   H     Me             CF2CHF2Me    Me   H     Et             CHF2Me    Me   H     Me             CHF2 R 3   R 4a  R 4b R 5a             R 5bMe    H    H    Ph              CH2CF3Me    H    H    Ph              CF2CHF2Me    H    H    Ph              CH2CF3Me    H    H    2-吡啶基        CF2CHF2Me    H    H    2-吡啶基        CHF2Me    H    H    2-ClPh          EtMe    H    H    2-ClPh          CBrF2Me    H    H    2-ClPh          CH2CF3Me    H    H    2-ClPh          CH2CF3Me    H    H    2-ClPh          CH2CF3Me    H    H    2-BrPh          CH2CF3Me    H    H    2-MePh          CH2CF3Me    H    H    2-CNPh          CH2CF3Me    H    H    2-FPh           CH2CF3Me    H    H    2,6-F2Ph       CH2CF3Me    H    H    2,4-F2Ph       CH2CF3Me    H    H    2,5-F2Ph       CF2CHF2Me    H    H    2-MeO Ph        CF3Me    H    H    3-Cl-2-吡啶基   CHF2Me    H    H    3-Cl-2-吡啶基   CBrF2Me    H    H    3-Cl-2-吡啶基   CH2CF3Me    H    H    3-CF3-2-       CH2CF3吡啶基Me    H    H    3-Me-2-         CF2CHF2吡啶基Me    H    H    3-F-2-吡啶基    CF3Me    H    H    3-Cl-2-吡啶基   CH2CF3Me    H    H    3-Cl-2-吡啶基   CH2CF3Me    H    H    3-Br-2-吡啶基   CClF2Me    H    H    3-Br-2-吡啶基   CH2CF3Me    H    H    3-Br-2-吡啶基   CF3Me    H    H    3-Br-2-吡啶基   CF3Me    H    Cl   Et              CHF2Me    H    Cl   Me              CH2CF3Me    H    Cl   Et              CH2CF3Me    H    Cl   Me              CH2CF3Me    H    Cl   Me              CH2CF3 R 3   R 4a  R 4b  R 5a   R 5bMe    Me    H    Me     CBrF2Me    Me    H    Me     CHF2Et    Me    H    Me     CH2CF3Me    Me    H    Me     EtMe    Me    H    Me     n-PrMe    Me    H    Me     CH2C2F5n-Pr  Me    H    Me     CH2CF3Me    Me    H    Me     CF3Et    Me    H    Me     C2F5Me    Me    H    Et     CHF2Me    Me    H    n-Pr   CH2CF3Me    Me    H    i-Pr   CHF2Me    Me    H    Cl     CH2CF3Me    Me    H    F      CH2CF3Me    Me    H    Me     CH2ClMe    Me    H    Me     CClF2Me    Me    H    Me     CH2CH2ClMe    Me    H    Me     n-C3F7Me    Me    H    Me     i-C3F7Me    Me    H    Me     AllylMe    Me    H    Me     CF2CHF2Me    Me    H    Me     i-C3F7Me    Me    H    Me     CF2CHF2Me    Me    H    Me     CF2CHF2Me    Me    H    CF3   CF2CHF2Me    Me    H    CF3   MeMe    Me    H    OMe    CH2CF3Me    Me    H    H      CH2CF3Me    Me    H    H      CH2CF3Me    Me    H    H      C2F5Et    Me    H    H      C2F5Me    Me    H    H      C2F5Me    Me    H    H      CF2CHF2Me    Me    H    H      CH2CF3Me    Me    H    H      n-C3F7Me    Me    H    H      i-C3F7Me    Me    H    H      CH2CF3 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Cl    Me    CF2CHF2Et    H    Cl    Me    CHF2Me    H    Cl    Me    CHF2Me    H    Cl    Me    CBrF2Me    H    Cl    Me    CHF2n-Pr  H    Cl    Me    CH2CF3Me    H    Cl    Me    EtEt    H    Cl    Me    n-PrMe    H    Cl    Et    CH2C2F5Me    H    Cl    n-Pr  CH2CF3Me    H    Cl    i-Pr  CF3Me    H    Cl    Cl    C2F5Me    H    Cl    F     CHF2Me    H    Cl    Me    CH2CF3Me    H    Cl    Me    CHF2Me    H    Cl    Me    CH2CF3Me    H    Cl    Me    CH2CF3Me    H    Cl    Me    CH2ClMe    H    Cl    Me    CClF2Me    H    Cl    Me    CH2CH2ClMe    H    Cl    Me    n-C3F7Me    H    Cl    Me    i-C3F7Me    H    Cl    Me    AllylMe    H    Cl    CF3  CF2CHF2Me    H    Cl    CF3  i-C3F7Me    H    Cl    OMe   CF2CHF2Me    H    Cl    H     CF2CHF2Me    H    Cl    H     CF2CHF2Me    H    Cl    H     MeEt    H    Cl    H     CH2CF3Me    H    Cl    H     CH2CF3Me    H    Cl    H     CH2CF3Me    H    Cl    H     C2F5Me    H    Cl    H     C2F5Me    H    Cl    H     C2F5Me    H    Cl    H     CF2CHF2Me    H    Cl    H     CH2CF3     R 3   R 4a  R 4b R 5a            R 5bMe    Me    H    H              CF2CHF2Me    Me    H    H              CHF2Me    Me    H    Ph             CH2CF3Me    Me    H    Ph             CF2CHF2Me    Me    H    Ph             CH2CF3Me    Me    H    2-吡啶基       CF2CHF2Me    Me    H    2-吡啶基       CHF2Me    Me    H    2-ClPh         EtMe    Me    H    2ClPh          CBrF2Me    Me    H    2-ClPh         CH2CF3Me    Me    H    2-ClPh         CH2CF3Me    Me    H    2-ClPh         CH2CF3Me    Me    H    2-BrPh         CH2CF3Me    Me    H    2-MePh         CH2CF3Me    Me    H    2-CNPh         CH2CF3Me    Me    H    2-FPh          CH2CF3Me    Me    H    2,6-F2Ph      CH2CF3Me    Me    H    2,4-F2Ph      CH2CF3Me    Me    H    2,5-F2Ph      CF2CHF2Me    Me    H    2-MeOPh        CF3Me    Me    H    3-Cl-2-吡啶基  CHF2Me    Me    H    3-Cl-2-吡啶基  CBrF2Me    Me    H    3-Cl-2-吡啶基  CH2CF3Me    Me    H    3-Cl-2-吡啶基  CH2CF3Me    Me    H    3-Cl-2-吡啶基  CH2CF3Me    Me    H    3-F-2-吡啶基   CF3Me    Me    H    3-CF3-2-      CH2CF3吡啶基Me    Me    H    3-Me-2-        CF2CHF2吡啶基Me    Me    H    3-Br-2-吡啶基  CClF2Me    Me    H    3-Br-2-吡啶基  CH2CF3Me    Me    H    3-Br-2-吡啶基  CF3Me    Me    H    3-Br-2-吡啶基  CF3Me    Cl    H    Me             CHF2Me    Cl    H    Et             CH2CF3Me    Cl    H    Me             CH2CF3 R 3   R 4a  R 4b  R 5a           R 5bMe    H    Cl    H              n-C3F7Me    H    Cl    Ph             i-C3F7Me    H    Cl    Ph             CH2CF3Me    H    Cl    Ph             CF2CHF2Me    H    Cl    2-吡啶基       CHF2Me    H    Cl    2-吡啶基       CH2CF3Me    H    Cl    2-ClPh         CF2CHF2Me    H    Cl    2-ClPh         CH2CF3Me    H    Cl    2-ClPh         CF2CHF2Me    H    Cl    2-ClPh         CHF2Me    H    Cl    2-ClPh         EtMe    H    Cl    2-BrPh         CBrF2Me    H    Cl    2-MePh         CH2CF3Me    H    Cl    2-CNPh         CH2CF3Me    H    Cl    2-FPh          CH2CF3Me    H    Cl    2,6-F2Ph      CH2CF3Me    H    Cl    2,4-F2Ph      CH2CF3Me    H    Cl    2,5-F2Ph      CH2CF3Me    H    Cl    2-MeOPh        CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CF2CHF2Me    H    Cl    3-Cl-2-吡啶基  CF3Me    H    Cl    3-Cl-2-吡啶基  CHF2Me    H    Cl    3-F-2-吡啶基   CBrF2Me    H    Cl    3-Br-2-吡啶基  CH2CF3Me    H    Cl    3-CF3-2-      CH2CF3吡啶基Me    H    Cl    3-Me-2-        CH2CF3吡啶基Me    H    Cl    3-Br-2-吡啶基  CF3Me    H    Cl    3-Br-2-吡啶基  CH2CF3Me    H    Cl    3-Br-2-吡啶基  CF2CHF2Me    Cl   H     F              CH2CF3Me    Cl   H     Me             CHF2Me    Cl   H     Me             CH2CF3Me    Cl   H     Me             CH2CF3 R 3   R 4a  R 4b  R 5a           R 5bMe    Cl    H    Et             CH2CF3Me    Cl    H    Me             CH2CF3Me    Cl    H    Me             CF2CHF2Me    Cl    H    Me             CHF2Et    Cl    H    Me             CHF2Me    Cl    H    Me             CBrF2Me    Cl    H    Me             CHF2Me    Cl    H    Me             CH2CF3n-Pr  Cl    H    Me             EtMe    Cl    H    Me             n-PrEt    Cl    H    Me             CH2C2F5Me    Cl    H    Et             CH2CF3Me    Cl    H    n-Pr           CF3Me    Cl    H    i-Pr           C2F5Me    Cl    H    Cl             CHF2Me    Cl    H    3-Cl-2-吡啶基  CH2CF3Me    Cl    H    3-Cl-2-吡啶基  CF2CHF2Me    Cl    H    3-Cl-2-吡啶基  CF3Me    Cl    H    3-Cl-2-吡啶基  CHF2Me    Cl    H    3-Cl-2-吡啶基  CBrF2Me    Cl    H    3-F-2-吡啶基   CH2CF3Me    Cl    H    3-CF3-2-      CH2CF3吡啶基Me    Cl    H    3-Br-2-吡啶基  CF3Me    Cl    H    3-Br-2-吡啶基  CH2CF3Me    Cl    H    3-Br-2-吡啶基  CF2CHF2Me    Cl    H    3-Br-2-吡啶基  CClF2Me    Cl    H    2-ClPh         CHF2Me    Cl    H    2-ClPh         EtMe    Cl    H    2-ClPh         CBrF2Me    Cl    H    2-BrPh         CH2CF3Me    Cl    H    2-MePh         CH2CF3Me    Cl    H    2-CNPh         CH2CF3Me    Cl    H    2-MeOPh        CH2CF3Me    Cl    H    2,5-F2Ph      CH2CF3 R 3   R 4a  R 4b  R 5a      R 5bMe    Cl    H    Me        CH2ClMe    Cl    H    Me        CClF2Me    Cl    H    Me        CH2CH2ClMe    Cl    H    Me        n-C3F7Me    Cl    H    Me        i-C3F7Me    Cl    H    Me        AllylMe    Cl    H    Me        CF2CHF2Me    Cl    H    CF3      i-C3F7Me    Cl    H    CF3      CF2CHF2Me    Cl    H    OMe       CF2CHF2Me    Cl    H    H         CF2CHF2Me    Cl    H    H         MeMe    Cl    H    H         CH2CF3Et    Cl    H    H         CH2CF3Me    Cl    H    H         CH2CF3Me    Cl    H    H         C2F5Me    Cl    H    H         C2F5Me    Cl    H    H         C2F5Me    Cl    H    H         CF2CHF2Me    Cl    H    H         CH2CF3Me    Cl    H    H         n-C3F7Me    Cl    H    3-Me-2-   CH2CF3吡啶基Me    Cl    H    H         i-C3F7Me    Cl    H    Ph        CH2CF3Me    Cl    H    Ph        CF2CHF2Me    Cl    H    Ph        CHF2Me    Cl    H    2-吡啶基  CH2CF3Me    Cl    H    2-吡啶基  CF2CHF2Me    Cl    H    2-ClPh    CH2CF3Me    Cl    H    2-ClPh    CF2CHF2Me    Cl    H    2-FPh     CH2CF3Me    Cl    H    2,6-F2Ph CH2CF3Me    Cl    H    2,4-F2Ph CH2CF3 table 5 R 3 R 4a R 4b R 5a R 5b Me H Me H CHF 2 Me H Me H CH 2 CF 3 Et H Me H CH 2 CF 3 Me H Me Me CH 2 CF 3 Me H Me Et CH 2 CF 3 Me H Me Me CF 2 CHF 2 Me H Me Et CHF 2 Me H Me Me CHF 2 Me H Me Me CBrF 2 Me H Me Me CH 2 R 3 R 4a R 4b R 5a R 5b Me H H H CHF 2 Me H H H CH 2 CF 3 Et H H H CH 2 CF 3 Me H H Me CH 2 CF 3 Me H H Et CH 2 CF 3 Me H H Me CF 2 CHF 2 Me H H Et CHF 2 Me H H Me CHF 2 Me H H Me CBrF 2 Me H H Me CHF 2 R 3 R 4a R 4b R 5a R 5b Et H Me Me CH 2 CF 3 Me H Me Me EtMe H Me Me n-PrMe H Me Me CH 2 C 2 F 5 n-Pr H Me Me CH 2 CF 3 Me H Me Me CF 3 Et H Me Me C 2 F 5 Me H Me Et CHF 2 Me H Me n-Pr CH 2 CF 3 Me H Me i-Pr CHF 2 Me H Me Cl CH 2 CF 3 Me H Me F CH 2 CF 3 Me H Me Me CH 2 ClMe H Me Me CCIF 2 Me H Me Me CH 2 CH 2 ClMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me AllylMe H Me Et CF 2 CHF 2 Me H Me Et iC 3 F 7 Me H Me i-Pr CF 2 CHF 2 Me H Me n-Pr CF 2 CHF 2 Me H Me CF 3 CF 2 CHF 2 Me H Me CF 3 MeMe H Me OMe CH 2 CF 3 Me H Me H CH 2 CF 3 Me H Me H CH 2 CF 3 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H C 2 F 5 Me H Me H CF 2 CHF 2 Me H Me i- Pr CH 2 CF 3 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me Ph CH 2 CF 3 Me H Me Ph CF 2 CHF 2 Me H Me Ph CF 3 R 3 R 4a R 4b R 5a R 5b Et H H Me CH 2 CF 3 Me H H Me EtMe H H Me n-PrMe H H Me CH 2 C 2 F 5 n-Pr H H Me CH 2 CF 3 Me H H Me CF 3 Et H H Me C 2 F 5 Me H H Et CHF 2 Me H H n-Pr CH 2 CF 3 Me H H i-Pr CHF 2 Me H H Cl CH 2 CF 3 Me H H F CH 2 CF 3 Me H H Me CH 2 ClMe H H Me CCIF 2 Me H H Me CH 2 CH 2 ClMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me AllylMe H H Me CF 2 CHF 2 Me H H Me iC 3 F 7 Me H H Me CF 2 CHF 2 Me H H Me CF 2 CHF 2 Me H H CF 3 CF 2 CHF 2 Me H H CF 3 MeMe H H OMe CH 2 CF 3 Me H H H CH 2 CF 3 Me H H H CH 2 CF 3 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H C 2 F 5 Me H H H CF 2 CHF 2 Me H H H CH 2 CF 3 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H CH 2 CF 3 Me H H H CF 2 CHF 2 Me H H H CHF 2 R 3 R 4a R 4b R 5a R 5b Me H Me 2-pyridyl CH 2 CF 3 Me H Me 2-pyridyl CF 2 CHF 2 Me H Me 2-ClPh CH 2 CF 3 Me H Me 2-ClPh CF 2 CHF 2 Me H Me 2-ClPh CHF 2 Me H Me 2-ClPh EtMe H Me 2-ClPh CBrF 2 Me H Me 2-BrPh CH 2 CF 3 Me H Me 2-MePh CH 2 CF 3 Me H Me 2-CNPh CH 2 CF 3 Me H Me 2-FPh CH 2 CF 3 Me H Me 2,6-F 2 Ph CH 2 CF 3 Me H Me 2,4-F 2 Ph CH 2 CF 3 Me H Me 2,5-F 2 Ph CH 2 CF 3 Me H Me 2-MeOPh CH 2 CF 3 Me H Me 3-Cl-2-pyridyl CH 2 CF 3 Me H Me 3-Cl-2-pyridyl CF 2 CHF 2 Me H Me 3 -Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl CHF 2 Me H Me 3-Cl-2-pyridyl CBrF 2 Me H Me 3-F-2-pyridyl CH 2 CF 3 Me H Me 3-CF 3 -2- CH 2 CF 3 pyridyl Me H Me 3-Me-2- CH 2 CF 3 pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br -2-pyridyl CH 2 CF 3 Me H Me 3-Br-2-pyridyl CF 2 CHF 2 Me H Me 3-Br-2-pyridyl CClF 2 Me Me H H CHF 2 Me H H CH 2 CF 3 Et Me H H CH 2 CF 3 Me Me H Me CH 2 CF 3 Me Me H Et CH 2 CF 3 Me Me H Me CF 2 CHF 2 Me Me H Et CHF 2 Me Me H Me CHF 2 R 3 R 4a R 4b R 5a R 5b Me H H Ph CH 2 CF 3 Me H H Ph CF 2 CHF 2 Me H H Ph CH 2 CF 3 Me H H 2-pyridyl CF 2 CHF 2 Me H H 2-pyridyl CHF 2 Me H H 2-ClPh EtMe H H 2-ClPh CBrF 2 Me H H 2-ClPh CH 2 CF 3 Me H H 2-ClPh CH 2 CF 3 Me H H 2-ClPh CH 2 CF 3 Me H H 2-BrPh CH 2 CF 3 Me H H 2 -MePh CH 2 CF 3 Me H H 2-CNPh CH 2 CF 3 Me H H 2-FPh CH 2 CF 3 Me H H 2,6-F 2 Ph CH 2 CF 3 Me H H 2,4-F 2 Ph CH 2 CF 3 Me H H 2,5-F 2 Ph CF 2 CHF 2 Me H H 2-MeO Ph CF 3 Me H H 3-Cl-2-pyridyl CHF 2 Me H H 3-Cl-2-pyridyl CBrF 2 Me H H 3-Cl -2-pyridyl CH 2 CF 3 Me H H 3-CF 3 -2- CH 2 CF 3 pyridyl Me H H 3-Me-2-CF 2 CHF 2 pyridyl Me H H 3-F-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl CH 2 CF 3 Me H H 3-Cl-2-pyridyl CH 2 CF 3 Me H H 3-Br-2-pyridyl CClF 2 Me H H 3-Br-2-pyridyl CH 2 CF 3 Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl CF 3 Me H Cl Et CHF 2 Me H Cl Me CH 2 CF 3 Me H Cl Et CH 2 CF 3 Me HCl Me CH 2 CF 3 Me H Cl Me CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H Me CBrF 2 Me Me H Me CHF 2 Et Me H Me CH 2 CF 3 Me Me H Me EtMe Me H Me n-PrMe Me H Me CH 2 C 2 F 5 n-Pr Me H Me CH 2 CF 3 Me Me H Me CF 3 Et Me H Me C 2 F 5 Me Me H Et CHF 2 Me Me H n-Pr CH 2 CF 3 Me Me H i-Pr CHF 2 Me Me HCl CH 2 CF 3 Me Me H F CH 2 CF 3 Me Me H Me CH 2 ClMe Me H Me CCIF 2 Me Me H Me CH 2 CH 2 ClMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me AllylMe Me H Me CF 2 CHF 2 Me Me H Me iC 3 F 7 Me Me H Me CF 2 CHF 2 Me Me H Me CF 2 CHF 2 Me Me H CF 3 CF 2 CHF 2 Me Me H CF 3 MeMe Me H OMe CH 2 CF 3 Me Me H H CH 2 CF 3 Me Me H H CH 2 CF 3 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H C 2 F 5 Me Me H H CF 2 CHF 2 Me Me H H CH 2 CF 3 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl Me CF 2 CHF 2 Et H Cl Me CHF 2 Me H Cl Me CHF 2 Me H Cl Me CBrF 2 Me H Cl Me CHF 2 n-Pr H Cl Me CH 2 CF 3 Me H Cl Me EtEt H Cl Me n-PrMe H Cl Et CH 2 C 2 F 5 Me H Cl n-Pr CH 2 CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl C 2 F 5 Me H Cl F CHF 2 Me H Cl Me CH 2 CF 3 Me H Cl Me CHF 2 Me H Cl Me CH 2 CF 3 Me H Cl Me CH 2 CF 3 Me H Cl Me CH 2 ClMe H Cl Me CCIF 2 Me H Cl Me CH 2 CH 2 ClMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me AllylMe H Cl CF 3 CF 2 CHF 2 Me H Cl CF 3 iC 3 F 7 Me H Cl OMe CF 2 CHF 2 Me H Cl H CF 2 CHF 2 Me H Cl H CF 2 CHF 2 Me H Cl H MeEt H Cl H CH 2 CF 3 Me H Cl H CH 2 CF 3 Me H Cl H CH 2 CF 3 Me H Cl H C 2 F 5 Me H Cl H C 2 F 5 Me H Cl H C 2 F 5 Me H Cl H CF 2 CHF 2 Me H Cl H CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H H CF 2 CHF 2 Me Me H H CHF 2 Me Me H Ph CH 2 CF 3 Me Me H Ph CF 2 CHF 2 Me Me H Ph CH 2 CF 3 Me Me H 2 -Pyridyl CF 2 CHF 2 Me Me H 2-Pyridyl CHF 2 Me H 2-ClPh EtMe Me H 2ClPh CBrF 2 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-BrPh CH 2 CF 3 Me Me H 2-MePh CH 2 CF 3 Me Me H 2-CNPh CH 2 CF 3 Me Me H 2-FPh CH 2 CF 3 Me Me H 2,6-F 2 Ph CH 2 CF 3 Me Me H 2,4-F 2 Ph CH 2 CF 3 Me Me H 2,5-F 2 Ph CF 2 CHF 2 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CHF 2 Me Me H 3-Cl-2-pyridyl CBrF 2 Me H 3-Cl-2-pyridyl CH 2 CF 3 Me Me H 3-Cl-2-pyridyl CH 2 CF 3 Me H 3-Cl-2-pyridyl CH 2 CF 3 Me H 3-F-2-pyridyl CF 3 Me Me H 3-CF 3 -2- CH 2 CF 3 pyridyl Me Me H 3-Me-2- CF 2 CHF 2 Pyridyl Me Me H 3-Br-2-Pyridyl CCIF 2 Me Me H 3-Br-2-Pyridyl CH 2 CF 3 Me Me H 3-Br-2- Pyridyl CF 3 Me Me H 3-Br-2-pyridyl CF 3 Me Cl H Me CHF 2 Me Cl H Et CH 2 CF 3 Me Cl H Me CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl H nC 3 F 7 Me H Cl Ph iC 3 F 7 Me H Cl Ph CH 2 CF 3 Me H Cl Ph CF 2 CHF 2 Me H Cl 2-pyridyl CHF 2 Me H Cl 2-pyridyl CH 2 CF 3 Me H Cl 2-ClPh CF 2 CHF 2 Me H Cl 2-ClPh CH 2 CF 3 Me H Cl 2-ClPh CF 2 CHF 2 Me H Cl 2-ClPh CHF 2 Me H Cl 2-ClPh EtMe H Cl 2-BrPh CBrF 2 Me H Cl 2-MePh CH 2 CF 3 Me H Cl 2-CNPh CH 2 CF 3 Me H Cl 2-FPh CH 2 CF 3 Me H Cl 2,6 -F 2 Ph CH 2 CF 3 Me H Cl 2,4-F 2 Ph CH 2 CF 3 Me H Cl 2,5-F 2 Ph CH 2 CF 3 Me H Cl 2-MeOPh CH 2 CF 3 Me H Cl 3 -Cl-2-pyridyl CH 2 CF 3 Me H Cl 3-Cl-2-pyridyl CH 2 CF 3 Me H Cl 3-Cl-2-pyridyl CF 2 CHF 2 Me H Cl 3-Cl-2- Pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl CHF 2 Me H Cl 3-F-2-pyridyl CBrF 2 Me H Cl 3-Br-2-pyridyl CH 2 CF 3 Me H Cl 3- CF 3 -2- CH 2 CF 3 pyridyl Me H Cl 3-Me-2- CH 2 CF 3 pyridyl Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl CH 2 CF 3 Me H Cl 3-Br-2-pyridyl CF 2 CHF 2 Me Cl H F CH 2 CF 3 Me Cl H Me CHF 2 Me Cl H Me CH 2 CF 3 Me Cl H Me CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Cl H Et CH 2 CF 3 Me Cl H Me CH 2 CF 3 Me Cl H Me CF 2 CHF 2 Me Cl H Me CHF 2 Et Cl H Me CHF 2 Me Cl H Me CBrF 2 Me Cl H Me CHF 2 Me Cl H Me CH 2 CF 3 n-Pr Cl H Me EtMe Cl H Me n-PrEt Cl H Me CH 2 C 2 F 5 Me Cl H Et CH 2 CF 3 Me Cl H n -Pr CF 3 Me Cl H i-Pr C 2 F 5 Me Cl H Cl CHF 2 Me Cl H 3-Cl-2-pyridyl CH 2 CF 3 Me Cl H 3-Cl-2-pyridyl CF 2 CHF 2 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl CHF 2 Me Cl H 3-Cl-2-pyridyl CBrF 2 Me Cl H 3-F-2-pyridyl CH 2 CF 3 Me Cl H 3-CF 3 -2- CH 2 CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl CH 2 CF 3 Me Cl H 3-Br-2-pyridyl CF 2 CHF 2 Me Cl H 3-Br-2-pyridyl CClF 2 Me Cl H 2-ClPh CHF 2 Me Cl H 2-ClPh EtMe Cl H 2-ClPh CBrF 2 Me Cl H 2-BrPh CH 2 CF 3 Me Cl H 2-MePh CH 2 CF 3 Me Cl H 2-CNPh CH 2 CF 3 Me Cl H 2-MeOPh CH 2 CF 3 Me Cl H 2,5-F 2 Ph CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Cl H Me CH 2 ClMe Cl H Me CCIF 2 Me Cl H Me CH 2 CH 2 ClMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me AllylMe Cl H Me CF 2 CHF 2 Me Cl H CF 3 iC 3 F 7 Me Cl H CF 3 CF 2 CHF 2 Me Cl H OMe CF 2 CHF 2 Me Cl H H CF 2 CHF 2 Me Cl H H MeMe Cl H H CH 2 CF 3 Et Cl H H CH 2 CF 3 Me Cl H H CH 2 CF 3 Me Cl H H C 2 F 5 Me Cl H H C 2 F 5 Me Cl H H C 2 F 5 Me Cl H H CF 2 CHF 2 Me Cl H H CH 2 CF 3 Me Cl H H nC 3 F 7 Me Cl H 3-Me-2- CH 2 CF 3 pyridyl Me Cl H H iC 3 F 7 Me Cl H Ph CH 2 CF 3 Me Cl H Ph CF 2 CHF 2 Me Cl H Ph CHF 2 Me Cl H 2-pyridyl CH 2 CF 3 Me Cl H 2-pyridyl CF 2 CHF 2 Me Cl H 2-ClPh CH 2 CF 3 Me Cl H 2-ClPh CF 2 CHF 2 Me Cl H 2-FPh CH 2 CF 3 MeClH2,6 - F2PhCH2CF3MeClH2,4 - F2PhCH2CF3 _

                               表6 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Me    H     CF3Me    H    Me    H     OCF3Et    H    Me    H     OCF3Me    H    Me    Me    BrMe    H    Me    Et    BrMe    H    Me    M     ClMe    H    Me    Et    ClMe    H    Me    Me    IMe    H    Me    Me    CF3Me    H    Me    Me    OCF3Et    H    Me    Me    CF3Me    H    Me    Me    SCF3Me    H    Me    Me    SCHF2Me    H    Me    Me    OCHF2n-Pr  H    Me    Me    CF3Me    H    Me    Me    C2F5Et    H    Me    Me    C2F5Me    H    Me    Et    CF3Me    H    Me    n-Pr  CF3Me    H    Me    i-Pr  CF3Me    H    Me    Cl    CF3Me    H    Me    F     CF3Me    H    Me    Me    SMeMe    H    Me    Me    OMeMe    H    Me    Me    OEtMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    Et R 3   R 4a  R 4b R 5a  R 5bMe    H    H    H     CF3Me    H    H    H     OCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3Me    H    H    Me    OCF3Et    H    H    Me    CF3Me    H    H    Me    SCF3Me    H    H    Me    SCHF2Me    H    H    Me    OCHF2n-Pr  H    H    Me    CF3Me    H    H    Me    C2F5Et    H    H    Me    C2F5Me    H    H    Et    CF3Me    H    H    n-Pr  CF3Me    H    H    i-Pr  CF3Me    H    H    Cl    CF3Me    H    H    F     CF3Me    H    H    Me    SMeMe    H    H    Me    OMeMe    H    H    Me    OEtMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    Et R 3   R 4a  R 4b  R 5a        R 5bMe    H    Me    Me          OCF2CHF2Me    H    Me    Me          SCF2CHF2Me    H    Me    Me          SO2MeMe    H    Me    Me          SO2CF3Me    H    Me    CF3        CF3Me    H    Me    CF3        MeMe    H    Me    OMe         CF3Me    H    Me    H           CF3Me    H    Me    H           OCHF2Me    H    Me    H           C2F5Et    H    Me    H           C2F5Me    H    Me    H           OCF3Me    H    Me    H           OCF2CHF2Me    H    Me    H           SCF2CHF2Me    H    Me    H           n-C3F7Me    H    Me    H           i-C3F7Me    H    Me    H           BrMe    H    Me    H           ClMe    H    Me    H           SCF3Me    H    Me    Ph          CF3Me    H    Me    Ph          ClMe    H    Me    Ph          BrMe    H    Me    2-吡啶基    CF3Me    H    Me    2-吡啶基    ClMe    H    Me    2-ClPh      CF3Me    H    Me    2-ClPh      OCF3Me    H    Me    2-ClPh      BrMe    H    Me    2-ClPh      ClMe    H    Me    2-ClPh      SCHF2Me    H    Me    2-BrPh      CF3Me    H    Me    2-MePh      CF3Me    H    Me    2-CNPh      CF3Me    H    Me    2-FPh       CF3Me    H    Me    2,6-F2Ph   CF3Me    H    Me    2,4-F2Ph   CF3Me    H    Me    2,5-F2Ph   CF3Me    H    Me    2-MeOPh     CF3 R 3   R 4a  R 4b R 5a        R 5bMe    H    H    Me         OCF2CHF2Me    H    H    Me         SCF2CHF2Me    H    H    Me         SO2MeMe    H    H    Me         SO2CF3Me    H    H    CF3       CF3Me    H    H    CF3       MeMe    H    H    OMe        CF3Me    H    H    H          CF3Me    H    H    H          OCHF2Me    H    H    H          C2F5Et    H    H    H          C2F5Me    H    H    H          OCF3Me    H    H    H          OCF2CHF2Me    H    H    H          SCF2CHF2Me    H    H    H          n-C3F7Me    H    H    H          i-C3F7Me    H    H    H          BrMe    H    H    H          ClMe    H    H    H          SCF3Me    H    H    Ph         CF3Me    H    H    Ph         ClMe    H    H    Ph         BrMe    H    H    2-吡啶基   CF3Me    H    H    2-吡啶基   ClMe    H    H    2-ClPh     CF3Me    H    H    2-ClPh     OCF3Me    H    H    2-ClPh     BrMe    H    H    2-ClPh     ClMe    H    H    2-ClPh     SCHF2Me    H    H    2-BrPh     CF3Me    H    H    2-MePh     CF3Me    H    H    2-CNPh     CF3Me    H    H    2-FPh      CF3Me    H    H    2,6-F2Ph  CF3Me    H    H    2,4-F2Ph  CF3Me    H    H    2,5-F2Ph  CF3Me    H    H    2-MeOPh    CF3 R 3    R 4a  R 4b      R 5a        R 5bMe    H     Me   3-Cl-2-吡啶基    CF3Me    H     Me   3-Cl-2-吡啶基    OCF3Me    H     Me   3-Cl-2-吡啶基    BrMe    H     Me   3-Cl-2-吡啶基    ClMe    H     Me   3-Cl-2-吡啶基    SCHF2Me    H     Me   3-F-2-吡啶基     CF3Me    H     Me   3-CF3-2-        CF3吡啶基Me    H     Me   3-Me-2-          CF3吡啶基Me    H     Me   3-Br-2-吡啶基    CF3Me    H     Me   3-Br-2-吡啶基    OCF3Me    H     Me   3-Br-2-吡啶基    BrMe    H     Me   3-Br-2-吡啶基    ClMe    Me    H    H                CF3Me    Me    H    H                OCF3Et    Me    H    H                OCF3Me    Me    H    Me               BrMe    Me    H    Et               BrMe    Me    H    Me               ClMe    Me    H    Et               ClMe    Me    H    Me               IMe    Me    H    Me               CF3Me    Me    H    Me               OCF3Et    Me    H    Me               CF3Me    Me    H    Me               SCF3Me    Me    H    Me               SCHF2Me    Me    H    Me               OCHF2n-Pr  Me    H    Me               CF3Me    Me    H    Me               C2F5Et    Me    H    Me               C2F5Me    Me    H    Et               CF3Me    Me    H    n-Pr             CF3Me    Me    H    i-Pr             CF3Me    Me    H    Cl               CF3Me    Me    H    F                CF3Me    Me    H    Me               SMe R 3   R 4a  R 4b      R 5a      R 5bMe    H    H    3-Cl-2-吡啶基  CF3Me    H    H    3-Cl-2-吡啶基  OCF3Me    H    H    3-Cl-2-吡啶基  BrMe    H    H    3-Cl-2-吡啶基  ClMe    H    H    3-Cl-2-吡啶基  SCHF2Me    H    H    3-F-2-吡啶基   CF3Me    H    H    3-CF3-2-      CF3吡啶基Me    H    H    3-Me-2-        CF3吡啶基Me    H    H    3-Br-2-吡啶基  CF3Me    H    H    3-Br-2-吡啶基  OCF3Me    H    H    3-Br-2-吡啶基  BrMe    H    H    3-Br-2-吡啶基  ClMe    H    Cl   Et             BrMe    H    Cl   Me             ClMe    H    Cl   Et             ClMe    H    Cl   Me             IMe    H    Cl   Me             CF3Me    H    Cl   Me             CCF3Et    H    Cl   Me             CF3Me    H    Cl   Me             SCF3Me    H    Cl   Me             SCHF2Me    H    Cl   Me             OCHF2n-Pr  H    Cl   Me             CF3Me    H    Cl   Me             C2F5Et    H    Cl   Me             C2F5Me    H    Cl   Et             CF3Me    H    Cl   n-Pr           CF3Me    H    Cl   i-Pr           CF3Me    H    Cl   Cl             CF3Me    H    Cl   F              CF3Me    H    Cl   Me             SMeMe    H    Cl   Me             OMeMe    H    Cl   Me             OEtMe    H    Cl   Me             n-C3F7Me    H    Cl   Me             i-C3F7 R 3  R 4a  R 4b R 5a       R 5bMe  Me    H    Me        OMeMe  Me    H    Me        OEtMe  Me    H    Me        n-C3F7Me  Me    H    Me        i-C3F7Me  Me    H    Me        EtMe  Me    H    Me        OCF2CHF2Me  Me    H    Me        SCF2CHF2Me  Me    H    Me        SO2MeMe  Me    H    Me        SO2CF3Me  Me    H    CF3      CF3Me  Me    H    CF3      MeMe  Me    H    OMe       CF3Me  Me    H    H         CF3Me  Me    H    H         OCHF2Me  Me    H    H         C2F5Et  Me    H    H         C2F5Me  Me    H    H         OCF3Me  Me    H    H         OCF2CHF2Me  Me    H    H         SCF2CHF2Me  Me    H    H         n-C3F7Me  Me    H    H         i-C3F7Me  Me    H    H         BrMe  Me    H    H         ClMe  Me    H    H         SCF3Me  Me    H    Ph        CF3Me  Me    H    Ph        ClMe  Me    H    Ph        BrMe  Me    H    2-吡啶基  CF3Me  Me    H    2-吡啶基  ClMe  Me    H    2-ClPh    CF3Me  Me    H    2-ClPh    OCF3Me  Me    H    2-ClPh    BrMe  Me    H    2-ClPh    ClMe  Me    H    2-ClPh    SCHF2Me  Me    H    2-BrPh    CF3Me  Me    H    2-MePh    CF3Me  Me    H    2-CNPh    CF3 R 3   R 4a  R 4b  R 5a      R 5bMe    H    Cl    Me        EtMe    H    Cl    Me        OCF2CHF2Me    H    Cl    Me        SCF2CHF2Me    H    Cl    Me        SO2MeMe    H    Cl    Me        SC2CF3Me    H    Cl    CF3      CF3Me    H    Cl    CF3      MeMe    H    Cl    OMe       CF3Me    H    Cl    H         CF3Me    H    Cl    H         OCHF2Me    H    Cl    H         C2F5Et    H    Cl    H         C2F5Me    H    Cl    H         OCF3Me    H    Cl    H         OCF2CHF2Me    H    Cl    H         SCF2CHF2Me    H    Cl    H         n-C3F7Me    H    Cl    H         i-C3F7Me    H    Cl    H         BrMe    H    Cl    H         ClMe    H    Cl    H         SCF3Me    H    Cl    Ph        CF3Me    H    Cl    Ph        ClMe    H    Cl    Ph        BrMe    H    Cl    2-吡啶基  CF3Me    H    Cl    2-吡啶基  ClMe    H    Cl    2-ClPh    CF3Me    H    Cl    2-ClPh    OCF3Me    H    Cl    2-ClPh    BrMe    H    Cl    2-ClPh    ClMe    H    Cl    2-ClPh    SCHF2Me    H    Cl    2-BrPh    CF3Me    H    Cl    2-MePh    CF3Me    H    Cl    2-CNPh    CF3Me    H    Cl    2-FPh     CF3Me    H    Cl    2,6-F2Ph CF3Me    H    Cl    2,4-F2Ph CF3Me    H    Cl    2,5-F2Ph CF3 R 3   R 4a  R 4b   R 5a          R 5bMe    Me    H    2-FPh          CF3Me    Me    H    2,6-F2Ph      CF3Me    Me    H    2,4-F2Ph      CF3Me    Me    H    2,5-F2Ph      CF3Me    Me    H    2-MeOPh        CF3Me    Me    H    3-Cl-2-吡啶基  CF3Me    Me    H    3-Cl-2-吡啶基  OCF3Me    Me    H    3-Cl-2-吡啶基  BrMe    Me    H    3-Cl-2-吡啶基  ClMe    Me    H    3-Cl-2-吡啶基  SCHF2Me    Me    H    3-F-2-吡啶基   CF3Me    Me    H    3-CF3-2-      CF3吡啶基Me    Me    H    3-Me-2-        CF3吡啶基Me    Me    H    3-Br-2-吡啶基  CF3Me    Me    H    3-Br-2-吡啶基  OCF3Me    Me    H    3-Br-2-吡啶基  BrMe    Me    H    3-Br-2-吡啶基  ClMe    Cl    H    Me             BrMe    Cl    H    Et             BrMe    Cl    H    Me             ClMe    Cl    H    Et             ClMe    Cl    H    Me             IMe    Cl    H    Me             CF3Me    Cl    H    Me             OCF3Et    Cl    H    Me             CF3Me    Cl    H    Me             SCF3Me    Cl    H    Me             SCHF2Me    Cl    H    Me             OCHF2n-Pr  Cl    H    Me             CF3Me    Cl    H    Me             C2F5Et    Cl    H    Me             C2F5Me    Cl    H    Et             CF3Me    Cl    H    n-Pr           CF3Me    Cl    H    i-Pr           CF3Me    Cl    H    Cl             CF3 R 3   R 4a  R 4b     R 5a        R 5bMe    H    Cl    2-MeOPh        CF3Me    H    Cl    3-Cl-2-吡啶基  CF3Me    H    Cl    3-Cl-2-吡啶基  OCF3Me    H    Cl    3-Cl-2-吡啶基  BrMe    H    Cl    3-Cl-2-吡啶基  ClMe    H    Cl    3-Cl-2-吡啶基  SCHF2Me    H    Cl    3-F-2-吡啶基   CF3Me    H    Cl    3-Br-2-吡啶基  CF3Me    H    Cl    3-Br-2-吡啶基  OCF3Me    H    Cl    3-Br-2-吡啶基  BrMe    H    Cl    3-Br-2-吡啶基  ClMe    H    Cl    3-CF3-2-      CF3吡啶基Me    H    Cl    3-Me-2-        CF3吡啶基Me    Cl    H    H              OCF3Me    Cl    H    H              OCF2CHF2Me    Cl    H    H              SCF2CHF2Me    Cl    H    H              n-C3F7Me    Cl    H    H              i-C3F7Me    Cl    H    H              BrMe    Cl    H    H              ClMe    Cl    H    H              SCF3Me    Cl    H    Ph             CF3Me    Cl    H    Ph             ClMe    Cl    H    Ph             BrMe    Cl    H    2-吡啶基       CF3Me    Cl    H    2-吡啶基       ClMe    Cl    H    2-ClPh         CF3Me    Cl    H    2-ClPh         OCF3Me    Cl    H    2-ClPh         BrMe    Cl    H    2-ClPh         ClMe    Cl    H    2-ClPh         SCHF2Me    Cl    H    2-BrPh         CF3Me    Cl    H    2-MePh         CF3Me    Cl    H    2-CNPh         CF3Me    Cl    H    2-FPh          CF3 R 3   R 4a  R 4b  R 5a      R 5bMe    Cl    H    F         CF3Me    Cl    H    Me        SMeMe    Cl    H    Me        OMeMe    Cl    H    Me        OEtMe    Cl    H    Me        n-C3F7Me    Cl    H    Me        i-C3F7Me    Cl    H    Me        EtMe    Cl    H    Me        OCF2CHF2Me    Cl    H    Me        SCF2CHF2Me    Cl    H    Me        SO2MeMe    Cl    H    Me        SO2CF3Me    Cl    H    3-CF3-2- CF3吡啶基Me    Cl    H    CF3      MeMe    Cl    H    OMe       CF3Me    Cl    H    H         CF3Me    Cl    H    H         OCHF2Me    Cl    H    H         C2F5   R 3 R 4a  R 4b   R 5a            R 5bMe  Cl    H    2,6-F2Ph        CF3Me  Cl    H    2,4-F2Ph        CF3Me  Cl    H    2,5-F2Ph        CF3Me  Cl    H    2-MeOPh          CF3Me  Cl    H    3-Cl-2-吡啶基    CF3Me  Cl    H    3-Cl-2-吡啶基    OCF3Me  Cl    H    3-Cl-2-吡啶基    BrMe  Cl    H    3-Cl-2-吡啶基    ClMe  Cl    H    3-Cl-2-吡啶基    SCHF2Me  Cl    H    3-F-2-吡啶基     CF3Me  Cl    H    CF3             CF3Me  Cl    H    3-Me-2-          CF3吡啶基Me  Cl    H    3-Br-2-吡啶基    CF3Me  Cl    H    3-Br-2-吡啶基    OCF3Me  Cl    H    3-Br-2-吡啶基    BrMe  Cl    H    3-Br-2-吡啶基    ClEt  Cl    H    H                C2F5 Table 6 R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me M ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me Et R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me Et R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H ClMe H Me H SCF 3 Me H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2 ,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H OCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H ClMe H H H SCF 3 Me H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-Pyridyl CF 3 Me H H 2-Pyridyl ClMe H H 2-ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridylClMeH Me 3-Cl- 2 -pyridylSCHF2MeHMe3-F- 2 -pyridylCF3MeHMe3- CF3-2 - CF3pyridylMeH Me 3-Me-2-CF 3- pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridylClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me BrMe Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMe R 3 R 4a R 4b R 5a R 5b Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl- 2-pyridylClMeHH 3-Cl-2-pyridylSCHF2MeHH3-F-2 - pyridylCF3MeHH3- CF3-2 - CF3pyridylMeHH3 -Me-2-CF 3- pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me CCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n -Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 R 3 R 4a R 4b R 5a R 5b Me Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SC 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H BrMe H Cl H ClMe H Cl H SCF 3 Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me HCl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me H 2-MeOPh CF 3 Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-Cl-2-pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me Me H 3-CF 3 -2- CF 3 pyridyl Me Me H 3-Me-2-CF 3- pyridyl Me Me H 3-Br-2-pyridyl CF 3 Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridylClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2 -Pyridyl BrMe H Cl 3-Cl-2-pyridylClMe H Cl 3-Cl-2-pyridylSCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridine Base CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me H Cl 3-Br-2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe H Cl 3-CF 3 -2- CF 3 Pyridyl Me H Cl 3-Me-2- CF 3 Pyridyl Me Cl H H OCF 3 Me Cl H H OCF 2 CHF 2 Me Cl H H SCF 2 CHF 2 Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-Pyridyl CF 3 Me Cl H 2-Pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 Me Cl H 2-BrPh CF 3 Me Cl H 2-MePh CF 3 Me Cl H 2-CNPh CF 3 Me ClH2- FPhCF3 R 3 R 4a R 4b R 5a R 5b Me Cl H F CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H 3-CF 3 -2- CF 3 Pyridyl Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H 2,6-F 2 Ph CF 3 Me Cl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2 -MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2- Pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H CF 3 CF 3 Me Cl H 3-Me-2-CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br-2-pyridyl ClEt Cl H H C 2 F 5

                              表7 R 3  R 4a  R 4b  R 5a   R 5bMe    H    Me    H     CF3Me    H    Me    H     OCF3Et    H    Me    H     OCF3Me    H    Me    Me    BrMe    H    Me    Et    BrMe    H    Me    Me    ClMe    H    Me    Et    ClMe    H    Me    Me    IMe    H    Me    Me    CF3   R 3  R 4a  R 4b R 5a   R 5bMe    H    H    H     CF3Me    H    H    H     OCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3   R 3   R 4a R 4b  R 5a  R 5bMe    H    Me    Me   OCF3Et    H    Me    Me   CF3Me    H    Me    Me   SCF3Me    H    Me    Me   SCHF2Me    H    Me    Me   OCHF2n-Pr  H    Me    Me   CF3Me    H    Me    Me   C2F5Et    H    Me    Me   C2F5Me    H    Me    Et   CF3Me    H    Me    n-Pr CF3Me    H    Me    i-Pr CF3Me    H    Me    Cl   CF3Me    H    Me    F    CF3Me    H    Me    Me   SMeMe    H    Me    Me   OMeMe    H    Me    Me   OEtMe    H    Me    Me   n-C3F7Me    H    Me    Me   i-C3F7Me    H    Me    Me   EtMe    H    Me    Me   OCF2CHF2Me    H    Me    Me   SCF2CHF2Me    H    Me    Me   SO2MeMe    H    Me    Me   SO2CF3Me    H    Me    CF3 CF3Me    H    Me    CF3 MeMe    H    Me    OMe  CF3Me    H    Me    H    CF3Me    H    Me    H    OCHF2Me    H    Me    H    C2F5Et    H    Me    H    C2F5Me    H    Me    H    OCF3Me    H    Me    H    OCF2CHF2Me    H    Me    H    SCF2CHF2Me    H    Me    H    n-C3F7Me    H    Me    H    i-C3F7Me    H    Me    H    BrMe    H    Me    H    Cl R 3   R 4a  R 4b R 5a  R 5bMe    H    H    Me   CCF3Et    H    H    Me   CF3Me    H    H    Me   SCF3Me    H    H    Me   SCHF2Me    H    H    Me   OCHF2n-Pr  H    H    Me   CF3Me    H    H    Me   C2F5Et    H    H    Me   C2F5Me    H    H    Et   CF3Me    H    H    n-Pr CF3Me    H    H    i-Pr CF3Me    H    H    Cl   CF3Me    H    H    F    CF3Me    H    H    Me   SMeMe    H    H    Me   OMeMe    H    H    Me   OEtMe    H    H    Me   n-C3F7Me    H    H    Me   i-C3F7Me    H    H    Me   EtMe    H    H    Me   OCF2CHF2Me    H    H    Me   SCF2CHF2Me    H    H    Me   SO2MeMe    H    H    Me   SO2CF3Me    H    H    CF3 CF3Me    H    H    CF3 MeMe    H    H    OMe  CF3Me    H    H    H    CF3Me    H    H    H    OCHF2Me    H    H    H    C2F5Et    H    H    H    C2F5Me    H    H    H    OCF3Me    H    H    H    OCF2CHF2Me    H    H    H    SCF2CHF2Me    H    H    H    n-C3F7Me    H    H    H    i-C3F7Me    H    H    H    BrMe    H    H    H    Cl R 3   R 4a  R 4b  R 5a           R 5bMe    H    Me    H              SCF3Me    H    Me    Ph             CF3Me    H    Me    Ph             ClMe    H    Me    Ph             BrMe    H    Me    2-吡啶基       CF3Me    H    Me    2-吡啶基       ClMe    H    Me    2-ClPh         CF3Me    H    Me    2-ClPh         OCF3Me    H    Me    2-ClPh         BrMe    H    Me    2-ClPh         ClMe    H    Me    2-ClPh         SCHF2Me    H    Me    2-BrPh         CF3Me    H    Me    2-MePh         CF3Me    H    Me    2-CNPh         CF3Me    H    Me    2-FPh          CF3Me    H    Me    2,6-F2Ph      CF3Me    H    Me    2,4-F2Ph      CF3Me    H    Me    2,5-F2Ph      CF3Me    H    Me    2-MeOPh        CF3Me    H    Me    3-Cl-2-吡啶基  CF3Me    H    Me    3-Cl-2-吡啶基  OCF3Me    H    Me    3-Cl-2-吡啶基  BrMe    H    Me    3-Cl-2-吡啶基  ClMe    H    Me    3-Cl-2-吡啶基  SCHF2Me    H    Me    3-F-2-吡啶基   CF3Me    H    Me    3-CF3-2-      CF3吡啶基Me    H    Me    3-Me-2-        CF3吡啶基Me    H    Me    3-Br-2-吡啶基  CF3Me    H    Me    3-Br-2-吡啶基  OCF3Me    H    Me    3-Br-2-吡啶基  BrMe    H    Me    3-Br-2-吡啶基  ClMe    Me   H     H              CF3Me    Me   H     H              OCF3Et    Me   H     H              OCF3Me    Me   H     Me             Br R 3   R 4a  R 4b R 5a             R 5bMe    H    H    H               SCF3Me    H    H    Ph              CF3Me    H    H    Ph              ClMe    H    H    Ph              BrMe    H    H    2-吡啶基        CF3Me    H    H    2-吡啶基        ClMe    H    H    2-ClPh          CF3Me    H    H    2-ClPh          OCF3Me    H    H    2-ClPh          BrMe    H    H    2-ClPh          ClMe    H    H    2-ClPh          SCHF2Me    H    H    2-BrPh          CF3Me    H    H    2-MePh          CF3Me    H    H    2-CNPh          CF3Me    H    H    2-FPh           CF3Me    H    H    2,6-F2Ph       CF3Me    H    H    2,4-F2Ph       CF3Me    H    H    2,5-F2Ph       CF3Me    H    H    2-MeOPh         CF3Me    H    H    3-Cl-2-吡啶基   CF3Me    H    H    3-Cl-2-吡啶基   OCF3Me    H    H    3-Cl-2-吡啶基   BrMe    H    H    3-Cl-2-吡啶基   ClMe    H    H    3-Cl-2-吡啶基   SCHF2Me    H    H    3-F-2-吡啶基    CF3Me    H    H    3-CF3-2-       CF3吡啶基Me    H    H    3-Me-2-         CF3吡啶基Me    H    H    3-Br-2-吡啶基   CF3Me    H    H    3-Br-2-吡啶基   OCF3Me    H    H    3-Br-2-吡啶基   BrMe    H    H    3-Br-2-吡啶基   ClMe    H    Cl   Et              BrMe    H    Cl   Me              ClMe    H    Cl   Et              ClMe    H    Cl   Me              I     R 3  R 4a  R 4b R 5a  R 5bMe   Me    H    Et   BrMe   Me    H    Me   ClMe   Me    H    Et   ClMe   Me    H    Me   IMe   Me    H    Me   CF3Me   Me    H    Me   OCF3Et   Me    H    Me   CF3Me   Me    H    Me   SCF3Me   Me    H    Me   SCHF2Me   Me    H    Me   OCHF2n-Pr Me    H    Me   CF3Me   Me    H    Me   C2F5Et   Me    H    Me   C2F5Me   Me    H    Et   CF3Me   Me    H    n-Pr CF3Me   Me    H    i-Pr CF3Me   Me    H    Cl   CF3Me   Me    H    F    CF3Me   Me    H    Me   SMeMe   Me    H    Me   OMeMe   Me    H    Me   OEtMe   Me    H    Me   n-C3F7Me   Me    H    Me   i-C3F7Me   Me    H    Me   EtMe   Me    H    Me   OCF2CHF2Me   Me    H    Me   SCF2CHF2Me   Me    H    Me   SO2MeMe   Me    H    Me   SO2CF3Me   Me    H    CF3 CF3Me   Me    H    CF3 MeMe   Me    H    OMe  CF3Me   Me    H    H    CF3Me   Me    H    H    OCHF2Me   Me    H    H    C2F5Et   Me    H    H    C2F5Me   Me    H    H    OCF3Me   Me    H    H    OCF2CHF2 R 3   R 4a  R 4b  R 5a  R 5bMe    H    Cl    Me    CF3Me    H    Cl    Me    OCF3Et    H    Cl    Me    CF3Me    H    Cl    Me    SCF3Me    H    Cl    Me    SCHF2Me    H    Cl    Me    OCHF2n-Pr  H    Cl    Me    CF3Me    H    Cl    Me    C2F5Et    H    Cl    Me    C2F5Me    H    Cl    Et    CF3Me    H    Cl    n-Pr  CF3Me    H    Cl    i-Pr  CF3Me    H    Cl    Cl    CF3Me    H    Cl    F     CF3Me    H    Cl    Me    SMeMe    H    Cl    Me    OMeMe    H    Cl    Me    OEtMe    H    Cl    Me    n-C3F7Me    H    Cl    Me    i-C3F7Me    H    Cl    Me    EtMe    H    Cl    Me    OCF2CHF2Me    H    Cl    Me    SCF2CHF2Me    H    Cl    Me    SO2MeMe    H    Cl    Me    SO2CF3Me    H    Cl    CF3  CF3Me    H    Cl    CF3  MeMe    H    Cl    OMe   CF3Me    H    Cl    H     CF3Me    H    Cl    H     OCHF2Me    H    Cl    H     C2F5Et    H    Cl    H     C2F5Me    H    Cl    H     OCF3Me    H    Cl    H     OCF2CHF2Me    H    Cl    H     SCF2CHF2Me    H    Cl    H     n-C3F7Me    H    Cl    H     i-C3F7Me    H    Cl    H     Br   R 3 R 4a  R 4b  R 5a             R 5bMe  Me    H    H                SCF2CHF2Me  Me    H    H                n-C3F7Me  Me    H    H                i-C3F7Me  Me    H    H                BrMe  Me    H    H                ClMe  Me    H    H                SCF3Me  Me    H    Ph               CF3Me  Me    H    Ph               ClMe  Me    H    Ph               BrMe  Me    H    2-吡啶基         CF3Me  Me    H    2-吡啶基         ClMe  Me    H    2-ClPh           CF3Me  Me    H    2-ClPh           OCF3Me  Me    H    2-ClPh           BrMe  Me    H    2-ClPh           ClMe  Me    H    2-ClPh           SCHF2Me  Me    H    2-BrPh           CF3Me  Me    H    2-MePh           CF3Me  Me    H    2-CNPh           CF3Me  Me    H    2-FPh            CF3Me  Me    H    2,6-F2Ph        CF3Me  Me    H    2,4-F2Ph        CF3Me  Me    H    2,5-F2Ph        CF3Me  Me    H    2-MeOPh          CF3Me  Me    H    3-Cl-2-吡啶基    CF3Me  Me    H    3-Cl-2-吡啶基    OCF3Me  Me    H    3-Cl-2-吡啶基    BrMe  H     Cl   3-CF3-2-        CF3吡啶基Me  Me    H    3-Cl-2-吡啶基    SCHF2Me  Me    H    3-F-2-吡啶基     CF3Me  Me    H    3-CF3-2-        CF3吡啶基Me  H     Cl   3-Br-2-吡啶基    BrMe  Me    H    3-Br-2-吡啶基    CF3Me  Me    H    3-Br-2-吡啶基    OCF3Me  Me    H    3-Br-2-吡啶基    Br R 3   R 4a  R 4b  R 5a           R 5bMe    H    Cl    H              ClMe    H    Cl    H              SCF3Me    H    Cl    Ph             CF3Me    H    Cl    Ph             ClMe    H    Cl    Ph             BrMe    H    Cl    2-吡啶基       CF3Me    H    Cl    2-吡啶基       ClMe    H    Cl    2-ClPh         CF3Me    H    Cl    2-ClPh         OCF3Me    H    Cl    2-ClPh         BrMe    H    Cl    2-ClPh         ClMe    H    Cl    2-ClPh         SCHF2Me    H    Cl    2-BrPh         CF3Me    H    Cl    2-MePh         CF3Me    H    Cl    2-CNPh         CF3Me    H    Cl    2-FPh          CF3Me    H    Cl    2,6-F2Ph      CF3Me    H    Cl    2,4-F2Ph      CF3Me    H    Cl    2,5-F2Ph      CF3Me    H    Cl    2-MeOPh        CF3Me    H    Cl    3-Cl-2-吡啶基  CF3Me    H    Cl    3-Cl-2-吡啶基  OCF3Me    H    Cl    3-Cl-2-吡啶基  BrMe    H    Cl    3-Cl-2-吡啶基  ClMe    H    Cl    3-Cl-2-吡啶基  SCHF2Me    H    Cl    3-F-2-吡啶基   CF3Me    Me   H     3-Cl-2-吡啶基  ClMe    H    Cl    3-Me-2-        CF3吡啶基Me    H    Cl    3-Br-2-吡啶基  CF3Me    H    Cl    3-Br-2-吡啶基  OCF3Me    Me   H     3-Me-2-        CF3吡啶基Me    H    Cl    3-Br-2-吡啶基  ClMe    Cl   H     H              OCF3Me    Cl   H     H              OCF2CHF2Me    Cl   H     H              SCF2CHF2 R 3  R 4a  R 4b R 5a          R 5bMe   Me   H   3-Br-2-吡啶基 ClMe   Cl   H   Me            BrMe   Cl   H   Et            BrMe   Cl   H   Me            ClMe   Cl   H   Et            ClMe   Cl   H   Me            IMe   Cl   H   Me            CF3Me   Cl   H   Me            OCF3Et   Cl   H   Me            CF3Me   Cl   H   Me            SCF3Me   Cl   H   Me            SCHF2Me   Cl   H   Me            OCHF2n-Pr Cl   H   Me            CF3Me   Cl   H   Me            C2F5Et   Cl   H   Me            C2F5Me   Cl   H   Et            CF3Me   Cl   H   n-Pr          CF3Me   Cl   H   i-Pr          CF3Me   Cl   H   Cl            CF3Me   Cl   H   F             CF3Me   Cl   H   Me            SMeMe   Cl   H   Me            OMeMe   Cl   H   Me            OEtMe   Cl   H   Me            n-C3F7Me   Cl   H   Me            i-C3F7Me   Cl   H   Me            EtMe   Cl   H   Me            OCF2CHF2Me   Cl   H   Me            SCF2CHF2Me   Cl   H   Me            SO2MeMe   Cl   H   3-Me-2-       CF3吡啶基Me   Cl   H   CF3          CF3Me   Cl   H   CF3          MeMe   Cl   H   OMe           CF3Me   Cl   H   H             CF3Me   Cl   H   H             OCHF2Me   Cl   H   H             C2F5 R 3   R 4a  R 4b  R 5a           R 5bMe    Cl    H    H              n-C3F7Me    Cl    H    H              i-C3F7Me    Cl    H    H              BrMe    Cl    H    H              ClMe    Cl    H    H              SCF3Me    Cl    H    Ph             CF3Me    Cl    H    Ph             ClMe    Cl    H    Ph             BrMe    Cl    H    2-吡啶基       CF3Me    Cl    H    2-吡啶基       ClMe    Cl    H    2-ClPh         CF3Me    Cl    H    2-ClPh         OCF3Me    Cl    H    2-ClPh         BrMe    Cl    H    2-ClPh         ClMe    Cl    H    2-ClPh         SCHF2Me    Cl    H    2-BrPh         CF3Me    Cl    H    2-MePh         CF3Me    Cl    H    2-CNPh         CF3Me     Cl    H    2-FPh          CF3Me    Cl    H    2,6-F2Ph      CF3Me    Cl    H    2,4-F2Ph      CF3Me    Cl    H    2,5-F2Ph      CF3Me    Cl    H    2-MeOPh        CF3Me    Cl    H    3-Cl-2-吡啶基  CF3Me    Cl    H    3-Cl-2-吡啶基  OCF3Me    Cl    H    3-Cl-2-吡啶基  BrMe    Cl    H    3-Cl-2-吡啶基  ClMe    Cl    H    3-Cl-2-吡啶基  SCHF2Me    Cl    H    3-F-2-吡啶基   CF3Me    Cl    H    3-CF3-2-      CF3吡啶基Me    Cl    H    Me             SO2CF3Me    Cl    H    3-Br-2-吡啶基  CF3Me    Cl    H    3-Br-2-吡啶基  OCF3Me    Cl    H    3-Br-2-吡啶基  BrMe    Cl    H    3-Br-2-吡啶基  ClEt    Cl    H    H              C2F5 Table 7 R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me EtMe H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H Cl R 3 R 4a R 4b R 5a R 5b Me H H Me CCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me EtMe H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H OCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H Cl R 3 R 4a R 4b R 5a R 5b Me H Me H SCF 3 Me H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2 -ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3- Cl-2-pyridylClMeHMe3-Cl- 2 -pyridylSCHF2MeHMe3-F - 2 -pyridylCF3MeHMe3- CF3-2 -CF3pyridylMeHMe3 -Me-2- CF 3 pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3 -Br-2-PyridinylClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me Br R 3 R 4a R 4b R 5a R 5b Me H H H SCF 3 Me H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-pyridyl CF 3 Me H H 2-pyridyl ClMe H H 2-ClPh CF 3 Me H H 2- ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2 -FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2-pyridyl ClMe H H 3-Cl-2-pyridyl SCHF 2 Me H H 3-F- 2-pyridyl CF 3 Me H H 3-CF 3 -2- CF 3 pyridyl Me H H 3-Me-2- CF 3 pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2 -pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me I R 3 R 4a R 4b R 5a R 5b Me Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMeMe Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 R 3 R 4a R 4b R 5a R 5b Me H Cl Me CF 3 Me H Cl Me OCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H Br R 3 R 4a R 4b R 5a R 5b Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me H 3-Cl-2-pyridyl BrMe H Cl 3-CF 3 -2- CF 3pyridyl Me Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me H 3-CF 3 -2- CF 3 pyridyl Me H Cl 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl Br R 3 R 4a R 4b R 5a R 5b Me H Cl H ClMe H Cl H SCF 3 Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe HCl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me H Cl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2-pyridyl BrMe H Cl 3-Cl-2-pyridylClMe H Cl 3-Cl-2-pyridylSCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridylClMe H Cl 3- Me-2- CF 3 pyridyl Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me Me H 3-Me-2- CF 3 pyridyl Me H Cl 3 - Br - 2 - PyridinylClMeClHHOCF3MeClHHOCF2CHF2MeClHHSCF2CHF2 R 3 R 4a R 4b R 5a R 5b Me Me H 3-Br-2-pyridyl ClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 Me Cl H F CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H 3-Me-2- CF 3 Pyridine Me Cl H CF 3 CF 3 Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-pyridyl CF 3 Me Cl H 2-pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 MeClH 2-BrPh CF 3 MeClH 2-MePh CF 3 MeClH 2-CNPh CF 3 MeClH 2-FPh CF 3 MeClH 2,6-F 2 PhCF 3 MeClH 2, 4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2-MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridine OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2-pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H 3-CF 3 -2- CF 3 pyridyl Me Cl H Me SO 2 CF 3 Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br-2-pyridyl ClEt Cl H H C 2 F 5

                                  表8

Figure A0180519000791
R 3   R 4a  R 4b  R 5a  R 5bMe    H    Me    H     CF3Me    H    Me    H     OCF3Et    H    Me    H     OCF3Me    H    Me    Me    BrMe    H    Me    Et    BrMe    H    Me    Me    ClMe    H    Me    Et    ClMe    H    Me    Me    IMe    H    Me    Me    CF3Me    H    Me    Me    OCF3Et    H    Me    Me    CF3Me    H    Me    Me    SCF3Me    H    Me    Me    SCHF2Me    H    Me    Me    OCHF2n-Pr  H    Me    Me    CF3Me    H    Me    Me    C2F5Et    H    Me    Me    C2F5Me    H    Me    Et    CF3Me    H    Me    n-Pr  CF3Me    H    Me    i-Pr  CF3Me    H    Me    Cl    CF3Me    H    Me    F     CF3Me    H    Me    Me    SMeMe    H    Me    Me    OMeMe    H    Me    Me    OEtMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    Et R 3   R 4a  R 4b R 5a   R 5bMe    H    H    H     CF3Me    H    H    H     CCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3Me    H    H    Me    OCF3Et    H    H    Me    CF3Me    H    H    Me    SCF3Me    H    H    Me    SCHF2Me    H    H    Me    OCHF2n-Pr  H    H    Me    CF3Me    H    H    Me    C2F5Et    H    H    Me    C2F5Me    H    H    Et    CF3Me    H    H    n-Pr  CF3Me    H    H    i-Pr  CF3Me    H    H    Cl    CF3Me    H    H    F     CF3Me    H    H    Me    SMeMe    H    H    Me    OMeMe    H    H    Me    OEtMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    Et   R 3   R 4a R 4b  R 5a         R 5bMe    H    Me    Me          OCF2CHF2Me    H    Me    Me          SCF2CHF2Me    H    Me    Me          SO2MeMe    H    Me    Me          SO2CF3Me    H    Me    CF3        CF3Me    H    Me    CF3        MeMe    H    Me    OMe         CF3Me    H    Me    H           CF3Me    H    Me    H           OCHF2Me    H    Me    H           C2F5Et    H    Me    H           C2F5Me    H    Me    H           OCF3Me    H    Me    H           OCF2CHF2Me    H    Me    H           SCF2CHF2Me    H    Me    H           n-C3F7Me    H    Me    H           i-C3F7Me    H    Me    H           BrMe    H    Me    H           ClMe    H    Me    H           SCF3Me    H    Me    Ph          CF3Me    H    Me    Ph          ClMe    H    Me    Ph          BrMe    H    Me    2-吡啶基    CF3Me    H    Me    2-吡啶基    ClMe    H    Me    2-ClPh      CF3Me    H    Me    2-ClPh      OCF3Me    H    Me    2-ClPh      BrMe    H    Me    2-ClPh      ClMe    H    Me    2-ClPh      SCHF2Me    H    Me    2-BrPh      CF3Me    H    Me    2-MePh      CF3Me    H    Me    2-CNPh      CF3Me    H    Me    2-FPh       CF3Me    H    Me    2,6-F2Ph   CF3Me    H    Me    2,4-F2Ph   CF3Me    H    Me    2,5-F2Ph   CF3Me    H    Me    2-MeOPh     CF3 R 3   R 4a  R 4b R 5a         R 5bMe    H    H    Me          OCF2CHF2Me    H    H    Me          SCF2CHF2Me    H    H    Me          SO2MeMe    H    H    Me          SO2CF3Me    H    H    CF3        CF3Me    H    H    CF3        MeMe    H    H    OMe         CF3Me    H    H    H           CF3Me    H    H    H           OCHF2Me    H    H    H           C2F5Et    H    H    H           C2F5Me    H    H    H           OCF3Me    H    H    H           OCF2CHF2Me    H    H    H           SCF2CHF2Me    H    H    H           n-C3F7Me    H    H    H           i-C3F7Me    H    H    H           BrMe    H    H    H           ClMe    H    H    H           SCF3Me    H    H    Ph          CF3Me    H    H    Ph          ClMe    H    H    Ph          BrMe    H    H    2-吡啶基    CF3Me    H    H    2-吡啶基    ClMe    H    H    2-ClPh      CF3Me    H    H    2-ClPh      OCF3Me    H    H    2-ClPh      BrMe    H    H    2-ClPh      ClMe    H    H    2-ClPh      SCHF2Me    H    H    2-BrPh      CF3Me    H    H    2-MePh      CF3Me    H    H    2-CNPh      CF3Me    H    H    2-FPh       CF3Me    H    H    2,6-F2Ph   CF3Me    H    H    2,4-F2Ph   CF3Me    H    H    2,5-F2Ph   CF3Me    H    H    2-MeOPh     CF3 R 3   R 4a  R 4b    R 5a         R 5bMe    H    Me    3-Cl-2-吡啶基  CF3Me    H    Me    3-Cl-2-吡啶基  OCF3Me    H    Me    3-Cl-2-吡啶基  BrMe    H    Me    3-Cl-2-吡啶基  ClMe    H    Me    3-Cl-2-吡啶基  SCHF2Me    H    Me    3-F-2-吡啶基   CF3Me    H    Me    3-CF3-2-      CF3吡啶基Me    H    Me    3-Me-2-        CF3吡啶基Me    H    Me    3-Br-2-吡啶基  CF3Me    H    Me    3-Br-2-吡啶基  OCF3Me    H    Me    3-Br-2-吡啶基  BrMe    H    Me    3-Br-2-吡啶基  ClMe    Me   H     H              CF3Me    Me   H     H              OCF3Et    Me   H     H              OCF3Me    Me   H     Me             BrMe    Me   H     Et             BrMe    Me   H     Me             ClMe    Me   H     Et             ClMe    Me   H     Me             IMe    Me   H     Me             CF3Me    Me   H     Me             OCF3Et    Me   H     Me             CF3Me    Me   H     Me             SCF3Me    Me   H     Me             SCHF2Me    Me   H     Me             OCHF2n-Pr  Me   H     Me             CF3Me    Me   H     Me             C2F5Et    Me   H     Me             C2F5Me    Me   H     Et             CF3Me    Me   H     n-Pr           CF3Me    Me   H     i-Pr           CF3Me    Me   H     Cl             CF3Me    Me   H     F              CF3Me    Me   H     Me             SMe R 3   R 4a  R 4b     R 5a         R 5bMe    H    H    3-Cl-2-吡啶基    CF3Me    H    H    3-Cl-2-吡啶基    OCF3Me    H    H    3-Cl-2-吡啶基    BrMe    H    H    3-Cl-2-吡啶基    ClMe    H    H    3-Cl-2-吡啶基    SCHF2Me    H    H    3-F-2-吡啶基     CF3Me    H    H    3-CF3-2-        CF3吡啶基Me    H    H    3-Me-2-          CF3吡啶基Me    H    H    3-Br-2-吡啶基    CF3Me    H    H    3-Br-2-吡啶基    OCF3Me    H    H    3-Br-2-吡啶基    BrMe    H    H    3-Br-2-吡啶基    ClMe    H    Cl   Et               BrMe    H    Cl   Me               ClMe    H    Cl   Et               ClMe    H    Cl   Me               IMe    H    Cl   Me               CF3Me    H    Cl   Me               OF3Et    H    Cl   Me               CF3Me    H    Cl   Me               SCF3Me    H    Cl   Me               SCHF2Me    H    Cl   Me               OCHF2n-Pr  H    Cl   Me               CF3Me    H    Cl   Me               C2F5Et    H    Cl   Me               C2F5Me    H    Cl   Et               CF3Me    H    Cl   n-Pr             CF3Me    H    Cl   i-Pr             CF3Me    H    Cl   Cl               CF3Me    H    Cl   F                CF3Me    H    Cl   Me               SMeMe    H    Cl   Me               OMeMe    H    Cl   Me               OEtMe    H    Cl   Me               n-C3F7Me    H    Cl   Me               i-C3F7     R 3 R 4a  R 4b  R 5a     R 5bMe  Me    H    Me       OMeMe  Me    H    Me       OEtMe  Me    H    Me       n-C3F7Me  Me    H    Me       i-C3F7Me  Me    H    Me       EtMe  Me    H    Me       OCF2CHF2Me  Me    H    Me       SCF2CHF2Me  Me    H    Me       SO2MeMe  Me    H    Me       SO2CF3Me  Me    H    CF3     CF3Me  Me    H    CF3     MeMe  Me    H    OMe      CF3Me  Me    H    H        CF3Me  Me    H    H        OCHF2Me  Me    H    H        C2F5Et  Me    H    H        C2F5Me  Me    H    H        OCF3Me  Me    H    H        OCF2CHF2Me  Me    H    H        SCF2CHF2Me  Me    H    H        n-C3F7Me  Me    H    H        i-C3F7Me  Me    H    H        BrMe  Me    H    H        ClMe  Me    H    H        SCF3Me  Me    H    Ph       CF3Me  Me    H    Ph       ClMe  Me    H    Ph       BrMe  Me    H    2-吡啶基 CF3Me  Me    H    2-吡啶基 ClMe  Me    H    2-ClPh   CF3Me  Me    H    2-ClPh   OCF3Me  Me    H    2-ClPh   BrMe  Me    H    2-ClPh   ClMe  Me    H    2-ClPh   SCHF2Me  Me    H    2-BrPh   CF3Me  Me    H    2-MePh   CF3Me  Me    H    2-CNPh   CF3 R 3   R 4a  R 4b  R 5a      R 5bMe    H    Cl    Me        ElMe    H    Cl    Me        OCF2CHF2Me    H    Cl    Me        SCF2CHF2Me    H    Cl    Me        SO2MeMe    H    Cl    Me        SO2CF3Me    H    Cl    CF3      CF3Me    H    Cl    CF3      MeMe    H    Cl    OMe       CF3Me    H    Cl    H         CF3Me    H    Cl    H         OCHF2Me    H    Cl    H         C2F5Et    H    Cl    H         C2F5Me    H    Cl    H         OCF3Me    H    Cl    H         OCF2CHF2Me    H    Cl    H         SCF2CHF2Me    H    Cl    H         n-C3F7Me    H    Cl    H         i-C3F7Me    H    Cl    H         BrMe    H    Cl    H         ClMe    H    Cl    H         SCF3Me    H    Cl    Ph        CF3Me    H    Cl    Ph        ClMe    H    Cl    Ph        BrMe    H    Cl    2-吡啶基  CF3Me    H    Cl    2-吡啶基  ClMe    H    Cl    2-ClPh    CF3Me    H    Cl    2-ClPh    OCF3Me    H    Cl    2-ClPh    BrMe    H    Cl    2-ClPh    ClMe    H    Cl    2-ClPh    SCHF2Me    H    Cl    2-BrPh    CF3Me    H    Cl    2-MePh    CF3Me    H    Cl    2-CNPh    CF3Me    H    Cl    2-FPh     CF3Me    H    Cl    2,6-F2Ph CF3Me    H    Cl    2,4-F2Ph CF3Me    H    Cl    2,5-F2Ph CF3   R 3  R 4a  R 4b  R 5a          R 5bMe   Me    H    2-FPh          CF3Me   Me    H    2,6-F2Ph      CF3Me   Me    H    2,4-F2Ph      CF3Me   Me    H    2,5-F2Ph      CF3Me   Me    H    2-MeOPh        CF3Me   Me    H    3-Cl-2-吡啶基  CF3Me   Me    H    3-Cl-2-吡啶基  OCF3Me   Me    H    3-CF3-2-      CF3吡啶基Me   Me    H    3-Me-2-        CF3吡啶基Me   Me    H    3-Cl-2-吡啶基  SCHF2Me   Me    H    3-F-2-吡啶基   CF3Me   Me    H    3-Cl-2-吡啶基  BrMe   Me    H    3-Cl-2-吡啶基  ClMe   Me    H    3-Br-2-吡啶基  CF3Me   Me    H    3-Br-2-吡啶基  OCF3Me   Me    H    3-Br-2-吡啶基  BrMe   Me    H    3-Br-2-吡啶基  ClMe   Cl    H    Me             BrMe   Cl    H    Et             BrMe   Cl    H    Me             ClMe   Cl    H    Et             ClMe   Cl    H    Me             IMe   Cl    H    Me             CF3Me   Cl    H    Me             OCF3Et   Cl    H    Me             CF3Me   Cl    H    Me             SCF3Me   Cl    H    Me             SCHF2Me   Cl    H    Me             OCHF2n-Pr Cl    H    Me             CF3Me   Cl    H    Me             C2F5Et   Cl    H    Me             C2F5Me   Cl    H    Et             CF3Me   Cl    H    n-Pr           CF3Me   Cl    H    i-Pr           CF3Me   Cl    H    Cl             CF3 R 3   R 4a  R 4b  R 5a            R 5bMe    H     Cl   2-MeOPh          CF3Me    H     Cl   3-Cl-2-吡啶基    CF3Me    H     Cl   3-Cl-2-吡啶基    OCF3Me    H     Cl   3-Cl-2-吡啶基    BrMe    H     Cl   3-Cl-2-吡啶基    ClMe    H     Cl   3-Cl-2-吡啶基    SCHF2Me    H     Cl   3-F-2-吡啶基     CF3Me    H     Cl   3-CF3-2-        CF3吡啶基Me    H     Cl   3-Me-2-          CF3吡啶基Me    H     Cl   3-Br-2-吡啶基    CF3Me    H     Cl   3-Br-2-吡啶基    OCF3Me    H     Cl   3-Br-2-吡啶基    BrMe    H     Cl   3-Br-2-吡啶基    ClMe    Cl    H    H                OCF3Me    Cl    H    H                OCF2CHF2Me    Cl    H    H                SCF2CHF2Me    Cl    H    H                n-C3F7Me    Cl    H    H                i-C3F7Me    Cl    H    H                BrMe    Cl    H    H                ClMe    Cl    H    H                SCF3Me    Cl    H    Ph               CF3Me    Cl    H    Ph               ClMe    Cl    H    Ph               BrMe    Cl    H    2-吡啶基         CF3Me    Cl    H    2-吡啶基         ClMe    Cl    H    2-ClPh           CF3Me    Cl    H    2-ClPh           OCF3Me    Cl    H    2-ClPh           BrMe    Cl    H    2-ClPh           ClMe    Cl    H    2-ClPh           SCHF2Me    Cl    H    2-BrPh           CF3Me    Cl    H    2-MePh           CF3Me    Cl    H    2-CNPh           CF3Me    Cl    H    2-FPh            CF3 R 3   R 4a  R 4b R 5a      R 5bMe    Cl    H    F         CF3Me    Cl    H    Me        SMeMe    Cl    H    Me        OMeMe    Cl    H    Me        OEtMe    Cl    H    Me        n-C3F7Me    Cl    H    Me        i-C3F7Me    Cl    H    Me        EtMe    Cl    H    Me        OCF2CHF2Me    Cl    H    Me        SCF2CHF2Me    Cl    H    Me        SO2MeMe    Cl    H    Me        SO2CF3Me    Cl    H    3-CF3-2- CF3吡啶基Me    Cl    H    CF3      MeMe    Cl    H    OMe       CF3Me    Cl    H    H         CF3Me    Cl    H    H         OCHF2Me    Cl    H    H         C2F5 R 3   R 4a  R 4b     R 5a        R 5bMe    Cl    H    2,6-F2Ph      CF3Me    Cl    H    2,4-F2Ph      CF3Me    Cl    H    2,5-F2Ph      CF3Me    Cl    H    2-MeOPh        CF3Me    Cl    H    3-Cl-2-吡啶基  CF3Me    Cl    H    3-Cl-2-吡啶基  OCF3Me    Cl    H    3-Cl-2-吡啶基  BrMe    Cl    H    3-Cl-2-吡啶基  ClMe    Cl    H    3-Cl-2-吡啶基  SCHF2Me    Cl    H    3-F-2-吡啶基   CF3Me    Cl    H    CF3           CF3Me    Cl    H    3-Me-2-        CF3吡啶基Me    Cl    H    3-Br-2-吡啶基  CF3Me    Cl    H    3-Br-2-吡啶基  OCF3Me    Cl    H    3-Br-2-吡啶基  BrMe    Cl    H    3-Br-2-吡啶基  ClEt    Cl    H    H              C2F5 Table 8
Figure A0180519000791
R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me Cl CF 3 Me H Me F CF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me Et R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H CCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pr CF 3 Me H H i-Pr CF 3 Me H H Cl CF 3 Me H H F CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me Et R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CF 3 CF 3 Me H Me CF 3 MeMe H Me OMe CF 3 Me H Me H CF 3 Me H Me H OCHF 2 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H OCF 3 Me H Me H OCF 2 CHF 2 Me H Me H SCF 2 CHF 2 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me H BrMe H Me H ClMe H Me H SCF 3 Me H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2 ,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H OMe CF 3 Me H H H CF 3 Me H H H OCHF 2 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H OCF 3 Me H H H OCF 2 CHF 2 Me H H H SCF 2 CHF 2 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H BrMe H H H ClMe H H H SCF 3 Me H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-Pyridyl CF 3 Me H H 2-Pyridyl ClMe H H 2-ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridylClMeH Me 3-Cl- 2 -pyridylSCHF2MeHMe3-F- 2 -pyridylCF3MeHMe3- CF3-2 - CF3pyridylMeH Me 3-Me-2-CF 3- pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridylClMe Me H H CF 3 Me Me H H OCF 3 Et Me H H OCF 3 Me Me H Me BrMe Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Cl CF 3 Me Me H F CF 3 Me Me H Me SMe R 3 R 4a R 4b R 5a R 5b Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl- 2-pyridylClMeHH 3-Cl-2-pyridylSCHF2MeHH3-F-2 - pyridylCF3MeHH3- CF3-2 - CF3pyridylMeHH3 -Me-2-CF 3- pyridyl Me H H 3-Br-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me OF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n -Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl CF 3 Me H Cl F CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me OEtMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 R 3 R 4a R 4b R 5a R 5b Me Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H OMe CF 3 Me Me H H CF 3 Me Me H H OCHF 2 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H OCF 3 Me Me H H OCF 2 CHF 2 Me Me H H SCF 2 CHF 2 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H BrMe Me H H ClMe Me H H SCF 3 Me Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-pyridyl CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2-BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl Me ElMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl OMe CF 3 Me H Cl H CF 3 Me H Cl H OCHF 2 Me H Cl H C 2 F 5 Et H Cl H C 2 F 5 Me H Cl H OCF 3 Me H Cl H OCF 2 CHF 2 Me H Cl H SCF 2 CHF 2 Me H Cl H nC 3 F 7 Me H Cl H iC 3 F 7 Me H Cl H BrMe H Cl H ClMe H Cl H SCF 3 Me H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2-pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2-MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me HCl 2,4-F 2 Ph CF 3 Me H Cl 2,5-F 2 Ph CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CF 3 Me Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-CF 3 -2- CF 3 Pyridyl Me Me H 3-Me-2- CF 3 Pyridyl Me Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me Me H 3-Cl-2- Pyridyl BrMe Me H 3-Cl-2-pyridyl ClMe Me H 3-Br-2-pyridyl CF 3 Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridylClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Cl CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl 2-MeOPh CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF3Me H Cl 3-Cl-2 -PyridylBrMeHCl 3-Cl-2-PyridylClMeHCl 3-Cl-2-PyridylSCHF 2 Me H Cl 3-F-2-PyridylCF 3 Me HCl 3-CF 3 -2- CF 3 Pyridyl Me H Cl 3-Me-2- CF 3 Pyridyl Me H Cl 3-Br-2-Pyridyl CF 3 Me H Cl 3-Br-2-Pyridyl OCF 3 Me H Cl 3-Br- 2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe Cl H H OCF 3 Me Cl H H OCF 2 CHF 2 Me Cl H H SCF 2 CHF 2 Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H H BrMe Cl H H ClMe Cl H H SCF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-Pyridyl CF 3 Me Cl H 2-Pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 2-ClPh OCF 3 Me Cl H 2-ClPh BrMe Cl H 2-ClPh ClMe Cl H 2-ClPh SCHF 2 Me Cl H 2-BrPh CF 3 Me Cl H 2-MePh CF 3 Me Cl H 2-CNPh CF 3 Me ClH2- FPhCF3 R 3 R 4a R 4b R 5a R 5b Me Cl H F CF 3 Me Cl H Me SMeMe Cl H Me OMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H 3-CF 3 -2- CF 3 Pyridyl Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H H CF 3 Me Cl H H OCHF 2 Me Cl H H C 2 F 5 R 3 R 4a R 4b R 5a R 5b Me Cl H 2,6-F 2 Ph CF 3 Me Cl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2 -MeOPh CF 3 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2- Pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H CF 3 CF 3 Me Cl H 3-Me-2-CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br-2-pyridyl ClEt Cl H H C 2 F 5

                          表9 R 3  R 4a  R 4b  R 5a  R 5bMe    H    Me    H    CF3Me    H    Me    H    OCF3Et    H    Me    H    OCF3Me    H    Me    Me   BrMe    H    Me    Et   BrMe    H    Me    Me   ClMe    H    Me    Et   ClMe    H    Me    Me   IMe    H    Me    Me   CF3 R 3  R 4a  R 4b  R 5a  R 5bMe    H    H    H     CF3Me    H    H    H     OCF3Et    H    H    H     OCF3Me    H    H    Me    BrMe    H    H    Et    BrMe    H    H    Me    ClMe    H    H    Et    ClMe    H    H    Me    IMe    H    H    Me    CF3   R 3  R 4a  R 4b  R 5a      R 5bMe    H    Me    Me        OCF3Et    H    Me    Me        CF3Me    H    Me    Me        SCF3Me    H    Me    Me        SCHF2Me    H    Me    Me        OCHF2n-Pr  H    Me    Me        CF3Me    H    Me    Me        C2F5Et    H    Me    Me        C2F5Me    H    Me    Et        CF3Me    H    Me    n-Pr      CF3Me    H    Me    i-Pr      CF3Me    H    Me    i-Pr      OCF3Me    H    Me    Me        SMeMe    H    Me    Me        OMeMe    H    Me    Me        OEtMe    H    Me    Me        n-C3F7Me    H    Me    Me        i-C3F7Me    H    Me    Me        EtMe    H    Me    Me        OCF2CHF2Me    H    Me    Me        SCF2CHF2Me    H    Me    Me        SO2MeMe    H    Me    Me        SO2CF3Me    H    Me    CHF2     CF3Me    H    Me    CHF2     MeMe    H    Me    Ph        CF3Me    H    Me    Ph        ClMe    H    Me    Ph        BrMe    H    Me    2-吡啶基  CF3Me    H    Me    2-吡啶基  ClMe    H    Me    2-ClPh    CF3Me    H    Me    2-ClPh    OCF3Me    H    Me    2-ClPh    BrMe    H    Me    2-ClPh    ClMe    H    Me    2-ClPh    SCHF2Me    H    Me    2-BrPh    CF3Me    H    Me    2-MePh    CF3Me    H    Me    2-CNPh    CF3   R 3  R 4a  R 4b R 5a      R 5bMe    H    H    Me        OCF3Et    H    H    Me        CF3Me    H    H    Me        SCF3Me    H    H    Me        SCHF2Me    H    H    Me        OCHF2n-Pr  H    H    Me        CF3Me    H    H    Me        C2F5Et    H    H    Me        C2F5Me    H    H    Et        CF3Me    H    H    n-Pt      CF3Me    H    H    i-Pr      CF3Me    H    H    Me        SMeMe    H    H    Me        OMeMe    H    H    Me        OEtMe    H    H    Me        n-C3F7Me    H    H    Me        i-C3F7Me    H    H    Me        EtMe    H    H    Me        OCF2CHF2Me    H    H    Me        SCF2CHF2Me    H    H    Me        SO2MeMe    H    H    Me        SO2CF3Me    H    H    CF3      CF3Me    H    H    CF3      MeMe    H    H    Ph        CF3Me    H    H    Ph        ClMe    H    H    Ph        BrMe    H    H    2-吡啶基  CF3Me    H    H    2-吡啶基  ClMe    H    H    2-ClPh    CF3Me    H    H    2-ClPh    OCF3Me    H    H    2-ClPh    BrMe    H    H    2-ClPh    ClMe    H    H    2-ClPh    SCHF2Me    H    H    2-BrPh    CF3Me    H    H    2-MePh    CF3Me    H    H    2-CNPh    CF3Me    H    H    2-FPh     CF3   R 3   R 4a R 4b    R 5a          R 5bMe    H    Me    2-FPh          CF3Me    H    Me    2,6-F2Ph      CF3Me    H    Me    2,4-F2Ph      CF3Me    H    Me    2,5-F2Ph      CF3Me    H    Me    2-MeOPh        CF3Me    H    Me    3-Cl-2-吡啶基  CF3Me    H    Me    3-Cl-2-吡啶基  OCF3Me    H    Me    3-Cl-2-吡啶基  BrMe    H    Me    3-Cl-2-吡啶基  ClMe    H    Me    3-Cl-2-吡啶基  SCHF2Me    H    Me    3-CF3-2-      CF3吡啶基Me    H    Me    3-Me-2-        CF3吡啶基Me    H    Me    3-F-2-吡啶基   CF3Me    H    Me    3-Br-2-吡啶基  CF3Me    H    Me    3-Br-2-吡啶基  OCF3Me    H    Me    3-Br-2-吡啶基  BrMe    H    Me    3-Br-2-吡啶基  ClMe    Me   H     Me             BrMe    Me   H     Et             BrMe    Me   H     Me             ClMe    Me   H     Et             ClMe    Me   H     Me             IMe    Me   H     Me             CF3Me    Me   H     Me             OCF3Et    Me   H     Me             CF3Me    Me   H     Me             SCF3Me    Me   H     Me             SCHF2Me    Me   H     Me             OCHF2n-Pr  Me   H     Me             CF3Me    Me   H     Me             C2F5Et    Me   H     Me             C2F5Me    Me   H     Et             CF3Me    Me   H     n-Pr           CF3Me    Me   H     i-Pr           CF3Me    Me   H     Me             SMe R 3   R 4a  R 4b     R 5a        R 5bMe    H    H     2,6-F2Ph      CF3Me    H    H     2,4-F2Ph      CF3Me    H    H     2,5-F2Ph      CF3Me    H    H     2-MeOPh        CF3Me    H    H     3-Cl-2-吡啶基  CF3Me    H    H     3-Cl-2-吡啶基  OCF3Me    H    H     3-Cl-2-吡啶基  BrMe    H    H     3-Cl-2-吡啶基  ClMe    H    H     3-Cl-2-吡啶基  SCHF2Me    H    H     3-F-2-吡啶基   CF3Me    H    H     3-CF3-2-      CF3吡啶基Me    H    H     3-Me-2-        CF3吡啶基Me    H    H     3-B-r2-吡啶基  CF3Me    H    H     3-Br-2-吡啶基  OCF3Me    H    H     3-Br-2-吡啶基  BrMe    H    H     3-Br-2-吡啶基  ClMe    H    Cl    Et             BrMe    H    Cl    Me             ClMe    H    Cl    Et             ClMe    H    Cl    Me             IMe    H    Cl    Me             CF3Me    H    Cl    Me             OCF3Et    H    Cl    Me             CF3Me    H    Cl    Me             SCF3Me    H    Cl    Me             SCHF2Me    H    Cl    Me             OCHF2n-Pr  H    Cl    Me             CF3Me    H    Cl    Me             C2F5Et    H    Cl    Me             C2F5Me    H    Cl    Et             CF3Me    H    Cl    n-Pr           CF3Me    H    Cl    i-Pr           CF3Me    H    Cl    Me             SMeMe    H    Cl    Me             OMeMe    H    Cl    Me             CEt R 3  R 4a  R 4b R 5a             R 5bMe  Me    H    Me              OMeMe  Me    H    Me              OEtMe  Me    H    Me              n-C3F7Me  Me    H    Me              i-C3F7Me  Me    H    Me              EtMe  Me    H    Me              OCF2CHF2Me  Me    H    Me              SCF2CHF2Me  Me    H    Me              SO2MeMe  Me    H    Me              SO2CF3Me  Me    H    CF3            CF3Me  Me    H    CF3            MeMe  Me    H    Ph              CF3Me  Me    H    Ph              ClMe  Me    H    Ph              BrMe  Me    H    2-吡啶基        CF3Me  Me    H    2-吡啶基        ClMe  Me    H    2-ClPh          CF3Me  Me    H    2-ClPh          OCF3Me  Me    H    2-ClPh          BrMe  Me    H    2-ClPh          ClMe  Me    H    2-ClPh          SCHF2Me  Me    H    2-BrPh          CF3Me  Me    H    2-MePh          CF3Me  Me    H    2-CNPh          CF3Me  Me    H    2-FPh           CF3Me  Me    H    2,6-F2Ph       CF3Me  Me    H    2,4-F2Ph       CF3Me  Me    H    2,5-F2Ph       CF3Me  Me    H    2-MeOPh         CF3Me  Me    H    3-Cl-2-吡啶基   CF3Me  Me    H    3-Cl-2-吡啶基   OCF3Me  Me    H    3-Cl-2-吡啶基   BrMe  Me    H    3-Cl-2-吡啶基   ClMe  Me    H    3-CF3-2-       CF3吡啶基Me  Me    H    3-Me-2-         CF3吡啶基 R 3    R 4a R 4b  R 5a            R 5bMe    H    Cl    Me             r-C3F7Me    H    Cl    Me             i-C3F7Me    H    Cl    Me             EtMe    H    Cl    Me             OCF2CHF2Me    H    Cl    Me             SCF2CHF2Me    H    Cl    Me             SO2MeMe    H    Cl    Me             SO2CF3Me    H    Cl    CF3           CF3Me    H    Cl    CF3           MeMe    H    Cl    Ph             CF3Me    H    Cl    Ph             ClMe    H    Cl    Ph             BrMe    H    Cl    2-吡啶基       CF3Me    H    Cl    2-吡啶基       ClMe    H    Cl    2-ClPh         CF3Me    H    Cl    2-ClPh         OCF3Me    H    Cl    2-ClPh         BrMe    H    Cl    2-ClPh         ClMe    H    Cl    2-ClPh         SCHF2Me    H    Cl    2-BrPh         CF3Me    H    Cl    2-MePh         CF3Me    H    Cl    2-CNPh         CF3Me    H    Cl    2-FPh          CF3Me    H    Cl    2,6-F2Ph      CF3Me    H    Cl    2,4-F2Ph      CF3Me    H    Cl    2,5-F2Ph      CF3Me    H    Cl    2-OMe          CF3Me    H    Cl    3-Cl-2-吡啶基  CF3Me    H    Cl    3-Cl-2-吡啶基  OCF3Me    H    Cl    3-Cl-2-吡啶基  BrMe    H    Cl    3-Cl-2-吡啶基  ClMe    H    Cl    3-Cl-2-吡啶基  SCHF2Me    H    Cl    3-F-2-吡啶基   CF3Me    H    Cl    3-CF3-2-      CF3吡啶基Me    H    Cl    3-Me-2-        CF3吡啶基 R 3  R 4a  R 4b    R 5a          R 5bMe   Me    H    3-Cl-2-吡啶基   SCHF2Me   Me    H    3-F-2-吡啶基    CF3Me   Me    H    3-Br2-吡啶基    CF3Me   Me    H    3-Br-2-吡啶基   OCF3Me   Me    H    3-Br-2-吡啶基   BrMe   Me    H    3-Br-2-吡啶基   ClMe   Cl    H    Me              BrMe   Cl    H    Et              BrMe   Cl    H    Me              ClMe   Cl    H    Et              ClMe   Cl    H    Me              IMe   Cl    H    Me              CF3Me   Cl    H    Me              OCF3Et   Cl    H    Me              CF3Me   Cl    H    Me              SCF3Me   Cl    H    Me              SCHF2Me   Cl    H    Me              OCHF2n-Pr Cl    H    Me              CF3Me   Cl    H    Me              C2F5Et   Cl    H    Me              C2F5Me   Cl    H    3-Cl-2-吡啶基   CF3Me   Cl    H    3-Cl-2-吡啶基   OCF3Me   Cl    H    3-Cl-2-吡啶基   BrMe   Cl    H    3-Cl-2-吡啶基   ClMe   Cl    H    3-Cl-2-吡啶基   SCHF2Me   Cl    H    3-F-2-吡啶基    CF3Me   Cl    H    3-CF3-2-       CF3吡啶基Me   Cl    H    3-Br-2-吡啶基   CF3Me   Cl    H    3-Br-2-吡啶基   OCF3Me   Cl    H    3-Br-2-吡啶基   BrMe   Cl    H    3-Br-2-吡啶基   ClMe   Cl    H    2,4-F2Ph       CF3Me   Cl    H    2,5-F2Ph       CF3Me   Cl    H    2-OMe           CF3Me   Cl    H    2-ClPh          OCF3 R 3  R 4a  R 4b     R 5a       R 5bMe   H     Cl   3-Br-2-吡啶基  CF3Me   H     Cl   3-Br-2-吡啶基  OCF3Me   H     Cl   3-Br-2-吡啶基  BrMe   H     Cl   3-Br-2-吡啶基  ClMe   Cl    H    Et             CF3Me   Cl    H    n-Pr           CF3Me   Cl    H    i-Pr           CF3Me   Cl    H    Me             SMeMe   Cl    H    Me             CMeMe   Cl    H    Me             OEtMe   Cl    H    Me             n-C3F7Me   Cl    H    Me             i-C3F7Me   Cl    H    Me             EtMe   Cl    H    Me             OCF2CHF2Me   Cl    H    Me             SCF2CHF2Me   Cl    H    Me             SO2MeMe   Cl    H    Me             SO2CF3Me   Cl    H    CF3           CF3Me   Cl    H    CF3           MeMe   Cl    H    OMe            CF3Me   Cl    H    Ph             CF3Me   Cl    H    Ph             ClMe   Cl    H    Ph             BrMe   Cl    H    2-吡啶基       CF3Me   Cl    H    2-吡啶基       ClMe   Cl    H    2-ClPh         CF3Me   Cl    H    3-Me-2-        CF3吡啶基Me   Cl    H    2-ClPh         BrMe   Cl    H    2-ClPh         ClMe   Cl    H    2-ClPh         SCHF2Me   Cl    H    2-BrPh         CF3Me   Cl    H    2-MePh         CF3Me   Cl    H    2-CNPh         CF3Me   Cl    H    2-FPh          CF3Me   Cl    H    2,6-F2Ph      CF3 Table 9 R 3 R 4a R 4b R 5a R 5b Me H Me H CF 3 Me H Me H OCF 3 Et H Me H OCF 3 Me H Me Me BrMe H Me Et BrMe H Me Me ClMe H Me Et ClMe H Me Me IMe H Me Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H H H CF 3 Me H H H OCF 3 Et H H H OCF 3 Me H H Me BrMe H H Et BrMe H H Me ClMe H H Et ClMe H H Me IMe H H Me CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me Me OCF 3 Et H Me Me CF 3 Me H Me Me SCF 3 Me H Me Me SCHF 2 Me H Me Me OCHF 2 n-Pr H Me Me CF 3 Me H Me Me C 2 F 5 Et H Me Me C 2 F 5 Me H Me Et CF 3 Me H Me n-Pr CF 3 Me H Me i-Pr CF 3 Me H Me i-Pr OCF 3 Me H Me Me SMeMe H Me Me OMeMe H Me Me OEtMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me EtMe H Me Me OCF 2 CHF 2 Me H Me Me SCF 2 CHF 2 Me H Me Me SO 2 MeMe H Me Me SO 2 CF 3 Me H Me CHF 2 CF 3 Me H Me CHF 2 MeMe H Me Ph CF 3 Me H Me Ph ClMe H Me Ph BrMe H Me 2-pyridyl CF 3 Me H Me 2-pyridyl ClMe H Me 2-ClPh CF 3 Me H Me 2-ClPh OCF 3 Me H Me 2-ClPh BrMe H Me 2-ClPh ClMe H Me 2-ClPh SCHF 2 Me H Me 2-BrPh CF 3 Me H Me 2-MePh CF 3 Me H Me 2-CNPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me OCF 3 Et H H Me CF 3 Me H H Me SCF 3 Me H H Me SCHF 2 Me H H Me OCHF 2 n-Pr H H Me CF 3 Me H H Me C 2 F 5 Et H H Me C 2 F 5 Me H H Et CF 3 Me H H n-Pt CF 3 Me H H i-Pr CF 3 Me H H Me SMeMe H H Me OMeMe H H Me OEtMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me EtMe H H Me OCF 2 CHF 2 Me H H Me SCF 2 CHF 2 Me H H Me SO 2 MeMe H H Me SO 2 CF 3 Me H H CF 3 CF 3 Me H H CF 3 MeMe H H Ph CF 3 Me H H Ph ClMe H H Ph BrMe H H 2-pyridyl CF 3 Me H H 2-pyridyl ClMe H H 2-ClPh CF 3 Me H H 2-ClPh OCF 3 Me H H 2-ClPh BrMe H H 2-ClPh ClMe H H 2-ClPh SCHF 2 Me H H 2-BrPh CF 3 Me H H 2-MePh CF 3 Me H H 2-CNPh CF 3 Me H H 2-FPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me 2-FPh CF 3 Me H Me 2,6-F 2 Ph CF 3 Me H Me 2,4-F 2 Ph CF 3 Me H Me 2,5-F 2 Ph CF 3 Me H Me 2-MeOPh CF 3 Me H Me 3-Cl-2-pyridyl CF 3 Me H Me 3-Cl-2-pyridyl OCF 3 Me H Me 3-Cl-2-pyridyl BrMe H Me 3-Cl-2-pyridyl ClMe H Me 3-Cl-2-pyridyl SCHF 2 Me H Me 3-CF 3 -2- CF 3 pyridyl Me H Me 3-Me-2- CF 3 pyridyl Me H Me 3-F-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3-Br-2-pyridyl OCF 3 Me H Me 3-Br-2-pyridyl BrMe H Me 3-Br-2-pyridylClMe Me H Me BrMe Me H Et BrMe Me H Me ClMe Me H Et ClMe Me H Me IMe Me H Me CF 3 Me Me H Me OCF 3 Et Me H Me CF 3 Me Me H Me SCF 3 Me Me H Me SCHF 2 Me Me H Me OCHF 2 n-Pr Me H Me CF 3 Me Me H Me C 2 F 5 Et Me H Me C 2 F 5 Me Me H Et CF 3 Me Me H n-Pr CF 3 Me Me H i-Pr CF 3 Me Me H Me SMe R 3 R 4a R 4b R 5a R 5b Me H H 2,6-F 2 Ph CF 3 Me H H 2,4-F 2 Ph CF 3 Me H H 2,5-F 2 Ph CF 3 Me H H 2-MeOPh CF 3 Me H H 3-Cl-2-pyridyl CF 3 Me H H 3-Cl-2-pyridyl OCF 3 Me H H 3-Cl-2-pyridyl BrMe H H 3-Cl-2-pyridyl ClMe H H 3-Cl- 2-pyridyl SCHF 2 Me H H 3-F-2-pyridyl CF 3 Me H H 3-CF 3 -2- CF 3 pyridyl Me H H 3-Me-2- CF 3 pyridyl Me H H 3-B-r2 -pyridyl CF 3 Me H H 3-Br-2-pyridyl OCF 3 Me H H 3-Br-2-pyridyl BrMe H H 3-Br-2-pyridyl ClMe H Cl Et BrMe H Cl Me ClMe H Cl Et ClMe H Cl Me IMe H Cl Me CF 3 Me H Cl Me OCF 3 Et H Cl Me CF 3 Me H Cl Me SCF 3 Me H Cl Me SCHF 2 Me H Cl Me OCHF 2 n-Pr H Cl Me CF 3 Me H Cl Me C 2 F 5 Et H Cl Me C 2 F 5 Me H Cl Et CF 3 Me H Cl n-Pr CF 3 Me H Cl i-Pr CF 3 Me H Cl Me SMeMe H Cl Me OMeMe H Cl Me CEt R 3 R 4a R 4b R 5a R 5b Me Me H Me OMeMe Me H Me OEtMe Me H Me nC 3 F 7 Me Me H Me iC 3 F 7 Me Me H Me EtMe Me H Me OCF 2 CHF 2 Me Me H Me SCF 2 CHF 2 Me Me H Me SO 2 MeMe Me H Me SO 2 CF 3 Me Me H CF 3 CF 3 Me Me H CF 3 MeMe Me H Ph CF 3 Me Me H Ph ClMe Me H Ph BrMe Me H 2-Pyridine CF 3 Me Me H 2-pyridyl ClMe Me H 2-ClPh CF 3 Me Me H 2-ClPh OCF 3 Me Me H 2-ClPh BrMe Me H 2-ClPh ClMe Me H 2-ClPh SCHF 2 Me Me H 2 -BrPh CF 3 Me Me H 2-MePh CF 3 Me Me H 2-CNPh CF 3 Me Me H 2-FPh CF 3 Me Me H 2,6-F 2 Ph CF 3 Me Me H 2,4-F 2 Ph CF 3 Me Me H 2,5-F 2 Ph CF 3 Me H 2-MeOPh CF 3 Me H 3-Cl-2-pyridyl CF 3 Me H 3-Cl-2-pyridyl OCF 3 Me Me H 3-Cl-2-pyridylBrMeMe H 3 - Cl-2-pyridylClMeMeH 3- CF3-2 -CF3pyridylMeMeH3-Me-2 - CF3pyridyl R 3 R 4a R 4b R 5a R 5b Me H Cl Me rC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me EtMe H Cl Me OCF 2 CHF 2 Me H Cl Me SCF 2 CHF 2 Me H Cl Me SO 2 MeMe H Cl Me SO 2 CF 3 Me H Cl CF 3 CF 3 Me H Cl CF 3 MeMe H Cl Ph CF 3 Me H Cl Ph ClMe H Cl Ph BrMe H Cl 2-pyridyl CF 3 Me H Cl 2- Pyridyl ClMe H Cl 2-ClPh CF 3 Me H Cl 2-ClPh OCF 3 Me H Cl 2-ClPh BrMe H Cl 2-ClPh ClMe H Cl 2-ClPh SCHF 2 Me H Cl 2-BrPh CF 3 Me H Cl 2 -MePh CF 3 Me H Cl 2-CNPh CF 3 Me H Cl 2-FPh CF 3 Me H Cl 2,6-F 2 Ph CF 3 Me H Cl 2,4-F 2 Ph CF 3 Me H Cl 2,5 -F 2 Ph CF 3 Me H Cl 2-OMe CF 3 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl OCF 3 Me H Cl 3-Cl-2-pyridine BrMe H Cl 3-Cl-2-pyridyl ClMe H Cl 3-Cl-2-pyridyl SCHF 2 Me H Cl 3-F-2-pyridyl CF 3 Me H Cl 3-CF 3 -2- CF 3 Pyridyl Me H Cl 3-Me-2-CF 3 pyridyl R 3 R 4a R 4b R 5a R 5b Me Me H 3-Cl-2-pyridyl SCHF 2 Me Me H 3-F-2-pyridyl CF 3 Me Me H 3-Br2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl OCF 3 Me Me H 3-Br-2-pyridyl BrMe Me H 3-Br-2-pyridyl ClMe Cl H Me BrMe Cl H Et BrMe Cl H Me ClMe Cl H Et ClMe Cl H Me IMe Cl H Me CF 3 Me Cl H Me OCF 3 Et Cl H Me CF 3 Me Cl H Me SCF 3 Me Cl H Me SCHF 2 Me Cl H Me OCHF 2 n-Pr Cl H Me CF 3 Me Cl H Me C 2 F 5 Et Cl H Me C 2 F 5 Me Cl H 3-Cl-2-pyridyl CF 3 Me Cl H 3-Cl-2-pyridyl OCF 3 Me Cl H 3-Cl-2-pyridyl BrMe Cl H 3-Cl-2-pyridyl ClMe Cl H 3-Cl-2-pyridyl SCHF 2 Me Cl H 3-F-2-pyridyl CF 3 Me Cl H 3-CF 3 -2- CF 3 pyridyl MeCl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl OCF 3 Me Cl H 3-Br-2-pyridyl BrMe Cl H 3-Br-2-pyridyl ClMe Cl H 2,4-F 2 Ph CF 3 Me Cl H 2,5-F 2 Ph CF 3 Me Cl H 2-OMe CF 3 Me Cl H 2-ClPh OCF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl OCF 3 Me H Cl 3-Br-2-pyridyl BrMe H Cl 3-Br-2-pyridyl ClMe Cl H Et CF 3 Me Cl H n-Pr CF 3 Me Cl H i-Pr CF 3 Me Cl H Me SMeMe Cl H Me CMeMe Cl H Me OEtMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H Me EtMe Cl H Me OCF 2 CHF 2 Me Cl H Me SCF 2 CHF 2 Me Cl H Me SO 2 MeMe Cl H Me SO 2 CF 3 Me Cl H CF 3 CF 3 Me Cl H CF 3 MeMe Cl H OMe CF 3 Me Cl H Ph CF 3 Me Cl H Ph ClMe Cl H Ph BrMe Cl H 2-Pyridyl CF 3 Me Cl H 2-Pyridyl ClMe Cl H 2-ClPh CF 3 Me Cl H 3-Me-2-CF 3pyridylMeClH 2-ClPh BrMeClH 2-ClPh ClMeClH 2-ClPh SCHF 2 MeClH 2-BrPh CF 3 MeClH 2-MePh CF 3 MeClH 2-CNPh CF 3 Me Cl H 2-FPh CF 3 Me Cl H 2,6-F 2 Ph CF 3

                                      表10 R 3    R 4a R 4b  R 5a   R 5bMe    H    Me    H     CHF2Me    H    Me    H     CH2CF3Et    H    Me    H     CH2CF3Me    H    Me    Me    CH2CF3Me    H    Me    Et    CH2CF3Me    H    Me    Me    CF2CHF2Me    H    Me    Et    CHF2Me    H    Me    Me    CHF2Me    H    Me    Me    CBrF2Me    H    Me    Me    CHF2Et    H    Me    Me    CH2CF3Me    H    Me    Me    EtMe    H    Me    M     n-PrMe    H    Me    Me    CH2C2F5n-Pr  H    Me    Me    CH2CF3Me    H    Me    Me    CF3Et    H    Me    Me    C2F5Me    H    Me    Et    CHF2Me    H    Me    n-Pr  CH2CF3Me    H    Me    i-Pr  CHF2Me    H    Me    Cl    CH2CF3Me    H    Me    F     CH2CF3Me    H    Me    Me    CH2ClMe    H    Me    Me    CClF2Me    H    Me    Me    CH2CH2ClMe    H    Me    Me    n-C3F7Me    H    Me    Me    i-C3F7Me    H    Me    Me    Allyl R 3   R 4a  R 4b R 5a   R 5bMe    H    H    H     CHF2Me    H    H    H     CH2CF3Et    H    H    H     CH2CF3Me    H    H    Me    CH2CF3Me    H    H    Et    CH2CF3Me    H    H    Me    CF2CHF2Me    H    H    Et    CHF2Me    H    H    Me    CHF2Me    H    H    Me    CBrF2Me    H    H    Me    CHF2Et    H    H    Me    CH2CF3Me    H    H    Me    EtMe    H    H    Me    n-PrMe    H    H    Me    CH2C2F5n-Pr  H    H    Me    CH2CF3Me    H    H    Me    CF3Et    H    H    Me    C2F5Me    H    H    Et    CHF2Me    H    H    n-Pr  CH2CF3Me    H    H    i-Pr  CHF2Me    H    H    Cl    CH2CF3Me    H    H    F     CH2CF3Me    H    H    Me    CH2ClMe    H    H    Me    CClF2Me    H    H    Me    CH2CH2ClMe    H    H    Me    n-C3F7Me    H    H    Me    i-C3F7Me    H    H    Me    Allyl R 3   R 4a  R 4b  R 5a             R 5bMe    H    Me    Et             CF3CHF2Me    H    Me    Et             i-C3F7Me    H    Me    i-Pr           CF2CHF2Me    H    Me    n-Pr           CF2CHF2Me    H    Me    CF3           CF2CHF2Me    H    Me    CF3           MeMe    H    Me    OMe            CH2CF3Me    H    Me    H              CH2CF3Me    H    Me    H              CH2CF3Me    H    Me    H              C2F5Et    H    Me    H              C2F5Me    H    Me    H              C2F5Me    H    Me    H              CF2CHF2Me    H    Me    i-Pr           CH2CF3Me    H    Me    H              n-C3F7Me    H    Me    H              i-C3F7Me    H    Me    Ph             CH2CF3Me    H    Me    Ph             CF2CHF2Me    H    Me    Ph             CHF2Me    H    Me    2-吡啶基       CH2CF3Me    H    Me    2-吡啶基       CF2CHF2Me    H    Me    2-ClPh         CH2CF3Me    H    Me    2-ClPh         CF2CHF2Me    H    Me    2-ClPh         CHF2Me    H    Me    2-ClPh         EtMe    H    Me    2-ClPh         CBrF2Me    H    Me    2-BrPh         CH2CF3Me    H    Me    2-MePh         CH2CF3Me    H    Me    2-CNPh         CH2CF3Me    H    Me    2-FPh          CH2CF3Me    H    Me    2,6-F2Ph      CH2CF3Me    H    Me    2,4-F2Ph      CH2CF3Me    H    Me    2,5-F2Ph      CH2CF3Me    H    Me    2-MeOPh        CH2CF3Me    H    Me    3-Cl-2-吡啶基  CH2CF3Me    H    Me    3-Cl-2-吡啶基  CF2CHF2Me    H    Me    3-Cl-2-吡啶基  CF3 R 3   R 4a  R 4b R 5a       R 5bMe    H    H    Me        CF2CHF2Me    H    H    Me        i-C3F7Me    H    H    Me        CF2CHF2Me    H    H    Me        CF2CHF2Me    H    H    CF3      CF2CHF2Me    H    H    CF3      MeMe    H    H    OMe       CH2CF3Me    H    H    H         CH2CF3Me    H    H    H         CH2CF3Me    H    H    H         C2F5Et    H    H    H         C2F5Me    H    H    H         C2F5Me    H    H    H         CF2CHF2Me    H    H    H         CH2CF3Me    H    H    H         n-C3F7Me    H    H    H         i-C3F7Me    H    H    H         CH2CF3Me    H    H    H         CF2CHF2Me    H    H    H         CHF2Me    H    H    Ph        CH2CF3Me    H    H    Ph        CF2CHF2Me    H    H    Ph        CH2CF3Me    H    H    2-吡啶基  CF2CHF2Me    H    H    2-吡啶基  CHF2Me    H    H    2-ClPh    EtMe    H    H    2-ClPh    CBrF2Me    H    H    2-ClPh    CH2CF3Me    H    H    2-ClPh    CH2CF3Me    H    H    2-ClPh    CH2CF3Me    H    H    2-BrPh    CH2CF3Me    H    H    2-MePh    CH2CF3Me    H    H    2-CNPh    CH2CF3Me    H    H    2-FPh     CH2CF3Me    H    H    2,6-F2Ph CH2CF3Me    H    H    2,4-F2Ph CH2CF3Me    H    H    2,5-F2Ph CF2CHF2Me    H    H    2-MeOPh   CF3 R 3   R 4a  R 4b      R 5a       R 5bMe    H    Me    3-Cl-2-吡啶基  CHF2Me    H    Me    3-Cl-2-吡啶基  CBrF2Me    H    Me    3-F-2-吡啶基   CH2CF3Me    H    Me    3-CF3-2-      CH2CF3吡啶基Me    H    Me    3-Me-2-        CH2CF3吡啶基Me    H    Me    3-Br-2-吡啶基  CF3Me    H    Me    3-Br-2-吡啶基  CH2CF3Me    H    Me    3-Br-2-吡啶基  CF2CHF2Me    H    Me    3-Br-2-吡啶基  CClF2Me    Me   H     H              CHF2Me    Me   H     H              CH2CF3Et    Me   H     H              CH2CF3Me    Me   H     Me             CH2CF3Me    Me   H     Et             CH2CF3Me    Me   H     Me             CF2CHF2Me    Me   H     Et             CHF2Me    Me   H     Me             CHF2Me    Me   H     Me             CBrF2Me    Me   H     Me             CHF2Et    Me   H     Me             CH2CF3Me    Me   H     Me             EtMe    Me   H     Me             n-PrMe    Me   H     Me             CH2C2F5n-Pr  Me   H     Me             CH2CF3Me    Me   H     Me             CF3Et    Me   H     Me             C2F5Me    Me   H     Et             CHF2Me    Me   H     n-Pr           CH2CF3Me    Me   H     i-Pr           CHF2Me    Me   H     Cl             CH2CF3Me    Me   H     F              CH2CF3Me    Me   H     Me             CH2ClMe    Me   H     Me             CClF2Me    Me   H     Me             CH2CH2ClMe    Me   H     M              n-C3F7 R 3   R 4a  R 4b       R 5a     R 5bMe    H    H    3-Cl-2-吡啶基  CHF2Me    H    H    3-Cl-2-吡啶基  CBrF2Me    H    H    3-Cl-2-吡啶基  CH2CF3Me    H    H    3-CF3-2-      CH2CF3吡啶基Me    H    H    3-Me-2-        CF2CHF2吡啶基Me    H    H    3-Cl-2-吡啶基  CH2CF3Me    H    H    3-Cl-2-吡啶基  CH2CF3Me    H    H    3-F-2-吡啶基   CF3Me    H    H    3-Br-2-吡啶基  CClF2Me    H    H    3-Br-2-吡啶基  CH2CF3Me    H    H    3-Br-2-吡啶基  CF3Me    H    H    3-Br-2-吡啶基  CF3Me    H    Cl   Et             CHF2Me    H    Cl   Me             CH2CF3Me    H    Cl   Et             CH2CF3Me    H    Cl   Me             CH2CF3Me    H    Cl   Me             CH2CF3Me    H    Cl   Me             CF2CHF2Et    H    Cl   Me             CHF2Me    H    Cl   Me             CHF2Me    H    Cl   Me             CBrF2Me    H    Cl   Me             CHF2n-Pr  H    Cl   Me             CH2CF3Me    H    Cl   Me             EtEt    H    Cl   Me             n-PrMe    H    Cl   Et             CH2C2F5Me    H    Cl   n-Pr           CH2CF3Me    H    Cl   i-Pr           CF3Me    H    Cl   Cl             C2F5Me    H    Cl   F              CHF2Me    H    Cl   Me             CH2CF3Me    H    Cl   Me             CHF2Me    H    Cl   Me             CH2CF3Me    H    Cl   Me             CH2CF3Me    H    Cl   Me             CH2Cl R 3  R 4a  R 4b R 5a         R 5bMe  Me    H    Me          i-C3F7Me  Me    H    Me          AllylMe  Me    H    Me          CF2CHF2Me  Me    H    Me          i-C3F7Me  Me    H    Me          CF2CHF2Me  Me    H    Me          CF2CHF2Me  Me    H    CF3        CF2CHF2Me  Me    H    CF3        MeMe  Me    H    OMe         CH2CF3Me  Me    H    H           CH2CF3Me  Me    H    H           CH2CF3Me  Me    H    H           C2F5Et  Me    H    H           C2F5Me  Me    H    H           C2F5Me  Me    H    H           CF2CHF2Me  Me    H    H           CH2CF3Me  Me    H    H           n-C3F7Me  Me    H    H           i-C3F7Me  Me    H    H           CH2CF3Me  Me    H    H           CF2CHF2Me  Me    H    H           CHF2Me  Me    H    Ph          CH2CF3Me  Me    H    Ph          CF2CHF2Me  Me    H    Ph          CH2CF3Me  Me    H    2-吡啶基    CF2CHF2Me  Me    H    2-吡啶基    CHF2Me  Me    H    2-ClPh      EtMe  Me    H    2-ClPh      CBrF2Me  Me    H    2-ClPh      CH2CF3Me  Me    H    2-ClPh      CH2CF3Me  Me    H    2-ClPh      CH2CF3Me  Me    H    2-BrPh      CH2CF3Me  Me    H    2-MePh      CH2CF3Me  Me    H    2-CNPh      CH2CF3Me  Me    H    2-FPh       CH2CF3Me  Me    H    2,6-F2Ph   CH2CF3Me  Me    H    2,4-F2Ph   CH2CF3   R 3  R 4a  R 4b  R 5a         R 5bMe    H    Cl    Me          CClF2Me    H    Cl    Me          CH2CH2ClMe    H    Cl    Me          n-C3F7Me    H    Cl    Me          i-C3F7Me    H    Cl    Me          AllylMe    H    Cl    CF3        CF2CHF2Me    H    Cl    CF3        i-C3F7Me    H    Cl    OMe         CF2CHF2Me    H    Cl    H           CF2CHF2Me    H    Cl    H           CF2CHF2Me    H    Cl    H           MeEt    H    Cl    H           CH2CF3Me    H    Cl    H           CH2CF3Me    H    Cl    H           CH2CF3Me    H    Cl    H           C2F5Me    H    Cl    H           C2F5Me    H    Cl    H           C2F5Me    H    Cl    H           CF2CHF2Me    H    Cl    H           CH2CF3Me    H    Cl    H           n-C3F7Me    H    Cl    Ph          i-C3F7Me    H    Cl    Ph          CH2CF3Me    H    Cl    Ph          CF2CHF2Me    H    Cl    2-吡啶基    CHF2Me    H    Cl    2-吡啶基    CH2CF3Me    H    Cl    2-ClPh      CF2CHF2Me    H    Cl    2-ClPh      CH2CF3Me    H    Cl    2-ClPh      CF2CHF2Me    H    Cl    2-ClPh      CHF2Me    H    Cl    2-ClPh      EtMe    H    Cl    2-BrPh      CBrF2Me    H    Cl    2-MePh      CH2CF3Me    H    Cl    2-CNPh      CH2CF3Me    H    Cl    2-FPh       CH2CF3Me    H    Cl    2,6-F2Ph   CH2CF3Me    H    Cl    2,4-F2Ph   CH2CF3Me    H    Cl    2,5-F2Ph   CH2CF3 R 3  R 4a  R 4b    R 5a           R 5bMe   Me    H    2,5-F2Ph      CF2CHF2Me   Me    H    2-MeOPh        CF3Me   Me    H    3-Cl-2-吡啶基  CHF2Me   Me    H    3-Cl-2-吡啶基  CBrF2Me   Me    H    3-Cl-2-吡啶基  CH2CF3Me   Me    H    3-Cl-2-吡啶基  CH2CF3Me   Me    H    3-Cl-2-吡啶基  CH2CF3Me   Me    H    3-CF3-2-      CH2CF3吡啶基Me   Me    H    3-Me-2-        CF2CHF2吡啶基Me   Me    H    3-F-2-吡啶基   CF3Me   Me    H    3-Br-2-吡啶基  CClF2Me   Me    H    3-Br-2-吡啶基  CH2CF3Me   Me    H    3-Br-2-吡啶基  CF3Me   Me    H    3-Br-2-吡啶基  CF3Me   Cl    H    Me             CHF2Me   Cl    H    Et             CH2CF3Me   Cl    H    Me             CH2CF3Me   Cl    H    Et             CH2CF3Me   Cl    H    Me             CH2CF3Me   Cl    H    Me             CF2CHF2Me   Cl    H    Me             CHF2Et   Cl    H    Me             CHF2Me   Cl    H    Me             CBrF2Me   Cl    H    Me             CHF2Me   Cl    H    Me             CH2CF3n-Pr Cl    H    Me             EtMe   Cl    H    Me             n-PrEt   Cl    H    Me             CH2C2F5Me   Cl    H    Et             CH2CF3Me   Cl    H    n-Pr           CF3Me   Cl    H    i-Pr           C2F5Me   Cl    H    Cl             CHF2Me   Cl    H    F              CH2CF3Me   Cl    H    Me             CHF2Me   Cl    H    Me             CH2CF3 R 3  R 4a  R 4b   R 5a            R 5bMe    H    Cl    2-MeOPh        CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CH2CF3Me    H    Cl    3-Cl-2-吡啶基  CF2CHF2Me    H    Cl    3-Cl-2-吡啶基  CF3Me    H    Cl    3-Cl-2-吡啶基  CHF2Me    H    Cl    3-F-2-吡啶基   CBrF2Me    H    Cl    3-CF3-2-      CH2CF3吡啶基Me    H    Cl    3-Me-2-        CH2CF3吡啶基Me    H    Cl    3-Br-2-吡啶基  CH2CF3Me    H    Cl    3-Br-2-吡啶基  CF3Me    H    Cl    3-Br-2-吡啶基  CH2CF3Me    H    Cl    3-Br-2-吡啶基  CF2CHF2Me    Cl   H     H              CF2CHF2Me    Cl   H     H              CH2CF3Me    Cl   H     H              n-C3F7Me    Cl   H     H              i-C3F7Me    Cl   H     Ph             CH2CF3Me    Cl   H     Ph             CF2CHF2Me    Cl   H     Ph             CHF2Me    Cl   H     2-吡啶基       CH2CF3Me    Cl   H     2-吡啶基       CF2CHF2Me    Cl   H     2-ClPh         CH2CF3Me    Cl   H     2-ClPh         CF2CHF2Me    Cl   H     2-ClPh         CHF2Me    Cl   H     2-ClPh         EtMe    Cl   H     2-ClPh         CBrF2Me    Cl   H     2-BrPh         CH2CF3Me    Cl   H     2-MePh         CH2CF3Me    Cl   H     2-CNPh         CH2CF3Me    Cl   H     2-FPh          CH2CF3Me    Cl   H     2,6-F2Ph      CH2CF3Me    Cl   H     2,4-F2Ph      CH2CF3Me    Cl   H     2,5-F2Ph      CH2CF3Me    Cl   H     2-MeOPh        CH2CF3 R 3  R 4a R 4b R 5a      R 5bMe  Cl  H    Me       CH2CF3Me  Cl  H    Me       CH2ClMe  Cl  H    Me       CClF2Me  Cl  H    Me       CH2CH2ClMe  Cl  H    Me       n-C3F7Me  Cl  H    Me       i-C3F7Me  Cl  H    3-Me-2-  CH2CF3吡啶基Me  Cl  H    Me       CF2CHF2Me  Cl  H    CF3      i-C3F7Me  Cl  H    CF3      CF2CHF2Me  Cl  H    OMe      CF2CHF2Me  Cl  H    H        CF2CHF2Me  Cl  H    H        MeMe  Cl  H    H        CH2CF3Et  Cl  H    H        CH2CF3Me  Cl  H    H        CH2CF3   R 3 R 4a  R 4b   R 5a            R 5bMe  Cl    H    3-Cl-2-吡啶基  CH2CF3Me  Cl    H    3-Cl-2-吡啶基  CF2CHF2Me  Cl    H    3-Cl-2-吡啶基  CF3Me  Cl    H    3-Cl-2-吡啶基  CHF2Me  Cl    H    3-Cl-2-吡啶基  CBrF2Me  Cl    H    3-F-2-吡啶基   CH2CF3Me  Cl    H    3-CF3-2-      CH2CF3吡啶基Me  Cl    H    3-Br-2-吡啶基  CF3Me  Cl    H    3-Br-2-吡啶基  CH2CF3Me  Cl    H    3-Br-2-吡啶基  CF2CHF2Me  Cl    H    3-Br-2-  啶基  CClF2Me  Cl    H    H              C2F5Me  Cl    H    H              C2F5Me  Cl    H    H              C2F5Me  Cl    H    Me             烯丙基 配制剂/效用 Table 10 R 3 R 4a R 4b R 5a R 5b Me H Me H CHF 2 Me H Me H CH 2 CF 3 Et H Me H CH 2 CF 3 Me H Me Me CH 2 CF 3 Me H Me Et CH 2 CF 3 Me H Me Me CF 2 CHF 2 Me H Me Et CHF 2 Me H Me Me CHF 2 Me H Me Me CBrF 2 Me H Me Me CHF 2 Et H Me Me CH 2 CF 3 Me H Me Me EtMe H Me M n-PrMe H Me Me CH 2 C 2 F 5 n-Pr H Me Me CH 2 CF 3 Me H Me Me CF 3 Et H Me Me C 2 F 5 Me H Me Et CHF 2 Me H Me n-Pr CH 2 CF 3 Me H Me i-Pr CHF 2 Me H Me Cl CH 2 CF 3 Me H Me F CH 2 CF 3 Me H Me Me CH 2 ClMe H Me Me CClF 2 Me H Me Me CH 2 CH 2 ClMe H Me Me nC 3 F 7 Me H Me Me iC 3 F 7 Me H Me Me Allyl R 3 R 4a R 4b R 5a R 5b Me H H H CHF 2 Me H H H CH 2 CF 3 Et H H H CH 2 CF 3 Me H H Me CH 2 CF 3 Me H H Et CH 2 CF 3 Me H H Me CF 2 CHF 2 Me H H Et CHF 2 Me H H Me CHF 2 Me H H Me CBrF 2 Me H H Me CHF 2 Et H H Me CH 2 CF 3 Me H H Me EtMe H H Me n-PrMe H H Me CH 2 C 2 F 5 n-Pr H H Me CH 2 CF 3 Me H H Me CF 3 Et H H Me C 2 F 5 Me H H Et CHF 2 Me H H n-Pr CH 2 CF 3 Me H H i-Pr CHF 2 Me H H Cl CH 2 CF 3 Me H H F CH 2 CF 3 Me H H Me CH 2 ClMe H H Me CClF 2 Me H H Me CH 2 CH 2 ClMe H H Me nC 3 F 7 Me H H Me iC 3 F 7 Me H H Me Allyl R 3 R 4a R 4b R 5a R 5b Me H Me Et CF 3 CHF 2 Me H Me Et iC 3 F 7 Me H Me i-Pr CF 2 CHF 2 Me H Me n-Pr CF 2 CHF 2 Me H Me CF 3 CF 2 CHF 2 Me H Me CF 3 MeMe H Me OMe CH 2 CF 3 Me H Me H CH 2 CF 3 Me H Me H CH 2 CF 3 Me H Me H C 2 F 5 Et H Me H C 2 F 5 Me H Me H C 2 F 5 Me H Me H CF 2 CHF 2 Me H Me i-Pr CH 2 CF 3 Me H Me H nC 3 F 7 Me H Me H iC 3 F 7 Me H Me Ph CH 2 CF 3 Me H Me Ph CF 2 CHF 2 Me H Me Ph CHF 2 Me H Me 2-pyridyl CH 2 CF 3 Me H Me 2-pyridyl CF 2 CHF 2 Me H Me 2-ClPh CH 2 CF 3 Me H Me 2-ClPh CF 2 CHF 2 Me H Me 2-ClPh CHF 2 Me H Me 2-ClPh EtMe H Me 2-ClPh CBrF 2 Me H Me 2-BrPh CH 2 CF 3 Me H Me 2-MePh CH 2 CF 3 Me H Me 2- CNPh CH 2 CF 3 Me H Me 2-FPh CH 2 CF 3 Me H Me 2,6-F 2 Ph CH 2 CF 3 Me H Me 2,4-F 2 Ph CH 2 CF 3 Me H Me 2,5- F 2 Ph CH 2 CF 3 Me H Me 2-MeOPh CH 2 CF 3 Me H Me 3-Cl-2-pyridyl CH 2 CF 3 Me H Me 3-Cl-2-pyridyl CF 2 CHF 2 Me H Me 3-Cl-2-pyridyl CF 3 R 3 R 4a R 4b R 5a R 5b Me H H Me CF 2 CHF 2 Me H H Me iC 3 F 7 Me H H Me CF 2 CHF 2 Me H H Me CF 2 CHF 2 Me H H CF 3 CF 2 CHF 2 Me H H CF 3 MeMe H H OMe CH 2 CF 3 Me H H H CH 2 CF 3 Me H H H CH 2 CF 3 Me H H H C 2 F 5 Et H H H C 2 F 5 Me H H H C 2 F 5 Me H H H CF 2 CHF 2 Me H H H CH 2 CF 3 Me H H H nC 3 F 7 Me H H H iC 3 F 7 Me H H H CH 2 CF 3 Me H H H CF 2 CHF 2 Me H H H CHF 2 Me H H Ph CH 2 CF 3 Me H H Ph CF 2 CHF 2 Me H H Ph CH 2 CF 3 Me H H 2-Pyridine CF 2 CHF 2 Me H H 2-pyridyl CHF 2 Me H H 2-ClPh EtMe H H 2-ClPh CBrF 2 Me H H 2-ClPh CH 2 CF 3 Me H H 2 -ClPh CH 2 CF 3 Me H H 2 -ClPh CH 2 CF 3 Me H H 2-BrPh CH 2 CF 3 Me H H 2-MePh CH 2 CF 3 Me H H 2-CNPh CH 2 CF 3 Me H H 2-FPh CH 2 CF 3 Me H H 2,6-F 2 Ph CH 2 CF 3 Me H H 2,4-F 2 Ph CH 2 CF 3 Me H H 2,5-F 2 Ph CF 2 CHF 2 Me H H 2-MeOPh CF 3 R 3 R 4a R 4b R 5a R 5b Me H Me 3-Cl-2-pyridyl CHF 2 Me H Me 3-Cl-2-pyridyl CBrF 2 Me H Me 3-F-2-pyridyl CH 2 CF 3 Me H Me 3-CF 3 -2- CH 2 CF 3 pyridyl Me H Me 3-Me-2- CH 2 CF 3 pyridyl Me H Me 3-Br-2-pyridyl CF 3 Me H Me 3- Br-2-pyridyl CH 2 CF 3 Me H Me 3-Br-2-pyridyl CF 2 CHF 2 Me H Me 3-Br-2-pyridyl CClF 2 Me Me H H CHF 2 Me Me H H CH 2 CF 3 Et Me H H CH 2 CF 3 Me Me H Me CH 2 CF 3 Me Me H Et CH 2 CF 3 Me Me H Me CF 2 CHF 2 Me Me H Et CHF 2 Me Me H Me CHF 2 Me Me H Me CBrF 2 Me Me H Me CHF 2 Et Me H Me CH 2 CF 3 Me Me H Me EtMe Me H Me n-PrMe Me H Me CH 2 C 2 F 5 n-Pr Me H Me CH 2 CF 3 Me Me H Me CF 3 Et Me H Me C 2 F 5 Me Me H Et CHF 2 Me Me H n-Pr CH 2 CF 3 Me H i-Pr CHF 2 Me Me H Cl CH 2 CF 3 Me Me H F CH 2 CF 3 Me Me H Me CH 2 ClMe Me H Me CClF 2 Me Me H Me CH 2 CH 2 ClMe Me H M nC 3 F 7 R 3 R 4a R 4b R 5a R 5b Me H H 3-Cl-2-pyridyl CHF 2 Me H H 3-Cl-2-pyridyl CBrF 2 Me H H 3-Cl-2-pyridyl CH 2 CF 3 Me H H 3-CF 3 -2-CH 2 CF 3 Pyridyl Me H H 3-Me-2- CF 2 CHF 2 Pyridyl Me H H 3-Cl-2-Pyridyl CH 2 CF 3 Me H H 3-Cl-2-Pyridine CH 2 CF 3 Me H H 3-F-2-pyridyl CF 3 Me H H 3-Br-2-pyridyl CCIF 2 Me H H 3-Br-2-pyridyl CH 2 CF 3 Me H H 3-Br-2 -pyridyl CF 3 Me H H 3-Br-2-pyridyl CF 3 Me H Cl Et CHF 2 Me H Cl Me CH 2 CF 3 Me H Cl Et CH 2 CF 3 Me H Cl Me CH 2 CF 3 Me H Cl Me CH 2 CF 3 Me H Cl Me CF 2 CHF 2 Et H Cl Me CHF 2 Me H Cl Me CHF 2 Me H Cl Me CBrF 2 Me H Cl Me CHF 2 n-Pr H Cl Me CH 2 CF 3 Me H Cl Me EtEt H Cl Me n-PrMe H Cl Et CH 2 C 2 F 5 Me H Cl n-Pr CH 2 CF 3 Me H Cl i-Pr CF 3 Me H Cl Cl C 2 F 5 Me H Cl F CHF 2 Me HCl Me CH 2 CF 3 Me H Cl Me CHF 2 Me H Cl Me CH 2 CF 3 Me H Cl Me CH 2 CF 3 Me H Cl Me CH 2 Cl R 3 R 4a R 4b R 5a R 5b Me Me H Me iC 3 F 7 Me Me H Me AllylMe Me H Me CF 2 CHF 2 Me Me H Me iC 3 F 7 Me Me H Me CF 2 CHF 2 Me Me H Me CF 2 CHF 2 Me Me H CF 3 CF 2 CHF 2 Me Me H CF 3 MeMe Me H OMe CH 2 CF 3 Me Me H H CH 2 CF 3 Me Me H H CH 2 CF 3 Me Me H H C 2 F 5 Et Me H H C 2 F 5 Me Me H H C 2 F 5 Me Me H H CF 2 CHF 2 Me Me H H CH 2 CF 3 Me Me H H nC 3 F 7 Me Me H H iC 3 F 7 Me Me H H CH 2 CF 3 Me Me H H CF 2 CHF 2 Me Me H H CHF 2 Me Me H Ph CH 2 CF 3 Me Me H Ph CF 2 CHF 2 Me Me H Ph CH 2 CF 3 Me Me H 2-pyridyl CF 2 CHF 2 Me Me H 2-pyridyl CHF 2 Me Me H 2-ClPh EtMe Me H 2-ClPh CBrF 2 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-ClPh CH 2 CF 3 Me Me H 2-BrPh CH 2 CF 3 Me Me H 2-MePh CH 2 CF 3 Me Me H 2-CNPh CH 2 CF 3 Me Me H 2-FPh CH 2 CF 3 Me Me H 2,6-F 2 Ph CH 2 CF 3 Me Me H 2,4-F 2 Ph CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me H Cl Me CClF 2 Me H Cl Me CH 2 CH 2 ClMe H Cl Me nC 3 F 7 Me H Cl Me iC 3 F 7 Me H Cl Me AllylMe H Cl CF 3 CF 2 CHF 2 Me H Cl CF 3 iC 3 F 7 Me H Cl OMe CF 2 CHF 2 Me H Cl H CF 2 CHF 2 Me H Cl H CF 2 CHF 2 Me H Cl H MeEt H Cl H CH 2 CF 3 Me H Cl H CH 2 CF 3 Me H Cl H CH 2 CF 3 Me H Cl H C 2 F 5 Me H Cl H C 2 F 5 Me H Cl H C 2 F 5 Me H Cl H CF 2 CHF 2 Me H Cl H CH 2 CF 3 Me H Cl H nC 3 F 7 Me H Cl Ph iC 3 F 7 Me H Cl Ph CH 2 CF 3 Me H Cl Ph CF 2 CHF 2 Me H Cl 2-pyridyl CHF 2 Me H Cl 2-pyridyl CH 2 CF 3 Me H Cl 2-ClPh CF 2 CHF 2 Me H Cl 2-ClPh CH 2 CF 3 Me H Cl 2-ClPh CF 2 CHF 2 Me H Cl 2-ClPh CHF 2 Me H Cl 2-ClPh EtMe H Cl 2-BrPh CBrF 2 Me H Cl 2-MePh CH 2 CF 3 Me H Cl 2-CNPh CH 2 CF 3 Me H Cl 2-FPh CH 2 CF 3 Me H Cl 2,6-F 2 Ph CH 2 CF 3 Me HCl 2,4-F 2 Ph CH 2 CF 3 Me H Cl 2,5-F 2 Ph CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Me H 2,5-F 2 Ph CF 2 CHF 2 Me Me H 2-MeOPh CF 3 Me Me H 3-Cl-2-pyridyl CHF 2 Me Me H 3- Cl-2-pyridyl CBrF 2 Me Me H 3-Cl-2-pyridyl CH 2 CF 3 Me H 3-Cl-2-pyridyl CH 2 CF 3 Me H 3 -Cl-2-pyridyl CH 2 CF 3 Me Me H 3-CF 3 -2- CH 2 CF 3 Pyridyl Me Me H 3-Me-2- CF 2 CHF 2 Pyridyl Me Me H 3-F-2-Pyridyl CF 3 Me Me H 3-Br-2-pyridyl CCIF 2 Me Me H 3-Br-2-pyridyl CH 2 CF 3 Me H 3-Br-2-pyridyl CF 3 Me Me H 3-Br-2-pyridyl CF 3 Me Cl H Me CHF 2 Me Cl H Et CH 2 CF 3 Me Cl H Me CH 2 CF 3 Me Cl H Et CH 2 CF 3 Me Cl H Me CH 2 CF 3 Me Cl H Me CF 2 CHF 2 Me Cl H Me CHF 2 Et Cl H Me CHF 2 Me Cl H Me CBrF 2 Me Cl H Me CHF 2 Me Cl H Me CH 2 CF 3 n-Pr Cl H Me EtMe Cl H Me n-PrEt Cl H Me CH 2 C 2 F 5 MeClH EtCH2CF3MeClHn - PrCF3MeClHi - PrC2F5MeClHClCHF2MeClHFCH2CF3MeClHMeCHF2MeClHMe _ _ _ CH2CF3 _ R 3 R 4a R 4b R 5a R 5b Me H Cl 2-MeOPh CH 2 CF 3 Me H Cl 3-Cl-2-pyridyl CH 2 CF 3 Me H Cl 3-Cl-2-pyridyl CH 2 CF 3 Me H Cl 3-Cl-2-pyridyl CF 2 CHF 2 Me H Cl 3-Cl-2-pyridyl CF 3 Me H Cl 3-Cl-2-pyridyl CHF 2 Me H Cl 3-F-2- Pyridyl CBrF 2 Me H Cl 3-CF 3 -2- CH 2 CF 3 Pyridyl Me H Cl 3-Me-2-CH 2 CF 3 Pyridyl Me H Cl 3-Br-2-Pyridyl CH 2 CF 3 Me H Cl 3-Br-2-pyridyl CF 3 Me H Cl 3-Br-2-pyridyl CH 2 CF 3 Me H Cl 3-Br-2-pyridyl CF 2 CHF 2 Me Cl H H CF 2 CHF 2 Me Cl H H CH 2 CF 3 Me Cl H H nC 3 F 7 Me Cl H H iC 3 F 7 Me Cl H Ph CH 2 CF 3 Me Cl H Ph CF 2 CHF 2 Me Cl H Ph CHF 2 Me Cl H 2-pyridyl CH 2 CF 3 Me Cl H 2-pyridyl CF 2 CHF 2 Me Cl H 2-ClPh CH 2 CF 3 Me Cl H 2-ClPh CF 2 CHF 2 Me Cl H 2-ClPh CHF 2 Me Cl H 2-ClPh EtMe Cl H 2-ClPh CBrF 2 Me Cl H 2-BrPh CH 2 CF 3 Me Cl H 2-MePh CH 2 CF 3 Me Cl H 2-CNPh CH 2 CF 3 Me Cl H 2-FPh CH 2 CF 3 Me Cl H 2,6-F 2 Ph CH 2 CF 3 Me Cl H 2,4-F 2 Ph CH 2 CF 3 Me Cl H 2,5-F 2 Ph CH 2 CF 3 Me Cl H 2-MeOPh CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Cl H Me CH 2 CF 3 Me Cl H Me CH 2 ClMe Cl H Me CClF 2 Me Cl H Me CH 2 CH 2 ClMe Cl H Me nC 3 F 7 Me Cl H Me iC 3 F 7 Me Cl H 3-Me-2- CH 2 CF 3 pyridyl Me Cl H Me CF 2 CHF 2 Me Cl H CF3 iC 3 F 7 Me Cl H CF3 CF 2 CHF 2 Me Cl H OMe CF 2 CHF 2 MeCl H H CF 2 CHF 2 Me Cl H H MeMe Cl H H CH 2 CF 3 Et Cl H H CH 2 CF 3 Me Cl H H CH 2 CF 3 R 3 R 4a R 4b R 5a R 5b Me Cl H 3-Cl-2-pyridyl CH 2 CF 3 Me Cl H 3-Cl-2-pyridyl CF 2 CHF 2 Me Cl H 3-Cl-2-pyridine Base CF 3 Me Cl H 3-Cl-2-pyridyl CHF 2 Me Cl H 3-Cl-2-pyridyl CBrF 2 Me Cl H 3-F-2-pyridyl CH 2 CF 3 Me Cl H 3-CF 3 -2- CH 2 CF 3 pyridyl Me Cl H 3-Br-2-pyridyl CF 3 Me Cl H 3-Br-2-pyridyl CH 2 CF 3 Me Cl H 3-Br-2-pyridyl CF 2 CHF 2 Me Cl H 3-Br-2-Dylinyl CClF 2 Me Cl H H C 2 F 5 Me Cl H H C 2 F 5 Me Cl H H C 2 F 5 Me Cl H Me Allyl Formulation/Efficacy

本发明的化合物通常与包含液体稀释剂、固体稀释剂或表面活性剂中至少之一的农业适用载体一起用作配制剂或组合物。配制剂或组合物的成分选择要与活性成分的物理性能、施用方式及环境因素(如土壤类型、湿度的稳定)相一致。有用的配制剂包括液体如溶液(包括可乳化的浓缩液)、悬浮液、乳化液(包括微滴乳状液和/或suspoemulsions(悬浮乳状液))等，它们可被任选地稠化为凝胶。有用的配制剂还包括固体，如粉剂、粉末、颗粒剂、丸剂、片剂、膜剂等，它们可分散于水(“可湿润的”)或可溶于水。活性成分可被(微)胶囊化和进一步形成悬浮或固体制剂；或者，活性成分的整个制剂可被胶囊化(或“涂刷”)。胶囊可以控制或延缓活性成分的释放。可喷洒的制剂可在合适的介质中通过，且喷用量为每公顷约一至几百升。强力组合物主要用作进一步制剂的中间体。The compounds of the invention are generally used as formulations or compositions with an agriculturally acceptable carrier comprising at least one of a liquid diluent, a solid diluent or a surfactant. The choice of ingredients for a formulation or composition should be consistent with the physical properties of the active ingredient, the mode of application, and environmental factors (eg, soil type, moisture stability). Useful formulations include liquids such as solutions (including emulsifiable concentrates), suspensions, emulsions (including microemulsions and/or suspoemulsions (suspoemulsions)), etc., which may optionally be thickened into coagulated glue. Useful formulations also include solids, such as dusts, powders, granules, pellets, tablets, films, etc., which are dispersible in water ("wettable") or soluble in water. The active ingredient can be (micro)encapsulated and further formed into a suspension or solid formulation; alternatively, the entire formulation of the active ingredient can be encapsulated (or "painted on"). Capsules allow controlled or delayed release of the active ingredient. Sprayable formulations can be passed through in a suitable medium and sprayed at rates from about one to several hundred liters per hectare. Potency compositions are mainly used as intermediates for further formulations.

所述组合物通常含有有效量的活性成分、以及下列大致范围的稀释剂和表面活性剂，各量之和为100重量％。The compositions generally contain an effective amount of the active ingredient, together with the following approximate ranges of diluents and surfactants, the sum of which amounts to 100% by weight.

                                           重量％                   weight%

                                活性 active

                                成分      稀释剂    表面活性剂 Ingredient Diluent Surfactant

可分散于水和可溶于水的          5-90       0-94         1-15Water-dispersible and water-soluble 5-90 0-94 1-15

颗粒剂、片剂和粉末剂Granules, Tablets and Powders

悬浮液，乳化液，溶液            5-50       40-95        0-15Suspension, emulsion, solution 5-50 40-95 0-15

(包括可乳化的浓缩液)(including emulsifiable concentrates)

粉剂                            1-25       70-99        0-5Powder 1-25 70-99 0-5

颗粒剂和丸剂                    0.01-99    5-99.99      0-15Granules and pills 0.01-99 5-99.99 0-15

强力组合物                      90-99      0-10         0-2Strong Composition 90-99 0-10 0-2

在Watkins等的《Handbook of Insecticide Dust Diluents andCarriers》(杀虫剂粉末吸收剂和载体手册)第二版(Dorland Books，Caldwell，New Jersey)中对典型的固体稀释剂作了描述。在Marsden的《Solvents Guide》(溶剂指南)第二版(Interscience，New York，1950)中对典型的液体稀释剂作了描述。在《McCutcheon’s Detergentsand Emulsifiers Annual》(McCutcheon洗涤剂和乳化剂年报，AlluredPubl.Corp.，Ridgewood，New Jersey)以及Sisely和Wood的《Encyclopedia of Surface Active Agents》(表面活性剂百科全书，Chemical Publ.Co.，Inc.，NewYork，1964)中列举了表面活性剂和推荐的应用。所有的制剂可含有小量的添加剂，以减缓泡沫、结块、腐蚀、微生物生长等，或含有增稠剂，以增加粘度。Typical solid diluents are described in Watkins et al., Handbook of Insecticide Dust Diluents and Carriers, Second Edition (Dorland Books, Caldwell, New Jersey). Typical liquid diluents are described in Marsden's Solvents Guide, Second Edition (Interscience, New York, 1950). In "McCutcheon's Detergents and Emulsifiers Annual" (McCutcheon Detergents and Emulsifiers Annual Report, AlluredPubl. , Inc., New York, 1964) lists surfactants and suggested applications. All formulations may contain minor amounts of additives to slow down foaming, caking, corrosion, microbial growth, etc., or thickeners to increase viscosity.

表面活性剂包括例如：聚乙氧基化醇，聚乙氧基化烷基酚，聚乙氧基化脱水山梨糖醇脂肪酸酯，磺基琥珀酸二烷基酯，烷基硫酸酯，烷基苯磺酸酯，有机硅氧烷，N，N-二烷基牛磺酸酯，木质素磺酸酯，萘磺酸盐甲醛缩合物，聚羧酸酯，和聚氧乙烯/聚氧丙烯嵌段共聚物。固体稀释剂包括例如：粘土(如膨润土、蒙脱土、硅镁土和高岭土)，淀粉，糖，二氧化硅，滑石，硅藻土，尿素，碳酸钙，碳酸钠和碳酸氢钠，和硫酸钠。液体稀释剂包括例如：水，N，N-二甲基甲酰胺，二甲亚砜，N-烷基吡咯烷酮，乙二醇，聚丙二醇，石蜡，烷基苯，烷基萘，橄榄油，蓖麻油，亚麻子油，桐油，芝麻油，玉米油，花生油，棉籽油，豆油，油菜籽油，椰子油，脂肪酸酯，酮类(如环己酮，2-庚酮，异佛尔酮和4-羟基-4-甲基-2-戊酮)，以及醇类(如甲醇，环己醇，癸醇和四氢糠醇)。Surfactants include, for example: polyethoxylated alcohols, polyethoxylated alkylphenols, polyethoxylated sorbitan fatty acid esters, dialkyl sulfosuccinates, alkyl sulfates, alkanes Benzene sulfonate, organosiloxane, N,N-dialkyl taurate, lignosulfonate, naphthalene sulfonate formaldehyde condensate, polycarboxylate, and polyoxyethylene/polyoxypropylene block copolymers. Solid diluents include, for example, clays (such as bentonite, montmorillonite, attapulgite, and kaolin), starches, sugars, silica, talc, diatomaceous earth, urea, calcium carbonate, sodium carbonate and bicarbonate, and sulfuric acid sodium. Liquid diluents include, for example: water, N,N-dimethylformamide, dimethylsulfoxide, N-alkylpyrrolidones, ethylene glycol, polypropylene glycol, paraffin, alkylbenzene, alkylnaphthalene, olive oil, castor Sesame oil, linseed oil, tung oil, sesame oil, corn oil, peanut oil, cottonseed oil, soybean oil, rapeseed oil, coconut oil, fatty acid esters, ketones (such as cyclohexanone, 2-heptanone, isophorone and 4 -hydroxy-4-methyl-2-pentanone), and alcohols (such as methanol, cyclohexanol, decanol and tetrahydrofurfuryl alcohol).

溶液(包括可乳化的浓缩液)可通过简单地对成分进行混合而制备。粉剂和粉末剂可通过混合和通常如在锤磨机或流体能碾压机中进行的研磨而制备。悬浮液通常通过湿磨制备，参见例如U.S.3,060,084。颗粒剂和丸剂可通过将活性物质喷在预制颗粒状载体上或通过附聚技术而制备。参见：Browning的“Agglomeration”，Chemical Engineering，1967年12月4日，第147-48页；《Perry’s Chemical Engineer’sHandbook》第4版(McGraw-Hill，New York，1963)第8-57页及以下；和PCT出版物WO91/13546。丸剂可如U.S.4,172,714所述而制备。可分散于水和可溶于水的颗粒剂可根据U.S.4,144,050、U.S.3,920,442和DE3,246,493制备。片剂可根据U.S.5,180,587、U.S.5,232,701和U.S.5,208,030制备。膜剂可根据GB2,095,558和U.S.3,299,566制备。Solutions, including emulsifiable concentrates, can be prepared by simply mixing the ingredients. Dusts and powders can be prepared by mixing and grinding, usually as in a hammer mill or fluid energy roller mill. Suspensions are usually prepared by wet milling, see eg U.S. 3,060,084. Granules and pellets can be prepared by spraying the active material onto preformed granular carriers or by agglomeration techniques. See: Browning, "Agglomeration," Chemical Engineering, Dec. 4, 1967, pp. 147-48; Perry's Chemical Engineer's Handbook, 4th Ed. (McGraw-Hill, New York, 1963), pp. 8-57 and infra; and PCT Publication WO 91/13546. Pellets may be prepared as described in U.S. 4,172,714. Water-dispersible and water-soluble granules can be prepared according to U.S. 4,144,050, U.S. 3,920,442 and DE 3,246,493. Tablets may be prepared according to U.S. 5,180,587, U.S. 5,232,701 and U.S. 5,208,030. Films can be prepared according to GB2,095,558 and U.S.3,299,566.

有关制剂领域的进一步信息，参见T.S.Woods的“The Formulator’sToolbox-Product Forms for Modern Agriculture(制剂工作者工具箱-现代农业的产品形式)”，收于《Pesticide Chemistry andBioscience，The Food-Environment Challenge》(杀虫剂化学和生物科学，食品-环境挑战)，T.Brooks和T.R.Roberts编辑，第9届国际杀虫剂化学大会科研报告集，剑桥，1999年，第120-133页。另外参见：U.S.3,235,361第6栏第16行至第7栏第19行及实施例10-41；U.S.3,309,192第5栏第43行至第7栏第62行及实施例8、12、15、39、41、52、53、58、132、138-140、162-164、166、167和169-182；U.S.2,891,855第3栏第66行至第5栏第17行及实施例1-4；Klingman著《Weed Control as a Science》(杂草控制科学)，John Wileyand Sons公司出版，纽约，1961年，第81-96页；和Hance等著《WeedControl Handbook》(杂草控制手册)第8版，Blackwell ScientificPublications出版，牛津，1989年。For further information on the formulation field, see "The Formulator's Toolbox - Product Forms for Modern Agriculture" by T.S. Woods, in Pesticide Chemistry and Bioscience, The Food-Environment Challenge (Pesticide Chemistry and Biological Sciences, Food-Environmental Challenges), edited by T. Brooks and T.R. Roberts, Proceedings of the 9th International Congress on Pesticide Chemistry, Cambridge, 1999, pp. 120-133. See also: U.S. 3,235,361, column 6, line 16 to column 7, line 19 and examples 10-41; U.S. 3,309,192 column 5, line 43 to column 7, line 62 and examples 8, 12, 15, 39 , 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167, and 169-182; U.S. 2,891,855 column 3, line 66 to column 5, line 17 and Examples 1-4; Klingman Weed Control as a Science, John Wiley and Sons, New York, 1961, pp. 81-96; and Hance et al., Weed Control Handbook, 8th ed., Published by Blackwell Scientific Publications, Oxford, 1989.

在以下实施例中，所有百分比均为重量百分比，且所有制剂均以常规方式制备。化合物号参见索引表A中的化合物。In the following examples, all percentages are by weight and all formulations were prepared in conventional manner. See Compounds in Index Table A for compound numbers.

                      实施例A 可湿润的粉末剂化合物1                                     65.0％十二烷基酚聚乙二醇醚                        2.0％木质素磺酸钠                                4.0％硅铝酸钠                                    6.0％蒙脱土(经煅烧)                              23.0％ Example A wettable powder compound 1 65.0% dodecylphenol polyglycol ether 2.0% sodium lignosulfonate 4.0% sodium aluminosilicate 6.0% montmorillonite (calcined) 23.0%

                   实施例B 颗粒剂化合物7                                     10.0％硅镁土颗粒(低挥发性物质，0.71/0.30mm；U.S.S.No.25-50筛)                           90.0％ Example B Granules Compound 7 10.0% Attapulgite Granules (low volatile matter, 0.71/0.30mm; USSNo.25-50 sieve) 90.0%

                   实施例C 挤压成形的丸剂化合物1                                     25.0％无水硫酸钠                                  10.0％粗木质素磺酸钙                              5.0％烷基萘磺酸钠                                1.0％钙/镁膨润土                                 59.0％ Example C Extruded pellets Compound 1 25.0% anhydrous sodium sulfate 10.0% crude calcium lignosulfonate 5.0% sodium alkylnaphthalene sulfonate 1.0% calcium/magnesium bentonite 59.0%

                   实施例D 可乳化的浓缩液化合物7                                     20.0％油溶性磺酸盐和聚氧乙烯醚的掺合物                                    10.0％异佛尔酮                                    70.0％ Example D Emulsifiable Concentrate Compound 7 20.0% Blend of Oil Soluble Sulfonate and Polyoxyethylene Ether 10.0% Isophorone 70.0%

                   实施例E 颗粒剂化合物1                                     0.5％纤维素                                      2.5％乳糖                                        4.0％玉米粉                                      93.0％ Embodiment E granule compound 1 0.5% cellulose 2.5% lactose 4.0% corn flour 93.0%

本发明化合物的特征在于有利的代谢和/或土壤基型式，且显示对一定范围的农业和非农业无脊椎害虫的防治活性。(在本发明的说明书范围内，“无脊椎害虫防治”意味着抑制无脊椎害虫的生长(包括致死)，显著减少其摄食量或害虫引起的其它伤害；相关的表述定义类似)。就本说明书而言，术语“无脊椎害虫”包括具有经济重要性的节肢类、腹足类、线虫类害虫。术语“节肢类”包括昆虫、螨、蜘蛛、蝎子、蜈蚣、百足虫、球潮虫和总和纲(symphylans)。术语“腹足类”包括蜗牛、蛞蝓(slugs)和其它柄眼目(Stylommatophora)。术语“线虫类”包括所有的蠕虫，如：蛔虫，犬心虫，植食性线虫类(线虫纲)，吸虫(Tematoda)，棘头虫纲，以及绦虫(多节绦虫纲)。本领域的技术人员应认识到，并非所有的化合物对于所有的害虫具有相同的效力。本发明的化合物显示了对经济上具重要性的农业、林业、温室、苗圃、观赏性植物、食品和纤维、公共健康和动物健康、家用和商用建筑、家用品和贮存品等方面的害虫的活性。这些包括鳞翅目的幼虫，如夜蛾科族的粟蚕蛾幼虫(armyworms)，切根虫(cutworms)，尺蠖(loopers)，以及heliothines(例如：秋粟蚕蛾幼虫(Spodoptera fugiperda J.E.Smith)，甜菜粟蚕蛾幼虫(Spodoptera exigua.Hübner)，黑切根虫(Agrotis ipsilon Hufnagel)，卷心菜尺蠖(粉斑夜蛾，Trichoplusiani Hübner)，烟草蚜虫(Heliothis virescens Fabricius))；螟蛾科族的蛀虫，鞘蛾，结网毛虫，锥形虫(coneworms)，卷叶菜虫和骨化虫(skeletonizers)(例如：欧洲玉米钻孔虫(Ostrinia nubilalisHübner)，脐橙虫(Amyelois transitella Walker)，玉米根结网毛虫(Crambus caliginosellus Clemens)，草地结网毛虫(Herpetogrammalicarsislis Walker))；卷蛾科族的叶滚虫(leafrollers)，蚜虫，种子虫(seed worms)，以及果虫(fruit worms)(例如：苹果蠹蛾(Cydia pomonella Linnaeus)，葡糖浆果蠹蛾(Endopiza viteanaClemens)，东方果蠹蛾(Grapholita molesta Busck))；以及许多其它经济上重要的鳞翅目(例如菱纹背蛾(Plutella xylostellaLinnaeus)，红铃虫(Pectinophora gossypiella Saunders)，舞毒蛾(Lymantria dispar Linnaeus))；Blattodea目的稚虫和成虫，包括Blattollidae和蜚蠊科族的蟑螂(例如东方蟑螂(Blatta orientalisLinnaeus)，亚洲蟑螂(Blatella asahinai Mizukubo)，德国蟑螂(Blattella germanica Linnaeus)，褐带蟑螂(Supella longipalpaFabricius)，美洲蟑螂(Periplaneta americana Linnaeus)，褐色蟑螂(Periplaneta brunnea Burmeister)，马得拉岛蟑螂(Leucophaeamaderae Fabricius))；鞘翅目的摄叶幼虫和成虫，包括长角象虫科、豆象科和象虫科族的象鼻虫(例如棉籽象鼻虫(Anthonomus grandisBoheman)，米水象鼻虫(rice water weevil，Lissorhoptrus oryzophilusKuschel)，谷象鼻虫(Sitophilus granarius Linnaeus)，米象鼻虫(Sitophilus oryzae Linnaeus))；叶甲科族的跳甲、黄瓜甲虫、根虫、叶甲、马铃薯甲虫和甜菜麦蛾(例如科罗拉多马铃薯甲虫(Leptinotarsa decemlineata Say)，西方玉米根虫(Diabroticavirgifera virgifera LeConte))；金龟子科族的金龟子和其它甲虫(例如日本甲虫(Popillia japonica Newman)和欧洲金龟子(Rhizotrogus majalis Razoumowsky))；皮蠹科族的地毯圆皮蠹；叩头虫科的铁线虫(wireworms)；Scolytidae族的棘胫小蠹(barkbeetles))和拟步行虫科的粉甲虫。另外包括：革翅目的成虫和幼虫，包括秋螋科的地蜈蚣(例如欧洲地蜈蚣(Forficula auriculariaLinnaeus)，黑地蜈蚣(Chelisoches morio Fabricius))；半翅目和同翅目的成虫和稚虫，如盲蝽科族的盲蝽，Cicadidae族的蝉，大叶蝉科族的叶蝉(例如Empoasca spp.)，樗鸡科族和飞虱科族的planthopper，角蝉科族的角蝉，木虱科族的木虱，粉虱科族的粉虱，蚜科族的蚜虫，根瘤蚜科族的根瘤蚜，粉蚧科族的粉蚧，蜡蚧科族、盾蚧科族和硕蚧科族的介壳虫(scales)，网蝽科族的网蝽，蝽科族的椿象，长蝽科族的麦长蝽(例如Blissus spp.)和其它seed bugs，沫蝉科族的沫蝉，缘蝽科族的南瓜缘蝽，以及红蝽科族的恙螨(red bugs)和棉蝽象。还包括螨目的成虫和稚虫，如叶螨科族的红蜘蛛和茶红叶螨(例如欧洲茶红叶螨(Panonychus ulmi Koch)，两点红蜘蛛(two spottedspider mite，Tetranychus urticae Koch)，McDaniel螨(Tetranychusmcdaniele McGregor))，毛足蛛科族的flatmite(例如柑橘flatmite(Brevipalpus lewisi McGregor))，瘿螨科族的锈螨和芽螨(budmites)，以及其它摄叶螨和对人和动物健康重要的螨，即Epidermoptidae族的尘螨(dust mites)，蠕形螨科族的腺囊螨，食甜螨科族的谷螨，硬蜱科类的扁虱(例如鹿虱(deer tick，Ixodesscapularis Say)，澳洲瘫痪虱(Australian paralysis tick，Ixodesholocyclus Neumann)，美洲犬虱(Dermacentor variabilis Say)，孤星虱(lone star tick，Amblyomma americanum Linnaeus))，以及瘙螨虱科族、蒲螨科族和疥螨科族的马瘙螨和疥螨；直翅目的成虫和未成虫，包括蚱蜢、蝗虫和蟋蟀(例如迁徙蚱蜢(例如Melanoplussanguinipes Fabricius，M.Differentialis Thomas)，美洲蚱蜢(例如Schistocerca americana Drury)，沙漠蝗虫(Schistocerca gregariaForskal)，迁徙蝗虫(Locusta migratoria Linnaeus)，家蟋蟀(Achetadomesticus Linnaeus)，蝼蛄(Gryllotalpa Spp.))；双翅目类的成虫和未成虫，包括：甜菜麦蛾，蠓，果蝇(实蝇科)，麦秆蝇(例如Oscinella frit Linnaeus)，土壤蛆，家蝇(例如Musca domesticaLinnaeus)，小家蝇(例如Fannia canicularis Linnaeus，F.femoalisStein)，厩螫蝇(例如Stomoxys calcitrans Linnaeus)，面蝇(faceflies)，角蝇，丽蝇(blow flies，例如Chrysomya spp.，Phormia spp.)，和其它蝇状蝇害虫(muscoid fly pests)，马蝇(例如Tabanus spp.)，肤蝇(例如Gastrophilus spp.，Oestrus spp.)，牛蝇(例如Hypodermaspp.)，鹿蝇(例如Chrysops spp.)，keds(例如Melophagus ovinusLinnaeus)，以及其它短角亚目，蚊(例如Aedes spp.，Anopheles spp.，Culex spp.)，黑蝇(例如Prosimulium spp.，Simulium spp.)，蠓，沙蝇，sciarids，和其它长角亚目；缨翅目类的成虫和未成虫，包括葱蓟马(Thrips tabaci Lindeman)和其它摄叶蓟马；膜翅目类的昆虫类害虫，包括：蚁(例如红工木蚁(Camponotus ferrugineus Fabricius)，黑工木蚁(Camponotus pennsylvanicus DeGeer)，法老蚁(Monomoriumpharaonis Linnaeus)，小火蚁(Wasmannia auropunctata Roger)，火蚁(Solenopsis geminata Fabricius)，红外来火蚁(Solenopsisinvicta Latreille)，阿根廷蚁(Iridomyrmex humilis Mayr)，褐狂蚁(Paratrechina longicornis Latreille)，铺道蚁(Tetramoriumcaespitum Linnaeus)，美洲草地蚁(Lasius alienus F_ster)，臭家蚁(Tapinoma sessile Say))，蜜蜂(包括木蜂)，胡蜂，鲜黄色胡蜂褐黄峰；等翅目的昆虫害虫，包括：东美散白蚁(Reticulitermesflavipes Kollar)，西美散白蚁(Reticulitermes hesperus Banks)，台湾乳白蚁(Coptotermes formosanus Shiraki)，移栖楹白蚁(Incisitermes immigrans Snyder)和其它经济上具重要性的白蚁；缨尾目的昆虫害虫，如蠹鱼(Lepisma saccharina Linnaeus)和家衣鱼(Thermobia domestica Packard)；食毛目的昆虫害虫，并包括头虱(Pediculus humanus capitis De Geer)，体虱(Pediculus humanushumanus Linnaeus)，雏鸡羽虱(Menacanthus stramineus Nitszch)，狗咬虱(dog biting louse，Trichodectes canis De Geer)，绒毛虱(fluff louse，Goniocotes gallinae De Geer)，羊体虱(sheep bodylouse，Bovicola ovis Schrank)，阔胸血虱(short-nosed cattlelouse，Haematopinus eurysternus Nitzsch)，牛颚虱(long-nosedcattle louse，Linognathus vituli Linnaeus)和其它攻击人和动物的吮吸寄生虱(sucking parasitic lice)和咀嚼寄生虱(chewingparasitic lice)；蚤目的昆虫害虫，包括东方鼠蚤(oriental rat flea，Xenopsylla cheopis Rothschild)，猫蚤(Ctenocephalides felisBouche)，犬蚤(Ctenocephalides canis Curtis)，母鸡蚤(Ceratophyllus gallinae Schrank)，鬼针草蚤(sticktight flea，Echidnophaga gallinacea Westwood)，人蚤(Pulex irritansLinnaeus)和其它折磨哺乳动物和鸟类的虱子。其它涵盖的节肢害虫包括：蜘蛛目的蜘蛛，如褐色隐居蜘蛛(brown recluse spider，Loxoscelesreclusa Gertsch & Mulaik)和黑寡妇蛛(Latrodectus mactansFabricius)，以及Scutigeromorpha目的蜈蚣，如家蜈蚣(Scutigeracoleoptrata Linnaeus)。活性还包括线虫纲、多节绦虫纲、吸虫纲和棘头虫纲的成员，包括经济上重要的Strongylida目、Ascaridida目、蛲虫目(Oxyurida)、Rhabditida目、Spirurida目和Enoplida目的成员，如(但不限于)经济上重要的农业害虫(例如Meloidogyne属的马氏异皮线虫，Pratylenchus属的小线虫，Trichodorus属的黄麻根瘤线虫等)以及动物和人的健康害虫(例如，所有经济上重要的吸虫，绦虫，和蛔虫，如马的Stongylus vulgaris，狗的Toxocara canis，羊的Haemonchuscontortus，狗的Dirofilaria immitis Leidy，马的Anoplocephalaperfoliata，反刍动物的Fasciola hepatica Linnaeus，等)。The compounds of the present invention are characterized by favorable metabolism and/or soil-based profiles and show control activity against a range of agricultural and non-agricultural invertebrate pests. (In the scope of the present invention, "invertebrate pest control" means inhibiting the growth (including killing) of invertebrate pests, significantly reducing their food intake or other damage caused by pests; related expressions and definitions are similar). For the purposes of this specification, the term "invertebrate pest" includes arthropod, gastropod, nematode pests of economic importance. The term "arthropods" includes insects, mites, spiders, scorpions, centipedes, centipedes, ballworms and symphylans. The term "gastropod" includes snails, slugs and other members of the order Stylommatophora. The term "nematodes" includes all helminths such as: roundworms, heartworms, herbivorous nematodes (Nematoda), trematodes (Tematoda), Acanthocephala, and tapeworms (Cestenia). Those skilled in the art will recognize that not all compounds are equally effective against all pests. The compounds of the present invention show activity against economically important pests of agriculture, forestry, greenhouses, nurseries, ornamental plants, food and fibres, public and animal health, domestic and commercial construction, household and stored products, etc. active. These include Lepidoptera larvae such as armyworms of the Noctuidae family, cutworms, loopers, and heliothines (e.g. Spodoptera fugiperda J.E.Smith, sugar beet millet Silkworm moth larvae (Spodoptera exigua. Hübner), black rootworms (Agrotis ipsilon Hufnagel), cabbage loopers (Trichoplusiani Hübner), tobacco aphids (Heliothis virescens Fabricius)); borers of the family Boreridae, Coleoptera, Web-spinning caterpillars, coneworms, rollworms and skeletonizers (e.g. Ostrinia nubilalis Hübner, Amyelois transitella Walker, Crambus caliginosellus Clemens), Herpetogrammalicarsislis Walker); leafrollers, aphids, seed worms, and fruit worms (e.g., Cydia pomonella Linnaeus), glucose berry moth (Endopiza viteanaClemens), oriental fruit moth (Grapholita molesta Busck)); and many other economically important Lepidoptera (such as diamondback moth (Plutella xylostellaLinnaeus), pink boll moth ( Pectinophora gossypiella Saunders), gypsy moth (Lymantria dispar Linnaeus)); larvae and adults of the order Blattodea, including cockroaches of the Blattollidae and Blattidae families (e.g., Oriental cockroach (Blatta orientalis Linnaeus), Asian cockroach (Blatella asahinai Mizukubo), German cockroach ( Blattella germanica Linnaeus), brown-banded cockroach (Supella longipalpa Fabricius), American cockroach (Periplaneta americana Linnaeus), brown cockroach (Periplaneta brunnea Burmeister), Madeira island cockroach (Leucophaeamaderae Fabricius)); leaf-shooting larvae and adults of Coleoptera, including long Weevils of the Horned Weevils, Lissorhoptrus oryzophilus Kuschel, Grain Weevils (Sitophilus granarius Linnaeus) ), rice weevil (Sitophilus oryzae Linnaeus)); flea beetles, cucumber beetles, rootworms, leaf beetles, potato beetles and sugar beet wheat moths of the Chrysophyllidae family (e.g. Colorado potato beetle (Leptinotarsa decemlineata Say), western corn rootworm ( Diabroticavirgifera virgifera LeConte)); scarabs and other beetles of the family Scarabidae (such as the Japanese beetle (Popillia japonica Newman) and the European scarab (Rhizotrogus majalis Razoumowsky)); carpet beetles of the family Dermestidae; wireworms); barkbeetles of the family Scolytidae) and mealy beetles of the family Pedidae. Also included: adults and larvae of the order Dermatoptera, including ground centipedes of the family Asteroptera (for example, Forficula auricularia Linnaeus, black ground centipede (Chelisoches morio Fabricius)); adults and larvae of the orders Hemiptera and Homoptera, such as Miridae of the family Miridae, cicadas of the family Cicadidae, leafhoppers of the family Cicadidae (e.g. Empoasca spp.), planthoppers of the family Aphididae and Planthoppers, planthoppers of the family Cicadae, psyllids Psyllids of the family Aphididae, mealybugs of the Aphididae family, aphids of the Aphididae family, phylloxera of the Phylloxera family, mealybugs of the Mealyacidae family, wax scale families, Coccidae and Scalucidae families Scales, stinkbugs of the genus family stinkbugs, stinkbugs of the stinkbug family, wheat longbugs (such as Blissus spp.) and other seed bugs of the genus spp. Cucurbita, and red bugs and cotton stinkbugs, family Red Bugs. Also includes adults and larvae of the order Acarina, such as red spider mite and tea red spider mite of the family Tetranychus ulmi Koch, two spotted spider mite (Tetranychus urticae Koch), McDaniel mite (Tetranychusmcdaniele McGregor )), flatmites of the Trichopedidae family (eg citrus flatmite (Brevipalpus lewisi McGregor)), rust mites and budmites of the Eriodidae family, and other spider mites and mites important to human and animal health, That is, dust mites (dust mites) of the Epidermoptidae family, adenocystic mites of the Demodidae family, meal mites of the Saccharidae family, and ticks of the Ixodidae family (such as deer ticks, Ixodesscapularis Say), Australia The paralysis tick (Australian paralysis tick, Ixodesholocyclus Neumann), the American dog tick (Dermacentor variabilis Say), the lone star tick (Amblyomma americanum Linnaeus)), and the families Pruriticae, Punyidae, and Sarcidae and scabies mites; adults and immatures of the order Orthoptera, including grasshoppers, locusts and crickets (e.g. migratory grasshoppers (e.g. Melanoplus sanguinipes Fabricius, M. Differentialis Thomas), American grasshoppers (e.g. Schistocerca americana Drury), desert locusts (Schistocerca gregaria Forskal), migratory locust (Locusta migratoria Linnaeus), house cricket (Achetadomesticus Linnaeus), mole cricket (Gryllotalpa Spp.)); adults and immatures of Diptera, including: sugar beet moths, midges, fruit flies (Tephritidae ), straw flies (eg Oscinella frit Linnaeus), soil maggots, houseflies (eg Musca domestica Linnaeus), houseflies (eg Fannia canicularis Linnaeus, F. femoalis Stein), stable flies (eg Stomoxys calcitrans Linnaeus), face flies ( faceflies), horn flies, blow flies (e.g. Chrysomya spp., Phormia spp.), and other muscoid fly pests, horse flies (e.g. Tabanus spp.), skin flies (e.g. Gastrophilus spp. , Oestrus spp.), gad flies (eg Hypodermas pp.), deer flies (eg Chrysops spp.), keds (eg Melophagus ovinus Linnaeus), and other Brachycera suborders, mosquitoes (eg Aedes spp., Anopheles spp., Culex spp .), black flies (e.g. Prosimulium spp., Simulium spp.), midges, sand flies, sciarids, and other Longocera; adults and imagoes of Thysanoptera, including Thrips tabaci Lindeman and Other leaf thrips; insect pests of the order Hymenoptera, including: ants (e.g. Camponotus ferrugineus Fabricius), black worker ants (Camponotus pennsylvanicus DeGeer), pharaoh ants (Monomorium pharaonis Linnaeus), small fire ants (Wasmannia auropunctata Roger), Fire Ant (Solenopsis geminata Fabricius), Infrared Fire Ant (Solenopsis invicta Latreille), Argentine Ant (Iridomyrmex humilis Mayr), Brown Mad Ant (Paratrechina longicornis Latreille), Pavement Ant (Tetramorium caespitum Linnaeus), American Grass Ants (Lasius alienus F_ster), stink house ants (Tapinoma sessile Say)), bees (including carpenter wasps), wasps, bright yellow wasps brown yellow peaks; insect pests of the order Isoptera, including: Eastern American scattered termites (Reticulitermesflavipes Kollar), Reticulitermes hesperus Banks, Coptotermes formosanus Shiraki, Incisitermes immigrans Snyder and other economically important termites; insect pests of the order Tasmania, such as silverfish (Lepisma saccharina Linnaeus) and housefish (Thermobia domestica Packard); insect pests of the order Trichophagous and include head lice (Pediculus humanus capitis De Geer), body lice (Pediculus humanus humanus Linnaeus), chick feather lice (Menacanthus stramineus Nitszch), dog biting lice (dog biting louse, Trichodectes canis De Geer), fluff louse, Goniocotes gallinae De Geer, sheep body louse (Bovicola ovis Schrank), short-nosed cattlelouse, Haematopinus eurysternus Nitzsch, Long-nosed cattle louse (Linognathus vituli Linnaeus) and other sucking and chewing parasitic lice that attack humans and animals; insect pests of the order Fleas, including the oriental rat flea , Xenopsylla cheopis Rothschild), cat flea (Ctenocephalides felisBouche), dog flea (Ctenocephalides canis Curtis), hen flea (Ceratophyllus gallinae Schrank), sticktight flea (Echidnophaga gallinacea Westwood), human flea (Pulex irritans and Linnaeus) Other lice that afflict mammals and birds. Other arthropod pests covered include: spiders of the order Araneus, such as brown recluse spiders (brown recluse spider, Loxosceles reclusa Gertsch & Mulaik) and black widow spiders (Latrodectus mctans Fabricius), and centipedes of the order Scutigeromorpha, such as house centipedes (Scutigeracoleoptrata Linnaeus). Activity also includes members of the classes Nematodes, Polycystidae, Trematodes and Acanthocephala, including members of the economically important Orders Strongylida, Ascaridida, Oxyurida, Rhabditida, Spirurida and Enoplida, such as (but not limited to) economically important agricultural pests (e.g. Meloidogyne genus Heteroderma martensii, Pratylenchus genus genus, Trichodorus genus Jute rootknot nematode, etc.) and animal and human health pests (e.g., all economically important flukes, tapeworms, and roundworms, such as Stongylus vulgaris in horses, Toxocara canis in dogs, Haemonchuscontortus in sheep, Dirofilaria immitis Leidy in dogs, Anoplocephalaperfoliata in horses, Fasciola hepatica Linnaeus in ruminants, etc.).

本发明的化合物对下列各目的害虫具有特别高的活性：鳞翅目(例如Alabama argillacea Hübner(棉叶波纹夜蛾)，Archips argyrospilaWalker(果黄卷蛾)，A.rosana Linnaeus(European leaf roller)和其它Archips种类，Chilo suppressalis Walker(二化螟)，Cnaphalocrosis medinalis Guenee(rice leafroller)，Crambuscaliginosellus Clemens(玉米根网螟)，Crambus teterrellus Zincken(早熟禾草螟)，Cydia pomonella Fabricius(苹蠹蛾)，Earias insulanaBoisduval(棉斑实蛾)，Earias vittella Fabricius(spottedbollworm)，Helicoverpa virescens Hübner(Ammerican bollworm)，Helicoverpa zea Boddie(玉米穗蛾)，Heliothis virescens Fabricius(烟芽夜蛾)，Herpetogramma licarsisalis Walker(sod webworm)，Lobesis botrana Denis & Schiffermüller(葡糖小卷蛾)，Pectinophoragossypiella Saunders(pink bollworm)，Phyllocnistis citrellaStainton(橘红潜叶甲)，Pieris brassicae Linnaeus(大菜粉蝶)，Pieris papae Linnaeus(小菜粉蝶)，Plutella xylostella Linnaeus(小菜蛾)，Spodoptera exigua Hübner(甜菜夜蛾)，Spodoptera lituraFabricius(斜纹夜蛾，cluster caterpillar)，Spodoptera frugiperdaJ.E.Smith(草地粘虫)，Trichoplusia ni Hübner(粉纹夜蛾)和Tutaabsoluta Meyrick(tomato leafminer))。本发明的化合物对同翅目的成员也有商业上明显的活性，包括：Acyrthisiphon pisum Harris(豌蚜)，Aphis craccivora Koch(豇豆蚜)，Aphis fabae Scopoli(黑豆蚜)，Aphis gossypii Glover(棉蚜，瓜蚜)，Aphis pomi De Geer(苹蚜)，Aphis spiraecola Patch(绣线菊蚜)，Aulacorthum solaniKaltenbach(指顶花无网蚜)，Chaetosiphon fragaefolii Cockerell(草莓中瘤钉毛蚜)，Diuraphis noxia Kurdjumov/Mordvilko(俄罗斯麦长管蚜)，Dysaphis plantaginea Paaserini(车前圆尾蚜)，Eriosoma lanigerum Hausmann(苹绵蚜)，Hyalopterus pruni Geoffroy(桃大尾蚜)，Lipaphis erysimi Kaltenbach(芜菁蚜)，Metopolophiumdirrhodum Walker(谷蚜)，Macrosipum euphorbiae Thomas(马铃薯长管蚜)，Myzus persicae Sulzer(peach-potato aphid，桃蚜)，Nasonovia ribisnigri Mosley(莴苣衲长管蚜)，Pemphigus spp.(根蚜和葡糖根疣蚜)，Phopalosiphum maidis Fitch(玉米蚜)，Rhopalosiphum padi Linnaeus(bird cherry-oat aphid)，Schizaphisgraminum Rondani(麦二叉蚜)，Sitobion avenae Fabricius(麦长管蚜)，Therioaphis maculata Buckton(苜蓿斑蚜)，Toxoptera aurantiiBoyer de Fonscolombe(桔声蚜)，和Toxoptera citricida Kirkaldy(热带桔二岔蚜)；Adelges spp.(球蚜)；Phylloxera devastatrixPergande(美核桃根瘤蚜)；Bemisia tabaci Gennadius(烟草粉虱，甘薯粉虱)；Bemisia argentifolii Bellows & Perring(silverleafwhitefly)，Dialeurodes citri Ashmead(柑桔粉虱)和Trialeurodesvaporariorum Westwood(温室粉虱)；Empoasca fabae Harris(蚕豆微叶蝉)，Laodelphax striatellus Fallen(小褐稻虱)，Macrolestesquadrilineatus Forbes(六点叶蝉)，Nephotettix cinticeps Uhler(茶微叶蝉)，Nephotettix nigropictus St l(黑尾叶蝉)，Nilaparvatalugens St l(稻褐飞虱)，Peregrinus maidis Ashmead(玉米蜡蝉)，Sogatella furcifera Horvath(白背稻虱)，Sogatodes orizicola Muir(rice delphacid)，Typhlocyba pomaria McAtee(苹白小叶蝉)，Erythroneoura spp.(葡糖斑叶蝉)；Magicidada septendecim Linnaeus(期蝉)；Icerya purchasi Maskell(吹绵蚧)，Quadraspidiotusperniciosus Comstock(梨圆盾蚧)；Planococcus citri Risso(柑桔粉蚧)；Pesudococcus spp.(其它粉蚧复合体)：Cacopsylla pyricolaFoerster(梨黄木虱)，Trioza diospyri Ashmead(柿木虱)。这些化合物还对半翅目的成员具有活性，包括：Acrosternum hilare Say(稻绿蝽)，Anasa tristis De Geer(南瓜绿蝽)，Blissus leucopterusleucopterus Say(麦长蝽)，Corythuca gossypii Fabricius(棉网蝽(cotton lace bug))，Cyrtopeltis modesta Distant(tomato bug)，Dysdercus suturellus Herrich-Sch_ffer(棉黑翅红蝽)，Euchistusservus Say(褐臭蝽)，Euchistus variolarius Palisot de Beauvois(一点褐蝽)，Graptosthetus spp.(蚜虫复合体)，Leptoglossuscorculus Say(松籽喙缘蝽)，Lygus lineolaris Palisot de Beauvois(牧草盲蝽)，Nezara viridula Linnaeus(稻绿蝽)，Oebalus pugnaxFabricius(稻褐蝽)，Oncopeltus fasciatus Dallas(大马利筋长蝽)，Pseudatomoscelis seriatus Reuter(棉跳盲蝽)。其它被本发明化合物防治的害虫目包括：缨翅目(例如Frankliniella occidentalisPergande(苜蓿蓟马)，Scirthothrips citri Moulton(桔实蓟马)，Sericothrips variabilis Beach(大豆蓟马)，和Thrips tabaciLindeman(葱蓟马))，和鞘翅目(例如Leptinotarsa decemlineata Say(马铃薯甲虫)，Epilachna varivestis Mulsant(墨西哥豆瓢虫)，以及Agriotes、Athous和Limonius种的铁线虫)。The compounds of the present invention have particularly high activity against the pests of the following purposes: Lepidoptera (such as Alabama argillacea Hübner (cotton leaf roller moth), Archips argyrospila Walker (fruit yellow roller moth), A.rosana Linnaeus (European leaf roller) and Other Archips species, Chilo suppressalis Walker (Chilo suppressalis Walker), Cnaphalocrosis medinalis Guenee (rice leafroller), Crambuscaliginosellus Clemens (Corn root mesh borer), Crambus teterrellus Zincken (Poaan grass moth), Cydia pomonella Fabricius (Codling moth), Earias insulana Boisduval (cotton moth), Earias vittella Fabricius (spotted bollworm), Helicoverpa virescens Hübner (American bollworm), Helicoverpa zea Boddie (corn ear moth), Heliothis virescens Fabricius (smog budworm), Herpetogramma licarsisalis Walker (sod webworm), Lobesis botrana Denis & Schiffermüller (glucose small tortilla moth), Pectinophoragossypiella Saunders (pink bollworm), Phyllocnistis citrella Stainton (orange red leafworm), Pieris brassicae Linnaeus (big cabbage white butterfly), Pieris papae Linnaeus (small cabbage white butterfly), Plutella xylostella Linnaeus ( moth), Spodoptera exigua Hübner (beet armyworm), Spodoptera lituraFabricius (spodoptera litura, cluster caterpillar), Spodoptera frugiperda J.E.Smith (meadow armyworm), Trichoplusia ni Hübner (Trichoplusia ni Hübner) and Tutaabsoluta Meyrick (tomato leafminer )). Compounds of the present invention also have commercially significant activity against members of the order Homoptera, including: Acyrthisiphon pisum Harris (pis aphid), Aphis craccivora Koch (cowpea aphid), Aphis fabae Scopoli (black bean aphid), Aphis gossypii Glover (cotton aphid, melon aphid Aphis), Aphis pomi De Geer (apple aphid), Aphis spiraecola Patch (spiraea aphid), Aulacorthum solani Kaltenbach (pointed flower aphid), Chaetosiphon fragaefolii Cockerell (strawberry aphid), Diuraphis noxia Kurdjumov/Mordvilko (Russian wheat long tube aphid), Dysaphis plantaginea Paaserini (plantaginea Paaserini), Eriosoma lanigerum Hausmann (apple aphid), Hyalopterus pruni Geoffroy (peach aphid), Lipaphis erysimi Kaltenbach (turnip aphid), Metopolophium dirrhodum Walker ( Grain aphid), Macrosipum euphorbiae Thomas (potato aphid), Myzus persicae Sulzer (peach-potato aphid, peach aphid), Nasonovia ribisnigri Mosley (lettuce aphid), Pemphigus spp. (root aphid and glucose phylloxera ), Phopalosiphum maidis Fitch (corn aphid), Rhopalosiphum padi Linnaeus (bird cherry-oat aphid), Schizaphisgraminum Rondani (wheat aphid), Sitobion avenae Fabricius (wheat long tube aphid), Therioaphis maculata Buckton (clover alfalfa), Toxoptera aurantii Boyer de Fonscolombe (Pylloxera), and Toxoptera citricida Kirkaldy (Tropical Aphid); Adelges spp. (Pylloxera); Phylloxera devastatrix Pergande (Pylloxera); Bemisia tabaci Gennadius (Tobacco Whitefly, Sweet Potato Whitefly) ; Bemisia argentifolii Bellows & Perring (silverleaf whitefly), Dialeurodes citri Ashmead (citrus whitefly) and Trialeurodes vaporariorum Westwood (greenhouse whitefly); Empoasca fabae Harris (vaba bean microleafhopper), Laodelphax striatellus Fallen (small brown ricefly), Macrolestesquadrilineatus For (Six-spotted Leafhopper), Nephotettix cinticeps Uhler (Tea Microleafhopper), Nephotettix nigropictus St l (Black-tailed leafhopper), Nilaparvatalugens St l (rice delphacid), Peregrinus maidis Ashmead (corn wax cicada), Sogatella furcifera Horvath (white-backed rice hopper), Sogatodes orizicola Muir (rice delphacid), Typhlocyba pomaria McAtee (apple white leafhopper), Erythroneoura spp. (glucose spot Leafhopper); Magicidada septendecim Linnaeus (period cicada); Icerya purchasi Maskell (blowing cotton scale), Quadraspidiotusperniciosus Comstock (pear round shield scale); Planococcus citri Risso (citrus mealybug); Pesudococcus spp. (other mealybug complexes) : Cacopsylla pyricola Foerster (Pear yellow psyllid), Trioza diospyri Ashmead (Psyllium persimmon). These compounds are also active against members of the order Hemiptera, including: Acrosternum hilare Say (rice green bug), Anasa tristis De Geer (pumpkin green bug), Blissus leucopterus leucopterus Say (wheat long bug), Corythuca gossypii Fabricius (cotton bug (cotton bug) lace bug)), Cyrtopeltis modesta Distant (tomato bug), Dysdercus suturellus Herrich-Schöffer (cotton black-winged red bug), Euchistus servus Say (brown stink bug), Euchistus variolarius Palisot de Beauvois (a little brown bug), Graptosthetus spp. (aphid complex), Leptoglossuscorculus Say (pine nut beak), Lygus lineolaris Palisot de Beauvois (grass ligus), Nezara viridula Linnaeus (rice green stink), Oebalus pugnaxFabricius (rice brown stinkbug), Oncopeltus fasciatus Dallas (large milkweed Long bug), Pseudatomoscelis seriatus Reuter (cotton jumping bug). Other pest orders controlled by the compounds of the present invention include: Thysanoptera (such as Frankliniella occidentalis Pergande (alfalfa thrips), Scirthothrips citri Moulton (citrus thrips), Sericothrips variabilis Beach (soybean thrips), and Thrips tabaciLindeman (onion thrips )), and Coleoptera (eg Leptinotarsa decemlineata Say (potato beetle), Epilachna varivestis Mulsant (Mexican bean ladybug), and iron nematodes of the species Agriotes, Athous, and Limonius).

本发明的化合物还可与一种或多种其它生物活性化合物或试剂混合，以形成多成分的杀虫剂，产生更广的农用范围，所述其它生物活性化合物或试剂包括：杀虫剂，杀真菌剂，杀线虫剂，杀菌剂，杀螨剂，生长调节剂(如扎根刺激剂(rooting stimulants))，化学灭菌剂，化学信息物(semiochemicals)，驱虫剂，诱引剂，信息素，摄食刺激剂(feeding stimulants)，其它生物活性化合物或昆虫病原细菌、病毒或真菌。因此，本发明的组合物可进一步包含生物有效量的至少一种附加生物活性化合物或试剂。本发明的化合物可与如下各例生物活性化合物或试剂进行配制：杀虫剂，如齐墩螨素(abamectin)，高灭磷，吡虫清，齐墩螨素(avermectin)，艾扎丁，谷硫磷，氟氯菊酯，联苯肼酯，噻嗪酮，虫螨威，氟唑虫清，定虫隆，毒死蜱，甲基毒死蜱，chromafenozide，clothianidin，氯氟氰菊酯，β-氯氟氰菊酯，(RS)氯氟氰菊酯，λ-氯氟氰菊酯，氯氰菊酯，灭蝇胺，溴氰菊酯，杀螨硫隆，二嗪农，氟脲杀，乐果，噁茂醚，emamectin，硫丹，高氰戊菊酯，ethiprole，苯硫威，双氧威，甲氰菊酯，唑螨酯，杀灭菊酯，锐劲特，flonicamid，氟氰戊菊酯，氟胺氰菊酯，氟虫脲，地虫磷，特丁苯酰肼，氟铃脲，吡虫啉，噁二唑虫，丙胺磷，氟丙氧脲，马拉松，蜗牛敌，甲胺磷，杀扑磷，灭多虫，蒙五一五，甲氧滴滴涕，久效磷，甲氧苯酰肼，硝虫噻嗪，双苯氟脲，甲氨叉威，一六零五，甲基一六零五，氯菊酯，三九一一，伏杀磷，亚胺硫磷，磷胺，抗蚜威，丙溴磷，拒嗪酮，pyridalyl，蚊蝇醚，鱼藤酮，艾克敌105，乙丙硫磷，双苯酰肼，伏虫隆，七氟菊酯，特丁磷，杀虫畏，thiacloprid，thiamethoxam，硫双灭多威，杀虫双，四溴菊酯，敌百虫，和杀虫隆；杀真菌剂，如噻二唑素，腈嘧菊酯，苯菌灵，灭瘟素，波尔多液(碱式硫酸铜)，糠菌唑，氯环丙酰胺，captafol，克菌丹，多菌灵，地茂散，百菌清，王铜，铜盐，cyflufenamid，清菌脲，环唑醇，环丙嘧啶，(S)-3，5-二氯-N-(3-氯-1-乙基-1-甲基-2-氧丙基)-4-甲基苯甲酰胺(RH 7281)，diclocymet(S-2900)，哒菌清，氯硝胺，噁茂唑，(S)-3，5-二氢-5-甲基-2-甲基硫代-5-苯基-3-苯氨基-4H-咪唑-4-酮(RP407213)，烯酰吗啉，dimoxystrobin，烯唑醇，烯唑醇-M，多果定，克瘟散，氧唑菌，噁唑铜菌，fenamidone，异嘧菌醇，腈苯唑，fencaramide(SZX0722)，拌种咯，苯锈啶，丁苯吗啉，薯瘟锡，毒菌锡，氟啶胺，氟联苯菌(RPA 403397)，喹唑菌酮，氟硅唑，氟酰胺，粉唑醇，灭菌丹，藻菌磷，呋氨丙灵，呋吡唑灵(S-82658)，己唑醇，环戊唑醇，异丙定，富士一号，春雷霉素，亚胺菌，代森锰锌，代森锰，mefenoxam，丙氧灭绣胺，甲霜灵，环戊唑菌，叉氨苯酰胺(SSF-126)，腈菌唑，甲胂铁铵(甲基胂酸铁)，噁霜灵，戊菌唑，戊菌隆，丙氯灵，百维灵，环丙唑，啶斑肟，pyraclostrobin，二甲嘧菌胺，咯喹酮，喹氧灵，螺噁茂胺，硫磺粉，戊唑醇，氟醚唑，涕必灵，溴氟唑菌，甲基托布津，福美双，tiadinil，三唑酮，唑菌醇，三环唑，trifloxystrobin，戊叉唑菌，有效霉素，和烯菌酮；杀线虫剂，如涕灭威，甲氨叉威，和克线磷；杀菌剂，如链霉素；杀螨剂，如虫螨脒，灭螨猛，乙酯杀螨醇，三环锡，开乐散，除螨灵，特苯噁唑，喹螨醚，杀螨锡，甲氰菊酯，唑螨酯，噻螨酮，克螨特，哒螨酮，和吡螨胺；以及生物试剂，如苏云金芽孢杆菌(Bacillus thuringiensis)，包括泽亚种(aizawai)和库尔斯塔克亚种(kurstaki)，苏云金芽孢杆菌δ-内毒素(delta endotoxin)，杆状病毒，以及食虫细菌、病毒和真菌。The compounds of the present invention may also be mixed with one or more other biologically active compounds or agents, including: insecticides, Fungicides, nematicides, bactericides, acaricides, growth regulators (such as rooting stimulants), chemical bactericides, semiochemicals, insect repellants, attractants, information hormones, feeding stimulants, other biologically active compounds or entomopathogenic bacteria, viruses or fungi. Accordingly, the compositions of the present invention may further comprise a biologically effective amount of at least one additional biologically active compound or agent. The compound of the present invention can be formulated with the following examples of biologically active compounds or reagents: insecticides, such as abamectin (abamectin), acefenphos, acetamiprid, avermectin (avermectin), azadine, azinphos, bifenthrin, bifenazin, buprofezin, fenfencarb, chlorfenapyr, difenuron, chlorpyrifos, chlorpyrifos-methyl, chromafenozide, clothianidin, cyhalothrin, beta-chloro Cyfluthrin, (RS) cyhalothrin, lambda-cyhalothrin, cypermethrin, cyromazine, deltamethrin, thiuron, diazinon, hexafluon, dimethoate, Profen, emamectin, endosulfan, esfenvalerate, ethiprole, fenthiocarb, fenoxycarb, fenpropathrin, pyraflux, methethrin, fipronil, flonicamid, flucyvalerate, Fluvalinate, flubenzuron, difenphos, terbufenozide, hexaflumuron, imidacloprid, oxadiazole, amiphos, flupropoxycarbamide, marathon, snail enemy, methamidophos, kill Phosphorus, methoxam, 515, methoxychlor, monocrotophos, methoxyfenozide, nitrothiazine, difenfluramide, methoxacarb, 1605, methyl 160 Five, permethrin, 3911, sulfaphos, imophos, phosphamide, pirimicarb, profenofos, azinone, pyridalyl, pyriproxyfen, rotenone, Acetyl 105, ethylene propylene Thionphos, difenazide, chlorfluron, tefluthrin, terbufos, dimefen, thiacloprid, thiamethoxam, thiodimethomyl, dimehypo, perbromethrin, trichlorfon, and thiamethoxam Champron; fungicides, such as thiadiazol, cypromethrin, benomyl, blasticidin, Bordeaux mixture (basic copper sulfate), furconazole, chlorcycline, captafol, captan, Carbendazim, Dimaosan, Chlorothalonil, Copper King, Copper Salt, Cyflufenamid, Chlorazuron, Cycloconazole, Cypromethanil, (S)-3,5-Dichloro-N-(3-Chloro- 1-Ethyl-1-methyl-2-oxypropyl)-4-methylbenzamide (RH 7281), diclocymet (S-2900), pyridoxalil, nichloramine, oxoxazole, (S )-3,5-dihydro-5-methyl-2-methylthio-5-phenyl-3-anilino-4H-imidazol-4-one (RP407213), dimethomorph, dimoxystrobin, ene Fenazole alcohol, diniconazole-M, dodine, Kewensan, oxyconazole, copper oxaconazole, fenamidone, isofyristrobin, carbendazole, fencaramide (SZX0722), seed dressing, fenpropidin, Fenpropimorph, yambatin, toxin, fluazinam, fluorinated biphenyl (RPA 403397), quinazolone, flusilazole, fluoramide, fuconazole, folpet, algalphos, Famiproline, furazolin (S-82658), hexaconazole, cycloteconazole, iprodine, Fuji No. 1, kasugamycin, imine bacteria, mancozeb, maneb, mefenoxam , Propoxypyrrole, metalaxyl, metconazole, biconazole (SSF-126), myclobutanil, ferric ammonium arsine (iron methyl arsinate), oxaxyl, penconazole, pentocuron, prochloraz, prochloraz, cyproconazole, pymetroxime, pyraclostrobin, pyrimethanil, pyroxaquinone, quinoxyfin, spiroxamine, sulfur powder, tebuconazole, fluoroether azoles, albizolin, bromfluconazole, thiophanate-methyl, thiram, tiadinil, triadimefon, pyraclostrobin, tricyclazole, trifloxystrobin, tricloconazole, validamycin, and meclofenone; Nematodes, such as aldicarb, methotrexate, and grammephos; fungicides, such as streptomycin; Lesan, Fabex, Tebenoxazole, Fenazazafen, Fenzafen, Fenpropathrin, Fenpyroximate, Hexythiazox, Capclofenac, Pyridaben, and Tebufenpyrad; and Biological Agents, Such as Bacillus thuringiensis, including subsp. aizawai and subsp. kurstaki, Bacillus thuringiensis delta endotoxin (delta endotoxin), baculovirus, and insectivorous bacteria, viruses and fungi.

有关这些农用防护剂的通用参考文献是：《The Pesticide Manual》(杀虫剂手册)，第十二版，C.D.S.Tomlin出版，British Crop ProtectionCouncil(英国作物保护委员会)，Farnham，Surrey，U.K.，2000。A general reference on these agricultural repellents is: "The Pesticide Manual", Twelfth Edition, published by C.D.S. Tomlin, British Crop Protection Council, Farnham, Surrey, U.K., 2000.

用于与本发明的化合物混合的优选杀虫剂和杀蜱剂包括：合成除虫菊酯类，如氯氰菊酯，(RS)氯氟氰菊酯，氟氯氰菊酯，β-氟氯氰菊酯，高氰戊菊酯，杀灭菊酯和四溴菊酯；氨基甲酸酯类，如fenothicarb，灭多虫，甲氨叉威，和硫双灭多威；neonicotinoids，如clothianidin，吡虫啉，和thiacloprid；二乙基溴乙酰胺钠通道堵塞剂(neuronal sodium channelblockers)，如噁二唑虫；杀虫大环内酯类，如艾克敌105，齐墩螨素(abamectin)，齐墩螨素(avermectin)，和emamectin；γ-氨基丁酸(GABA)对抗剂(antagonists)，如硫丹，ethiprole，和锐劲特；杀虫剂尿素，如氟虫脲和杀虫隆；保幼激素，如噁茂醚和蚊蝇醚；拒嗪酮；以及虫螨脒。用于与本发明的化合物混合的优选优选生物试剂包括苏云金芽孢杆菌和苏云金芽孢杆菌δ-内毒素，以及天然存在的和遗传改良的病毒杀虫剂，包括杆状病毒目(baculoviridae)的成员以及食昆虫的真菌。Preferred insecticides and acaricides for use in admixture with the compounds of the present invention include: synthetic pyrethrins such as cypermethrin, (RS) cyhalothrin, cyfluthrin, beta-cyfluthrin, esfenvalerate, Memetrin and perbromethrin; carbamates, such as fenothicarb, methoxam, methotrexate, and thiodicarb; neonicotinoids, such as clothianidin, imidacloprid, and thiacloprid; diethylbromoacetamide Neuronal sodium channel blockers, such as oxadiazole; insecticidal macrolides, such as Acetyl 105, abamectin, avermectin, and emamectin; gamma - GABA antagonists, such as endosulfan, ethiprole, and fipronil; insecticides urea, such as flufenuron and triflumeron; juvenile hormones, such as oxolofen and pyriproxyfen ; azinazinone; and acarid. Preferred preferred biological agents for use in admixture with the compounds of the invention include Bacillus thuringiensis and Bacillus thuringiensis delta-endotoxin, as well as naturally occurring and genetically modified viral insecticides, including members of the baculoviridae order and Insect-eating fungi.

最优选的混合物包括：本发明的化合物与(RS)氯氟氰菊酯的混合物；本发明的化合物与氟氯氰菊酯的混合物；本发明的化合物与β-氟氯氰菊酯的混合物；本发明的化合物与高氰戊菊酯的混合物；本发明的化合物与灭多虫的混合物；本发明的化合物与吡虫啉的混合物；本发明的化合物与thiacloprid的混合物；本发明的化合物与噁二唑虫的混合物；本发明的化合物与齐墩螨素(abamectin)的混合物；本发明的化合物与硫丹的混合物；本发明的化合物与ethiprole的混合物；本发明的化合物与锐劲特的混合物；本发明的化合物与氟虫脲的混合物；本发明的化合物与蚊蝇醚的混合物；本发明的化合物与拒嗪酮的混合物；本发明的化合物与虫螨脒的混合物；本发明的化合物与苏云金芽孢杆菌的混合物；以及本发明的化合物与苏云金芽孢杆菌δ-内毒素的混合物。The most preferred mixtures include: mixtures of compounds of the invention and (RS) cyfluthrin; mixtures of compounds of the invention and cyfluthrin; mixtures of compounds of the invention and β-cyfluthrin; compounds of the invention and high The mixture of fenvalerate; the mixture of the compound of the present invention and methedox; the mixture of the compound of the present invention and imidacloprid; the mixture of the compound of the present invention and thiacloprid; the mixture of the compound of the present invention and oxadiazole; The mixture of the compound of the present invention and abamectin (abamectin); the mixture of the compound of the present invention and endosulfan; the mixture of the compound of the present invention and ethiprole; the mixture of the compound of the present invention and fipronil; A mixture of urea; a mixture of a compound of the present invention and pyriproxyfen; a mixture of a compound of the present invention and azinone; a mixture of a compound of the present invention and acarid; a mixture of a compound of the present invention and Bacillus thuringiensis; Mixture of inventive compound with Bacillus thuringiensis delta-endotoxin.

在某些情况下，与具有相似防治范围但不同作用方式的其它无脊椎害虫防治化合物或试剂的结合对于抗力控制(resistance management)是特别有利的。因此，本发明的组合物可进一步包含生物有效量的至少一种附加的具有相似防治范围但不同作用方式的无脊椎害虫防治化合物或试剂。使遗传改良以表达植物防护化合物(例如蛋白质)的植物或该植物的处所与生物有效量的本发明化合物相接触，也可提供更广的植物防护范围，并对于抗力控制是特别有利的。Combinations with other invertebrate pest control compounds or agents having a similar range of control but a different mode of action are particularly advantageous for resistance management in certain instances. Accordingly, the compositions of the present invention may further comprise a biologically effective amount of at least one additional invertebrate pest control compound or agent having a similar control spectrum but a different mode of action. Contacting plants genetically modified to express plant protection compounds (eg proteins), or the locus of such plants, with biologically effective amounts of the compounds of the invention also provides a broader range of plant protection and is particularly advantageous for resistance control.

通过向害虫的环境(包括害虫出现的农业和/或非农业处所)、向需防护的区域、或直接向需要防治的害虫以生物有效量施用一种或多种本发明的化合物，无脊椎害虫可被防治，并实现对农作物、园艺作物和特殊作物、以及动物和人类健康的保护。因此，本发明进一步包括一种防治叶居和土居无脊椎害虫及保护农业和/或非农业作物的方法，包括使无脊椎害虫或其环境与生物有效量的一种或多种本发明的化合物接触，或与含至少一种所述化合物的组合物或含至少一种所述化合物和至少一种附加生物活性化合物或试剂的组合物接触。优选的接触方法是通过喷洒。或者，可向植物叶或土壤施用含本发明化合物的颗粒状组合物。通过由植物与含本发明化合物的组合物接触而引起的植物吸收，本发明的化合物得以有效释放，所述组合物是作为液体配制剂的土壤浸润、用于土壤的颗粒制剂、保育箱处理或移植浸渍而施用的。其它接触方法包括通过直接或滞留性喷雾、航空喷洒、种皮、微胶囊、系统吸收、饵诱、耳标(eartags)、大丸药、喷雾器、熏蒸剂、气溶胶、粉尘和许多其它方法而施用本发明的化合物或组合物。By applying one or more compounds of the present invention in a biologically effective amount to the pest's environment (including agricultural and/or non-agricultural places where the pest occurs), to the area to be protected, or directly to the pest in need of control, invertebrate pests Can be controlled and achieve the protection of crops, horticultural crops and special crops, as well as animal and human health. Therefore, the present invention further includes a method of controlling foliar and soil-dwelling invertebrate pests and protecting agricultural and/or non-agricultural crops, comprising administering an effective amount of one or more compounds of the present invention to the invertebrate pest or its environment and biologically effective amount. Contacting, or contacting with a composition comprising at least one such compound or a composition comprising at least one such compound and at least one additional biologically active compound or agent. The preferred method of contact is by spraying. Alternatively, granular compositions containing a compound of the invention may be applied to plant foliage or to the soil. The compounds of the invention are effectively released by plant uptake caused by contact of the plants with a composition containing the compounds of the invention, either as a soil drench as a liquid formulation, a granular formulation for soil, an incubator treatment or Applied for transplant dipping. Other contact methods include application by direct or persistent sprays, aerial sprays, seed coats, microcapsules, systemic absorption, baits, eartags, boluses, nebulizers, fumigants, aerosols, dusts, and many others A compound or composition of the invention.

可将本发明的组合物掺入无脊椎害虫食用的诱饵，或掺入装置如捕集器等中。颗粒或诱饵含有0.01-5％的活性成分、0.05-10％的含试剂(一种或多种)的水份以及40-99％的植物粉，能以很低的施用率有效地防治土壤害虫，特别是对于通过摄食而非直接接触而致命的活性成分剂量而言。The compositions of the present invention may be incorporated into baits eaten by invertebrate pests, or incorporated into devices such as traps and the like. Granules or baits contain 0.01-5% active ingredients, 0.05-10% water containing reagents (one or more) and 40-99% plant powder, which can effectively control soil pests at a very low application rate , especially for doses of the active ingredient that are lethal through ingestion rather than direct contact.

本发明的化合物可以以其纯净态施用，但更为经常施用的是一种配制剂，其含有合适的载体、稀释剂和表面活性剂，且根据所考虑的终用途可能与食物结合。优选的施用方法涉及所述化合物的水分散体或精制油溶液。与喷淋油、喷淋油浓缩物、粘展剂、辅料、其它溶剂以及增效剂如增效醚结合通常增强化合物的效力。The compounds of the invention may be administered in their pure form, but more frequently will be administered as a formulation containing suitable carriers, diluents and surfactants, possibly in combination with food depending on the end use contemplated. Preferred methods of application involve aqueous dispersions or refined oil solutions of the compounds. Combination with spray oils, spray oil concentrates, spreaders, adjuvants, other solvents, and synergists such as butanobuterol generally enhances the efficacy of the compounds.

有效防治所需的施用率(即“生物有效量”)将取决于诸如下列因素：需防治的无脊椎害虫的种类，害虫的生活周期，生活期，害虫的大小，季节，宿主作物或动物，摄食习性，周围环境湿度，稳定，等。在一般情况下，每公顷约0.01-2kg活性成分的施用率足以防治农业生态系统中的害虫，但少至0.0001千克/公顷可以足够，而也可以需要多达8千克/公顷。对于非农用，有效用量范围约为1.0-50mg/m2，但少至0.1mg/m2可以足够，而也可以需要多达150mg/m2。本领域的技术人员可容易地确定所期望程度的无脊椎害虫防治所必需的生物有效量。The rate of application required for effective control (i.e. "biologically effective amount") will depend on factors such as: the species of invertebrate pest to be controlled, the pest life cycle, life period, pest size, season, host crop or animal, Feeding habits, ambient humidity, stability, etc. In general, application rates of about 0.01-2 kg active ingredient per hectare are sufficient to control pests in agroecosystems, but as little as 0.0001 kg/ha may be sufficient, while as much as 8 kg/ha may be required. For non-agricultural use, effective amounts range from about 1.0-50 mg/ m2 , but as little as 0.1 mg/ m2 may be sufficient, while as much as 150 mg/ m2 may be required. Those skilled in the art can readily determine the biologically effective amount necessary for the desired degree of invertebrate pest control.

下列本发明的生物实施例中的试验说明了本发明化合物对于特定害虫的防治效力。“防治效力”表示阻止引起大量降低供给的节肢动物的发育。然而，所述化合物提供的害虫防治保护作用并不局限于这些种类。对于化合物的描述，参见索引表A-E。在下列索引表中使用了以下缩写：t为叔，n为正，i为异，s为仲，Me为甲基，Et为乙基，Pr为丙基，Br为丁基；相应地，i-Pr为异丙基，s-Bu为仲丁基，等等，Ac为COCH3。缩写“Ex.”代表“实施例”，其后的数字表明所述化合物是在那个实施例中制备的。The tests in the following biological examples of the invention demonstrate the control efficacy of the compounds of the invention against specific pests. "Control efficacy" means arresting the development of arthropods causing a substantial reduction in supply. However, the pest control protection afforded by the compounds is not limited to these species. For compound descriptions, see Index Tables AE. The following abbreviations are used in the following index tables: t for tertiary, n for positive, i for iso, s for secondary, Me for methyl, Et for ethyl, Pr for propyl, Br for butyl; correspondingly, i -Pr is isopropyl, s-Bu is sec-butyl, etc., Ac is COCH3 . The abbreviation "Ex." stands for "Example", followed by a number indicating that the compound was prepared in that Example.

                          索引表A

Figure A0180519001071
化合物    R2     R3     R4    m          R5         熔点℃(Ex.1)    Me      H       H       2      2-Me-4-F         2492      i-Pr    H       H       2      2-Me-4-Cl        ＞2503      n-Pr    H       H       2      2-Me-4-Cl        212 4     i-Bu   H    H    2    2-Me-4-Cl      ***5     Me     Me   H    2    2-Me-4-Cl      ***6     Et     H    H    2    2-Me-4-Cl      ***7     Me     H    H    2    2-Me-4-Cl      2448    allyl   H    H    2    2，4-di-Me     2439    环-Pr   H    H    2    2-Me-4-Cl      24610    H      H    H    2    2-Me-4-Cl      ***11    Me     H    H    2    2-Me-4-OCF3   ＞25012    Me     H    H    1    4-OCF3        ＞25013    Me     H    H    2    2，4-di-Cl     ＞25014    Me     H    H    2    2-Me-5-Cl      24115    Me     H    H    2    2-Me-3-Cl      ＞25016    Me     H    H    1    2-Me           23617    Me     H    H    2    2-Me-4-Br      23418    Me     H    H    1    4-i-Pr         ＞25019    Me     H    H    1    4-NHAc         22420    Me     H    H    1    2-Br           21021    Me     H    H    1    2-OPh          19322    Me     H    H    1    4-OMe          18823    Me     H    H    1    4-(吗啉-4-基)  24624    Me     H    H    1    2-F            17725    Me     H    H    1    4-I            23526    Me     H    H    2    2-Me-4-NO2    24227    Me     H    H    1    3-CF3         23528    Me     H    H    1    3-I            21629    Me     H    H    2    2-Me-4-OMe     20530    Me     H    H    1    3-Br           23031    Me     H    H    1    4-Ac           22632    Me     H    H    1    4-Br           22033    Me     H    H    1    4-CN           21634    Me     H    H    1    3-NO2         24235    Me     H    H    1    4-Cl           19736    Me     H    H    1    3-CH3         22037    Me     H    H    1    3-Cl           20938    Me     H    H    2    2，5-di-Me     20439    Me     H    H    2    2-Me-6-OMe     22340    Me     H    H2   2    2，3-di-Me     18741    Me     H    H    1    2-OMe          192 42    Me   H     H         1    4-CO2Et                 20243    Me   H     H         1    4-NMeAc                  21044    Me   H     H         2    2，6-di-Me               ＞25045    Me   H     H         1    2-(吡咯-1-基)            20846    Me   H     H         1    4-NO2                   22447    Me   H     H         1    3-OCH2Ph                21448    Me   H     H         2    2，4-di-Me               21349    Me   H     H         1    3-CN                     20050    Me   H     H         1    3-OCF3                  ＞25051    Me   H     H         2    2-Me-3-NO2              23352    Me   H     H         1    2-OEt                    22453    Me   H     H         1    4-(4-ClPhO)              22454    Me   H     H         1    4-CH3                   24855    Me   H     H         1    4-O-i-Pr                 18356    Me   H     H         1    4-F                      24757    Me   H     H         1    2-SMe                    20458    Me   H     H         1    2-t-Bu                   24859    Me   H     H         1    3-SMe                    21860    Me   H     H         1    4-OEt                    19561    Me   H     H         1    2-CH2CN                 19162    Me   H     H         1    2-Et                     20063    i-Pr H     4-NO2/    2    2-Me-4-Cl                *** index table A
Figure A0180519001071
Compound R 2 R 3 R 4 m R 5 melting point ℃ (Ex.1) Me H H 2 2-Me-4-F 2492 i-Pr H H 2 2-Me-4-Cl >2503 n-Pr H H 2 2-Me -4-Cl 212 4 i-Bu H H 2 2-Me-4-Cl ***5 Me Me H 2 2-Me-4-Cl ***6 Et H H 2 2-Me-4-Cl *** 7 Me H H 2 2-Me-4-Cl 2448 allyl H H 2 2,4-di-Me 2439 Cyclo-Pr H H 2 2-Me-4-Cl 24610 H H H 2 2-Me-4-Cl ***11 Me H H 2 2-Me-4-OCF 3 >25012 Me H H 1 4-OCF 3 >25013 Me H H 2 2,4-di-Cl >25014 Me H H 2 2-Me-5-Cl 24115 Me H H 2 2-Me -3-Cl >25016 Me H H 1 2-Me 23617 Me H H 2 2-Me-4-Br 23418 Me H H 1 4-i-Pr >25019 Me H H 1 4-NHAc 22420 Me H H 1 2-Br 21021 Me H H 1 2-OPh 19322 Me H H 1 4-OMe 18823 Me H H 1 4-(morpholin-4-yl) 24624 Me H H 1 2-F 17725 Me H H 1 4-I 23526 Me H H 2 2-Me-4-NO 2 24227 Me H H 1 3-CF 3 23528 Me H H 1 3-I 21629 Me H H 2 2-Me-4-OMe 20530 Me H H 1 3-Br 23031 Me H H 1 4-Ac 22632 Me H H 1 4-Br 22033 Me H H 1 4-CN 21634 Me H H 1 3-NO 2 24235 Me H H 1 4-Cl 19736 Me H H 1 3-CH 3 22037 Me H H 1 3-Cl 20938 Me H H 2 2,5-di-Me 20439 Me H H 2 2-Me-6-OMe 22340 Me H H2 2 2,3-di-Me 18741 Me H H 1 2-OMe 192 42 Me H H 1 4-CO 2 Et 20243 Me H H 1 4-NMeAc 21044 Me H H 2 2,6 -di-Me >25045 Me H H 1 2-(pyrrol-1-yl) 20846 Me H H 1 4-NO 2 22447 Me H H 1 3-OCH 2 Ph 21448 Me H H 2 2,4-di-Me 21349 Me H H 1 3-CN 20050 Me H H 1 3-OCF 3 >25051 Me H H 2 2-Me-3-NO 2 23352 Me H H 1 2-OEt 22453 Me H H 1 4-(4-ClPhO) 22454 Me H H 1 4-CH 3 24855 Me H H 1 4-Oi-Pr 18356 Me H H 1 4-F 24757 Me H H 1 2-SMe 20458 Me H H 1 2-t-Bu 24859 Me H H 1 3-SMe 21860 Me H H 1 4-OEt 19561 Me H H 1 2-CH 2 CN 19162 Me H H 1 2-Et 20063 i-Pr H 4-NO2/ 2 2-Me-4-Cl ***

              5-NO25-NO2

             (1/1混合)64    Me   H     4-Br/     2    2-Me-4-Cl                ***(1/1 mix) 64 Me H 4-Br/ 2 2-Me-4-Cl ***

              5-Br5-Br

             (1/1混合)65    Me   H     H         1    2-CONH(i-Pr)-6-Me        24866*  Me   H     H         2    2-Me-4-Cl                ***67*  Me   H     H         2    2-Me-4-OCF3             ***68    Me   H     H         2    2-Me-5-NO2              24269    Me   H     H         2    2-Me-4-CF3              25070    Me   H     H         1    4-CF3                   24671    Me   H     H         1    2-Ph                     16372    Me   H     H         2    2-(1-Me-四唑-5-基)-6-Me  20273    Me   H     H         1    2-CONHMe                 23574    Me   H     H         2    2-Me-6-Cl                23175    Me   H     H         2    3-NO2-4-Me              22376    Me    H    H    3    2-F-4-Cl-5-NO2    25077    Me    H    H    2    2-Br-4-Me          19878    Me    H    H    3    2-Br-4，6-di-F     19779    Me    H    H    2    2，5-di-NO2       22380    Me    H    H    2    2-F-4-Cl           25081    Me    H    H    2    2-Me-3-F           24282    Me    H    H    2    2-Br-4-F           126.583    Me    H    H    1    2-(吗啉-4-基)      19384    Me    H    H    2    3-NO2-4-F         24885    Me    H    H    2    3，4-di-F          11086    Me    H    H    2    2-Cl-4-F           25087    Me    H    H    1    2-CF3             21788    Me    H    H    2    2-CN-4-Cl          25089    Me    H    H    1    2-Ac               23790    Me    H    H    1    2-OCF3            20991    Me    H    H    1    2-SCF3            21192    Me    H    H    2    2-CF3-4-Br        250*该试样含25重量％的1，8-萘二甲酸酐***参见索引表E的NMR数据(1/1 mix) 65 Me H H 1 2-CONH(i-Pr)-6-Me 24866 * Me H H 2 2-Me-4-Cl ***67 * Me H H 2 2-Me-4-OCF 3 ***68 Me H H 2 2-Me-5-NO 2 24269 Me H H 2 2-Me-4-CF 3 25070 Me H H 1 4-CF 3 24671 Me H H 1 2-Ph 16372 Me H H 2 2-(1 -Me-tetrazol-5-yl)-6-Me 20273 Me H H 1 2-CONHMe 23574 Me H H 2 2-Me-6-Cl 23175 Me H H 2 3-NO 2 -4-Me 22376 Me H H 3 2- F-4-Cl-5-NO 2 25077 Me H H 2 2-Br-4-Me 19878 Me H H 3 2-Br-4,6-di-F 19779 Me H H 2 2,5-di-NO 2 22380 Me H H 2 2-F-4-Cl 25081 Me H H 2 2-Me-3-F 24282 Me H H 2 2-Br-4-F 126.583 Me H H 1 2-(morpholin-4-yl) 19384 Me H H 2 3 -NO 2 -4-F 24885 Me H H 2 3,4-di-F 11086 Me H H 2 2-Cl-4-F 25087 Me H H 1 2-CF 3 21788 Me H H 2 2-CN-4-Cl 25089 Me H H 1 2-Ac 23790 Me H H 1 2-OCF 3 20991 Me H H 1 2-SCF 3 21192 Me H H 2 2-CF 3 -4-Br 250 * This sample contains 25% by weight of 1,8-naphthylene Anhydrides*** See Index Table E for NMR data

                    索引表B

Figure A0180519001101
化合物     R2     R3     R4       J       熔点℃93        Me      H        H   199化合物     R2   R3   R4        J        熔点℃94        Me    H     H 
Figure A0180519001111
  17595        Me    H     H 
Figure A0180519001112
   126.596        Me    H     H        21797        Me    H     H 
Figure A0180519001114
  171 index table B
Figure A0180519001101
Compound R 2 R 3 R 4 J Melting point ℃ 93 Me H H Compound 199 R 2 R 3 R 4 J Melting point ℃ 94 Me H H
Figure A0180519001111
17595 Me H H
Figure A0180519001112
126.596 Me H H 21797 Me H H
Figure A0180519001114
171

                      索引表C

Figure A0180519001115
化合物      R2     R3   R4   m       R5       熔点℃98(Ex.2)    i-Pr     H      H     2    3，4-di-F      22799        i-Pr     H      H     2    2，3-di-Me     242100       i-Pr     H      H     2    2，4-di-F      204101       i-Pr     H      H     1    4-OCF3        186102       i-pr     H      H     1    4-Cl           218103       i-Pr     H      H     1    4-Et           206104    i-Pr      H    H        1    4-CF3          165105    Me        H    H        2    3，4-di-F       250106    Me        H    H        2    2，3-di-Me      184.5107    Me        H    H        2    2，4-di-F       207108    Me        H    H        1    4-Cl            250109    Me        H    H        1    4-Et            250110    Me        H    H        1    4-CF3          208111    Me        H    H        1    4-OCF3         144112    Me        H    H        1    2-Me            173.5113    i-pr      H    H        1    2-Me            176.5114    i-Pr      H    H        2    2-Me-4-O-CF3   173.5115    i-Pr      H    H        2    2-Me-4-CF3     194.5116    Me        H    H        2    2-Me-4-OCF3    173.5117    Me        H    H        2    2-Me-4-CF3     204.5 index table C
Figure A0180519001115
Compound R 2 R 3 R 4 m R 5 melting point ℃ 98 (Ex.2) i-Pr H H 2 3,4-di-F 22799 i-Pr H H 2 2,3-di-Me 242100 i-Pr H H 2 2 , 4-di-F 204101 i-Pr H H 1 4-OCF 3 186102 i-pr H H 1 4-Cl 218103 i-Pr H H 1 4-Et 206104 i-Pr H H 1 4-CF 3 165105 Me H H 2 3, 4-di-F 250106 Me H H 2 2,3-di-Me 184.5107 Me H H 2 2,4-di-F 207108 Me H H 1 4-Cl 250109 Me H H 1 4-Et 250110 Me H H 1 4-CF 3 208111 Me H H 1 4-OCF 3 144112 Me H H 1 2-Me 173.5113 i-pr H H 1 2-Me 176.5114 i-Pr H H 2 2-Me-4-O-CF 3 173.5115 i-Pr H H 2 2-Me-4 -CF 3 194.5116 Me H H 2 2-Me-4-OCF 3 173.5117 Me H H 2 2-Me-4-CF 3 204.5

                           索引表D

Figure A0180519001121
化合物       R2      R3       R4        J            熔点℃118       i-Pr      H          H        1-萘基           210119       i-Pr      H          H        2-噻吩基         208120(Ex.3)    Me        H          H        2-噻吩基         215121       Me        H          H        1-萘基           214121       i-Pr      H          H      210123       Me        H          H 
Figure A0180519001123
    210124           Me          H            H 
Figure A0180519001131
 215.5125           i-Pr        H            H 
Figure A0180519001132
 186 index table D
Figure A0180519001121
Compound R 2 R 3 R 4 J Melting point °C118 i-Pr H H 1-naphthyl 210119 i-Pr H H 2-thienyl 208120(Ex.3) Me H H 2-thienyl 215121 Me H H 1-naphthyl 214121 i- Pr H H 210123 Me H H
Figure A0180519001123
210124 Me H H
Figure A0180519001131
215.5125 i-Pr H H
Figure A0180519001132
186

                     索引表E  化合物号   1 H NMR数据(为CDCl 3 溶液，除非另作说明) a Index Table E Compound No. 1 H NMR Data (as CDCl 3 solution unless otherwise stated) a

4         (DMSO-d6)δ：0.9(m，6H)，2.37(s，3H)，3.01(m 1H)，3.96(d，2H)、7.27-8.48(m，10H)，4 (DMSO-d6)δ: 0.9(m, 6H), 2.37(s, 3H), 3.01(m 1H), 3.96(d, 2H), 7.27-8.48(m, 10H),

          9.84(br s，1H).9.84(br s, 1H).

5         (DMSO-d6)δ：2.36(s，3H)，2.88(s，3H)，2.94(s，3H)，7.28-8.08(m，10H)，9.99(s，1H).5 (DMSO-d6)δ: 2.36(s, 3H), 2.88(s, 3H), 2.94(s, 3H), 7.28-8.08(m, 10H), 9.99(s, 1H).

          (DMSO-d6)δ：1.07(t，3H)，2.37(s，3H)，3.22(m，2H)，7.30-8.06(m，9H)，8,40 (t，1H)，(DMSO-d6)δ: 1.07(t, 3H), 2.37(s, 3H), 3.22(m, 2H), 7.30-8.06(m, 9H), 8,40(t, 1H),

          9.86(s，1H).9.86(s, 1H).

10        (DMSO-d6)δ：2.36(s，3H)，7.25-8.08(m，11H)，9.88(s，1H)，10 (DMSO-d6)δ: 2.36(s, 3H), 7.25-8.08(m, 11H), 9.88(s, 1H),

63        (DMSO-d6)δ：1.09(d，6H)，2.36(s，3H)，4.03(m，1H)，7.27-8.52(m，9H)，10.04(s，1H).63 (DMSO-d6)δ: 1.09(d, 6H), 2.36(s, 3H), 4.03(m, 1H), 7.27-8.52(m, 9H), 10.04(s, 1H).

64        (DMSO-d6)δ：2.36(s，3H)，2.69(d，3H)，7.33-8,84(r，8H)，8.45(br q，1H)，9,98(s，1H)，64 (DMSO-d6)δ: 2.36(s, 3H), 2.69(d, 3H), 7.33-8,84(r, 8H), 8.45(br q, 1H), 9,98(s, 1H),

66        (DMSO-d6)δ：2.37(s，3H)，2.71(d，3H)，7.27-8.10(m，9H)，8,34(br q，1H)，9.88(s，1H).66 (DMSO-d6)δ: 2.37(s, 3H), 2.71(d, 3H), 7.27-8.10(m, 9H), 8,34(br q, 1H), 9.88(s, 1H).

67        (DMSO-d6)δ：2.41(s、3H)，2.72(d，3H)，7.26-8.08(m，9H)，8,36(br q，1H)，9,95(s，1H).a 1H NMR数据单位为ppm，四甲基硅烷低磁场。耦合标记为：(s)为单一态，(d)为双重态，(t)为三重态，(q)为四重态，(m)为多重态，(dd)为双重态的双重态，(dt)为三重态的双重态，(br s)为宽单一态，(bs q)为宽四重态。67 (DMSO-d6) δ: 2.41 (s, 3H), 2.72 (d, 3H), 7.26-8.08 (m, 9H), 8,36 (br q, 1H), 9,95 (s, 1H). a 1 H NMR data in ppm, tetramethylsilane downfield. Couplings are marked: (s) for singlets, (d) for doublets, (t) for triplets, (q) for quartets, (m) for multiplets, (dd) for doublets of doublets, (dt) is a triplet doublet, (br s) is a wide singlet, and (bs q) is a wide quartet.

                     本发明的生物实施例 Biological Examples of the Invention

                           试验A Test A

为了评估对草地粘虫(Spodoptera frugiperda)的防治，试验装置由小开口容器组成，其中装有已放置4-5天的玉米植物。已用10-15条1天龄的幼虫对该玉米预先进行了害虫感染，幼虫是在一片害虫饵料上，用取样器从有许多幼虫在其上生长的硬化了的害虫饵料片上移取一小块试样，然后将该含幼虫和饵料的试样转移到试验装置中。作为饵料试样而移到试验设备上的幼虫将变干。To evaluate control of the grass armyworm (Spodoptera frugiperda), the test unit consisted of small open containers containing maize plants that had been standing for 4-5 days. The corn had been pre-infested with 10-15 1-day-old larvae on a piece of pest bait, and a small sampler was taken from the hardened piece of pest bait on which many larvae had grown. Block the sample and transfer the sample containing larvae and bait to the test unit. Larvae transferred to the test equipment as bait samples will dry out.

除非另作说明，用含下列物质的溶液配制试验化合物：10％的丙酮，90％的水和300ppm的X-77_Spreader Lo-Foam Formula非离子型表面活性剂，该表面活性剂含有烷基芳基聚氧乙烯、游离脂肪酸、二醇和异丙醇(Loveland Industries，Inc.)。通过SUJ2雾化喷嘴施用1ml的所述配制化合物液体，该雾化喷嘴位于各试验装置上方1.27cm(0.5英寸)处，带有1/8 JJ定制的箱体(Spraying System Co.)。在这一屏蔽中的所有实验化合物均以250ppm喷洒，并重复喷洒3次。在喷洒所述配制的试验化合物后，使各试验装置干燥1小时，然后在顶上加盖黑色遮蔽盖。在25℃、70％相对湿度的成长室中将试验装置放置6天。然后目测植物摄食损坏度。Unless otherwise stated, test compounds were prepared in solutions containing: 10% acetone, 90% water and 300 ppm of X-77_Spreader Lo-Foam Formula nonionic surfactant containing alkylaryl Polyoxyethylene, free fatty acid, glycol, and isopropanol (Loveland Industries, Inc.). 1 ml of the formulated compound liquid was applied through a SUJ2 atomizing nozzle positioned 1.27 cm (0.5 inches) above each test unit with a 1/8 JJ custom-made box (Spraying System Co.). All test compounds in this screen were sprayed at 250 ppm and the sprays were repeated 3 times. After spraying the formulated test compound, each test device was allowed to dry for 1 hour and then covered with a black masking cap. The test units were placed in a growth chamber at 25°C and 70% relative humidity for 6 days. Plant feeding damage was then assessed visually.

在所试验的化合物中，下列通过了极佳的植物防护程度(10％或更低的摄食损坏)：1、7、11、16、48、66和67。Of the compounds tested, the following passed an excellent degree of plant protection (10% or less damage from feeding): 1, 7, 11, 16, 48, 66 and 67.

                       试验B Test B

为了评估对烟草夜蛾幼虫(Heliothis virescens)的防治，试验装置由小开口容器组成，其中装有已放置6-7天的棉花植物。已用8条2天龄的幼虫对该棉花预先进行了害虫感染，幼虫是在一片害虫饵料上，使用了如试验A所述的取样器。To evaluate control of tobacco armyworm larvae (Heliothis virescens), the test unit consisted of small open containers containing cotton plants that had been left standing for 6-7 days. The cotton had been pre-infested with eight 2-day-old larvae on a patch of pest bait using a sampler as described in Test A.

试验化合物的配制和以250ppm进行喷洒均如试验A所述。重复喷洒3次。喷洒后，将试验装置放置在成长室中，然后如试验A所述进行目测评定。The test compound was formulated and sprayed at 250 ppm as described in Test A. Repeat spraying 3 times. After spraying, the test units were placed in the growth chamber and then visually assessed as described for Test A.

在所试验的化合物中，下列通过了极佳的植物防护程度(10％或更低的摄食损坏)：1、7和16。Of the compounds tested, the following passed an excellent degree of plant protection (10% or less damage from feeding): 1, 7 and 16.

                       试验C Test C

为了评估对菱纹背蛾(Plutella xylostella)的防治，试验装置由小开口容器组成，其中装有已放置12-14天的萝卜植物。已用10-15条新生幼虫对该萝卜预先进行了害虫感染，幼虫是在一片害虫饵料上，使用了如试验A所述的取样器。To evaluate control of diamondback moth (Plutella xylostella), the test unit consisted of small open containers containing radish plants that had been left for 12-14 days. The radishes had been pre-infested with 10-15 newborn larvae on a patch of pest bait using a sampler as described in Test A.

试验化合物的配制和以250ppm进行喷洒均如试验A所述。重复喷洒3次。喷洒后，将试验装置放置在成长室中，然后如试验A所述进行目测评定。The test compound was formulated and sprayed at 250 ppm as described in Test A. Repeat spraying 3 times. After spraying, the test units were placed in the growth chamber and then visually assessed as described for Test A.

在所试验的化合物中，下列通过了极佳的植物防护程度(10％或更低的摄食损坏)：1、7、11、12、14、16、20、24、37、48、51、54、55、56、61、66、67、69、70、72、75、81、85、86、89、90、91、93和97。Of the compounds tested, the following passed an excellent degree of plant protection (10% or less damage from feeding): 1, 7, 11, 12, 14, 16, 20, 24, 37, 48, 51, 54 , 55, 56, 61, 66, 67, 69, 70, 72, 75, 81, 85, 86, 89, 90, 91, 93 and 97.

                       试验D Test D

为了评估对甜菜黏虫(Spodoptera exigua)的防治，试验装置由小开口容器组成，其中装有已放置4-5天的玉米植物。已用10-15条1天龄的幼虫对该玉米预先进行了害虫感染，幼虫是在一片害虫饵料上，使用了如试验A所述的取样器。To evaluate control of the sugar beet armyworm (Spodoptera exigua), the test unit consisted of small open containers containing maize plants that had been standing for 4-5 days. The corn had been pre-infested with 10-15 1-day-old larvae on a patch of pest bait using a sampler as described in Test A.

试验化合物的配制和以250ppm进行喷洒均如试验A所述。重复喷洒3次。喷洒后，将试验装置放置在成长室中，然后如试验A所述进行目测评定。The test compound was formulated and sprayed at 250 ppm as described in Test A. Repeat spraying 3 times. After spraying, the test units were placed in the growth chamber and then visually assessed as described for Test A.

在所试验的化合物中，下列通过了极佳的植物防护程度(10％或更低的摄食损坏)：1、40和54。Of the compounds tested, the following passed an excellent degree of plant protection (10% or less damage from feeding): 1, 40 and 54.

Claims (17)

1.选自下列式I或式II的化合物及其N-氧化物和农业适用盐：其中每一J独立地是苯基环、萘基环体系、5或6元杂芳环或芳香8、9或10元杂双环稠环体系，其中，每一环或环体系任选地是用1-5个R5取代的；A和B独立地是O或S；n为0-4；R1是H：或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基和C3-C6环烷基氨基；或者R1是C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基或C3-C8二烷基氨基羰基；R2是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C4烷氧基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷氧基羰基或C2-C6烷基羰基；R3是H；或C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、NO2、羟基、C1-C4烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基和C1-C4烷基磺酰基；或者R2和R3可通过与它们相连的氮而在一起形成环，该环含2-6个碳原子并任选地含有一个另外的氮、硫或氧原子，该环可任选地被选自C1-C2烷基、卤素、CN、NO2和C1-C2烷氧基的1-4个取代基取代；和每一R4和每一R5独立地是H、C1-C6烷基、C2-C6链烯基、C2-C6炔基、C3-C6环烷基、C1-C6卤代烷基、C2-C6卤代链烯基、C2-C6卤代炔基、C3-C6卤代环烷基、卤素、CN、CO2H、CONH2、NO2、羟基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基、C2-C4烷氧基羰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C2-C6烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基、或C3-C6三烷基甲硅烷基；或者每一R4和每一R5独立地是苯基、苄基、苯氧基、5或6元杂芳环或芳香8、9或10元杂双环稠环体系，每一环任选地为1或3个独立地选自下列的取代基取代：C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C2-C4卤代链烯基、C2-C4卤代炔基、C3-C6卤代环烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C3-C6(烷基)环烷基氨基、C2-C4烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基、或C3-C6三烷基甲硅烷基；或者(R5)2当连在相邻碳原子上时可以合在一起成为-OCF2O-、-CF2CF2O-或-OCF2CF2O-。1. Compounds selected from the following formula I or formula II and their N-oxides and agriculturally applicable salts: wherein each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring, or an aromatic 8-, 9-, or 10-membered heterobicyclic fused ring system, wherein each ring or ring system is optionally 1-5 R 5 substituted; A and B are independently O or S; n is 0-4; R 1 is H: or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, each optionally substituted by one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino and C 3 -C 6 cycloalkylamino; or R 1 is C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkyl Aminocarbonyl or C 3 -C 8 dialkylaminocarbonyl; R 2 is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 ring Alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkoxycarbonyl or C 2 -C 6 alkylcarbonyl; R 3 is H; or C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, Each is optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO 2 , hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 Alkylsulfinyl and C 1 -C 4 alkylsulfonyl; or R 2 and R 3 may be joined together through the nitrogen attached to them to form a ring containing 2 to 6 carbon atoms and optionally containing a Another nitrogen, sulfur or oxygen atom, the ring may be optionally substituted by 1-4 substituents selected from C 1 -C 2 alkyl, halogen, CN, NO 2 and C 1 -C 2 alkoxy; and each R 4 and each R 5 is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 6 haloalkenyl, C 2 -C 6 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, CO 2 H, CONH 2 , NO 2 , hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkane Sulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl, C 2 -C 4 alkoxycarbonyl, C 1 -C 4 Alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino, C 2 -C 6 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkyl Aminocarbonyl, C 3 -C 8 dialkylaminocarbonyl, or C 3 -C 6 trialkylsilyl; or each R 4 and each R 5 are independently phenyl, benzyl, phenoxy, 5 or 6-membered heteroaryl ring or aromatic 8-, 9- or 10-membered heterobicyclic condensed ring system, each ring is optionally substituted by 1 or 3 substituents independently selected from the following: C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 2 -C 4 haloalkenyl, C 2 -C 4 Haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio , C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 -C 6 cycloalkylamino , C 3 -C 6 (alkyl)cycloalkylamino, C 2 -C 4 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylaminocarbonyl, C 3 -C 8 di Alkylaminocarbonyl, or C 3 -C 6 trialkylsilyl; or (R 5 ) 2 can be combined into -OCF 2 O-, -CF 2 CF 2 O when connected to adjacent carbon atoms -or - OCF2CF2O- . 2.权利要求1的式I化合物，其中A和B均为0；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和n为0-2。2. The formula I compound of claim 1, wherein A and B are 0; R is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and n is 0-2. 3.权利要求1的式II化合物，其中A和B均为0；R1是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；和n为0-2。3. The compound of formula II according to claim 1, wherein A and B are 0; R is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; and n is 0-2. 4.权利要求2或3的化合物，其中J是苯基环或选自如下J-1、J-2、J-3和J-4的5元或6元杂芳环，每一J环任选地用1-3个R5取代
Figure A0180519000041
Q是O、S或NR5；W、X、Y和Z独立地是N或CR5，前提是在J-3和J-4中W、X、Y或Z至少之一是N；R2是H、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C2-C6烷基羰基或C2-C6烷氧基羰基；R3是C1-C6烷基、C2-C6链烯基、C2-C6炔基或C3-C6环烷基，各自任选地为一个或多个选自下列的取代基取代：卤素、CN、C1-C2烷氧基、C1-C2烷基硫代、C1-C2烷基亚硫酰基和C1-C2烷基磺酰基；一个R4基团在2位或7位连接萘基环体系，且该R4是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基或C1-C4卤代烷基磺酰基；每一R5独立地是H、C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基，C3-C8二烷基氨基羰基；或每一R5独立地是苯基、苄基或5元或6元杂芳环，每一环任选地为下列的取代基取代：C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C2-C4卤代链烯基、C2-C4卤代炔基、C3-C6卤代环烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4烷基氨基、C2-C8二烷基氨基、C3-C6环烷基氨基、C3-C6(烷基)环烷基氨基、C2-C4烷基羰基、C2-C6烷氧基羰基、C2-C6烷基氨基羰基、C3-C8二烷基氨基羰基或C3-C6三烷基甲硅烷基；或(R5)2当与相邻碳原子连接时可以合在一起成为-OCF2O-、-CF2CF2O-或-OCF2CF2O-；和n为1-2。4. The compound of claim 2 or 3, wherein J is a phenyl ring or a 5-membered or 6-membered heteroaryl ring selected from the following J-1, J-2, J-3 and J-4, each J ring is optionally optionally substituted with 1-3 R 5
Figure A0180519000041
Q is O, S or NR 5 ; W, X, Y and Z are independently N or CR 5 , provided that at least one of W, X, Y or Z in J-3 and J-4 is N; R 2 is H, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkylcarbonyl or C 2 -C 6 alkoxycarbonyl; R 3 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or C 3 -C 6 cycloalkyl, each optionally one or A plurality of substituents selected from the group consisting of halogen, CN, C 1 -C 2 alkoxy, C 1 -C 2 alkylthio, C 1 -C 2 alkylsulfinyl and C 1 -C 2 alkane Sulfonyl; one R 4 group is connected to the naphthyl ring system at the 2-position or 7-position, and the R 4 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl or C 1 -C 4 haloalkylsulfonyl; each R 5 is independently H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl , C 3 -C 8 dialkylaminocarbonyl; or each R 5 is independently phenyl, benzyl, or a 5-membered or 6-membered heteroaryl ring, each ring optionally substituted by the following substituents: C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 2 -C 4 haloalkenyl , C 2 -C 4 haloalkynyl, C 3 -C 6 halocycloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 - C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkylamino, C 2 -C 8 dialkylamino, C 3 - C 6 cycloalkylamino, C 3 -C 6 (alkyl) cycloalkylamino, C 2 -C 4 alkylcarbonyl, C 2 -C 6 alkoxycarbonyl, C 2 -C 6 alkylaminocarbonyl, C 3 -C 8 dialkylaminocarbonyl or C 3 -C 6 trialkylsilyl; or (R 5 ) 2 can be combined into -OCF 2 O-, -CF when connected to adjacent carbon atoms 2 CF 2 O- or -OCF 2 CF 2 O-; and n is 1-2. 5.权利要求4的式I化合物，其中R2是H；R3是C1-C4烷基；和至少一个R5取代基与NR1C(＝B)部分邻位。5. The compound of formula I according to claim 4, wherein R2 is H; R3 is C1 - C4 alkyl; and at least one R5 substituent is ortho to the NR1C (=B) moiety. 6.权利要求5的化合物，其中R3是甲基。6. The compound of claim 5, wherein R3 is methyl. 7.权利要求4的式II化合物，其中R1是H或C1-C4烷基；R2是H或C1-C4烷基；R3是任选地用卤素、CN、OCH3或S(O)pCH3取代的C1-C4烷基；一个R5基团在与C(＝B)NR1部分邻位的位置上与J相连，且该R5是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；C3-C8二烷基氨基羰基或苯基、苄基，或5元或6元杂芳环，每一环任选地为下列的取代基取代：卤素、CN、NO2、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C1-C4烷氧基或C1-C4卤代烷氧基；而任选的第二R5基团独立地是C1-C4烷基、C1-C4卤代烷基、卤素、CN、NO2、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷基硫代、C1-C4烷基亚硫酰基、C1-C4烷基磺酰基、C1-C4卤代烷基硫代、C1-C4卤代烷基亚硫酰基、C1-C4卤代烷基磺酰基或C2-C4烷氧基羰基；C3-C8二烷基氨基羰基或苯基、苄基，或5元或6元杂芳环，每一环任选地为下列的取代基取代：卤素、CN、NO2、C1-C4烷基、C2-C4链烯基、C2-C4炔基、C3-C6环烷基、C1-C4卤代烷基、C1-C4烷氧基或C1-C4卤代烷氧基。7. The formula II compound of claim 4, wherein R 1 is H or C 1 -C 4 alkyl; R 2 is H or C 1 -C 4 alkyl; R 3 is optionally halogen, CN, OCH 3 or S(O) p CH 3 substituted C 1 -C 4 alkyl; one R 5 group is attached to J at a position ortho to the C(=B)NR 1 moiety, and the R 5 is C 1 - C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl; C 3 -C 8 dialkylaminocarbonyl or phenyl, benzyl, or 5-membered or 6-membered heteroaromatic ring, each ring is optionally substituted by the following substituents: Halogen, CN, NO 2 , C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy; and the optional second R 5 group is independently C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, halogen, CN, NO 2 , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl Acyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfinyl, C 1 -C 4 haloalkylsulfonyl or C 2 -C 4 alkoxycarbonyl; C 3 -C 8 dioxane Aminocarbonyl or phenyl, benzyl, or 5-membered or 6-membered heteroaromatic ring, each ring is optionally substituted with the following substituents: halogen, CN, NO 2 , C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 6 cycloalkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy. 7.权利要求6的化合物，其中J是苯基、吡唑、吡咯、吡啶或嘧啶，每一个均被在与C(＝B)NR1部分邻位的位置上与J相连的一个R5和第二个任选的R5取代。7. The compound of claim 6, wherein J is phenyl, pyrazole, pyrrole, pyridine or pyrimidine, each of which is connected to J at a position ortho to the C(=B)NR moiety and The second optional R 5 is substituted. 8.权利要求7的化合物，其中R1和R2均是H；一个R4在与NR1C(＝X)J部分邻位的7位上连接，并选自C1-C3烷基、CF3、OCF3、OCHF2、S(O)pCF3、S(O)pCHF2和卤素，而任选的第二R4在与NR1C(＝X)J部分对位的5位上连接，并选自卤素、C1-C3烷基和C1-C3卤代烷基。8. The compound of claim 7, wherein R 1 and R 2 are both H; one R 4 is attached at the 7-position ortho to the NR 1 C(=X)J moiety, and is selected from C 1 -C 3 alkyl , CF 3 , OCF 3 , OCHF 2 , S(O) p CF 3 , S(O) p CHF 2 and halogen, while the optional second R 4 is in the para position to the NR 1 C(=X)J moiety 5-position, and selected from halogen, C 1 -C 3 alkyl and C 1 -C 3 haloalkyl. 9.权利要求8的化合物，其中J是J-1；Q是NR5a；X是N或CH；Y是CH；Z是CR5b；R5a是用一个或两个选自卤素、C1-C4烷基、C1-C4卤代烷基或C1-C4卤代烷氧基所取代的苯基或2-吡啶基；和R5b是卤素或CF3。9. The compound of claim 8, wherein J is J-1; Q is NR 5a ; X is N or CH; Y is CH; Z is CR 5b ; C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 haloalkoxy substituted phenyl or 2-pyridyl; and R 5b is halogen or CF 3 . 10.权利要求1的化合物，选自N-甲基-N′-(2-溴-4-氟苯基)-1，8-萘-二甲酰、N-甲基8-[(3，4-二氟苯基)羰基氨基]-1-萘甲酰和N-甲基8-[(2-噻吩基)羰基氨基]-1-萘甲酰。10. The compound of claim 1, selected from N-methyl-N'-(2-bromo-4-fluorophenyl)-1,8-naphthalene-diformyl, N-methyl 8-[(3, 4-difluorophenyl)carbonylamino]-1-naphthoyl and N-methyl 8-[(2-thienyl)carbonylamino]-1-naphthoyl. 11.一种用于防治无脊椎害虫的组合物，包含生物有效量的权利要求1的化合物以及表面活性剂、固体稀释剂或液体稀释剂中的至少一种。11. A composition for controlling invertebrate pests, comprising a biologically effective amount of the compound of claim 1 and at least one of a surfactant, a solid diluent or a liquid diluent. 12.权利要求11的组合物，还包含有效量的至少一种附加生物活性化合物或试剂。12. The composition of claim 11, further comprising an effective amount of at least one additional biologically active compound or agent. 13.权利要求12的组合物，其中，至少一种附加生物活性化合物或试剂选自由合成除虫菊酯类、氨基甲酸酯类、neonicotinoids、二乙基溴乙酰胺钠通道堵塞剂、杀虫大环内酯类、γ-氨基丁酸(GABA)对抗剂、杀虫剂尿素和保幼激素组成的一组节肢害虫杀灭剂。13. The composition of claim 12, wherein at least one additional biologically active compound or agent is selected from the group consisting of synthetic pyrethrins, carbamates, neonicotinoids, sodium diethylbromoacetamide channel blockers, insecticidal macrocycles A group of arthropod insecticides consisting of esters, gamma-aminobutyric acid (GABA) antagonists, insecticide urea, and juvenile hormones. 14.权利要求12的组合物，其中，至少一种附加生物活性化合物或试剂选自以下杀虫剂、杀线虫剂、杀螨剂或生物试剂：齐墩螨素(abamectin)，高灭磷，吡虫清，齐墩螨素(avermectin)，艾扎丁，谷硫磷，氟氯菊酯，联苯肼酯，噻嗪酮，虫螨威，氟唑虫清，定虫隆，毒死蜱，甲基毒死蜱，chromafenozide，clothianidin，氯氟氰菊酯，β-氯氟氰菊酯，(RS)氯氟氰菊酯，λ-氯氟氰菊酯，氯氰菊酯，灭蝇胺，溴氰菊酯，杀螨硫隆，二嗪农，氟脲杀，乐果，噁茂醚，emamectin，硫丹，高氰戊菊酯，ethiprole，苯硫威，双氧威，甲氰菊酯，唑螨酯，杀灭菊酯，锐劲特，flonicamid，氟氰戊菊酯，氟胺氰菊酯，氟虫脲，地虫磷，特丁苯酰肼，氟铃脲，吡虫啉，噁二唑虫，丙胺磷，氟丙氧脲，马拉松，蜗牛敌，甲胺磷，杀扑磷，灭多虫，蒙五一五，甲氧滴滴涕，久效磷，甲氧苯酰肼，硝虫噻嗪，双苯氟脲，甲氨叉威，一六零五，甲基一六零五，氯菊酯，三九一一，伏杀磷，亚胺硫磷，磷胺，抗蚜威，丙溴磷，拒嗪酮，pyridalyl，蚊蝇醚，鱼藤酮，艾克敌105，乙丙硫磷，双苯酰肼，伏虫隆，七氟菊酯，特丁磷，杀虫畏，thiacloprid，thiamethoxam，硫双灭多威，杀虫双，四溴菊酯，敌百虫和杀虫隆，涕灭威，甲氨叉威，克线磷，虫螨脒，灭螨猛，乙酯杀螨醇，三环锡，开乐散，除螨灵，特苯噁唑，喹螨醚，杀螨锡，甲氰菊酯，唑螨酯，噻螨酮，克螨特，哒螨酮，吡螨胺，苏云金芽孢杆菌(Bacillusthuringiensis)，苏云金芽孢杆菌δ-内毒素，杆状病毒，以及食虫细菌、病毒和真菌。14. The composition of claim 12, wherein at least one additional biologically active compound or agent is selected from the group consisting of the following insecticides, nematicides, acaricides or biological agents: abamectin, abafen, Acetamiprid, avermectin, azadin, azinfos, bifenthrin, bifenazate, buprofezin, fenfencarb, chlorfenapyr, diflunron, chlorpyrifos, formazan Base chlorpyrifos, chromafenozide, clothianidin, cyhalothrin, beta-cyhalothrin, (RS) cyhalothrin, lambda-cyhalothrin, cypermethrin, cyromazine, deltamethrin, Thiuron, diazinon, hexacarb, dimethoate, oxamethrin, emamectin, endosulfan, esfenvalerate, ethiprole, fenthiocarb, fenoxycarb, fenpropathrin, fenpyroximate, Permethrin, fipronil, flonicamid, flucyvalerate, fluvalinate, flubenzuron, fenfenfos, terbufenozide, hexaflumuron, imidacloprid, oxadiazole, afenamiphos, Flupropoxycarbamide, marathon, snail enemy, methamidophos, metaphos, methoxam, 515, methoxychlor, monocrotophos, methoxyfenozide, nitrothiazide, diphenylfluramide , Methoxacarb, 1605, Methyl 1605, Permethrin, 3911, Phoxafos, imophos, phosphamide, pirimicarb, profenofos, azinone , pyridalyl, pyriproxyfen, rotenone, Acetyl 105, etethion, bisfenozide, chlorfluron, tefluthrin, terbufos, dimefen, thiacloprid, thiamethoxam, thiodimethomyl , dimehypo, perbromethrin, trichlorfon and triflumeron, aldicarb, methoxacarb, grammafos, chamiprid, acarid, ethyl ester fofol, tricyclic tin, open Lesan, Fabex, Tebenoxazole, Fenazazak, Fenzafen, Fenpropathrin, Fenpyroximate, Hexythiazox, Caprodite, Pyridaben, Tebufenpyrad, Bacillus thuringiensis (Bacillus thuringiensis ), Bacillus thuringiensis delta-endotoxin, baculovirus, and entomophagous bacteria, viruses, and fungi. 15.权利要求14的组合物，其中，至少一种附加生物活性化合物或试剂选自：氯氰菊酯，(RS)氯氟氰菊酯，氟氯氰菊酯，β-氟氯氰菊酯，高氰戊菊酯，杀灭菊酯，四溴菊酯，fenothicarb，灭多虫，甲氨叉威，硫双灭多威，clothianidin，吡虫啉，thiacloprid，噁二唑虫，艾克敌105，齐墩螨素(abamectin)，齐墩螨素(avermectin)，emamectin，硫丹，ethiprole，锐劲特，氟虫脲，杀虫隆，噁茂醚，蚊蝇醚，拒嗪酮，虫螨脒，苏云金芽孢杆菌，苏云金芽孢杆菌δ-内毒素，以及及食昆虫的真菌。15. The composition of claim 14, wherein at least one additional bioactive compound or agent is selected from the group consisting of: cypermethrin, (RS) cyhalothrin, cyfluthrin, beta-cyfluthrin, esfenvalerate, Permethrin, tetrabromothrin, fenothicarb, methoxam, methoxacarb, thiodicarb, clothianidin, imidacloprid, thiacloprid, oxadiazole, aikedi 105, abamectin, Avermectin (avermectin), emamectin, endosulfan, ethiprole, fipronil, flubenzuron, triflumeron, oxolofen, pyriproxyfen, azinone, chrysanthemum, Bacillus thuringiensis, Bacillus thuringiensis delta - Endotoxins, and insect-eating fungi. 16.一种防治无脊椎害虫的方法，包括使该无脊椎害虫或其环境与生物有效量的权利要求1的化合物或权利要求11的组合物相接触。16. A method of controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of the compound of claim 1 or the composition of claim 11.
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