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TW202404935A - Herbicidal compounds - Google Patents

Herbicidal compounds Download PDF

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TW202404935A
TW202404935A TW112118446A TW112118446A TW202404935A TW 202404935 A TW202404935 A TW 202404935A TW 112118446 A TW112118446 A TW 112118446A TW 112118446 A TW112118446 A TW 112118446A TW 202404935 A TW202404935 A TW 202404935A
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威廉 蓋伊 懷廷翰
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瑞士商先正達農作物保護公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • 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
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01P—BIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P13/00—Herbicides; Algicides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—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 carboxyl groups bound to the same carbon skeleton
    • C07C323/51—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/52—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C07D213/71—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Plant Pathology (AREA)
  • Environmental Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Dentistry (AREA)
  • Agronomy & Crop Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Compounds of the formula (I)

Description

除草化合物herbicidal compounds

本發明關於具有除草活性的化合物，以及用於製備此類衍生物之方法和中間體。本發明進一步延伸到包含此類衍生物的除草組成物，並且延伸到此類化合物和組成物在有用植物的作物中用於控制不希望的植物生長之用途：特別是用於控制雜草之用途。The present invention relates to compounds having herbicidal activity, as well as to processes and intermediates for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, and to the use of such compounds and compositions for controlling undesirable plant growth in crops of useful plants: in particular for controlling weeds. .

US 2014/048827、WO 2016/120116和WO 2020/239607描述了除草衍生物。US 2014/048827, WO 2016/120116 and WO 2020/239607 describe herbicidal derivatives.

本發明基於以下發現：如本文所定義的具有式 (I) 的化合物展現了出人意料地良好的除草活性。因此，根據本發明，提供了一種具有式 (I) 的化合物或其農藝學上可接受的鹽： (I) 其中 X 1係C-R 1、氮或N +-O -； X 2係C-R 17或氮； X 3係C-R 18或氮； X 4係C-R 19或氮； 前提係X 1、X 2、X 3和X 4中最多兩個係氮，並且X 3和X 4兩者不皆為氮； Y係C-H或氮； B係O、S或NR 5； D係-[C(R 6)(R 7)] n-； m係從0至2的整數； n係從1至4的整數； R 1係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 2係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、CO 2R 9或CONR 10R 11；或者 R 1和R 2與它們所附接的碳原子一起形成5員或6員環，其可以是飽和的或部分或完全不飽和的，並且可以視需要含有一個或兩個選自氮、氧和硫的雜原子，並且可以被1至4個由R 16表示的基團取代；或者 R 2和R 19與它們所附接的碳原子一起形成5員或6員環，其可以是飽和的或部分或完全不飽和的，並且可以視需要含有一個或兩個選自氮、氧和硫的雜原子，並且可以被1至4個由R 16表示的基團取代； R 3係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷硫基或C 1-C 4烷基磺醯基； R 4係氫、鹵素、氰基、硝基、胺基羰基、胺基硫代羰基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基或C 1-C 4烷基磺醯基； R 5係氫、羥基、C 1-C 6烷基或C 1-C 4烷氧基； R 6和R 7各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、羥基、C 1-C 4烷氧基、C 1-C 4烷氧基羰基或CH 2OR 12；前提係R 6和R 7在同一碳原子上不皆為羥基； 或者，在同一碳原子或不同碳原子上的兩個R 6和R 7基團一起形成C 1-C 5伸烷基鏈，該鏈含有0、1或2個氧原子，被1至3個由R 15表示的基團取代； 或者，在同一碳原子上的兩個R 6和R 7基團一起形成C 2-C 3烯烴； R 8係OR 9、SR 9或NR 10R 11； R 9係氫、C 1-C 10烷基、C 1-C 10鹵代烷基、C 3-C 6烯基、C 3-C 6鹵代烯基、C 3-C 6炔基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 6-C 10芳基C 1-C 3烷基、被1至4個由R 13表示的基團取代的C 6-C 10芳基C 1-C 3烷基、雜芳基C 1-C 3烷基、或被1至3個由R 13表示的基團取代的雜芳基C 1-C 3烷基； R 10係氫、C 1-C 6烷基、SO 2R 14； R 11係氫或C 1-C 6烷基；或者 R 10和R 11與它們所附接的氮一起形成3員至6員雜環基環； R 12係氫、C 1-C 4烷基或C 1-C 4烷基羰基； R 13係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基； R 14係C 1-C 4烷基、C 1-C 4鹵代烷基或C 1-C 4烷基(C 1-C 4烷基)胺基； R 15係氫、鹵素、C 1-C 4烷基或C 1-C 4鹵代烷基； R 16係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基； R 17係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 18係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 19係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 20和R 21各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、C 1-C 4烷氧基或-CH 2OR 12； 或者兩個R 20和R 21基團與它們所附接的碳原子一起形成C 2-C 5伸烷基鏈，其中所述C 2-C 5伸烷基鏈包含0、1或2個氧原子，並且其中所述C 2-C 5伸烷基鏈被1至3個由R 15表示的基團取代； 或者兩個R 20和R 21基團與它們所附接的碳原子一起形成C 2-C 3烯烴；並且 前提係R 1、R 2、R 17、R 18和R 19不全係氫。 The present invention is based on the discovery that compounds of formula (I) as defined herein exhibit surprisingly good herbicidal activity. Therefore, according to the present invention, there is provided a compound of formula (I) or an agronomically acceptable salt thereof: ( I) Where X 1 is CR 1 , nitrogen or N + -O - ; X 2 is CR 17 or nitrogen; X 3 is CR 18 or nitrogen; At most two of X 3 and X 4 are nitrogen, and both X 3 and R 7 )] n -; m is an integer from 0 to 2; n is an integer from 1 to 4; R 1 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 Alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonate C 1 -C 4 alkylthio group, C 1 -C 4 alkylthio group, C 1 -C 4 alkylsulfinyl group, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 Haloalkylsulfinyl, C 1 -C 4 haloalkyl sulfonyl, amine, C 1 -C 4 alkylamino, di(C 1 -C 4 alkyl)amine, C 1 -C 4 alkyl Carbonylamine group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkyl group Aminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkylsulfonylamine, -CO 2 R 9 or -CONR 10 R 11 ; R 2 is hydrogen or halogen , cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxyC 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxyC 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkyl Sulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4 alkylamino group, Di(C 1 -C 4 alkyl)amine, C 1 -C 4 alkylcarbonylamino, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine, C 1 -C 4 alkyl Oxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkylsulfonylamine , CO 2 R 9 or CONR 10 R 11 ; or R 1 and R 2 together with the carbon atom to which they are attached form a 5- or 6-membered ring, which may be saturated or partially or fully unsaturated, and may be Requires one or two heteroatoms selected from nitrogen, oxygen and sulfur, and may be substituted by 1 to 4 groups represented by R 16 ; or R 2 and R 19 together with the carbon atoms to which they are attached form 5 A membered or 6-membered ring, which may be saturated or partially or completely unsaturated, and may optionally contain one or two heteroatoms selected from nitrogen, oxygen and sulfur, and may be represented by 1 to 4 R 16 Substituted with a group; R 3 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio or C 1 -C 4 alkylsulfonyl; R 4 is hydrogen, halogen, cyano, nitro, aminocarbonyl, aminothiocarbonyl, C 1 -C 4 alkyl, C 1 - C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy or C 1 -C 4 alkylsulfonyl group; R 5 is hydrogen, hydroxyl, C 1 -C 6 alkyl or C 1 -C 4 alkoxy; R 6 and R 7 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkoxycarbonyl or CH 2 OR 12 ; provided that R 6 and R 7 are not both hydroxyl groups on the same carbon atom; or, two R 6 and R 7 groups on the same carbon atom or different carbon atoms groups together form a C 1 -C 5 alkylene chain containing 0, 1 or 2 oxygen atoms substituted by 1 to 3 groups represented by R 15 ; alternatively, two R on the same carbon atom 6 and R 7 groups together form C 2 -C 3 alkene; R 8 is OR 9 , SR 9 or NR 10 R 11 ; R 9 is hydrogen, C 1 -C 10 alkyl, C 1 -C 10 haloalkyl, C 3 -C 6 alkenyl, C 3 -C 6 haloalkenyl, C 3 -C 6 alkynyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 6 -C 10 aryl C 1 -C 3 alkyl, C 6 -C 10 aryl C 1 -C 3 alkyl substituted by 1 to 4 groups represented by R 13 base, heteroaryl C 1 -C 3 alkyl, or heteroaryl C 1 -C 3 alkyl substituted by 1 to 3 groups represented by R 13 ; R 10 is hydrogen, C 1 -C 6 alkyl radical, SO 2 R 14 ; R 11 is hydrogen or C 1 -C 6 alkyl; or R 10 and R 11 together with the nitrogen to which they are attached form a 3- to 6-membered heterocyclyl ring; R 12 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkylcarbonyl; R 13 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 - C 4 haloalkoxy, cyano or C 1 -C 4 alkylsulfonyl group; R 14 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkyl (C 1 - C 4 alkyl) amino group; R 15 is hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl; R 16 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl group, C 1 -C 4 alkoxy group, C 1 -C 4 haloalkoxy group, cyano group or C 1 -C 4 alkyl sulfonyl group; R 17 is hydrogen, halogen, cyano group, nitro group, C 1 - C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy , C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 Haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4 alkylamino group, di(C 1 -C 4 alkyl) Amino group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamine group, C 1 -C 4 alkylaminocarbonylamino group, C 1 -C 4 alkylsulfonylamine group, C 1 -C 4 haloalkylsulfonylamine group, -CO 2 R 9 or -CONR 10 R 11 ; R 18 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy, C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfenyl C1- C4 alkylsulfonyl group, C1- C4 haloalkylthio group, C1 - C4 haloalkylsulfenyl group, C1 - C4 haloalkylsulfonyl group, amino group, C 1 -C 4 alkylamine, di(C 1 -C 4 alkyl)amine, C 1 -C 4 alkylcarbonylamino, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl) Amino group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkylaminocarbonylamino group, C 1 -C 4 alkylsulfonylamine group, C 1 - C 4 haloalkylsulfonamide, -CO 2 R 9 or -CONR 10 R 11 ; R 19 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl , C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy , C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy , C 1 -C 4 alkylthio group, C 1 -C 4 alkylsulfenyl group, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl group Sulfonyl group, C 1 -C 4 haloalkyl sulfonyl group, amine group, C 1 -C 4 alkylamino group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamine group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkylaminocarbonyl group Amino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkylsulfonylamine, -CO 2 R 9 or -CONR 10 R 11 ; R 20 and R 21 are each independently Hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 4 alkoxy or -CH 2 OR 12 ; or both R 20 and R 21 groups to which they are attached The carbon atoms together form a C 2 -C 5 alkylene chain, wherein the C 2 -C 5 alkylene chain contains 0, 1 or 2 oxygen atoms, and wherein the C 2 -C 5 alkylene chain Substituted by 1 to 3 groups represented by R 15 ; or the two R 20 and R 21 groups together with the carbon atoms to which they are attached form a C 2 -C 3 alkene; and provided that R 1 , R 2 , R 17 , R 18 and R 19 are not all hydrogen.

根據本發明之第二方面，提供了一種農用化學組成物，其包含除草有效量的具有式 (I) 的化合物和農用化學上可接受的稀釋劑或載體。這樣一種農業組成物可以進一步包含至少一種另外的活性成分。According to a second aspect of the present invention, there is provided an agrochemical composition comprising a herbicidally effective amount of a compound of formula (I) and an agrochemically acceptable diluent or carrier. Such an agricultural composition may further comprise at least one additional active ingredient.

根據本發明之第三方面，提供了一種用於控制或預防不希望的植物生長之方法，其中將除草有效量的具有式 (I) 的化合物或包含這種化合物作為活性成分的組成物施用至該等植物、其部分或其場所。According to a third aspect of the present invention, there is provided a method for controlling or preventing undesirable plant growth, wherein a herbicidally effective amount of a compound of formula (I) or a composition comprising such a compound as an active ingredient is applied to such plants, parts or places thereof.

根據本發明之第四方面，提供了具有式 (I) 的化合物作為除草劑之用途。According to a fourth aspect of the invention there is provided the use of a compound of formula (I) as a herbicide.

根據本發明之第五方面，提供了一種用於製備具有式 (I) 的化合物之方法。According to a fifth aspect of the present invention, there is provided a method for preparing a compound of formula (I).

當取代基被表示為「被視需要取代」時，這意指它們可以帶有或可以不帶有一個或多個相同或不同的取代基，例如一個、兩個或三個R 13取代基。例如，被1、2或3個鹵素取代的C 1-C 6烷基可以包括但不限於-CH 2Cl、-CHCl 2、-CCl 3、-CH 2F、-CHF 2、-CF 3、-CH 2CF 3或-CF 2CH 3基團。作為另一個實例，被1、2或3個鹵素取代的C 1-C 6烷氧基可以包括但不限於CH 2ClO-、CHCl 2O-、CCl 3O-、CH 2FO-、CHF 2O-、CF 3O-、CF 3CH 2O-或CH 3CF 2O-基團。 When substituents are expressed as "optionally substituted" this means that they may or may not bear one or more identical or different substituents, for example one, two or three R 13 substituents. For example, C 1 -C 6 alkyl substituted by 1, 2 or 3 halogens may include, but is not limited to, -CH 2 Cl, -CHCl 2 , -CCl 3 , -CH 2 F, -CHF 2 , -CF 3 , -CH 2 CF 3 or -CF 2 CH 3 group. As another example, C 1 -C 6 alkoxy substituted with 1, 2 or 3 halogens may include, but is not limited to, CH 2 ClO-, CHCl 2 O-, CCl 3 O-, CH 2 FO-, CHF 2 O-, CF 3 O-, CF 3 CH 2 O- or CH 3 CF 2 O- groups.

如本文使用的，術語「鹵素（halogen或halo）」係指氟（fluorine，fluoro）、氯（chlorine，chloro）、溴（bromine，bromo）或碘（iodine，iodo），較佳的是氟、氯或溴。As used herein, the term "halogen (halo)" refers to fluorine (fluoro), chlorine (chloro), bromine (bromo) or iodine (iodine, iodo), preferably fluorine, Chlorine or bromine.

如本文使用的，「氰基」意指-CN基團。As used herein, "cyano" means a -CN group.

如本文使用的，「胺基」意指-NH 2基團。 As used herein, "amine" means a -NH group.

如本文使用的，「羥基」意指-OH基團。As used herein, "hydroxy" means the -OH group.

如本文使用的，「硝基」意指-NO 2基團。 As used herein, "nitro" means the -NO group.

如本文使用的，術語「C 1-C 10烷基」係指僅由碳原子和氫原子組成的直鏈的或支鏈的烴鏈基團，該烴鏈基團不含不飽和度、具有從一至十個碳原子、並且藉由單鍵附接至分子的其餘部分。C 1-C 6烷基、C 1-C 4烷基、C 1-C 3烷基和C 1-C 2烷基應相應地解釋。C 1-C 10烷基的實例包括但不限於甲基（Me）、乙基（Et）、正丙基、1-甲基乙基（異丙基）、正丁基和1-二甲基乙基（三級丁基）。 As used herein, the term "C 1 -C 10 alkyl" refers to a linear or branched hydrocarbon chain group consisting only of carbon atoms and hydrogen atoms, which hydrocarbon chain group does not contain unsaturation, has From one to ten carbon atoms and attached to the rest of the molecule by a single bond. C 1 -C 6 alkyl, C 1 -C 4 alkyl, C 1 -C 3 alkyl and C 1 -C 2 alkyl should be interpreted accordingly. Examples of C 1 -C 10 alkyl groups include, but are not limited to, methyl (Me), ethyl (Et), n-propyl, 1-methylethyl (isopropyl), n-butyl, and 1-dimethyl Ethyl (tertiary butyl).

如本文使用的，術語「C 1-C 4烷氧基」係指具有式-OR a的基團，其中R a係如上一般定義的C 1-C 4烷基。C 1-C 3烷氧基應相應地解釋。C 1-4烷氧基的實例包括但不限於甲氧基、乙氧基、丙氧基、異丙氧基和三級丁氧基。 As used herein, the term "C 1 -C 4 alkoxy" refers to a group of formula -OR a , wherein R a is C 1 -C 4 alkyl as generally defined above. C 1 -C 3 alkoxy should be interpreted accordingly. Examples of C 1-4 alkoxy include, but are not limited to, methoxy, ethoxy, propoxy, isopropoxy and tertiary butoxy.

如本文使用的，術語「C 1-C 10鹵代烷基」係指被一個或多個相同或不同的鹵素原子取代的如上一般定義的C 1-C 10烷基基團。C 1-C 6鹵代烷基和C 1-C 4鹵代烷基應相應地解釋。C 1-C 10鹵代烷基的實例包括但不限於氯甲基、氟甲基、氟乙基、二氟甲基、三氟甲基和2,2,2-三氟乙基。 As used herein, the term "C 1 -C 10 haloalkyl" refers to a C 1 -C 10 alkyl group as generally defined above substituted by one or more halogen atoms, which may be the same or different. C 1 -C 6 haloalkyl and C 1 -C 4 haloalkyl should be interpreted accordingly. Examples of C 1 -C 10 haloalkyl groups include, but are not limited to, chloromethyl, fluoromethyl, fluoroethyl, difluoromethyl, trifluoromethyl, and 2,2,2-trifluoroethyl.

如本文使用的，術語「C 2-C 6烯基」係指僅由碳原子和氫原子組成的直鏈或支鏈的烴鏈基團，該烴鏈基團含有至少一個可以具有 ( E)- 或 ( Z)-組態的雙鍵，具有從二至六個碳原子，藉由單鍵附接至分子的其餘部分。C 3-C 6烯基、C 2-C 4烯基和C 2-C 3烯基應相應地解釋。C 2-C 6烯基的實例包括但不限於丙-1-烯基、烯丙基（丙-2-烯基）和丁-1-烯基。 As used herein, the term "C 2 -C 6 alkenyl" refers to a straight or branched hydrocarbon chain group consisting only of carbon atoms and hydrogen atoms, which hydrocarbon chain group contains at least one member that may have ( E ) A double bond in the - or ( Z )-configuration, with from two to six carbon atoms, attached to the rest of the molecule by a single bond. C 3 -C 6 alkenyl, C 2 -C 4 alkenyl and C 2 -C 3 alkenyl should be interpreted accordingly. Examples of C 2 -C 6 alkenyl include, but are not limited to, prop-1-enyl, allyl (prop-2-enyl), and but-1-enyl.

如本文使用的，術語「C 2-C 6鹵代烯基」係指被一個或多個相同或不同的鹵素原子取代的如上一般定義的C 2-C 6烯基。C 3-C 6鹵代烯基、C 2-C 4鹵代烯基和C 2-C 3鹵代烯基應相應地解釋。C 2-C 6鹵代烯基的實例包括但不限於氯乙烯、氟乙烯、1,1-二氟乙烯、1,1-二氯乙烯和1,1,2-三氯乙烯。 As used herein, the term "C 2 -C 6 haloalkenyl" refers to a C 2 -C 6 alkenyl group as generally defined above substituted by one or more halogen atoms, which may be the same or different. C 3 -C 6 haloalkenyl, C 2 -C 4 haloalkenyl and C 2 -C 3 haloalkenyl should be interpreted accordingly. Examples of C 2 -C 6 haloalkenyl groups include, but are not limited to, vinyl chloride, vinyl fluoride, 1,1-difluoroethylene, 1,1-dichloroethylene, and 1,1,2-trichloroethylene.

如本文使用的，術語「C 2-C 6炔基」係指僅由碳原子和氫原子組成的直鏈或支鏈的烴鏈基團，該烴鏈基團包含至少一個三鍵，具有從二至六個碳原子，並且藉由單鍵附接至分子的其餘部分。C 2-C 4炔基和C 3-C 6炔基應相應地解釋。C 2-C 6炔基的實例包括但不限於丙-1-炔基、炔丙基（丙-2-炔基）和丁-1-炔基。 As used herein, the term "C 2 -C 6 alkynyl" refers to a straight or branched hydrocarbon chain group consisting only of carbon atoms and hydrogen atoms, the hydrocarbon chain group containing at least one triple bond, having from Two to six carbon atoms and attached to the rest of the molecule by single bonds. C 2 -C 4 alkynyl and C 3 -C 6 alkynyl should be interpreted accordingly. Examples of C 2 -C 6 alkynyl groups include, but are not limited to, prop-1-ynyl, propargyl (prop-2-ynyl), and but-1-ynyl.

如本文使用的，術語「C 1-C 6鹵代烷氧基」係指被一個或多個相同的或不同的鹵素原子取代的如上所定義的C 1-C 6烷氧基基團。C 1-C 4鹵代烷氧基應相應地解釋。C 1-C 6鹵代烷氧基的實例包括但不限於氟甲氧基、二氟甲氧基、氟乙氧基、三氟甲氧基和三氟乙氧基。 As used herein, the term "C 1 -C 6 haloalkoxy" refers to a C 1 -C 6 alkoxy group as defined above substituted by one or more halogen atoms, which may be the same or different. C 1 -C 4 haloalkoxy should be interpreted accordingly. Examples of C 1 -C 6 haloalkoxy include, but are not limited to, fluoromethoxy, difluoromethoxy, fluoroethoxy, trifluoromethoxy, and trifluoroethoxy.

如本文使用的，術語「C 1-C 4鹵代烷氧基C 1-C 6烷基」係指具有式R b-O-R a-的基團，其中R b係如上一般定義的C 1-C 4鹵代烷基基團，並且R a係如上一般定義的C 1-C 6伸烷基基團。 As used herein, the term "C 1 -C 4 haloalkoxy C 1 -C 6 alkyl" refers to a group having the formula R b -OR a -, where R b is C 1 -C 4 as generally defined above haloalkyl group, and R a is a C 1 -C 6 alkylene group as generally defined above.

如本文使用的，術語「C 1-C 4烷氧基C 1-C 6烷基」係指具有式R b-O-R a-的基團，其中R b係如上一般定義的C 1-C 4烷基基團，並且R a係如上一般定義的C 1-C 6伸烷基基團。 As used herein, the term "C 1 -C 4 alkoxy C 1 -C 6 alkyl" refers to a group having the formula R b -OR a -, where R b is C 1 -C 4 as generally defined above an alkyl group, and R a is a C 1 -C 6 alkylene group as generally defined above.

如本文使用的，術語「C 1-C 4烷氧基C 1-C 4烷氧基」係指具有式R b-O-R a-O-的基團，其中R b係如上一般定義的C 1-C 4烷基基團，並且R a係如上一般定義的C 1-C 4伸烷基基團。 As used herein, the term "C 1 -C 4 alkoxy C 1 -C 4 alkoxy" refers to a group having the formula R b -OR a -O-, where R b is C 1 as generally defined above -C 4 alkyl group, and R a is a C 1 -C 4 alkylene group as generally defined above.

如本文使用的，術語「C 1-C 6烷基羰基」係指具有式-C(O)R a的基團，其中R a係如上一般定義的C 1-C 6烷基基團。C 1-C 6烷基羰基的實例包括但不限於乙醯基。 As used herein, the term "C 1 -C 6 alkylcarbonyl" refers to a group having the formula -C(O)R a , where R a is a C 1 -C 6 alkyl group as generally defined above. Examples of C 1 -C 6 alkylcarbonyl groups include, but are not limited to, acetyl groups.

如本文使用的，術語「C 1-C 6烷氧基羰基」係指具有式-C(O)OR a的基團，其中R a係如上一般定義的C 1-C 6烷基基團。 As used herein, the term "C 1 -C 6 alkoxycarbonyl" refers to a group having the formula -C(O)OR a , where R a is a C 1 -C 6 alkyl group as generally defined above.

如本文使用的，術語「C 1-C 4烷基胺基」係指具有式R aNH-的基團，其中R a係如上一般定義的C 1-C 4烷基。 As used herein, the term "C 1 -C 4 alkylamino" refers to a group having the formula Ra NH- , wherein R a is C 1 -C 4 alkyl as generally defined above.

如本文使用的，術語「二(C 1-C 4烷基)胺基」係指具有式-N(R a)(R b)的基團，其中R a和R b各自單獨地是如上一般定義的C 1-C 4烷基基團。術語「二(C 1-C 3烷基)胺基」應相應地解釋。 As used herein, the term "di(C 1 -C 4 alkyl)amine" refers to a group having the formula -N(R a )(R b ), wherein each of R a and R b individually is as above Defined C 1 -C 4 alkyl group. The term "di(C 1 -C 3 alkyl)amine" should be interpreted accordingly.

如本文使用的，術語「C 1-C 4烷基羰基胺基」係指具有式-C(O)NHR a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkylcarbonylamino" refers to a group having the formula -C(O)NHR a , where R a is a C 1 -C 4 alkyl group as generally defined above .

如本文使用的，術語「C 1-C 4烷基羰基(C 1-C 4烷基)胺基」係指具有式-NH(R a)C(O)R b的基團，其中R a和R b各自獨立地是如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine" refers to a group having the formula -NH(R a )C(O)R b , where R a and R b are each independently a C 1 -C 4 alkyl group as generally defined above.

如本文使用的，術語「C 1-C 4烷氧基羰基胺基」係指具有式-NHC(O)OR a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkoxycarbonylamino" refers to a group having the formula -NHC(O)OR a , where R a is a C 1 -C 4 alkyl group as generally defined above group.

如本文使用的，術語「胺基羰基」係指具有式-C(O)NH 2的基團。 As used herein, the term "aminocarbonyl" refers to a group having the formula -C(O)NH.

如本文使用的，術語「胺基羰基胺基」係指具有式-NHC(O)H 2的基團。 As used herein, the term "aminocarbonylamino" refers to a group having the formula -NHC(O)H.

如本文使用的，術語「胺基硫代羰基」係指具有式-C(S)NH 2的基團。 As used herein, the term "aminothiocarbonyl" refers to a group having the formula -C(S)NH.

如本文使用的，術語「C 1-C 4烷基胺基羰基胺基」係指具有式-NHC(O)NHR a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkylaminocarbonylamino" refers to a group having the formula -NHC(O) NHRA , where R a is C 1 -C 4 alkyl as generally defined above group.

如本文使用的，術語「C 1-C 4烷基磺醯基胺基」係指具有式-NHS(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkylsulfonylamine" refers to a group having the formula -NHS(O) 2 R a , where R a is a C 1 -C 4 alkyl as generally defined above base group.

如本文使用的，術語「C 1-C 4鹵代烷基磺醯基胺基」係指具有式-NHS(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4鹵代烷基基團。 As used herein, the term "C 1 -C 4 haloalkylsulfonylamine" refers to a group having the formula -NHS(O) 2 R a , where R a is a C 1 -C 4 haloalkyl as generally defined above base group.

如本文使用的，術語「C 1-C 4烷硫基」係指具有式-SR a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。術語「C 1-C 3烷基氫硫基」和「C 1-C 2烷基氫硫基」應相應地解釋。C 1-C 4烷基氫硫基的實例包括但不限於甲基氫硫基。 As used herein, the term "C 1 -C 4 alkylthio" refers to a group of formula -SR a , wherein R a is a C 1 -C 4 alkyl group as generally defined above. The terms "C 1 -C 3 alkyl mercapto" and "C 1 -C 2 alkyl mercapto" should be interpreted accordingly. Examples of C 1 -C 4 alkylthio groups include, but are not limited to, methylthio groups.

如本文使用的，術語「C 1-C 4鹵代烷硫基」係指具有式-SR a的基團，其中R a係如上一般定義的C 1-C 4鹵代烷基基團。 As used herein, the term "C 1 -C 4 haloalkylthio" refers to a group of formula -SR a , wherein R a is a C 1 -C 4 haloalkyl group as generally defined above.

如本文使用的，術語「C 1-C 4烷基亞磺醯基」係指具有式-S(O)R a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。術語「C 1-C 3烷基亞磺醯基」和「C 1-C 2烷基亞磺醯基」應相應地解釋。C 1-C 4烷基亞磺醯基的實例包括但不限於甲基亞磺醯基。 As used herein, the term "C 1 -C 4 alkylsulfenyl" refers to a group having the formula -S(O)R a , where R a is a C 1 -C 4 alkyl group as generally defined above group. The terms "C 1 -C 3 alkyl sulfinyl" and "C 1 -C 2 alkyl sulfinyl" should be interpreted accordingly. Examples of C 1 -C 4 alkylsulfinyl groups include, but are not limited to, methylsulfinyl groups.

如本文使用的，術語「C 1-C 4烷基磺醯基」係指具有式-S(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。術語「C 1-C 3烷基磺醯基」和「C 1-C 2烷基磺醯基」應相應地解釋。C 1-C 4烷基磺醯基的實例包括但不限於甲基磺醯基。 As used herein, the term "C 1 -C 4 alkylsulfonyl" refers to a group having the formula -S(O) 2 R a , where R a is a C 1 -C 4 alkyl group as generally defined above group. The terms "C 1 -C 3 alkylsulfonyl" and "C 1 -C 2 alkylsulfonyl" should be interpreted accordingly. Examples of C 1 -C 4 alkylsulfonyl groups include, but are not limited to, methylsulfonyl groups.

如本文使用的，術語「C 1-C 4烷基磺醯氧基」係指具有式-OS(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4烷基基團。 As used herein, the term "C 1 -C 4 alkylsulfonyloxy" refers to a group having the formula -OS(O) 2 R a , where R a is C 1 -C 4 alkyl as generally defined above group.

如本文使用的，術語「C 1-C 4鹵代烷基磺醯氧基」係指具有式-OS(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4鹵代烷基基團。 As used herein, the term "C 1 -C 4 haloalkyl sulfonyloxy" refers to a group having the formula -OS(O) 2 R a , where R a is a C 1 -C 4 haloalkyl group as generally defined above group.

如本文使用的，術語「C 1-C 4鹵代烷基亞磺醯基」係指具有式-S(O)R a的基團，其中R a係如以上一般定義的C 1-C 4鹵代烷基基團。 As used herein, the term "C 1 -C 4 haloalkyl sulfenyl" refers to a group having the formula -S(O)R a , wherein R a is a C 1 -C 4 haloalkyl group as generally defined above group.

如本文使用的，術語「C 1-C 4鹵代烷基磺醯基」係指具有式-S(O) 2R a的基團，其中R a係如上一般定義的C 1-C 4鹵代烷基基團。 As used herein, the term "C 1 -C 4 haloalkyl sulfonyl" refers to a group having the formula -S(O) 2 R a , wherein R a is a C 1 -C 4 haloalkyl group as generally defined above group.

如本文使用的，術語「C 3-C 6環烷基」係指飽和或部分不飽和並且含有3至6個碳原子的穩定的單環基團。C 3-C 4環烷基應相應地解釋。C 3-C 6環烷基的實例包括但不限於環丙基、環丁基、環戊基和環己基。 As used herein, the term "C 3 -C 6 cycloalkyl" refers to a stable monocyclic group that is saturated or partially unsaturated and contains 3 to 6 carbon atoms. C 3 -C 4 cycloalkyl should be interpreted accordingly. Examples of C 3 -C 6 cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

如本文使用的，術語「C 6-C 10芳基」係指僅由碳原子和氫原子組成的6員至10員芳香族環系統，該芳香族環系統可以是單環的、二環的或三環的。此類環系統的實例包括苯基、萘基、或茚基。 As used herein, the term "C 6 -C 10 aryl" refers to a 6- to 10-membered aromatic ring system consisting only of carbon atoms and hydrogen atoms. The aromatic ring system may be monocyclic or bicyclic. Or three rings. Examples of such ring systems include phenyl, naphthyl, or indenyl.

如本文使用的，術語「C 6-C 10芳基C 1-C 3烷基」係指如上一般定義的芳基部分，該芳基部分藉由如上定義的C 1-C 3伸烷基連接基附接至分子的剩餘部分。 As used herein, the term "C 6 -C 10 aryl C 1 -C 3 alkyl" refers to an aryl moiety as generally defined above linked by a C 1 -C 3 alkyl alkylene group as defined above The base is attached to the remainder of the molecule.

如本文使用的，除非另外明確說明，否則術語「雜芳基」係指包含1、2、3或4個單獨地選自氮、氧和硫的雜原子的5員或6員單環芳香族環。該雜芳基基團可以經碳原子或雜原子鍵合至分子的其餘部分。雜芳基的實例包括呋喃基、吡咯基、咪唑基、噻吩基、吡唑基、噻唑基、異噻唑基、㗁唑基、異㗁唑基、三唑基、四唑基、吡𠯤基、嗒𠯤基、嘧啶基或吡啶基。As used herein, unless expressly stated otherwise, the term "heteroaryl" refers to a 5- or 6-membered monocyclic aromatic group containing 1, 2, 3, or 4 heteroatoms individually selected from nitrogen, oxygen, and sulfur. ring. The heteroaryl group may be bonded to the remainder of the molecule via a carbon atom or a heteroatom. Examples of heteroaryl groups include furyl, pyrrolyl, imidazolyl, thienyl, pyrazolyl, thiazolyl, isothiazolyl, ethazolyl, isothiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidinyl, pyrimidinyl or pyridinyl.

如本文使用的，除非另外明確說明，否則術語「雜芳基C 1-C 3烷基」係指藉由如上定義的C 1-C 3伸烷基連接基附接至分子的剩餘部分的如上一般定義的雜芳基部分。 As used herein, unless expressly stated otherwise, the term "heteroaryl C 1 -C 3 alkyl" refers to a molecule as above attached to the remainder of the molecule via a C 1 -C 3 alkylene linker as defined above. Generally defined heteroaryl moiety.

如本文使用的，除非另外明確說明，否則術語「雜環基」或「雜環的」係指包含1、2或3個單獨地選自氮、氧和硫的雜原子的穩定的4員至6員非芳香族單環基團。該雜環基基團可以經由碳原子或雜原子鍵合至分子的其餘部分。雜環基的實例包括但不限於吡咯啉基、吡咯啶基、四氫呋喃基、四氫噻吩基、四氫噻喃基、哌啶基、哌𠯤基、四氫哌喃基、二氫異㗁唑基、二氧戊環基、𠰌啉基或δ-內醯胺基（δ-lactamyl）。As used herein, unless expressly stated otherwise, the term "heterocyclyl" or "heterocyclic" refers to a stable 4- to 4-membered group containing 1, 2, or 3 heteroatoms individually selected from nitrogen, oxygen, and sulfur. 6-membered non-aromatic monocyclic group. The heterocyclyl group can be bonded to the remainder of the molecule via a carbon atom or a heteroatom. Examples of heterocyclic groups include, but are not limited to, pyrrolinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, piperidinyl, piperanyl, tetrahydropyranyl, dihydroisinozole base, dioxolane group, 𠰌linyl group or δ-lactamyl group (δ-lactamyl).

在具有式 (I) 的化合物中一個或多個可能的不對稱碳原子的存在意味著所述化合物能以手性異構物形式存在，即鏡像異構物或非鏡像異構物的形式。作為圍繞單鍵的受限旋轉的結果，還可能存在阻轉異構物。式 (I) 旨在包括所有那些可能的異構物形式及其混合物。本發明包括具有式 (I) 的化合物的所有那些可能的異構物形式及其混合物。同樣地，式 (I) 旨在包括所有可能的互變異構物（包括內醯胺-內醯亞胺互變異構和酮-烯醇互變異構）（當存在時）。本發明包括具有式 (I) 的化合物的所有可能的互變異構物形式。類似地，在存在雙取代烯烴的情況下，該等能以 E或 Z形式或作為任何比例的二者的混合物而存在。本發明包括具有式 (I) 的化合物的所有該等可能的異構物形式及其混合物。 The presence of one or more possible asymmetric carbon atoms in compounds of formula (I) means that the compounds can exist as chiral isomers, ie as enantiomers or diastereomers. Atropisomers may also exist as a result of restricted rotation around single bonds. Formula (I) is intended to include all those possible isomeric forms and mixtures thereof. The present invention includes all those possible isomeric forms of the compounds of formula (I) and mixtures thereof. Likewise, formula (I) is intended to include all possible tautomers (including lactam-lactamimine tautomerism and keto-enol tautomerism) when present. The present invention includes all possible tautomeric forms of the compounds of formula (I). Similarly, where disubstituted olefins are present, these can exist in the E or Z form or as a mixture of the two in any proportion. The present invention includes all such possible isomeric forms of the compounds of formula (I) and mixtures thereof.

具有式 (I) 的化合物通常以農藝學上可接受的鹽、兩性離子或農藝學上可接受的兩性離子鹽的形式提供。本發明涵蓋所有此類農藝學上可接受的鹽、兩性離子及其全部比例的混合物。Compounds of formula (I) are generally provided in the form of an agronomically acceptable salt, a zwitterion or an agronomically acceptable zwitterionic salt. The present invention encompasses all such agronomically acceptable salts, zwitterions and mixtures thereof in all proportions.

本發明之合適的農藝學上可接受的鹽可以具有以下陽離子，該等陽離子包括但不限於金屬、胺的共軛酸和有機陽離子。合適的金屬的實例包括鋁、鈣、銫、銅、鋰、鎂、錳、鉀、鈉、鐵和鋅。合適的胺的實例包括烯丙胺、氨、戊胺、精胺酸、苯乙苄胺、苄星、丁烯基-2-胺、丁胺、丁基乙醇胺、環己胺、癸胺、二戊胺、二丁胺、二乙醇胺、二乙胺、二乙三胺、二庚胺、二己胺、二異戊胺、二異丙胺、二甲胺、二辛胺、二丙醇胺、二炔丙胺、二丙胺、十二胺、乙醇胺、乙胺、乙基丁胺、乙二胺、乙基庚胺、乙基辛胺、乙基丙醇胺、十七胺、庚胺、十六胺、己烯基-2-胺、己胺、己基庚胺、己基辛胺、組胺酸、吲哚啉、異戊胺、異丁醇胺、異丁胺、異丙醇胺、異丙胺、離胺酸、葡甲胺、甲氧基乙胺、甲胺、甲基丁胺、甲基乙胺、甲基己胺、甲基異丙胺、甲基壬胺、甲基十八胺、甲基十五胺、𠰌啉、N,N-二乙基乙醇胺、N-甲基哌𠯤、壬胺、十八胺、辛胺、油胺、十五胺、戊烯基-2-胺、苯氧基乙胺、甲基吡啶、哌𠯤、哌啶、丙醇胺、丙胺、丙二胺、吡啶、吡咯啶、二級丁胺、硬脂醯胺、牛脂胺、十四胺、三丁胺、十三胺、三甲胺、三庚胺、三己胺、三異丁胺、三異癸胺、三異丙胺、三甲胺、三戊胺、三丙胺、三(羥甲基)胺基甲烷和十一胺。合適的有機陽離子的實例包括苄基三丁基銨、苄基三甲基銨、苄基三苯基鏻、膽鹼、四丁基銨、四丁基鏻、四乙基銨、四乙基鏻、四甲基銨、四甲基鏻、四丙基銨、四丙基鏻、三丁基鋶、三丁基氧化鋶、三乙基鋶、三乙基氧化鋶、三甲基鋶、三甲基氧化鋶、三丙基鋶和三丙基氧化鋶。Suitable agronomically acceptable salts of the present invention may have cations including, but not limited to, metals, amine conjugate acids, and organic cations. Examples of suitable metals include aluminum, calcium, cesium, copper, lithium, magnesium, manganese, potassium, sodium, iron and zinc. Examples of suitable amines include allylamine, ammonia, pentylamine, arginine, phenethylbenzylamine, benzathine, butenyl-2-amine, butylamine, butylethanolamine, cyclohexylamine, decylamine, dipentylamine Amine, dibutylamine, diethanolamine, diethylamine, diethylenetriamine, diheptylamine, dihexylamine, diisoamylamine, diisopropylamine, dimethylamine, dioctylamine, dipropanolamine, diyne Propylamine, dipropylamine, dodecylamine, ethanolamine, ethylamine, ethylbutylamine, ethylenediamine, ethylheptylamine, ethyloctylamine, ethylpropanolamine, heptadecaamine, heptylamine, hexadecylamine, Hexenyl-2-amine, hexylamine, hexylheptylamine, hexyloctylamine, histidine, indoline, isopentylamine, isobutanolamine, isobutylamine, isopropanolamine, isopropylamine, dissociated amine Acid, meglumine, methoxyethylamine, methylamine, methylbutylamine, methylethylamine, methylhexylamine, methylisopropylamine, methylnonylamine, methyloctadecylamine, methylpentadecaamine Amine, N, N-diethylethanolamine, N-methylpiperdine, nonylamine, octadecaylamine, octylamine, oleylamine, pentadecylamine, pentenyl-2-amine, phenoxyethyl Amine, methylpyridine, piperidine, piperidine, propanolamine, propylamine, propylenediamine, pyridine, pyrrolidine, secondary butylamine, stearamide, tallowamine, tetradecaneamine, tributylamine, thirteen Amine, trimethylamine, triheptylamine, trihexylamine, triisobutylamine, triisodecylamine, triisopropylamine, trimethylamine, tripentylamine, tripropylamine, tris(hydroxymethyl)aminomethane and undecaamine . Examples of suitable organic cations include benzyltributylammonium, benzyltrimethylammonium, benzyltriphenylphosphonium, choline, tetrabutylammonium, tetrabutylphosphonium, tetraethylammonium, tetraethylphosphonium , tetramethylammonium, tetramethylphosphonium, tetrapropylammonium, tetrapropylphosphonium, tributylsulfonium, tributylsulfonium oxide, triethylsulfonium, triethylsulfonium oxide, trimethylsulfonium, trimethyl sulfonium oxide, tripropyl sulfonium oxide and tripropyl sulfonium oxide.

以下清單提供了關於根據本發明之具有式 (I) 的化合物的取代基X 1、X 2、X 3、X 4、Y、B、D、m、n、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11、R 12、R 13、R 14、R 15、R 16、R 17、R 18、R 19、R 20和R 21的定義，包括較佳的定義。對於該等取代基中的任何一個，以下給出的任何定義都可以結合以下或在本文檔中的其他地方給出的任何其他取代基的任何定義。 The following list provides the substituents X 1 , X 2 , X 3 , X 4 , Y, B, D, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , R 17 , R 18 , R 19 , R 20 and R 21 definitions, including preferred definitions. Any definition given below for any of these substituents may be combined with any definition given below or elsewhere in this document for any other substituent.

X 1係C-R 1、氮或N +-O -，較佳的是C-R 1或N +-O -，並且更較佳的是C-R 1。 X 1 is CR 1 , nitrogen or N + -O - , preferably CR 1 or N + -O - , and more preferably CR 1 .

X 2係C-R 17或氮，較佳的是氮。 X2 is CR 17 or nitrogen, preferably nitrogen.

X 3係C-R 18或氮，較佳的是C-R 18。 X 3 is CR 18 or nitrogen, preferably CR 18 .

X 4係C-R 19或氮，較佳的是C-R 19。 X 4 is CR 19 or nitrogen, preferably CR 19 .

較佳的是，前提係X 2、X 3和X 4中最多一個係氮，更較佳的是前提係X 2、X 3和X 4中的一個係氮。 Preferably, at most one of the prerequisite systems X 2 , X 3 and X 4 is nitrogen, and more preferably at most one of the prerequisite systems X 2 , X 3 and X 4 is nitrogen.

Y係C-H或氮。較佳的是，Y係C-H。Y is C-H or nitrogen. Preferably, Y is C-H.

B係O、S或NR 5。較佳的是，B係O、NH或NCH 3，更較佳的是，B係O或NH。 B is O, S or NR 5 . Preferably, B is O, NH or NCH 3 , more preferably, B is O or NH.

m係從0至2的整數。較佳的是，m係0或2，更較佳的是，m係0。m is an integer from 0 to 2. Preferably, m is 0 or 2, more preferably, m is 0.

n係從1至4的整數。較佳的是，n係從1至2的整數，更較佳的是，n係2。n is an integer from 1 to 4. Preferably, n is an integer from 1 to 2, and more preferably, n is 2.

R 1係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11。較佳的是，R 1係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基或C 1-C 4鹵代烷氧基，更較佳的是氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基，最較佳的是R 1係氫、氟、氯、甲基或三氟甲基。在一組實施方式中，R 1係鹵素，較佳的是氯。 R 1 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4- alkylamine group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkyl sulfonamide group, -CO 2 R 9 or -CONR 10 R 11 . Preferably, R 1 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy, more preferably It is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl, and the most preferred one is R 1 being hydrogen, fluorine, chlorine, methyl or trifluoromethyl. In one set of embodiments, R1 is halogen, preferably chlorine.

R 2係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、CO 2R 9或CONR 10R 11。較佳的是，R 2係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基或C 1-C 4鹵代烷氧基，更較佳的是氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基，最較佳的是氫、氟、氯、甲基或三氟甲基。還更較佳的是，R 2係氫；或者 R 2和R 19與它們所附接的碳原子一起形成5員或6員環，其可以是飽和的或部分或完全不飽和的，並且可以視需要含有一個或兩個選自氮、氧和硫的雜原子，並且可以被1至4個由R 16表示的基團取代。較佳的是，R 2和R 19與它們所附接的碳原子一起形成5員飽和環，其視需要含有一個或兩個氧原子，並且可以被1或2個由R 16表示的基團取代。 R 2 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4- alkylamine group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkyl sulfonamide group, CO 2 R 9 or CONR 10 R 11 . Preferably, R 2 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy, more preferably It is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl, and the most preferred is hydrogen, fluorine, chlorine, methyl or trifluoromethyl. Still more preferably, R 2 is hydrogen; or R 2 and R 19 together with the carbon atom to which they are attached form a 5- or 6-membered ring, which may be saturated or partially or fully unsaturated, and may Optionally contains one or two heteroatoms selected from nitrogen, oxygen and sulfur, and may be substituted by 1 to 4 groups represented by R 16 . Preferably, R 2 and R 19 together with the carbon atoms to which they are attached form a 5-membered saturated ring, optionally containing one or two oxygen atoms, and may be substituted by 1 or 2 groups represented by R 16 replace.

R 3係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷硫基或C 1-C 4烷基磺醯基。較佳的是，R 3係氫、氯或氟，更較佳的是氫或氟。甚至更較佳的是，R 3係氟。 R 3 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkylthio or C 1 -C 4 alkylsulfonyl group. Preferably, R 3 is hydrogen, chlorine or fluorine, more preferably hydrogen or fluorine. Even more preferably, R3 is fluorine.

R 4係氫、鹵素、氰基、硝基、胺基羰基、胺基硫代羰基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基或C 1-C 4烷基磺醯基。較佳的是，R 4係氫、氯、溴、氰基或胺基硫代羰基，更較佳的是氯、溴或氰基，還更較佳的是氯或溴。甚至更較佳的是，R 4係氯。 R 4 is hydrogen, halogen, cyano, nitro, aminocarbonyl, aminothiocarbonyl, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy or C 1 -C 4 alkylsulfonyl. Preferably, R 4 is hydrogen, chlorine, bromine, cyano or aminothiocarbonyl, more preferably chlorine, bromine or cyano, still more preferably chlorine or bromine. Even more preferably, R 4 is chlorine.

R 5係氫、羥基、C 1-C 6烷基或C 1-C 4烷氧基。較佳的是，R 5係氫。 R 5 is hydrogen, hydroxyl, C 1 -C 6 alkyl or C 1 -C 4 alkoxy. Preferably, R5 is hydrogen.

R 6和R 7各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、羥基、C 1-C 4烷氧基、C 1-C 4烷氧基羰基或-CH 2OR 12；前提係R 6和R 7在同一碳原子上不皆為羥基，或者在同一碳原子或不同碳原子上的兩個R 6和R 7基團一起形成C 1-C 5伸烷基鏈，該鏈含有0、1或2個氧原子，被1至3個由R 15表示的基團取代；或者，在同一碳原子上的兩個R 6和R 7基團一起形成C 2-C 3烯烴。較佳的是，R 6和R 7各自獨立地是氫、鹵素、C 1-C 4烷基或C 1-C 4烷氧基羰基，更較佳的是氫、鹵素或C 1-C 2烷基，還更較佳的是氫、氯或甲基。甚至還更較佳的是，R 6和R 7各自獨立地是氫或甲基。在特別較佳的實施方式中，R 6和R 7兩者皆為氫。 R 6 and R 7 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, hydroxyl, C 1 -C 4 alkoxy, C 1 -C 4 alkoxycarbonyl, or -CH 2 OR 12 ; provided that R 6 and R 7 are not both hydroxyl groups on the same carbon atom, or two R 6 and R 7 groups on the same carbon atom or different carbon atoms together form C 1 -C 5 Alkylene chain containing 0, 1 or 2 oxygen atoms substituted by 1 to 3 groups represented by R 15 ; alternatively, two R 6 and R 7 groups on the same carbon atom together form C 2 -C 3 alkenes. Preferably, R 6 and R 7 are each independently hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxycarbonyl, more preferably hydrogen, halogen or C 1 -C 2 Alkyl, still more preferably hydrogen, chlorine or methyl. Even more preferably, R 6 and R 7 are each independently hydrogen or methyl. In particularly preferred embodiments, both R 6 and R 7 are hydrogen.

R 8係OR 9、SR 9或NR 10R 11。較佳的是，R 8係OR 9。 R 8 is OR 9 , SR 9 or NR 10 R 11 . Preferably, R8 is OR9 .

R 9係氫、C 1-C 10烷基、C 1-C 10鹵代烷基、C 3-C 6烯基、C 3-C 6鹵代烯基、C 3-C 6炔基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 6-C 10芳基C 1-C 3烷基、被1至4個由R 13表示的基團取代的C 6-C 10芳基C 1-C 3烷基、雜芳基C 1-C 3烷基、或被1至3個由R 13表示的基團取代的雜芳基C 1-C 3烷基。較佳的是，R 9係氫、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 2烷氧基C 1-C 2烷基、苯基C 1-C 2烷基、或被1-2個基團R 13取代的苯基C 1-C 2烷基，更較佳的是氫、C 1-C 4烷基、C 1-C 2烷氧基C 1-C 2烷基、或苯基C 1-C 2烷基，還更較佳的是氫、C 1-C 4烷基或苯基C 1-C 2烷基。甚至更較佳的是，R 9係C 1-C 4烷基。甚至還更較佳的是，R 9係甲基。 R 9 is hydrogen, C 1 -C 10 alkyl, C 1 -C 10 haloalkyl, C 3 -C 6 alkenyl, C 3 -C 6 haloalkenyl, C 3 -C 6 alkynyl, C 1 - C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 6 -C 10 aryl C 1 -C 3 alkyl, substituted by 1 to 4 A C 6 -C 10 aryl C 1 -C 3 alkyl group, a heteroaryl C 1 -C 3 alkyl group substituted by a group represented by R 13 , or a heteroaryl group substituted by 1 to 3 groups represented by R 13 Aryl C 1 -C 3 alkyl. Preferably, R 9 is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 2 alkoxy C 1 -C 2 alkyl, phenyl C 1 -C 2 alkyl group, or phenyl C 1 -C 2 alkyl substituted by 1-2 groups R 13 , more preferably hydrogen, C 1 -C 4 alkyl, C 1 -C 2 alkoxy C 1 - C 2 alkyl, or phenyl C 1 -C 2 alkyl, more preferably hydrogen, C 1 -C 4 alkyl or phenyl C 1 -C 2 alkyl. Even more preferably, R 9 is C 1 -C 4 alkyl. Even more preferably, R 9 is methyl.

R 10係氫、C 1-C 6烷基、SO 2R 14。較佳的是，R 10係氫或SO 2R 14，更較佳的是SO 2R 14。 R 10 is hydrogen, C 1 -C 6 alkyl, SO 2 R 14 . Preferably, R 10 is hydrogen or SO 2 R 14 , more preferably SO 2 R 14 .

R 11係氫或C 1-C 6烷基。較佳的是，R 11係氫。 R 11 is hydrogen or C 1 -C 6 alkyl. Preferably, R 11 is hydrogen.

或者，R 10和R 11與它們所附接的氮一起形成3員至6員雜環基環。 Alternatively, R 10 and R 11 together with the nitrogen to which they are attached form a 3 to 6 membered heterocyclyl ring.

R 12係氫、C 1-C 4烷基或C 1-C 4烷基羰基。較佳的是，R 12係氫、C 1-C 2烷基或C 1-C 2烷基羰基，更較佳的是氫或甲基。 R 12 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkylcarbonyl. Preferably, R 12 is hydrogen, C 1 -C 2 alkyl or C 1 -C 2 alkylcarbonyl, more preferably hydrogen or methyl.

R 13係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基。較佳的是，R 13係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基。 R 13 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, cyano or C 1 -C 4 alkyl sulfonate Jiji. Preferably, R 13 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, cyano or C 1 - C 4 alkylsulfonyl group.

R 14係C 1-C 4烷基、C 1-C 4鹵代烷基或C 1-C 4烷基(C 1-C 4烷基)胺基。較佳的是，R 14係C 1-C 4烷基或C 1-C 4烷基(C 1-C 4烷基)胺基，更較佳的是甲基或異丙基(甲基)胺基。 R 14 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkyl (C 1 -C 4 alkyl)amine group. Preferably, R 14 is C 1 -C 4 alkyl or C 1 -C 4 alkyl (C 1 -C 4 alkyl) amino group, more preferably methyl or isopropyl (methyl) Amino group.

R 15係氫、鹵素、C 1-C 4烷基或C 1-C 4鹵代烷基。較佳的是，R 15係氫、鹵素或C 1-C 2烷基，更較佳的是氫或甲基，還更較佳的是氫。 R 15 is hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl. Preferably, R 15 is hydrogen, halogen or C 1 -C 2 alkyl, more preferably hydrogen or methyl, still more preferably hydrogen.

R 16係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基。較佳的是，R 16係鹵素，更較佳的是氟。 R 16 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, cyano or C 1 -C 4 alkyl sulfonate Jiji. Preferably, R 16 is halogen, more preferably fluorine.

R 17係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11。較佳的是，R 17係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基或C 1-C 4鹵代烷氧基，更較佳的是氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基，最較佳的是氫、氟、氯、甲基或三氟甲基。 R 17 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4- alkylamine group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkyl sulfonamide group, -CO 2 R 9 or -CONR 10 R 11 . Preferably, R 17 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy, more preferably It is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl, and the most preferred is hydrogen, fluorine, chlorine, methyl or trifluoromethyl.

R 18係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11。較佳的是，R 18係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基或C 1-C 4鹵代烷氧基，更較佳的是氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基，還更較佳的是氫、氟、氯、甲基或三氟甲基。甚至更較佳的是，R 18係氫。 R 18 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4- alkylamine group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkyl sulfonamide group, -CO 2 R 9 or -CONR 10 R 11 . Preferably, R 18 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy, more preferably is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl, and more preferably hydrogen, fluorine, chlorine, methyl or trifluoromethyl. Even more preferably, R18 is hydrogen.

R 19係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11。較佳的是，R 19係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基或C 1-C 4鹵代烷氧基，更較佳的是氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基，還更較佳的是氫、氟、氯、甲基、二氟甲基、三氟甲基或1,1-二氟乙基。甚至更較佳的是，R 19係氯。 R 19 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4- alkylamine group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkyl sulfonamide group, -CO 2 R 9 or -CONR 10 R 11 . Preferably, R 19 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy, more preferably is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl, and more preferably hydrogen, fluorine, chlorine, methyl, difluoromethyl, trifluoromethyl or 1, 1-Difluoroethyl. Even more preferably, R19 is chlorine.

R 20和R 21各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、C 1-C 4烷氧基或-CH 2OR 12。較佳的是，R 20和R 21各自獨立地是氫、C 1-C 4烷基或C 1-C 2烷氧基，更較佳的是氫或C 1-C 2烷基，還更較佳的是氫或甲基。 R 20 and R 21 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 4 alkoxy, or -CH 2 OR 12 . Preferably, R 20 and R 21 are each independently hydrogen, C 1 -C 4 alkyl or C 1 -C 2 alkoxy, more preferably hydrogen or C 1 -C 2 alkyl, and more preferably Preferred is hydrogen or methyl.

在其中X 1、X 2、X 3和X 4中的兩個係氮的實施方式中，較佳的是X 2或X 3係氮。在其中X 1、X 2、X 3和X 4中的一個係氮的實施方式中，較佳的是X 2係氮。 In embodiments in which two of X 1 , X 2 , X 3 and X 4 are nitrogen, preferably X 2 or X 3 is nitrogen. In embodiments in which one of X 1 , X 2 , X 3 and X 4 is nitrogen, preferably X 2 is nitrogen.

一個亞組的較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係氮； X 3係C-R 18； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係1或2； R 1係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基； R 2係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基； R 3係氫、氯或氟； R 4係氯、溴或氰基； R 6和R 7各自獨立地是氫、鹵素或C 1-C 2烷基； R 8係OR 9； R 9係氫、C 1-C 4烷基、C 1-C 2烷氧基C 1-C 2烷基或苯基C 1-C 2烷基； R 18係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基； R 19係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基。 R 20和R 21各自獨立地是氫或C 1-C 2烷基。 Preferred compounds of a subgroup are the following compounds, among which: X1 is CR1 ; X2 is nitrogen; X3 is CR18 ; X4 is CR19 ; Y is CH; B is O or NH ; m is 0; n is 1 or 2; R 1 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl; R 2 is hydrogen, fluorine, chlorine, C 1 -C 2 Alkyl or C 1 -C 2 haloalkyl; R 3 is hydrogen, chlorine or fluorine; R 4 is chlorine, bromine or cyano; R 6 and R 7 are each independently hydrogen, halogen or C 1 -C 2 alkyl ; R 8 is OR 9 ; R 9 is hydrogen, C 1 -C 4 alkyl, C 1 -C 2 alkoxy C 1 -C 2 alkyl or phenyl C 1 -C 2 alkyl; R 18 is hydrogen , fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl; R 19 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl. R 20 and R 21 are each independently hydrogen or C 1 -C 2 alkyl.

另一個亞組的較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係C-R 17； X 3係氮； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係1或2； R 1係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基； R 2和R 19與它們所附接的碳原子一起形成5員或6員環，其含有一個或兩個選自氮、氧和硫的雜原子，並且被1至4個由R 16表示的基團取代； R 3係氫、氯或氟； R 4係氯、溴或氰基； R 6和R 7獨立地是氫、鹵素或C 1-C 2烷基； R 8係OR 9； R 9係氫、C 1-C 4烷基、C 1-C 2烷氧基C 1-C 2烷基或苯基C 1-C 2烷基； R 16係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基； R 17係氫、氟、氯、C 1-C 2烷基或C 1-C 2鹵代烷基。 R 20和R 21各自獨立地是氫或C 1-C 2烷基。 Preferred compounds of another subgroup are the following compounds, among which: X1 is CR1 ; X2 is CR17 ; X3 is nitrogen; X4 is CR19 ; Y is CH; B is O or NH; m is 0; n is 1 or 2; R 1 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 haloalkyl; R 2 and R 19 and the carbon atoms to which they are attached Together they form a 5- or 6-membered ring containing one or two heteroatoms selected from nitrogen, oxygen and sulfur and substituted by 1 to 4 groups represented by R 16 ; R 3 is hydrogen, chlorine or fluorine; R 4 is chlorine, bromine or cyano; R 6 and R 7 are independently hydrogen, halogen or C 1 -C 2 alkyl; R 8 is OR 9 ; R 9 is hydrogen, C 1 -C 4 alkyl, C 1 -C 2 alkoxy C 1 -C 2 alkyl or phenyl C 1 -C 2 alkyl; R 16 series halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, cyano or C 1 -C 4 alkylsulfonyl; R 17 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl or C 1 -C 2 Haloalkyl. R 20 and R 21 are each independently hydrogen or C 1 -C 2 alkyl.

一個亞組的更較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係氮； X 3係C-R 18； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係2； R 1係氫、氟、氯、甲基或三氟甲基； R 2係氫、氟、氯、甲基或三氟甲基； R 3係氫或氟； R 4係氯或溴； R 6和R 7各自獨立地是氫、氯或甲基； R 8係OR 9； R 9係氫、C 1-C 4烷基或苯基C 1-C 2烷基； R 18係氫、氟、氯、甲基或三氟甲基； R 19係氫、氟、氯、甲基、二氟甲基、三氟甲基或1,1-二氟乙基。 R 20和R 21各自獨立地是氫或甲基。 A subgroup of more preferred compounds are compounds in which: X1 is CR1 ; X2 is nitrogen; X3 is CR18 ; X4 is CR19 ; Y is CH; B is O or NH; m is 0; n is 2; R 1 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl; R 2 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl; R 3 is hydrogen or fluorine ; R 4 is chlorine or bromine; R 6 and R 7 are each independently hydrogen, chlorine or methyl; R 8 is OR 9 ; R 9 is hydrogen, C 1 -C 4 alkyl or phenyl C 1 -C 2 Alkyl; R 18 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl; R 19 is hydrogen, fluorine, chlorine, methyl, difluoromethyl, trifluoromethyl or 1,1-difluoroethyl . R 20 and R 21 are each independently hydrogen or methyl.

另一個亞組的更較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係C-R 17； X 3係氮； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係2； R 1係氫、氟、氯、甲基或三氟甲基； R 2和R 19與它們所附接的碳原子一起形成飽和5員環，其含有一個或兩個氧原子並且被1至3個由R 16表示的基團取代； R 3係氫或氟； R 4係氯或溴； R 6和R 7各自獨立地是氫、氯或甲基； R 8係OR 9； R 9係氫、C 1-C 4烷基或苯基C 1-C 2烷基； R 16係鹵素； R 17係氫、氟、氯、甲基或三氟甲基；並且 R 20和R 21各自獨立地是氫或甲基。 More preferred compounds of another subgroup are the following compounds, among which: X1 is CR1 ; X2 is CR17 ; X3 is nitrogen ; or NH; m is 0; n is 2; R 1 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl; R 2 and R 19 together with the carbon atoms to which they are attached form a saturated 5-membered ring containing One or two oxygen atoms and substituted by 1 to 3 groups represented by R 16 ; R 3 is hydrogen or fluorine; R 4 is chlorine or bromine; R 6 and R 7 are each independently hydrogen, chlorine or methyl ; R 8 is OR 9 ; R 9 is hydrogen, C 1 -C 4 alkyl or phenyl C 1 -C 2 alkyl; R 16 is halogen; R 17 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl group; and R 20 and R 21 are each independently hydrogen or methyl.

另一個亞組的更更較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係氮； X 3係C-R 18； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係2； R 1係鹵素； R 2係氫； R 3係鹵素； R 4係鹵素； R 6和R 7皆為氫； R 8係OR 9； R 9係C 1-C 3烷基； R 18係氫； R 19係鹵素；並且 R 20和R 21各自獨立地是氫或甲基。 More preferred compounds of another subgroup are the following compounds, among which: X1 is CR1 ; X2 is nitrogen; X3 is CR18 ; X4 is CR19 ; Y is CH; B is O or NH; m is 0; n is 2; R 1 is halogen; R 2 is hydrogen; R 3 is halogen; R 4 is halogen; R 6 and R 7 are both hydrogen; R 8 is OR 9 ; R 9 is C 1 -C 3 alkyl; R 18 is hydrogen; R 19 is halogen; and R 20 and R 21 are each independently hydrogen or methyl.

一個亞組的特別較佳的化合物係以下化合物，在該等化合物中： X 1係C-R 1； X 2係氮； X 3係C-R 18； X 4係C-R 19； Y係C-H； B係O或NH； m係0； n係2； R 1係氯； R 2係氫； R 3係氟； R 4係氯； R 6和R 7皆為氫； R 8係OR 9； R 9係甲基； R 18係氫； R 19係氯；並且 R 20和R 21各自獨立地是氫或甲基。 實例的表 Particularly preferred compounds of a subgroup are compounds in which : X1 is CR1 ; X2 is nitrogen; X3 is CR18 ; NH; m is 0; n is 2; R 1 is chlorine; R 2 is hydrogen; R 3 is fluorine; R 4 is chlorine; R 6 and R 7 are both hydrogen; R 8 is OR 9 ; R 9 is methyl ; R 18 is hydrogen; R 19 is chlorine; and R 20 and R 21 are each independently hydrogen or methyl. instance table

下表1揭露了1140種具有式 (I) 的特定化合物，分別指定為化合物1-1至1-1140，其中R 3係氫，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H，並且B係氧。 [ 表 1 ] 化合物編號 X 1 X 2 X 3 X 4 R 2 D R 8 1-1 CCl CH CH CCH 3 H CH 2 OH 1-2 CCl CH CH CCH 3 H CH 2 OCH 3 1-3 CCl CH CH CCH 3 H CH 2 OCH 2CH 3 1-4 CCl CH CH CCH 3 H CH 2 OCH 2Ph 1-5 CCl CH CH CCH 3 H CH 2 NHSO 2CH 3 1-6 CCl CH CH CCH 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-7 N CH N CCF 3 H CH 2 OH 1-8 N CH N CCF 3 H CH 2 OCH 3 1-9 N CH N CCF 3 H CH 2 OCH 2CH 3 1-10 N CH N CCF 3 H CH 2 OCH 2Ph 1-11 N CH N CCF 3 H CH 2 NHSO 2CH 3 1-12 N CH N CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-13 NO CCl CH CCF 3 H CH 2 OH 1-14 NO CCl CH CCF 3 H CH 2 OCH 3 1-15 NO CCl CH CCF 3 H CH 2 OCH 2CH 3 1-16 NO CCl CH CCF 3 H CH 2 OCH 2Ph 1-17 NO CCl CH CCF 3 H CH 2 NHSO 2CH 3 1-18 NO CCl CH CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-19 CF N CH CF H CH 2 OH 1-20 CF N CH CF H CH 2 OCH 3 1-21 CF N CH CF H CH 2 OCH 2CH 3 1-22 CF N CH CF H CH 2 OCH 2Ph 1-23 CF N CH CF H CH 2 NHSO 2CH 3 1-24 CF N CH CF H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-25 CCl N CH CF H CH 2 OH 1-26 CCl N CH CF H CH 2 OCH 3 1-27 CCl N CH CF H CH 2 OCH 2CH 3 1-28 CCl N CH CF H CH 2 OCH 2Ph 1-29 CCl N CH CF H CH 2 NHSO 2CH 3 1-30 CCl N CH CF H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-31 CCl N CH CCl H CH 2 OH 1-32 CCl N CH CCl H CH 2 OCH 3 1-33 CCl N CH CCl H CH 2 OCH 2CH 3 1-34 CCl N CH CCl H CH 2 OCH 2Ph 1-35 CCl N CH CCl H CH 2 NHSO 2CH 3 1-36 CCl N CH CCl H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-37 CCF 3 N CH CCl H CH 2 OH 1-38 CCF 3 N CH CCl H CH 2 OCH 3 1-39 CCF 3 N CH CCl H CH 2 OCH 2CH 3 1-40 CCF 3 N CH CCl H CH 2 OCH 2Ph 1-41 CCF 3 N CH CCl H CH 2 NHSO 2CH 3 1-42 CCF 3 N CH CCl H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-43 CCl N CH CBr H CH 2 OH 1-44 CCl N CH CBr H CH 2 OCH 3 1-45 CCl N CH CBr H CH 2 OCH 2CH 3 1-46 CCl N CH CBr H CH 2 OCH 2Ph 1-47 CCl N CH CBr H CH 2 NHSO 2CH 3 1-48 CCl N CH CBr H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-49 CCl N CH CCH 3 H CH 2 OH 1-50 CCl N CH CCH 3 H CH 2 OCH 3 1-51 CCl N CH CCH 3 H CH 2 OCH 2CH 3 1-52 CCl N CH CCH 3 H CH 2 OCH 2Ph 1-53 CCl N CH CCH 3 H CH 2 NHSO 2CH 3 1-54 CCl N CH CCH 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-55 CCl N CH CCF 2H H CH 2 OH 1-56 CCl N CH CCF 2H H CH 2 OCH 3 1-57 CCl N CH CCF 2H H CH 2 OCH 2CH 3 1-58 CCl N CH CCF 2H H CH 2 OCH 2Ph 1-59 CCl N CH CCF 2H H CH 2 NHSO 2CH 3 1-60 CCl N CH CCF 2H H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-61 CCl N CH CCF 2CH 3 H CH 2 OH 1-62 CCl N CH CCF 2CH 3 H CH 2 OCH 3 1-63 CCl N CH CCF 2CH 3 H CH 2 OCH 2CH 3 1-64 CCl N CH CCF 2CH 3 H CH 2 OCH 2Ph 1-65 CCl N CH CCF 2CH 3 H CH 2 NHSO 2CH 3 1-66 CCl N CH CCF 2CH 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-67 CCl N CH CCF 3 H CH 2 OH 1-68 CCl N CH CCF 3 H CH 2 OCH 3 1-69 CCl N CH CCF 3 H CH 2 OCH 2CH 3 1-70 CCl N CH CCF 3 H CH 2 OCH 2Ph 1-71 CCl N CH CCF 3 H CH 2 NHSO 2CH 3 1-72 CCl N CH CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-73 CH N CH CCF 3 H CH 2 OH 1-74 CH N CH CCF 3 H CH 2 OCH 3 1-75 CH N CH CCF 3 H CH 2 OCH 2CH 3 1-76 CH N CH CCF 3 H CH 2 OCH 2Ph 1-77 CH N CH CCF 3 H CH 2 NHSO 2CH 3 1-78 CH N CH CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-79 CF N CH CCF 3 H CH 2 OH 1-80 CF N CH CCF 3 H CH 2 OCH 3 1-81 CF N CH CCF 3 H CH 2 OCH 2CH 3 1-82 CF N CH CCF 3 H CH 2 OCH 2Ph 1-83 CF N CH CCF 3 H CH 2 NHSO 2CH 3 1-84 CF N CH CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-85 CBr N CH CCF 3 H CH 2 OH 1-86 CBr N CH CCF 3 H CH 2 OCH 3 1-87 CBr N CH CCF 3 H CH 2 OCH 2CH 3 1-88 CBr N CH CCF 3 H CH 2 OCH 2Ph 1-89 CBr N CH CCF 3 H CH 2 NHSO 2CH 3 1-90 CBr N CH CCF 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-91 CCl N CH CSO 2CH 3 H CH 2 OH 1-92 CCl N CH CSO 2CH 3 H CH 2 OCH 3 1-93 CCl N CH CSO 2CH 3 H CH 2 OCH 2CH 3 1-94 CCl N CH CSO 2CH 3 H CH 2 OCH 2Ph 1-95 CCl N CH CSO 2CH 3 H CH 2 NHSO 2CH 3 1-96 CCl N CH CSO 2CH 3 H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-97 CH CH N *COCF 2O CH 2 OH 1-98 CH CH N *COCF 2O CH 2 OCH 3 1-99 CH CH N *COCF 2O CH 2 OCH 2CH 3 1-100 CH CH N *COCF 2O CH 2 OCH 2Ph 1-101 CH CH N *COCF 2O CH 2 NHSO 2CH 3 1-102 CH CH N *COCF 2O CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-103 CH F N CH CF 3 CH 2 OH 1-104 CH F N CH CF 3 CH 2 OCH 3 1-105 CH F N CH CF 3 CH 2 OCH 2CH 3 1-106 CH F N CH CF 3 CH 2 OCH 2Ph 1-107 CH F N CH CF 3 CH 2 NHSO 2CH 3 1-108 CH F N CH CF 3 CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-109 CH CCl CCl N H CH 2 OH 1-110 CH CCl CCl N H CH 2 OCH 3 1-111 CH CCl CCl N H CH 2 OCH 2CH 3 1-112 CH CCl CCl N H CH 2 OCH 2Ph 1-113 CH CCl CCl N H CH 2 NHSO 2CH 3 1-114 CH CCl CCl N H CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-115 CCl CH CH CCH 3 H CH(CH 3) OH 1-116 CCl CH CH CCH 3 H CH(CH 3) OCH 3 1-117 CCl CH CH CCH 3 H CH(CH 3) OCH 2CH 3 1-118 CCl CH CH CCH 3 H CH(CH 3) OCH 2Ph 1-119 CCl CH CH CCH 3 H CH(CH 3) NHSO 2CH 3 1-120 CCl CH CH CCH 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-121 N CH N CCF 3 H CH(CH 3) OH 1-122 N CH N CCF 3 H CH(CH 3) OCH 3 1-123 N CH N CCF 3 H CH(CH 3) OCH 2CH 3 1-124 N CH N CCF 3 H CH(CH 3) OCH 2Ph 1-125 N CH N CCF 3 H CH(CH 3) NHSO 2CH 3 1-126 N CH N CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-127 NO CCl CH CCF 3 H CH(CH 3) OH 1-128 NO CCl CH CCF 3 H CH(CH 3) OCH 3 1-129 NO CCl CH CCF 3 H CH(CH 3) OCH 2CH 3 1-130 NO CCl CH CCF 3 H CH(CH 3) OCH 2Ph 1-131 NO CCl CH CCF 3 H CH(CH 3) NHSO 2CH 3 1-132 NO CCl CH CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-133 CF N CH CF H CH(CH 3) OH 1-134 CF N CH CF H CH(CH 3) OCH 3 1-135 CF N CH CF H CH(CH 3) OCH 2CH 3 1-136 CF N CH CF H CH(CH 3) OCH 2Ph 1-137 CF N CH CF H CH(CH 3) NHSO 2CH 3 1-138 CF N CH CF H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-139 CCl N CH CF H CH(CH 3) OH 1-140 CCl N CH CF H CH(CH 3) OCH 3 1-141 CCl N CH CF H CH(CH 3) OCH 2CH 3 1-142 CCl N CH CF H CH(CH 3) OCH 2Ph 1-143 CCl N CH CF H CH(CH 3) NHSO 2CH 3 1-144 CCl N CH CF H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-145 CCl N CH CCl H CH(CH 3) OH 1-146 CCl N CH CCl H CH(CH 3) OCH 3 1-147 CCl N CH CCl H CH(CH 3) OCH 2CH 3 1-148 CCl N CH CCl H CH(CH 3) OCH 2Ph 1-149 CCl N CH CCl H CH(CH 3) NHSO 2CH 3 1-150 CCl N CH CCl H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-151 CCF 3 N CH CCl H CH(CH 3) OH 1-152 CCF 3 N CH CCl H CH(CH 3) OCH 3 1-153 CCF 3 N CH CCl H CH(CH 3) OCH 2CH 3 1-154 CCF 3 N CH CCl H CH(CH 3) OCH 2Ph 1-155 CCF 3 N CH CCl H CH(CH 3) NHSO 2CH 3 1-156 CCF 3 N CH CCl H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-157 CCl N CH CBr H CH(CH 3) OH 1-158 CCl N CH CBr H CH(CH 3) OCH 3 1-159 CCl N CH CBr H CH(CH 3) OCH 2CH 3 1-160 CCl N CH CBr H CH(CH 3) OCH 2Ph 1-161 CCl N CH CBr H CH(CH 3) NHSO 2CH 3 1-162 CCl N CH CBr H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-163 CCl N CH CCH 3 H CH(CH 3) OH 1-164 CCl N CH CCH 3 H CH(CH 3) OCH 3 1-165 CCl N CH CCH 3 H CH(CH 3) OCH 2CH 3 1-166 CCl N CH CCH 3 H CH(CH 3) OCH 2Ph 1-167 CCl N CH CCH 3 H CH(CH 3) NHSO 2CH 3 1-168 CCl N CH CCH 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-169 CCl N CH CCF 2H H CH(CH 3) OH 1-170 CCl N CH CCF 2H H CH(CH 3) OCH 3 1-171 CCl N CH CCF 2H H CH(CH 3) OCH 2CH 3 1-172 CCl N CH CCF 2H H CH(CH 3) OCH 2Ph 1-173 CCl N CH CCF 2H H CH(CH 3) NHSO 2CH 3 1-174 CCl N CH CCF 2H H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-175 CCl N CH CCF 2CH 3 H CH(CH 3) OH 1-176 CCl N CH CCF 2CH 3 H CH(CH 3) OCH 3 1-177 CCl N CH CCF 2CH 3 H CH(CH 3) OCH 2CH 3 1-178 CCl N CH CCF 2CH 3 H CH(CH 3) OCH 2Ph 1-179 CCl N CH CCF 2CH 3 H CH(CH 3) NHSO 2CH 3 1-180 CCl N CH CCF 2CH 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-181 CCl N CH CCF 3 H CH(CH 3) OH 1-182 CCl N CH CCF 3 H CH(CH 3) OCH 3 1-183 CCl N CH CCF 3 H CH(CH 3) OCH 2CH 3 1-184 CCl N CH CCF 3 H CH(CH 3) OCH 2Ph 1-185 CCl N CH CCF 3 H CH(CH 3) NHSO 2CH 3 1-186 CCl N CH CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-187 CH N CH CCF 3 H CH(CH 3) OH 1-188 CH N CH CCF 3 H CH(CH 3) OCH 3 1-189 CH N CH CCF 3 H CH(CH 3) OCH 2CH 3 1-190 CH N CH CCF 3 H CH(CH 3) OCH 2Ph 1-191 CH N CH CCF 3 H CH(CH 3) NHSO 2CH 3 1-192 CH N CH CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-193 CF N CH CCF 3 H CH(CH 3) OH 1-194 CF N CH CCF 3 H CH(CH 3) OCH 3 1-195 CF N CH CCF 3 H CH(CH 3) OCH 2CH 3 1-196 CF N CH CCF 3 H CH(CH 3) OCH 2Ph 1-197 CF N CH CCF 3 H CH(CH 3) NHSO 2CH 3 1-198 CF N CH CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-199 CBr N CH CCF 3 H CH(CH 3) OH 1-200 CBr N CH CCF 3 H CH(CH 3) OCH 3 1-201 CBr N CH CCF 3 H CH(CH 3) OCH 2CH 3 1-202 CBr N CH CCF 3 H CH(CH 3) OCH 2Ph 1-203 CBr N CH CCF 3 H CH(CH 3) NHSO 2CH 3 1-204 CBr N CH CCF 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-205 CCl N CH CSO 2CH 3 H CH(CH 3) OH 1-206 CCl N CH CSO 2CH 3 H CH(CH 3) OCH 3 1-207 CCl N CH CSO 2CH 3 H CH(CH 3) OCH 2CH 3 1-208 CCl N CH CSO 2CH 3 H CH(CH 3) OCH 2Ph 1-209 CCl N CH CSO 2CH 3 H CH(CH 3) NHSO 2CH 3 1-210 CCl N CH CSO 2CH 3 H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-211 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-212 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-213 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-214 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-215 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-216 CH CH N *COCF 2O CH(CH 3) CH(CH 3) 1-217 CH CF N CH CF 3 CH(CH 3) OH 1-218 CH CF N CH CF 3 CH(CH 3) OCH 3 1-219 CH CF N CH CF 3 CH(CH 3) OCH 2CH 3 1-220 CH CF N CH CF 3 CH(CH 3) OCH 2Ph 1-221 CH CF N CH CF 3 CH(CH 3) NHSO 2CH 3 1-222 CH CF N CH CF 3 CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-223 CH CCl CCl N H CH(CH 3) OH 1-224 CH CCl CCl N H CH(CH 3) OCH 3 1-225 CH CCl CCl N H CH(CH 3) OCH 2CH 3 1-226 CH CCl CCl N H CH(CH 3) OCH 2Ph 1-227 CH CCl CCl N H CH(CH 3) NHSO 2CH 3 1-228 CH CCl CCl N H CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-229 CCl CH CH CCH 3 H C(CH 3) 2 OH 1-230 CCl CH CH CCH 3 H C(CH 3) 2 OCH 3 1-231 CCl CH CH CCH 3 H C(CH 3) 2 OCH 2CH 3 1-232 CCl CH CH CCH 3 H C(CH 3) 2 OCH 2Ph 1-233 CCl CH CH CCH 3 H C(CH 3) 2 NHSO 2CH 3 1-234 CCl CH CH CCH 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-235 N CH N CCF 3 H C(CH 3) 2 OH 1-236 N CH N CCF 3 H C(CH 3) 2 OCH 3 1-237 N CH N CCF 3 H C(CH 3) 2 OCH 2CH 3 1-238 N CH N CCF 3 H C(CH 3) 2 OCH 2Ph 1-239 N CH N CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-240 N CH N CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-241 NO CCl CH CCF 3 H C(CH 3) 2 OH 1-242 NO CCl CH CCF 3 H C(CH 3) 2 OCH 3 1-243 NO CCl CH CCF 3 H C(CH 3) 2 OCH 2CH 3 1-244 NO CCl CH CCF 3 H C(CH 3) 2 OCH 2Ph 1-245 NO CCl CH CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-246 NO CCl CH CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-247 CF N CH CF H C(CH 3) 2 OH 1-248 CF N CH CF H C(CH 3) 2 OCH 3 1-249 CF N CH CF H C(CH 3) 2 OCH 2CH 3 1-250 CF N CH CF H C(CH 3) 2 OCH 2Ph 1-251 CF N CH CF H C(CH 3) 2 NHSO 2CH 3 1-252 CF N CH CF H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-253 CCl N CH CF H C(CH 3) 2 OH 1-254 CCl N CH CF H C(CH 3) 2 OCH 3 1-255 CCl N CH CF H C(CH 3) 2 OCH 2CH 3 1-256 CCl N CH CF H C(CH 3) 2 OCH 2Ph 1-257 CCl N CH CF H C(CH 3) 2 NHSO 2CH 3 1-258 CCl N CH CF H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-259 CCl N CH CCl H C(CH 3) 2 OH 1-260 CCl N CH CCl H C(CH 3) 2 OCH 3 1-261 CCl N CH CCl H C(CH 3) 2 OCH 2CH 3 1-262 CCl N CH CCl H C(CH 3) 2 OCH 2Ph 1-263 CCl N CH CCl H C(CH 3) 2 NHSO 2CH 3 1-264 CCl N CH CCl H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-265 CCF 3 N CH CCl H C(CH 3) 2 OH 1-266 CCF 3 N CH CCl H C(CH 3) 2 OCH 3 1-267 CCF 3 N CH CCl H C(CH 3) 2 OCH 2CH 3 1-268 CCF 3 N CH CCl H C(CH 3) 2 OCH 2Ph 1-269 CCF 3 N CH CCl H C(CH 3) 2 NHSO 2CH 3 1-270 CCF 3 N CH CCl H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-271 CCl N CH CBr H C(CH 3) 2 OH 1-272 CCl N CH CBr H C(CH 3) 2 OCH 3 1-273 CCl N CH CBr H C(CH 3) 2 OCH 2CH 3 1-274 CCl N CH CBr H C(CH 3) 2 OCH 2Ph 1-275 CCl N CH CBr H C(CH 3) 2 NHSO 2CH 3 1-276 CCl N CH CBr H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-277 CCl N CH CCH 3 H C(CH 3) 2 OH 1-278 CCl N CH CCH 3 H C(CH 3) 2 OCH 3 1-279 CCl N CH CCH 3 H C(CH 3) 2 OCH 2CH 3 1-280 CCl N CH CCH 3 H C(CH 3) 2 OCH 2Ph 1-281 CCl N CH CCH 3 H C(CH 3) 2 NHSO 2CH 3 1-282 CCl N CH CCH 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-283 CCl N CH CCF 2H H C(CH 3) 2 OH 1-284 CCl N CH CCF 2H H C(CH 3) 2 OCH 3 1-285 CCl N CH CCF 2H H C(CH 3) 2 OCH 2CH 3 1-286 CCl N CH CCF 2H H C(CH 3) 2 OCH 2Ph 1-287 CCl N CH CCF 2H H C(CH 3) 2 NHSO 2CH 3 1-288 CCl N CH CCF 2H H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-289 CCl N CH CCF 2CH 3 H C(CH 3) 2 OH 1-290 CCl N CH CCF 2CH 3 H C(CH 3) 2 OCH 3 1-291 CCl N CH CCF 2CH 3 H C(CH 3) 2 OCH 2CH 3 1-292 CCl N CH CCF 2CH 3 H C(CH 3) 2 OCH 2Ph 1-293 CCl N CH CCF 2CH 3 H C(CH 3) 2 NHSO 2CH 3 1-294 CCl N CH CCF 2CH 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-295 CCl N CH CCF 3 H C(CH 3) 2 OH 1-296 CCl N CH CCF 3 H C(CH 3) 2 OCH 3 1-297 CCl N CH CCF 3 H C(CH 3) 2 OCH 2CH 3 1-298 CCl N CH CCF 3 H C(CH 3) 2 OCH 2Ph 1-299 CCl N CH CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-300 CCl N CH CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-301 CH N CH CCF 3 H C(CH 3) 2 OH 1-302 CH N CH CCF 3 H C(CH 3) 2 OCH 3 1-303 CH N CH CCF 3 H C(CH 3) 2 OCH 2CH 3 1-304 CH N CH CCF 3 H C(CH 3) 2 OCH 2Ph 1-305 CH N CH CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-306 CH N CH CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-307 CF N CH CCF 3 H C(CH 3) 2 OH 1-308 CF N CH CCF 3 H C(CH 3) 2 OCH 3 1-309 CF N CH CCF 3 H C(CH 3) 2 OCH 2CH 3 1-310 CF N CH CCF 3 H C(CH 3) 2 OCH 2Ph 1-311 CF N CH CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-312 CF N CH CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-313 CBr N CH CCF 3 H C(CH 3) 2 OH 1-314 CBr N CH CCF 3 H C(CH 3) 2 OCH 3 1-315 CBr N CH CCF 3 H C(CH 3) 2 OCH 2CH 3 1-316 CBr N CH CCF 3 H C(CH 3) 2 OCH 2Ph 1-317 CBr N CH CCF 3 H C(CH 3) 2 NHSO 2CH 3 1-318 CBr N CH CCF 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-319 CCl N CH CSO 2CH 3 H C(CH 3) 2 OH 1-320 CCl N CH CSO 2CH 3 H C(CH 3) 2 OCH 3 1-321 CCl N CH CSO 2CH 3 H C(CH 3) 2 OCH 2CH 3 1-322 CCl N CH CSO 2CH 3 H C(CH 3) 2 OCH 2Ph 1-323 CCl N CH CSO 2CH 3 H C(CH 3) 2 NHSO 2CH 3 1-324 CCl N CH CSO 2CH 3 H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-325 CH CH N *COCF 2O C(CH 3) 2 OH 1-326 CH CH N *COCF 2O C(CH 3) 2 OCH 3 1-327 CH CH N *COCF 2O C(CH 3) 2 OCH 2CH 3 1-328 CH CH N *COCF 2O C(CH 3) 2 OCH 2Ph 1-329 CH CH N *COCF 2O C(CH 3) 2 NHSO 2CH 3 1-330 CH CH N *COCF 2O C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-331 CH CF N CH CF 3 C(CH 3) 2 OH 1-332 CH CF N CH CF 3 C(CH 3) 2 OCH 3 1-333 CH CF N CH CF 3 C(CH 3) 2 OCH 2CH 3 1-334 CH CF N CH CF 3 C(CH 3) 2 OCH 2Ph 1-335 CH CF N CH CF 3 C(CH 3) 2 NHSO 2CH 3 1-336 CH CF N CH CF 3 C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-337 CH CCl CCl N H C(CH 3) 2 OH 1-338 CH CCl CCl N H C(CH 3) 2 OCH 3 1-339 CH CCl CCl N H C(CH 3) 2 OCH 2CH 3 1-340 CH CCl CCl N H C(CH 3) 2 OCH 2Ph 1-341 CH CCl CCl N H C(CH 3) 2 NHSO 2CH 3 1-342 CH CCl CCl N H C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-343 CCl CH CH CCH 3 H CH 2CH 2 OH 1-344 CCl CH CH CCH 3 H CH 2CH 2 OCH 3 1-345 CCl CH CH CCH 3 H CH 2CH 2 OCH 2CH 3 1-346 CCl CH CH CCH 3 H CH 2CH 2 OCH 2Ph 1-347 CCl CH CH CCH 3 H CH 2CH 2 NHSO 2CH 3 1-348 CCl CH CH CCH 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-349 N CH N CCF 3 H CH 2CH 2 OH 1-350 N CH N CCF 3 H CH 2CH 2 OCH 3 1-351 N CH N CCF 3 H CH 2CH 2 OCH 2CH 3 1-352 N CH N CCF 3 H CH 2CH 2 OCH 2Ph 1-353 N CH N CCF 3 H CH 2CH 2 NHSO 2CH 3 1-354 N CH N CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-355 NO CCl CH CCF 3 H CH 2CH 2 OH 1-356 NO CCl CH CCF 3 H CH 2CH 2 OCH 3 1-357 NO CCl CH CCF 3 H CH 2CH 2 OCH 2CH 3 1-358 NO CCl CH CCF 3 H CH 2CH 2 OCH 2Ph 1-359 NO CCl CH CCF 3 H CH 2CH 2 NHSO 2CH 3 1-360 NO CCl CH CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-361 CF N CH CF H CH 2CH 2 OH 1-362 CF N CH CF H CH 2CH 2 OCH 3 1-363 CF N CH CF H CH 2CH 2 OCH 2CH 3 1-364 CF N CH CF H CH 2CH 2 OCH 2Ph 1-365 CF N CH CF H CH 2CH 2 NHSO 2CH 3 1-366 CF N CH CF H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-367 CCl N CH CF H CH 2CH 2 OH 1-368 CCl N CH CF H CH 2CH 2 OCH 3 1-369 CCl N CH CF H CH 2CH 2 OCH 2CH 3 1-370 CCl N CH CF H CH 2CH 2 OCH 2Ph 1-371 CCl N CH CF H CH 2CH 2 NHSO 2CH 3 1-372 CCl N CH CF H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-373 CCl N CH CCl H CH 2CH 2 OH 1-374 CCl N CH CCl H CH 2CH 2 OCH 3 1-375 CCl N CH CCl H CH 2CH 2 OCH 2CH 3 1-376 CCl N CH CCl H CH 2CH 2 OCH 2Ph 1-377 CCl N CH CCl H CH 2CH 2 NHSO 2CH 3 1-378 CCl N CH CCl H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-379 CCF 3 N CH CCl H CH 2CH 2 OH 1-380 CCF 3 N CH CCl H CH 2CH 2 OCH 3 1-381 CCF 3 N CH CCl H CH 2CH 2 OCH 2CH 3 1-382 CCF 3 N CH CCl H CH 2CH 2 OCH 2Ph 1-383 CCF 3 N CH CCl H CH 2CH 2 NHSO 2CH 3 1-384 CCF 3 N CH CCl H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-385 CCl N CH CBr H CH 2CH 2 OH 1-386 CCl N CH CBr H CH 2CH 2 OCH 3 1-387 CCl N CH CBr H CH 2CH 2 OCH 2CH 3 1-388 CCl N CH CBr H CH 2CH 2 OCH 2Ph 1-389 CCl N CH CBr H CH 2CH 2 NHSO 2CH 3 1-390 CCl N CH CBr H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-391 CCl N CH CCH 3 H CH 2CH 2 OH 1-392 CCl N CH CCH 3 H CH 2CH 2 OCH 3 1-393 CCl N CH CCH 3 H CH 2CH 2 OCH 2CH 3 1-394 CCl N CH CCH 3 H CH 2CH 2 OCH 2Ph 1-395 CCl N CH CCH 3 H CH 2CH 2 NHSO 2CH 3 1-396 CCl N CH CCH 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-397 CCl N CH CCF 2H H CH 2CH 2 OH 1-398 CCl N CH CCF 2H H CH 2CH 2 OCH 3 1-399 CCl N CH CCF 2H H CH 2CH 2 OCH 2CH 3 1-400 CCl N CH CCF 2H H CH 2CH 2 OCH 2Ph 1-401 CCl N CH CCF 2H H CH 2CH 2 NHSO 2CH 3 1-402 CCl N CH CCF 2H H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-403 CCl N CH CCF 2CH 3 H CH 2CH 2 OH 1-404 CCl N CH CCF 2CH 3 H CH 2CH 2 OCH 3 1-405 CCl N CH CCF 2CH 3 H CH 2CH 2 OCH 2CH 3 1-406 CCl N CH CCF 2CH 3 H CH 2CH 2 OCH 2Ph 1-407 CCl N CH CCF 2CH 3 H CH 2CH 2 NHSO 2CH 3 1-408 CCl N CH CCF 2CH 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-409 CCl N CH CCF 3 H CH 2CH 2 OH 1-410 CCl N CH CCF 3 H CH 2CH 2 OCH 3 1-411 CCl N CH CCF 3 H CH 2CH 2 OCH 2CH 3 1-412 CCl N CH CCF 3 H CH 2CH 2 OCH 2Ph 1-413 CCl N CH CCF 3 H CH 2CH 2 NHSO 2CH 3 1-414 CCl N CH CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-415 CH N CH CCF 3 H CH 2CH 2 OH 1-416 CH N CH CCF 3 H CH 2CH 2 OCH 3 1-417 CH N CH CCF 3 H CH 2CH 2 OCH 2CH 3 1-418 CH N CH CCF 3 H CH 2CH 2 OCH 2Ph 1-419 CH N CH CCF 3 H CH 2CH 2 NHSO 2CH 3 1-420 CH N CH CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-421 CF N CH CCF 3 H CH 2CH 2 OH 1-422 CF N CH CCF 3 H CH 2CH 2 OCH 3 1-423 CF N CH CCF 3 H CH 2CH 2 OCH 2CH 3 1-424 CF N CH CCF 3 H CH 2CH 2 OCH 2Ph 1-425 CF N CH CCF 3 H CH 2CH 2 NHSO 2CH 3 1-426 CF N CH CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-427 CBr N CH CCF 3 H CH 2CH 2 OH 1-428 CBr N CH CCF 3 H CH 2CH 2 OCH 3 1-429 CBr N CH CCF 3 H CH 2CH 2 OCH 2CH 3 1-430 CBr N CH CCF 3 H CH 2CH 2 OCH 2Ph 1-431 CBr N CH CCF 3 H CH 2CH 2 NHSO 2CH 3 1-432 CBr N CH CCF 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-433 CCl N CH CSO 2CH 3 H CH 2CH 2 OH 1-434 CCl N CH CSO 2CH 3 H CH 2CH 2 OCH 3 1-435 CCl N CH CSO 2CH 3 H CH 2CH 2 OCH 2CH 3 1-436 CCl N CH CSO 2CH 3 H CH 2CH 2 OCH 2Ph 1-437 CCl N CH CSO 2CH 3 H CH 2CH 2 NHSO 2CH 3 1-438 CCl N CH CSO 2CH 3 H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-439 CH CH N *COCF 2O CH 2CH 2 OH 1-440 CH CH N *COCF 2O CH 2CH 2 OCH 3 1-441 CH CH N *COCF 2O CH 2CH 2 OCH 2CH 3 1-442 CH CH N *COCF 2O CH 2CH 2 OCH 2Ph 1-443 CH CH N *COCF 2O CH 2CH 2 NHSO 2CH 3 1-444 CH CH N *COCF 2O CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-445 CH CF N CH CF 3 CH 2CH 2 OH 1-446 CH CF N CH CF 3 CH 2CH 2 OCH 3 1-447 CH CF N CH CF 3 CH 2CH 2 OCH 2CH 3 1-448 CH CF N CH CF 3 CH 2CH 2 OCH 2Ph 1-449 CH CF N CH CF 3 CH 2CH 2 NHSO 2CH 3 1-450 CH CF N CH CF 3 CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-451 CH CCl CCl N H CH 2CH 2 OH 1-452 CH CCl CCl N H CH 2CH 2 OCH 3 1-453 CH CCl CCl N H CH 2CH 2 OCH 2CH 3 1-454 CH CCl CCl N H CH 2CH 2 OCH 2Ph 1-455 CH CCl CCl N H CH 2CH 2 NHSO 2CH 3 1-456 CH CCl CCl N H CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-457 CCl CH CH CCH 3 H CH(CH 3)CH 2 OH 1-458 CCl CH CH CCH 3 H CH(CH 3)CH 2 OCH 3 1-459 CCl CH CH CCH 3 H CH(CH 3)CH 2 OCH 2CH 3 1-460 CCl CH CH CCH 3 H CH(CH 3)CH 2 OCH 2Ph 1-461 CCl CH CH CCH 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-462 CCl CH CH CCH 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-463 N CH N CCF 3 H CH(CH 3)CH 2 OH 1-464 N CH N CCF 3 H CH(CH 3)CH 2 OCH 3 1-465 N CH N CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-466 N CH N CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-467 N CH N CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-468 N CH N CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-469 NO CCl CH CCF 3 H CH(CH 3)CH 2 OH 1-470 NO CCl CH CCF 3 H CH(CH 3)CH 2 OCH 3 1-471 NO CCl CH CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-472 NO CCl CH CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-473 NO CCl CH CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-474 NO CCl CH CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-475 CF N CH CF H CH(CH 3)CH 2 OH 1-476 CF N CH CF H CH(CH 3)CH 2 OCH 3 1-477 CF N CH CF H CH(CH 3)CH 2 OCH 2CH 3 1-478 CF N CH CF H CH(CH 3)CH 2 OCH 2Ph 1-479 CF N CH CF H CH(CH 3)CH 2 NHSO 2CH 3 1-480 CF N CH CF H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-481 CCl N CH CF H CH(CH 3)CH 2 OH 1-482 CCl N CH CF H CH(CH 3)CH 2 OCH 3 1-483 CCl N CH CF H CH(CH 3)CH 2 OCH 2CH 3 1-484 CCl N CH CF H CH(CH 3)CH 2 OCH 2Ph 1-485 CCl N CH CF H CH(CH 3)CH 2 NHSO 2CH 3 1-486 CCl N CH CF H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-487 CCl N CH CCl H CH(CH 3)CH 2 OH 1-488 CCl N CH CCl H CH(CH 3)CH 2 OCH 3 1-489 CCl N CH CCl H CH(CH 3)CH 2 OCH 2CH 3 1-490 CCl N CH CCl H CH(CH 3)CH 2 OCH 2Ph 1-491 CCl N CH CCl H CH(CH 3)CH 2 NHSO 2CH 3 1-492 CCl N CH CCl H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-493 CCF 3 N CH CCl H CH(CH 3)CH 2 OH 1-494 CCF 3 N CH CCl H CH(CH 3)CH 2 OCH 3 1-495 CCF 3 N CH CCl H CH(CH 3)CH 2 OCH 2CH 3 1-496 CCF 3 N CH CCl H CH(CH 3)CH 2 OCH 2Ph 1-497 CCF 3 N CH CCl H CH(CH 3)CH 2 NHSO 2CH 3 1-498 CCF 3 N CH CCl H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-499 CCl N CH CBr H CH(CH 3)CH 2 OH 1-500 CCl N CH CBr H CH(CH 3)CH 2 OCH 3 1-501 CCl N CH CBr H CH(CH 3)CH 2 OCH 2CH 3 1-502 CCl N CH CBr H CH(CH 3)CH 2 OCH 2Ph 1-503 CCl N CH CBr H CH(CH 3)CH 2 NHSO 2CH 3 1-504 CCl N CH CBr H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-505 CCl N CH CCH 3 H CH(CH 3)CH 2 OH 1-506 CCl N CH CCH 3 H CH(CH 3)CH 2 OCH 3 1-507 CCl N CH CCH 3 H CH(CH 3)CH 2 OCH 2CH 3 1-508 CCl N CH CCH 3 H CH(CH 3)CH 2 OCH 2Ph 1-509 CCl N CH CCH 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-510 CCl N CH CCH 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-511 CCl N CH CCF 2H H CH(CH 3)CH 2 OH 1-512 CCl N CH CCF 2H H CH(CH 3)CH 2 OCH 3 1-513 CCl N CH CCF 2H H CH(CH 3)CH 2 OCH 2CH 3 1-514 CCl N CH CCF 2H H CH(CH 3)CH 2 OCH 2Ph 1-515 CCl N CH CCF 2H H CH(CH 3)CH 2 NHSO 2CH 3 1-516 CCl N CH CCF 2H H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-517 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 OH 1-518 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 OCH 3 1-519 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 OCH 2CH 3 1-520 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 OCH 2Ph 1-521 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-522 CCl N CH CCF 2CH 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-523 CCl N CH CCF 3 H CH(CH 3)CH 2 OH 1-524 CCl N CH CCF 3 H CH(CH 3)CH 2 OCH 3 1-525 CCl N CH CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-526 CCl N CH CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-527 CCl N CH CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-528 CCl N CH CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-529 CH N CH CCF 3 H CH(CH 3)CH 2 OH 1-530 CH N CH CCF 3 H CH(CH 3)CH 2 OCH 3 1-531 CH N CH CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-532 CH N CH CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-533 CH N CH CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-534 CH N CH CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-535 CF N CH CCF 3 H CH(CH 3)CH 2 OH 1-536 CF N CH CCF 3 H CH(CH 3)CH 2 OCH 3 1-537 CF N CH CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-538 CF N CH CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-539 CF N CH CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-540 CF N CH CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-541 CBr N CH CCF 3 H CH(CH 3)CH 2 OH 1-542 CBr N CH CCF 3 H CH(CH 3)CH 2 OCH 3 1-543 CBr N CH CCF 3 H CH(CH 3)CH 2 OCH 2CH 3 1-544 CBr N CH CCF 3 H CH(CH 3)CH 2 OCH 2Ph 1-545 CBr N CH CCF 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-546 CBr N CH CCF 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-547 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 OH 1-548 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 OCH 3 1-549 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 OCH 2CH 3 1-550 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 OCH 2Ph 1-551 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 NHSO 2CH 3 1-552 CCl N CH CSO 2CH 3 H CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-553 CH CH N *COCF 2O CH(CH 3)CH 2 OH 1-554 CH CH N *COCF 2O CH(CH 3)CH 2 OCH 3 1-555 CH CH N *COCF 2O CH(CH 3)CH 2 OCH 2CH 3 1-556 CH CH N *COCF 2O CH(CH 3)CH 2 OCH 2Ph 1-557 CH CH N *COCF 2O CH(CH 3)CH 2 NHSO 2CH 3 1-558 CH CH N *COCF 2O CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-559 CH CF N CH CF 3 CH(CH 3)CH 2 OH 1-560 CH CF N CH CF 3 CH(CH 3)CH 2 OCH 3 1-561 CH CF N CH CF 3 CH(CH 3)CH 2 OCH 2CH 3 1-562 CH CF N CH CF 3 CH(CH 3)CH 2 OCH 2Ph 1-563 CH CF N CH CF 3 CH(CH 3)CH 2 NHSO 2CH 3 1-564 CH CF N CH CF 3 CH(CH 3)CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-565 CH CCl CCl N H CH(CH 3)CH 2 OH 1-566 CH CCl CCl N H CH(CH 3)CH 2 OCH 3 1-567 CH CCl CCl N H CH(CH 3)CH 2 OCH 2CH 3 1-568 CH CCl CCl N H CH(CH 3)CH 2 OCH 2Ph 1-569 CH CCl CCl N H CH(CH 3)CH 2 NHSO 2CH 3 1-570 CH CCl CCl N H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-571 CCl CH CH CCH 3 H CH 2CH(CH 3) OH 1-572 CCl CH CH CCH 3 H CH 2CH(CH 3) OCH 3 1-573 CCl CH CH CCH 3 H CH 2CH(CH 3) OCH 2CH 3 1-574 CCl CH CH CCH 3 H CH 2CH(CH 3) OCH 2Ph 1-575 CCl CH CH CCH 3 H CH 2CH(CH 3) NHSO 2CH 3 1-576 CCl CH CH CCH 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-577 N CH N CCF 3 H CH 2CH(CH 3) OH 1-578 N CH N CCF 3 H CH 2CH(CH 3) OCH 3 1-579 N CH N CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-580 N CH N CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-581 N CH N CCF 3 H CH 2CH(CH 3) NHSO 2CH 3 1-582 N CH N CCF 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-583 NO CCl CH CCF 3 H CH 2CH(CH 3) OH 1-584 NO CCl CH CCF 3 H CH 2CH(CH 3) OCH 3 1-585 NO CCl CH CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-586 NO CCl CH CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-587 NO CCl CH CCF 3 H CH 2CH(CH 3) NHSO 2CH 3 1-588 NO CCl CH CCF 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-589 CF N CH CF H CH 2CH(CH 3) OH 1-590 CF N CH CF H CH 2CH(CH 3) OCH 3 1-591 CF N CH CF H CH 2CH(CH 3) OCH 2CH 3 1-592 CF N CH CF H CH 2CH(CH 3) OCH 2Ph 1-593 CF N CH CF H CH 2CH(CH 3) NHSO 2CH 3 1-594 CF N CH CF H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-595 CCl N CH CF H CH 2CH(CH 3) OH 1-596 CCl N CH CF H CH 2CH(CH 3) OCH 3 1-597 CCl N CH CF H CH 2CH(CH 3) OCH 2CH 3 1-598 CCl N CH CF H CH 2CH(CH 3) OCH 2Ph 1-599 CCl N CH CF H CH 2CH(CH 3) NHSO 2CH 3 1-600 CCl N CH CF H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-601 CCl N CH CCl H CH 2CH(CH 3) OH 1-602 CCl N CH CCl H CH 2CH(CH 3) OCH 3 1-603 CCl N CH CCl H CH 2CH(CH 3) OCH 2CH 3 1-604 CCl N CH CCl H CH 2CH(CH 3) OCH 2Ph 1-605 CCl N CH CCl H CH 2CH(CH 3) NHSO 2CH 3 1-606 CCl N CH CCl H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-607 CCF 3 N CH CCl H CH 2CH(CH 3) OH 1-608 CCF 3 N CH CCl H CH 2CH(CH 3) OCH 3 1-609 CCF 3 N CH CCl H CH 2CH(CH 3) OCH 2CH 3 1-610 CCF 3 N CH CCl H CH 2CH(CH 3) OCH 2Ph 1-611 CCF 3 N CH CCl H CH 2CH(CH 3) NHSO 2CH 3 1-612 CCF 3 N CH CCl H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-613 CCl N CH CBr H CH 2CH(CH 3) OH 1-614 CCl N CH CBr H CH 2CH(CH 3) OCH 3 1-615 CCl N CH CBr H CH 2CH(CH 3) OCH 2CH 3 1-616 CCl N CH CBr H CH 2CH(CH 3) OCH 2Ph 1-617 CCl N CH CBr H CH 2CH(CH 3) NHSO 2CH 3 1-618 CCl N CH CBr H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-619 CCl N CH CCH 3 H CH 2CH(CH 3) OH 1-620 CCl N CH CCH 3 H CH 2CH(CH 3) OCH 3 1-621 CCl N CH CCH 3 H CH 2CH(CH 3) OCH 2CH 3 1-622 CCl N CH CCH 3 H CH 2CH(CH 3) OCH 2Ph 1-623 CCl N CH CCH 3 H CH 2CH(CH 3) NHSO 2CH 3 1-624 CCl N CH CCH 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-625 CCl N CH CCF 2H H CH 2CH(CH 3) OH 1-626 CCl N CH CCF 2H H CH 2CH(CH 3) OCH 3 1-627 CCl N CH CCF 2H H CH 2CH(CH 3) OCH 2CH 3 1-628 CCl N CH CCF 2H H CH 2CH(CH 3) OCH 2Ph 1-629 CCl N CH CCF 2H H CH 2CH(CH 3) NHSO 2CH 3 1-630 CCl N CH CCF 2H H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-631 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) OH 1-632 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) OCH 3 1-633 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) OCH 2CH 3 1-634 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) OCH 2Ph 1-635 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) NHSO 2CH 3 1-636 CCl N CH CCF 2CH 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-637 CCl N CH CCF 3 H CH 2CH(CH 3) OH 1-638 CCl N CH CCF 3 H CH 2CH(CH 3) OCH 3 1-639 CCl N CH CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-640 CCl N CH CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-641 CCl N CH CCF 3 H CH 2CH(CH 3) NHSO 2CH 3 1-642 CCl N CH CCF 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-643 CH N CH CCF 3 H CH 2CH(CH 3) OH 1-644 CH N CH CCF 3 H CH 2CH(CH 3) OCH 3 1-645 CH N CH CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-646 CH N CH CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-647 CH N CH CCF 3 H CH 2CHCH 3 NHSO 2CH 3 1-648 CH N CH CCF 3 H CH 2CHCH 3 NHSO 2N(CH 3)CH(CH 3) 2 1-649 CF N CH CCF 3 H CH 2CH(CH 3) OH 1-650 CF N CH CCF 3 H CH 2CH(CH 3) OCH 3 1-651 CF N CH CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-652 CF N CH CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-653 CF N CH CCF 3 H CH 2CH(CH 3) NHSO 2CH 3 1-654 CF N CH CCF 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-655 CBr N CH CCF 3 H CH 2CH(CH 3) OH 1-656 CBr N CH CCF 3 H CH 2CH(CH 3) OCH 3 1-657 CBr N CH CCF 3 H CH 2CH(CH 3) OCH 2CH 3 1-658 CBr N CH CCF 3 H CH 2CH(CH 3) OCH 2Ph 1-659 CBr N CH CCF 3 H CH 2CH(CH 3) NHSO 2CH 3 1-660 CBr N CH CCF 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-661 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) OH 1-662 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) OCH 3 1-663 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) OCH 2CH 3 1-664 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) OCH 2Ph 1-665 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) NHSO 2CH 3 1-666 CCl N CH CSO 2CH 3 H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-667 CH CH N *COCF 2O CH 2CH(CH 3) OH 1-668 CH CH N *COCF 2O CH 2CH(CH 3) OCH 3 1-669 CH CH N *COCF 2O CH 2CH(CH 3) OCH 2CH 3 1-670 CH CH N *COCF 2O CH 2CH(CH 3) OCH 2Ph 1-671 CH CH N *COCF 2O CH 2CH(CH 3) NHSO 2CH 3 1-672 CH CH N *COCF 2O CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-673 CH CF N CH CF 3 CH 2CH(CH 3) OH 1-674 CH CF N CH CF 3 CH 2CH(CH 3) OCH 3 1-675 CH CF N CH CF 3 CH 2CH(CH 3) OCH 2CH 3 1-676 CH CF N CH CF 3 CH 2CH(CH 3) OCH 2Ph 1-677 CH CF N CH CF 3 CH 2CH(CH 3) NHSO 2CH 3 1-678 CH CF N CH CF 3 CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-679 CH CCl CCl N H CH 2CH(CH 3) OH 1-680 CH CCl CCl N H CH 2CH(CH 3) OCH 3 1-681 CH CCl CCl N H CH 2CH(CH 3) OCH 2CH 3 1-682 CH CCl CCl N H CH 2CH(CH 3) OCH 2Ph 1-683 CH CCl CCl N H CH 2CH(CH 3) NHSO 2CH 3 1-684 CH CCl CCl N H CH 2CH(CH 3) NHSO 2N(CH 3)CH(CH 3) 2 1-685 CCl CH CH CCH 3 H C(CH 3) 2CH 2 OH 1-686 CCl CH CH CCH 3 H C(CH 3) 2CH 2 OCH 3 1-687 CCl CH CH CCH 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-688 CCl CH CH CCH 3 H C(CH 3) 2CH 2 OCH 2Ph 1-689 CCl CH CH CCH 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-690 CCl CH CH CCH 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-691 N CH N CCF 3 H C(CH 3) 2CH 2 OH 1-692 N CH N CCF 3 H C(CH 3) 2CH 2 OCH 3 1-693 N CH N CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-694 N CH N CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-695 N CH N CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-696 N CH N CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-697 NO CCl CH CCF 3 H C(CH 3) 2CH 2 OH 1-698 NO CCl CH CCF 3 H C(CH 3) 2CH 2 OCH 3 1-699 NO CCl CH CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-700 NO CCl CH CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-701 NO CCl CH CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-702 NO CCl CH CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-703 CF N CH CF H C(CH 3) 2CH 2 OH 1-704 CF N CH CF H C(CH 3) 2CH 2 OCH 3 1-705 CF N CH CF H C(CH 3) 2CH 2 OCH 2CH 3 1-706 CF N CH CF H C(CH 3) 2CH 2 OCH 2Ph 1-707 CF N CH CF H C(CH 3) 2CH 2 NHSO 2CH 3 1-708 CF N CH CF H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-709 CCl N CH CF H C(CH 3) 2CH 2 OH 1-710 CCl N CH CF H C(CH 3) 2CH 2 OCH 3 1-711 CCl N CH CF H C(CH 3) 2CH 2 OCH 2CH 3 1-712 CCl N CH CF H C(CH 3) 2CH 2 OCH 2Ph 1-713 CCl N CH CF H C(CH 3) 2CH 2 NHSO 2CH 3 1-714 CCl N CH CF H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-715 CCl N CH CCl H C(CH 3) 2CH 2 OH 1-716 CCl N CH CCl H C(CH 3) 2CH 2 OCH 3 1-717 CCl N CH CCl H C(CH 3) 2CH 2 OCH 2CH 3 1-718 CCl N CH CCl H C(CH 3) 2CH 2 OCH 2Ph 1-719 CCl N CH CCl H C(CH 3) 2CH 2 NHSO 2CH 3 1-720 CCl N CH CCl H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-721 CCF 3 N CH CCl H C(CH 3) 2CH 2 OH 1-722 CCF 3 N CH CCl H C(CH 3) 2CH 2 OCH 3 1-723 CCF 3 N CH CCl H C(CH 3) 2CH 2 OCH 2CH 3 1-724 CCF 3 N CH CCl H C(CH 3) 2CH 2 OCH 2Ph 1-725 CCF 3 N CH CCl H C(CH 3) 2CH 2 NHSO 2CH 3 1-726 CCF 3 N CH CCl H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-727 CCl N CH CBr H C(CH 3) 2CH 2 OH 1-728 CCl N CH CBr H C(CH 3) 2CH 2 OCH 3 1-729 CCl N CH CBr H C(CH 3) 2CH 2 OCH 2CH 3 1-730 CCl N CH CBr H C(CH 3) 2CH 2 OCH 2Ph 1-731 CCl N CH CBr H C(CH 3) 2CH 2 NHSO 2CH 3 1-732 CCl N CH CBr H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-733 CCl N CH CCH 3 H C(CH 3) 2CH 2 OH 1-734 CCl N CH CCH 3 H C(CH 3) 2CH 2 OCH 3 1-735 CCl N CH CCH 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-736 CCl N CH CCH 3 H C(CH 3) 2CH 2 OCH 2Ph 1-737 CCl N CH CCH 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-738 CCl N CH CCH 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-739 CCl N CH CCF 2H H C(CH 3) 2CH 2 OH 1-740 CCl N CH CCF 2H H C(CH 3) 2CH 2 OCH 3 1-741 CCl N CH CCF 2H H C(CH 3) 2CH 2 OCH 2CH 3 1-742 CCl N CH CCF 2H H C(CH 3) 2CH 2 OCH 2Ph 1-743 CCl N CH CCF 2H H C(CH 3) 2CH 2 NHSO 2CH 3 1-744 CCl N CH CCF 2H H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-745 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 OH 1-746 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 OCH 3 1-747 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-748 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 OCH 2Ph 1-749 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-750 CCl N CH CCF 2CH 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-751 CCl N CH CCF 3 H C(CH 3) 2CH 2 OH 1-752 CCl N CH CCF 3 H C(CH 3) 2CH 2 OCH 3 1-753 CCl N CH CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-754 CCl N CH CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-755 CCl N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-756 CCl N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-757 CH N CH CCF 3 H C(CH 3) 2CH 2 OH 1-758 CH N CH CCF 3 H C(CH 3) 2CH 2 OCH 3 1-759 CH N CH CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-760 CH N CH CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-761 CH N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-762 CH N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-763 CF N CH CCF 3 H C(CH 3) 2CH 2 OH 1-764 CF N CH CCF 3 H C(CH 3) 2CH 2 OCH 3 1-765 CF N CH CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-766 CF N CH CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-767 CF N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-768 CF N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-769 CBr N CH CCF 3 H C(CH 3) 2CH 2 OH 1-770 CBr N CH CCF 3 H C(CH 3) 2CH 2 OCH 3 1-771 CBr N CH CCF 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-772 CBr N CH CCF 3 H C(CH 3) 2CH 2 OCH 2Ph 1-773 CBr N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-774 CBr N CH CCF 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-775 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 OH 1-776 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 OCH 3 1-777 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 OCH 2CH 3 1-778 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 OCH 2Ph 1-779 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 NHSO 2CH 3 1-780 CCl N CH CSO 2CH 3 H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-781 CH CH N *COCF 2O C(CH 3) 2CH 2 OH 1-782 CH CH N *COCF 2O C(CH 3) 2CH 2 OCH 3 1-783 CH CH N *COCF 2O C(CH 3) 2CH 2 OCH 2CH 3 1-784 CH CH N *COCF 2O C(CH 3) 2CH 2 OCH 2Ph 1-785 CH CH N *COCF 2O C(CH 3) 2CH 2 NHSO 2CH 3 1-786 CH CH N *COCF 2O C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-787 CH CF N CH CF 3 C(CH 3) 2CH 2 OH 1-788 CH CF N CH CF 3 C(CH 3) 2CH 2 OCH 3 1-789 CH CF N CH CF 3 C(CH 3) 2CH 2 OCH 2CH 3 1-790 CH CF N CH CF 3 C(CH 3) 2CH 2 OCH 2Ph 1-791 CH CF N CH CF 3 C(CH 3) 2CH 2 NHSO 2CH 3 1-792 CH CF N CH CF 3 C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-793 CH CCl CCl N H C(CH 3) 2CH 2 OH 1-794 CH CCl CCl N H C(CH 3) 2CH 2 OCH 3 1-795 CH CCl CCl N H C(CH 3) 2CH 2 OCH 2CH 3 1-796 CH CCl CCl N H C(CH 3) 2CH 2 OCH 2Ph 1-797 CH CCl CCl N H C(CH 3) 2CH 2 NHSO 2CH 3 1-798 CH CCl CCl N H C(CH 3) 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-799 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OH 1-800 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 3 1-801 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-802 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 2Ph 1-803 CCl CH CH CCH 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-804 CCl CH CH CCH 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-805 N CH N CCF 3 H CH 2C(CH 3) 2 OH 1-806 N CH N CCF 3 H CH 2C(CH 3) 2 OCH 3 1-807 N CH N CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-808 N CH N CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-809 N CH N CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-810 N CH N CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-811 NO CCl CH CCF 3 H CH 2C(CH 3) 2 OH 1-812 NO CCl CH CCF 3 H CH 2C(CH 3) 2 OCH 3 1-813 NO CCl CH CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-814 NO CCl CH CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-815 NO CCl CH CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-816 NO CCl CH CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-817 CF N CH CF H CH 2C(CH 3) 2 OH 1-818 CF N CH CF H CH 2C(CH 3) 2 OCH 3 1-819 CF N CH CF H CH 2C(CH 3) 2 OCH 2CH 3 1-820 CF N CH CF H CH 2C(CH 3) 2 OCH 2Ph 1-821 CF N CH CF H CH 2C(CH 3) 2 NHSO 2CH 3 1-822 CF N CH CF H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-823 CCl N CH CF H CH 2C(CH 3) 2 OH 1-824 CCl N CH CF H CH 2C(CH 3) 2 OCH 3 1-825 CCl N CH CF H CH 2C(CH 3) 2 OCH 2CH 3 1-826 CCl N CH CF H CH 2C(CH 3) 2 OCH 2Ph 1-827 CCl N CH CF H CH 2C(CH 3) 2 NHSO 2CH 3 1-828 CCl N CH CF H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-829 CCl N CH CCl H CH 2C(CH 3) 2 OH 1-830 CCl N CH CCl H CH 2C(CH 3) 2 OCH 3 1-831 CCl N CH CCl H CH 2C(CH 3) 2 OCH 2CH 3 1-832 CCl N CH CCl H CH 2C(CH 3) 2 OCH 2Ph 1-833 CCl N CH CCl H CH 2C(CH 3) 2 NHSO 2CH 3 1-834 CCl N CH CCl H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-835 CCF 3 N CH CCl H CH 2C(CH 3) 2 OH 1-836 CCF 3 N CH CCl H CH 2C(CH 3) 2 OCH 3 1-837 CCF 3 N CH CCl H CH 2C(CH 3) 2 OCH 2CH 3 1-838 CCF 3 N CH CCl H CH 2C(CH 3) 2 OCH 2Ph 1-839 CCF 3 N CH CCl H CH 2C(CH 3) 2 NHSO 2CH 3 1-840 CCF 3 N CH CCl H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-841 CCl N CH CBr H CH 2C(CH 3) 2 OH 1-842 CCl N CH CBr H CH 2C(CH 3) 2 OCH 3 1-843 CCl N CH CBr H CH 2C(CH 3) 2 OCH 2CH 3 1-844 CCl N CH CBr H CH 2C(CH 3) 2 OCH 2Ph 1-845 CCl N CH CBr H CH 2C(CH 3) 2 NHSO 2CH 3 1-846 CCl N CH CBr H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-847 CCl N CH CCH 3 H CH 2C(CH 3) 2 OH 1-848 CCl N CH CCH 3 H CH 2C(CH 3) 2 OCH 3 1-849 CCl N CH CCH 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-850 CCl N CH CCH 3 H CH 2C(CH 3) 2 OCH 2Ph 1-851 CCl N CH CCH 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-852 CCl N CH CCH 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-853 CCl N CH CCF 2H H CH 2C(CH 3) 2 OH 1-854 CCl N CH CCF 2H H CH 2C(CH 3) 2 OCH 3 1-855 CCl N CH CCF 2H H CH 2C(CH 3) 2 OCH 2CH 3 1-856 CCl N CH CCF 2H H CH 2C(CH 3) 2 OCH 2Ph 1-857 CCl N CH CCF 2H H CH 2C(CH 3) 2 NHSO 2CH 3 1-858 CCl N CH CCF 2H H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-859 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 OH 1-860 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 OCH 3 1-861 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-862 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 OCH 2Ph 1-863 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-864 CCl N CH CCF 2CH 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-865 CCl N CH CCF 3 H CH 2C(CH 3) 2 OH 1-866 CCl N CH CCF 3 H CH 2C(CH 3) 2 OCH 3 1-867 CCl N CH CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-868 CCl N CH CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-869 CCl N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-870 CCl N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-871 CH N CH CCF 3 H CH 2C(CH 3) 2 OH 1-872 CH N CH CCF 3 H CH 2C(CH 3) 2 OCH 3 1-873 CH N CH CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-874 CH N CH CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-875 CH N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-876 CH N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-877 CF N CH CCF 3 H CH 2C(CH 3) 2 OH 1-878 CF N CH CCF 3 H CH 2C(CH 3) 2 OCH 3 1-879 CF N CH CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-880 CF N CH CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-881 CF N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-882 CF N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-883 CBr N CH CCF 3 H CH 2C(CH 3) 2 OH 1-884 CBr N CH CCF 3 H CH 2C(CH 3) 2 OCH 3 1-885 CBr N CH CCF 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-886 CBr N CH CCF 3 H CH 2C(CH 3) 2 OCH 2Ph 1-887 CBr N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-888 CBr N CH CCF 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-889 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 OH 1-890 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 OCH 3 1-891 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-892 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 OCH 2Ph 1-893 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-894 CCl N CH CSO 2CH 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-895 CH CH N *COCF 2O CH 2C(CH 3) 2 OH 1-896 CH CH N *COCF 2O CH 2C(CH 3) 2 OCH 3 1-897 CH CH N *COCF 2O CH 2C(CH 3) 2 OCH 2CH 3 1-898 CH CH N *COCF 2O CH 2C(CH 3) 2 OCH 2Ph 1-899 CH CH N *COCF 2O CH 2C(CH 3) 2 NHSO 2CH 3 1-900 CH CH N *COCF 2O CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-901 CH CF N CH CF 3 CH 2C(CH 3) 2 OH 1-902 CH CF N CH CF 3 CH 2C(CH 3) 2 OCH 3 1-903 CH CF N CH CF 3 CH 2C(CH 3) 2 OCH 2CH 3 1-904 CH CF N CH CF 3 CH 2C(CH 3) 2 OCH 2Ph 1-905 CH CF N CH CF 3 CH 2C(CH 3) 2 NHSO 2CH 3 1-906 CH CF N CH CF 3 CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-907 CH CCl CCl N H CH 2C(CH 3) 2 OH 1-908 CH CCl CCl N H CH 2C(CH 3) 2 OCH 3 1-909 CH CCl CCl N H CH 2C(CH 3) 2 OCH 2CH 3 1-910 CH CCl CCl N H CH 2C(CH 3) 2 OCH 2Ph 1-911 CH CCl CCl N H CH 2C(CH 3) 2 NHSO 2CH 3 1-912 CH CCl CCl N H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-913 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OH 1-914 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 3 1-915 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 2CH 3 1-916 CCl CH CH CCH 3 H CH 2C(CH 3) 2 OCH 2Ph 1-917 CCl CH CH CCH 3 H CH 2C(CH 3) 2 NHSO 2CH 3 1-918 CCl CH CH CCH 3 H CH 2C(CH 3) 2 NHSO 2N(CH 3)CH(CH 3) 2 1-919 N CH N CCF 3 H CH 2CH 2CH 2 OH 1-920 N CH N CCF 3 H CH 2CH 2CH 2 OCH 3 1-921 N CH N CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-922 N CH N CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-923 N CH N CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-924 N CH N CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-925 NO CCl CH CCF 3 H CH 2CH 2CH 2 OH 1-926 NO CCl CH CCF 3 H CH 2CH 2CH 2 OCH 3 1-927 NO CCl CH CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-928 NO CCl CH CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-929 NO CCl CH CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-930 NO CCl CH CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-931 CF N CH CF H CH 2CH 2CH 2 OH 1-932 CF N CH CF H CH 2CH 2CH 2 OCH 3 1-933 CF N CH CF H CH 2CH 2CH 2 OCH 2CH 3 1-934 CF N CH CF H CH 2CH 2CH 2 OCH 2Ph 1-935 CF N CH CF H CH 2CH 2CH 2 NHSO 2CH 3 1-936 CF N CH CF H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-937 CCl N CH CF H CH 2CH 2CH 2 OH 1-938 CCl N CH CF H CH 2CH 2CH 2 OCH 3 1-939 CCl N CH CF H CH 2CH 2CH 2 OCH 2CH 3 1-940 CCl N CH CF H CH 2CH 2CH 2 OCH 2Ph 1-941 CCl N CH CF H CH 2CH 2CH 2 NHSO 2CH 3 1-942 CCl N CH CF H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-943 CCl N CH CCl H CH 2CH 2CH 2 OH 1-944 CCl N CH CCl H CH 2CH 2CH 2 OCH 3 1-945 CCl N CH CCl H CH 2CH 2CH 2 OCH 2CH 3 1-946 CCl N CH CCl H CH 2CH 2CH 2 OCH 2Ph 1-947 CCl N CH CCl H CH 2CH 2CH 2 NHSO 2CH 3 1-948 CCl N CH CCl H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-949 CCF 3 N CH CCl H CH 2CH 2CH 2 OH 1-950 CCF 3 N CH CCl H CH 2CH 2CH 2 OCH 3 1-951 CCF 3 N CH CCl H CH 2CH 2CH 2 OCH 2CH 3 1-952 CCF 3 N CH CCl H CH 2CH 2CH 2 OCH 2Ph 1-953 CCF 3 N CH CCl H CH 2CH 2CH 2 NHSO 2CH 3 1-954 CCF 3 N CH CCl H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-955 CCl N CH CBr H CH 2CH 2CH 2 OH 1-956 CCl N CH CBr H CH 2CH 2CH 2 OCH 3 1-957 CCl N CH CBr H CH 2CH 2CH 2 OCH 2CH 3 1-958 CCl N CH CBr H CH 2CH 2CH 2 OCH 2Ph 1-959 CCl N CH CBr H CH 2CH 2CH 2 NHSO 2CH 3 1-960 CCl N CH CBr H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-961 CCl N CH CCH 3 H CH 2CH 2CH 2 OH 1-962 CCl N CH CCH 3 H CH 2CH 2CH 2 OCH 3 1-963 CCl N CH CCH 3 H CH 2CH 2CH 2 OCH 2CH 3 1-964 CCl N CH CCH 3 H CH 2CH 2CH 2 OCH 2Ph 1-965 CCl N CH CCH 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-966 CCl N CH CCH 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-967 CCl N CH CCF 2H H CH 2CH 2CH 2 OH 1-968 CCl N CH CCF 2H H CH 2CH 2CH 2 OCH 3 1-969 CCl N CH CCF 2H H CH 2CH 2CH 2 OCH 2CH 3 1-970 CCl N CH CCF 2H H CH 2CH 2CH 2 OCH 2Ph 1-971 CCl N CH CCF 2H H CH 2CH 2CH 2 NHSO 2CH 3 1-972 CCl N CH CCF 2H H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-973 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 OH 1-974 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 OCH 3 1-975 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 OCH 2CH 3 1-976 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 OCH 2Ph 1-977 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-978 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-979 CCl N CH CCF 3 H CH 2CH 2CH 2 OH 1-980 CCl N CH CCF 3 H CH 2CH 2CH 2 OCH 3 1-981 CCl N CH CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-982 CCl N CH CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-983 CCl N CH CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-984 CCl N CH CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-985 CH N CH CCF 3 H CH 2CH 2CH 2 OH 1-986 CH N CH CCF 3 H CH 2CH 2CH 2 OCH 3 1-987 CH N CH CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-988 CH N CH CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-989 CH N CH CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-990 CH N CH CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-991 CF N CH CCF 3 H CH 2CH 2CH 2 OH 1-992 CF N CH CCF 3 H CH 2CH 2CH 2 OCH 3 1-993 CF N CH CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-994 CF N CH CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-995 CF N CH CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-996 CF N CH CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-997 CBr N CH CCF 3 H CH 2CH 2CH 2 OH 1-998 CBr N CH CCF 3 H CH 2CH 2CH 2 OCH 3 1-999 CBr N CH CCF 3 H CH 2CH 2CH 2 OCH 2CH 3 1-1000 CBr N CH CCF 3 H CH 2CH 2CH 2 OCH 2Ph 1-1001 CBr N CH CCF 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-1002 CBr N CH CCF 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1003 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 OH 1-1004 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 OCH 3 1-1005 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 OCH 2CH 3 1-1006 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 OCH 2Ph 1-1007 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 NHSO 2CH 3 1-1008 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1009 CH CH N *COCF 2O CH 2CH 2CH 2 OH 1-1010 CH CH N *COCF 2O CH 2CH 2CH 2 OCH 3 1-1011 CH CH N *COCF 2O CH 2CH 2CH 2 OCH 2CH 3 1-1012 CH CH N *COCF 2O CH 2CH 2CH 2 OCH 2Ph 1-1013 CH CH N *COCF 2O CH 2CH 2CH 2 NHSO 2CH 3 1-1014 CH CH N *COCF 2O CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1015 CH CF N CH CF 3 CH 2CH 2CH 2 OH 1-1016 CH CF N CH CF 3 CH 2CH 2CH 2 OCH 3 1-1017 CH CF N CH CF 3 CH 2CH 2CH 2 OCH 2CH 3 1-1018 CH CF N CH CF 3 CH 2CH 2CH 2 OCH 2Ph 1-1019 CH CF N CH CF 3 CH 2CH 2CH 2 NHSO 2CH 3 1-1020 CH CF N CH CF 3 CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1021 CH CCl CCl N H CH 2CH 2CH 2 OH 1-1022 CH CCl CCl N H CH 2CH 2CH 2 OCH 3 1-1023 CH CCl CCl N H CH 2CH 2CH 2 OCH 2CH 3 1-1024 CH CCl CCl N H CH 2CH 2CH 2 OCH 2Ph 1-1025 CH CCl CCl N H CH 2CH 2CH 2 NHSO 2CH 3 1-1026 CH CCl CCl N H CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1027 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 OH 1-1028 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1029 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1030 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1031 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1032 CCl CH CH CCH 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1033 N CH N CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1034 N CH N CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1035 N CH N CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1036 N CH N CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1037 N CH N CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1038 N CH N CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1039 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1040 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1041 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1042 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1043 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1044 NO CCl CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1045 CF N CH CF H CH 2CH 2CH 2CH 2 OH 1-1046 CF N CH CF H CH 2CH 2CH 2CH 2 OCH 3 1-1047 CF N CH CF H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1048 CF N CH CF H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1049 CF N CH CF H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1050 CF N CH CF H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1051 CCl N CH CF H CH 2CH 2CH 2CH 2 OH 1-1052 CCl N CH CF H CH 2CH 2CH 2CH 2 OCH 3 1-1053 CCl N CH CF H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1054 CCl N CH CF H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1055 CCl N CH CF H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1056 CCl N CH CF H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1057 CCl N CH CCl H CH 2CH 2CH 2CH 2 OH 1-1058 CCl N CH CCl H CH 2CH 2CH 2CH 2 OCH 3 1-1059 CCl N CH CCl H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1060 CCl N CH CCl H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1061 CCl N CH CCl H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1062 CCl N CH CCl H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1063 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 OH 1-1064 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 OCH 3 1-1065 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1066 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1067 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1068 CCF 3 N CH CCl H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1069 CCl N CH CBr H CH 2CH 2CH 2CH 2 OH 1-1070 CCl N CH CBr H CH 2CH 2CH 2CH 2 OCH 3 1-1071 CCl N CH CBr H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1072 CCl N CH CBr H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1073 CCl N CH CBr H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1074 CCl N CH CBr H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1075 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 OH 1-1076 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1077 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1078 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1079 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1080 CCl N CH CCH 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1081 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 OH 1-1082 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 OCH 3 1-1083 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1084 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1085 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1086 CCl N CH CCF 2H H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1087 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 OH 1-1088 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1089 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1090 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1091 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1092 CCl N CH CCF 2CH 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1093 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1094 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1095 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1096 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1097 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1098 CCl N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1099 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1100 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1101 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1102 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1103 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1104 CH N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1105 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1106 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1107 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1108 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1109 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1110 CF N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1111 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 OH 1-1112 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1113 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1114 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1115 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1116 CBr N CH CCF 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1117 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 OH 1-1118 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 OCH 3 1-1119 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1120 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1121 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1122 CCl N CH CSO 2CH 3 H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1123 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 OH 1-1124 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 OCH 3 1-1125 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1126 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 OCH 2Ph 1-1127 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1128 CH CH N *COCF 2O CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1129 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 OH 1-1130 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 OCH 3 1-1131 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1132 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 OCH 2Ph 1-1133 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1134 CH CF N CH CF 3 CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 1-1135 CH CCl CCl N H CH 2CH 2CH 2CH 2 OH 1-1136 CH CCl CCl N H CH 2CH 2CH 2CH 2 OCH 3 1-1137 CH CCl CCl N H CH 2CH 2CH 2CH 2 OCH 2CH 3 1-1138 CH CCl CCl N H CH 2CH 2CH 2CH 2 OCH 2Ph 1-1139 CH CCl CCl N H CH 2CH 2CH 2CH 2 NHSO 2CH 3 1-1140 CH CCl CCl N H CH 2CH 2CH 2CH 2 NHSO 2N(CH 3)CH(CH 3) 2 *其中X 4係C-R 19，並且R 2和R 19與它們所附接的碳原子一起形成包含兩個氧原子的飽和5員環，並且該環被2個由R 16表示的基團取代，其中兩個R 16基團皆為氟。 Table 1 below discloses 1140 specific compounds of formula (I), designated compounds 1-1 to 1-1140, where R 3System hydrogen, R 4Chlorine, R 20System hydrogen, R twenty oneis hydrogen, m is 0, Y is C-H, and B is oxygen. [ surface 1 ] Compound number X 1 X 2 X 3 X 4 R 2 D R 8 1-1 CCl CH CH CCH 3 H CH 2 OH 1-2 CCl CH CH CCH 3 H CH 2 OCH 3 1-3 CCl CH CH CCH 3 H CH 2 OCH 2 CH 3 1-4 CCl CH CH CCH 3 H CH 2 OCH 2 Ph 1-5 CCl CH CH CCH 3 H CH 2 NHSO 2 CH 3 1-6 CCl CH CH CCH 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-7 N CH N CCF 3 H CH 2 OH 1-8 N CH N CCF 3 H CH 2 OCH 3 1-9 N CH N CCF 3 H CH 2 OCH 2 CH 3 1-10 N CH N CCF 3 H CH 2 OCH 2 Ph 1-11 N CH N CCF 3 H CH 2 NHSO 2 CH 3 1-12 N CH N CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-13 NO CCl CH CCF 3 H CH 2 OH 1-14 NO CCl CH CCF 3 H CH 2 OCH 3 1-15 NO CCl CH CCF 3 H CH 2 OCH 2 CH 3 1-16 NO CCl CH CCF 3 H CH 2 OCH 2 Ph 1-17 NO CCl CH CCF 3 H CH 2 NHSO 2 CH 3 1-18 NO CCl CH CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-19 CF N CH CF H CH 2 OH 1-20 CF N CH CF H CH 2 OCH 3 1-21 CF N CH CF H CH 2 OCH 2 CH 3 1-22 CF N CH CF H CH 2 OCH 2 Ph 1-23 CF N CH CF H CH 2 NHSO 2 CH 3 1-24 CF N CH CF H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-25 CCl N CH CF H CH 2 OH 1-26 CCl N CH CF H CH 2 OCH 3 1-27 CCl N CH CF H CH 2 OCH 2 CH 3 1-28 CCl N CH CF H CH 2 OCH 2 Ph 1-29 CCl N CH CF H CH 2 NHSO 2 CH 3 1-30 CCl N CH CF H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-31 CCl N CH CCl H CH 2 OH 1-32 CCl N CH CCl H CH 2 OCH 3 1-33 CCl N CH CCl H CH 2 OCH 2 CH 3 1-34 CCl N CH CCl H CH 2 OCH 2 Ph 1-35 CCl N CH CCl H CH 2 NHSO 2 CH 3 1-36 CCl N CH CCl H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-37 CCF 3 N CH CCl H CH 2 OH 1-38 CCF 3 N CH CCl H CH 2 OCH 3 1-39 CCF 3 N CH CCl H CH 2 OCH 2 CH 3 1-40 CCF 3 N CH CCl H CH 2 OCH 2 Ph 1-41 CCF 3 N CH CCl H CH 2 NHSO 2 CH 3 1-42 CCF 3 N CH CCl H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-43 CCl N CH CBr H CH 2 OH 1-44 CCl N CH CBr H CH 2 OCH 3 1-45 CCl N CH CBr H CH 2 OCH 2 CH 3 1-46 CCl N CH CBr H CH 2 OCH 2 Ph 1-47 CCl N CH CBr H CH 2 NHSO 2 CH 3 1-48 CCl N CH CBr H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-49 CCl N CH CCH 3 H CH 2 OH 1-50 CCl N CH CCH 3 H CH 2 OCH 3 1-51 CCl N CH CCH 3 H CH 2 OCH 2 CH 3 1-52 CCl N CH CCH 3 H CH 2 OCH 2 Ph 1-53 CCl N CH CCH 3 H CH 2 NHSO 2 CH 3 1-54 CCl N CH CCH 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-55 CCl N CH CCF2H H CH 2 OH 1-56 CCl N CH CCF2H H CH 2 OCH 3 1-57 CCl N CH CCF2H H CH 2 OCH 2 CH 3 1-58 CCl N CH CCF2H H CH 2 OCH 2 Ph 1-59 CCl N CH CCF2H H CH 2 NHSO 2 CH 3 1-60 CCl N CH CCF2H H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-61 CCl N CH CCF 2 CH 3 H CH 2 OH 1-62 CCl N CH CCF 2 CH 3 H CH 2 OCH 3 1-63 CCl N CH CCF 2 CH 3 H CH 2 OCH 2 CH 3 1-64 CCl N CH CCF 2 CH 3 H CH 2 OCH 2 Ph 1-65 CCl N CH CCF 2 CH 3 H CH 2 NHSO 2 CH 3 1-66 CCl N CH CCF 2 CH 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-67 CCl N CH CCF 3 H CH 2 OH 1-68 CCl N CH CCF 3 H CH 2 OCH 3 1-69 CCl N CH CCF 3 H CH 2 OCH 2 CH 3 1-70 CCl N CH CCF 3 H CH 2 OCH 2 Ph 1-71 CCl N CH CCF 3 H CH 2 NHSO 2 CH 3 1-72 CCl N CH CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-73 CH N CH CCF 3 H CH 2 OH 1-74 CH N CH CCF 3 H CH 2 OCH 3 1-75 CH N CH CCF 3 H CH 2 OCH 2 CH 3 1-76 CH N CH CCF 3 H CH 2 OCH 2 Ph 1-77 CH N CH CCF 3 H CH 2 NHSO 2 CH 3 1-78 CH N CH CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-79 CF N CH CCF 3 H CH 2 OH 1-80 CF N CH CCF 3 H CH 2 OCH 3 1-81 CF N CH CCF 3 H CH 2 OCH 2 CH 3 1-82 CF N CH CCF 3 H CH 2 OCH 2 Ph 1-83 CF N CH CCF 3 H CH 2 NHSO 2 CH 3 1-84 CF N CH CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-85 CBr N CH CCF 3 H CH 2 OH 1-86 CBr N CH CCF 3 H CH 2 OCH 3 1-87 CBr N CH CCF 3 H CH 2 OCH 2 CH 3 1-88 CBr N CH CCF 3 H CH 2 OCH 2 Ph 1-89 CBr N CH CCF 3 H CH 2 NHSO 2 CH 3 1-90 CBr N CH CCF 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-91 CCl N CH CSO 2 CH 3 H CH 2 OH 1-92 CCl N CH CSO 2 CH 3 H CH 2 OCH 3 1-93 CCl N CH CSO 2 CH 3 H CH 2 OCH 2 CH 3 1-94 CCl N CH CSO 2 CH 3 H CH 2 OCH 2 Ph 1-95 CCl N CH CSO 2 CH 3 H CH 2 NHSO 2 CH 3 1-96 CCl N CH CSO 2 CH 3 H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-97 CH CH N *COCF 2O CH 2 OH 1-98 CH CH N *COCF 2O CH 2 OCH 3 1-99 CH CH N *COCF 2O CH 2 OCH 2 CH 3 1-100 CH CH N *COCF 2O CH 2 OCH 2 Ph 1-101 CH CH N *COCF 2O CH 2 NHSO 2 CH 3 1-102 CH CH N *COCF 2O CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-103 CH F N CH CF 3 CH 2 OH 1-104 CH F N CH CF 3 CH 2 OCH 3 1-105 CH F N CH CF 3 CH 2 OCH 2 CH 3 1-106 CH F N CH CF 3 CH 2 OCH 2 Ph 1-107 CH F N CH CF 3 CH 2 NHSO 2 CH 3 1-108 CH F N CH CF 3 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-109 CH CCl CCl N H CH 2 OH 1-110 CH CCl CCl N H CH 2 OCH 3 1-111 CH CCl CCl N H CH 2 OCH 2 CH 3 1-112 CH CCl CCl N H CH 2 OCH 2 Ph 1-113 CH CCl CCl N H CH 2 NHSO 2 CH 3 1-114 CH CCl CCl N H CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-115 CCl CH CH CCH 3 H CH(CH 3 ) OH 1-116 CCl CH CH CCH 3 H CH(CH 3 ) OCH 3 1-117 CCl CH CH CCH 3 H CH(CH 3 ) OCH 2 CH 3 1-118 CCl CH CH CCH 3 H CH(CH 3 ) OCH 2 Ph 1-119 CCl CH CH CCH 3 H CH(CH 3 ) NHSO 2 CH 3 1-120 CCl CH CH CCH 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-121 N CH N CCF 3 H CH(CH 3 ) OH 1-122 N CH N CCF 3 H CH(CH 3 ) OCH 3 1-123 N CH N CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-124 N CH N CCF 3 H CH(CH 3 ) OCH 2 Ph 1-125 N CH N CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-126 N CH N CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-127 NO CCl CH CCF 3 H CH(CH 3 ) OH 1-128 NO CCl CH CCF 3 H CH(CH 3 ) OCH 3 1-129 NO CCl CH CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-130 NO CCl CH CCF 3 H CH(CH 3 ) OCH 2 Ph 1-131 NO CCl CH CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-132 NO CCl CH CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-133 CF N CH CF H CH(CH 3 ) OH 1-134 CF N CH CF H CH(CH 3 ) OCH 3 1-135 CF N CH CF H CH(CH 3 ) OCH 2 CH 3 1-136 CF N CH CF H CH(CH 3 ) OCH 2 Ph 1-137 CF N CH CF H CH(CH 3 ) NHSO 2 CH 3 1-138 CF N CH CF H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-139 CCl N CH CF H CH(CH 3 ) OH 1-140 CCl N CH CF H CH(CH 3 ) OCH 3 1-141 CCl N CH CF H CH(CH 3 ) OCH 2 CH 3 1-142 CCl N CH CF H CH(CH 3 ) OCH 2 Ph 1-143 CCl N CH CF H CH(CH 3 ) NHSO 2 CH 3 1-144 CCl N CH CF H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-145 CCl N CH CCl H CH(CH 3 ) OH 1-146 CCl N CH CCl H CH(CH 3 ) OCH 3 1-147 CCl N CH CCl H CH(CH 3 ) OCH 2 CH 3 1-148 CCl N CH CCl H CH(CH 3 ) OCH 2 Ph 1-149 CCl N CH CCl H CH(CH 3 ) NHSO 2 CH 3 1-150 CCl N CH CCl H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-151 CCF 3 N CH CCl H CH(CH 3 ) OH 1-152 CCF 3 N CH CCl H CH(CH 3 ) OCH 3 1-153 CCF 3 N CH CCl H CH(CH 3 ) OCH 2 CH 3 1-154 CCF 3 N CH CCl H CH(CH 3 ) OCH 2 Ph 1-155 CCF 3 N CH CCl H CH(CH 3 ) NHSO 2 CH 3 1-156 CCF 3 N CH CCl H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-157 CCl N CH CBr H CH(CH 3 ) OH 1-158 CCl N CH CBr H CH(CH 3 ) OCH 3 1-159 CCl N CH CBr H CH(CH 3 ) OCH 2 CH 3 1-160 CCl N CH CBr H CH(CH 3 ) OCH 2 Ph 1-161 CCl N CH CBr H CH(CH 3 ) NHSO 2 CH 3 1-162 CCl N CH CBr H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-163 CCl N CH CCH 3 H CH(CH 3 ) OH 1-164 CCl N CH CCH 3 H CH(CH 3 ) OCH 3 1-165 CCl N CH CCH 3 H CH(CH 3 ) OCH 2 CH 3 1-166 CCl N CH CCH 3 H CH(CH 3 ) OCH 2 Ph 1-167 CCl N CH CCH 3 H CH(CH 3 ) NHSO 2 CH 3 1-168 CCl N CH CCH 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-169 CCl N CH CCF2H H CH(CH 3 ) OH 1-170 CCl N CH CCF2H H CH(CH 3 ) OCH 3 1-171 CCl N CH CCF2H H CH(CH 3 ) OCH 2 CH 3 1-172 CCl N CH CCF2H H CH(CH 3 ) OCH 2 Ph 1-173 CCl N CH CCF2H H CH(CH 3 ) NHSO 2 CH 3 1-174 CCl N CH CCF2H H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-175 CCl N CH CCF 2 CH 3 H CH(CH 3 ) OH 1-176 CCl N CH CCF 2 CH 3 H CH(CH 3 ) OCH 3 1-177 CCl N CH CCF 2 CH 3 H CH(CH 3 ) OCH 2 CH 3 1-178 CCl N CH CCF 2 CH 3 H CH(CH 3 ) OCH 2 Ph 1-179 CCl N CH CCF 2 CH 3 H CH(CH 3 ) NHSO 2 CH 3 1-180 CCl N CH CCF 2 CH 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-181 CCl N CH CCF 3 H CH(CH 3 ) OH 1-182 CCl N CH CCF 3 H CH(CH 3 ) OCH 3 1-183 CCl N CH CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-184 CCl N CH CCF 3 H CH(CH 3 ) OCH 2 Ph 1-185 CCl N CH CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-186 CCl N CH CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-187 CH N CH CCF 3 H CH(CH 3 ) OH 1-188 CH N CH CCF 3 H CH(CH 3 ) OCH 3 1-189 CH N CH CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-190 CH N CH CCF 3 H CH(CH 3 ) OCH 2 Ph 1-191 CH N CH CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-192 CH N CH CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-193 CF N CH CCF 3 H CH(CH 3 ) OH 1-194 CF N CH CCF 3 H CH(CH 3 ) OCH 3 1-195 CF N CH CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-196 CF N CH CCF 3 H CH(CH 3 ) OCH 2 Ph 1-197 CF N CH CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-198 CF N CH CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-199 CBr N CH CCF 3 H CH(CH 3 ) OH 1-200 CBr N CH CCF 3 H CH(CH 3 ) OCH 3 1-201 CBr N CH CCF 3 H CH(CH 3 ) OCH 2 CH 3 1-202 CBr N CH CCF 3 H CH(CH 3 ) OCH 2 Ph 1-203 CBr N CH CCF 3 H CH(CH 3 ) NHSO 2 CH 3 1-204 CBr N CH CCF 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-205 CCl N CH CSO 2 CH 3 H CH(CH 3 ) OH 1-206 CCl N CH CSO 2 CH 3 H CH(CH 3 ) OCH 3 1-207 CCl N CH CSO 2 CH 3 H CH(CH 3 ) OCH 2 CH 3 1-208 CCl N CH CSO 2 CH 3 H CH(CH 3 ) OCH 2 Ph 1-209 CCl N CH CSO 2 CH 3 H CH(CH 3 ) NHSO 2 CH 3 1-210 CCl N CH CSO 2 CH 3 H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-211 CH CH N *COCF 2 O CH(CH 3 ) CH(CH 3 ) 1-212 CH CH N *COCF 2O CH(CH 3 ) CH(CH 3 ) 1-213 CH CH N *COCF 2 O CH(CH 3 ) CH(CH 3 ) 1-214 CH CH N *COCF 2 O CH(CH 3 ) CH(CH 3 ) 1-215 CH CH N *COCF 2 O CH(CH 3 ) CH(CH 3 ) 1-216 CH CH N *COCF 2 O CH(CH 3 ) CH(CH 3 ) 1-217 CH CF N CH CF 3 CH(CH 3 ) OH 1-218 CH CF N CH CF 3 CH(CH 3 ) OCH 3 1-219 CH CF N CH CF 3 CH(CH 3 ) OCH 2 CH 3 1-220 CH CF N CH CF 3 CH(CH 3 ) OCH 2 Ph 1-221 CH CF N CH CF 3 CH(CH 3 ) NHSO 2 CH 3 1-222 CH CF N CH CF 3 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-223 CH CCl CCl N H CH(CH 3 ) OH 1-224 CH CCl CCl N H CH(CH 3 ) OCH 3 1-225 CH CCl CCl N H CH(CH 3 ) OCH 2 CH 3 1-226 CH CCl CCl N H CH(CH 3 ) OCH 2 Ph 1-227 CH CCl CCl N H CH(CH 3 ) NHSO 2 CH 3 1-228 CH CCl CCl N H CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-229 CCl CH CH CCH 3 H C(CH 3 ) 2 OH 1-230 CCl CH CH CCH 3 H C(CH 3 ) 2 OCH 3 1-231 CCl CH CH CCH 3 H C(CH 3 ) 2 OCH 2 CH 3 1-232 CCl CH CH CCH 3 H C(CH 3 ) 2 OCH 2 Ph 1-233 CCl CH CH CCH 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-234 CCl CH CH CCH 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-235 N CH N CCF 3 H C(CH 3 ) 2 OH 1-236 N CH N CCF 3 H C(CH 3 ) 2 OCH 3 1-237 N CH N CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-238 N CH N CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-239 N CH N CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-240 N CH N CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-241 NO CCl CH CCF 3 H C(CH 3 ) 2 OH 1-242 NO CCl CH CCF 3 H C(CH 3 ) 2 OCH 3 1-243 NO CCl CH CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-244 NO CCl CH CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-245 NO CCl CH CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-246 NO CCl CH CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-247 CF N CH CF H C(CH 3 ) 2 OH 1-248 CF N CH CF H C(CH 3 ) 2 OCH 3 1-249 CF N CH CF H C(CH 3 ) 2 OCH 2 CH 3 1-250 CF N CH CF H C(CH 3 ) 2 OCH 2 Ph 1-251 CF N CH CF H C(CH 3 ) 2 NHSO 2 CH 3 1-252 CF N CH CF H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-253 CCl N CH CF H C(CH 3 ) 2 OH 1-254 CCl N CH CF H C(CH 3 ) 2 OCH 3 1-255 CCl N CH CF H C(CH 3 ) 2 OCH 2 CH 3 1-256 CCl N CH CF H C(CH 3 ) 2 OCH 2 Ph 1-257 CCl N CH CF H C(CH 3 ) 2 NHSO 2 CH 3 1-258 CCl N CH CF H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-259 CCl N CH CCl H C(CH 3 ) 2 OH 1-260 CCl N CH CCl H C(CH 3 ) 2 OCH 3 1-261 CCl N CH CCl H C(CH 3 ) 2 OCH 2 CH 3 1-262 CCl N CH CCl H C(CH 3 ) 2 OCH 2 Ph 1-263 CCl N CH CCl H C(CH 3 ) 2 NHSO 2 CH 3 1-264 CCl N CH CCl H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-265 CCF 3 N CH CCl H C(CH 3 ) 2 OH 1-266 CCF 3 N CH CCl H C(CH 3 ) 2 OCH 3 1-267 CCF 3 N CH CCl H C(CH 3 ) 2 OCH 2 CH 3 1-268 CCF 3 N CH CCl H C(CH 3 ) 2 OCH 2 Ph 1-269 CCF 3 N CH CCl H C(CH 3 ) 2 NHSO 2 CH 3 1-270 CCF 3 N CH CCl H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-271 CCl N CH CBr H C(CH 3 ) 2 OH 1-272 CCl N CH CBr H C(CH 3 ) 2 OCH 3 1-273 CCl N CH CBr H C(CH 3 ) 2 OCH 2 CH 3 1-274 CCl N CH CBr H C(CH 3 ) 2 OCH 2 Ph 1-275 CCl N CH CBr H C(CH 3 ) 2 NHSO 2 CH 3 1-276 CCl N CH CBr H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-277 CCl N CH CCH 3 H C(CH 3 ) 2 OH 1-278 CCl N CH CCH 3 H C(CH 3 ) 2 OCH 3 1-279 CCl N CH CCH 3 H C(CH 3 ) 2 OCH 2 CH 3 1-280 CCl N CH CCH 3 H C(CH 3 ) 2 OCH 2 Ph 1-281 CCl N CH CCH 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-282 CCl N CH CCH 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-283 CCl N CH CCF2H H C(CH 3 ) 2 OH 1-284 CCl N CH CCF2H H C(CH 3 ) 2 OCH 3 1-285 CCl N CH CCF2H H C(CH 3 ) 2 OCH 2 CH 3 1-286 CCl N CH CCF2H H C(CH 3 ) 2 OCH 2 Ph 1-287 CCl N CH CCF2H H C(CH 3 ) 2 NHSO 2 CH 3 1-288 CCl N CH CCF2H H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-289 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 OH 1-290 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 OCH 3 1-291 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 OCH 2 CH 3 1-292 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 OCH 2 Ph 1-293 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-294 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-295 CCl N CH CCF 3 H C(CH 3 ) 2 OH 1-296 CCl N CH CCF 3 H C(CH 3 ) 2 OCH 3 1-297 CCl N CH CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-298 CCl N CH CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-299 CCl N CH CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-300 CCl N CH CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-301 CH N CH CCF 3 H C(CH 3 ) 2 OH 1-302 CH N CH CCF 3 H C(CH 3 ) 2 OCH 3 1-303 CH N CH CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-304 CH N CH CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-305 CH N CH CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-306 CH N CH CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-307 CF N CH CCF 3 H C(CH 3 ) 2 OH 1-308 CF N CH CCF 3 H C(CH 3 ) 2 OCH 3 1-309 CF N CH CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-310 CF N CH CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-311 CF N CH CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-312 CF N CH CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-313 CBr N CH CCF 3 H C(CH 3 ) 2 OH 1-314 CBr N CH CCF 3 H C(CH 3 ) 2 OCH 3 1-315 CBr N CH CCF 3 H C(CH 3 ) 2 OCH 2 CH 3 1-316 CBr N CH CCF 3 H C(CH 3 ) 2 OCH 2 Ph 1-317 CBr N CH CCF 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-318 CBr N CH CCF 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-319 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 OH 1-320 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 OCH 3 1-321 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 OCH 2 CH 3 1-322 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 OCH 2 Ph 1-323 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 NHSO 2 CH 3 1-324 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-325 CH CH N *COCF 2 O C(CH 3 ) 2 OH 1-326 CH CH N *COCF 2 O C(CH 3 ) 2 OCH 3 1-327 CH CH N *COCF 2O C(CH 3 ) 2 OCH 2 CH 3 1-328 CH CH N *COCF 2 O C(CH 3 ) 2 OCH 2 Ph 1-329 CH CH N *COCF 2 O C(CH 3 ) 2 NHSO 2 CH 3 1-330 CH CH N *COCF 2O C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-331 CH CF N CH CF 3 C(CH 3 ) 2 OH 1-332 CH CF N CH CF 3 C(CH 3 ) 2 OCH 3 1-333 CH CF N CH CF 3 C(CH 3 ) 2 OCH 2 CH 3 1-334 CH CF N CH CF 3 C(CH 3 ) 2 OCH 2 Ph 1-335 CH CF N CH CF 3 C(CH 3 ) 2 NHSO 2 CH 3 1-336 CH CF N CH CF 3 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-337 CH CCl CCl N H C(CH 3 ) 2 OH 1-338 CH CCl CCl N H C(CH 3 ) 2 OCH 3 1-339 CH CCl CCl N H C(CH 3 ) 2 OCH 2 CH 3 1-340 CH CCl CCl N H C(CH 3 ) 2 OCH 2 Ph 1-341 CH CCl CCl N H C(CH 3 ) 2 NHSO 2 CH 3 1-342 CH CCl CCl N H C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-343 CCl CH CH CCH 3 H CH 2 CH 2 OH 1-344 CCl CH CH CCH 3 H CH 2 CH 2 OCH 3 1-345 CCl CH CH CCH 3 H CH 2 CH 2 OCH 2 CH 3 1-346 CCl CH CH CCH 3 H CH 2 CH 2 OCH 2 Ph 1-347 CCl CH CH CCH 3 H CH 2 CH 2 NHSO 2 CH 3 1-348 CCl CH CH CCH 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-349 N CH N CCF 3 H CH 2 CH 2 OH 1-350 N CH N CCF 3 H CH 2 CH 2 OCH 3 1-351 N CH N CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-352 N CH N CCF 3 H CH 2 CH 2 OCH 2 Ph 1-353 N CH N CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-354 N CH N CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-355 NO CCl CH CCF 3 H CH 2 CH 2 OH 1-356 NO CCl CH CCF 3 H CH 2 CH 2 OCH 3 1-357 NO CCl CH CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-358 NO CCl CH CCF 3 H CH 2 CH 2 OCH 2 Ph 1-359 NO CCl CH CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-360 NO CCl CH CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-361 CF N CH CF H CH 2 CH 2 OH 1-362 CF N CH CF H CH 2 CH 2 OCH 3 1-363 CF N CH CF H CH 2 CH 2 OCH 2 CH 3 1-364 CF N CH CF H CH 2 CH 2 OCH 2 Ph 1-365 CF N CH CF H CH 2 CH 2 NHSO 2 CH 3 1-366 CF N CH CF H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-367 CCl N CH CF H CH 2 CH 2 OH 1-368 CCl N CH CF H CH 2 CH 2 OCH 3 1-369 CCl N CH CF H CH 2 CH 2 OCH 2 CH 3 1-370 CCl N CH CF H CH 2 CH 2 OCH 2 Ph 1-371 CCl N CH CF H CH 2 CH 2 NHSO 2 CH 3 1-372 CCl N CH CF H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-373 CCl N CH CCl H CH 2 CH 2 OH 1-374 CCl N CH CCl H CH 2 CH 2 OCH 3 1-375 CCl N CH CCl H CH 2 CH 2 OCH 2 CH 3 1-376 CCl N CH CCl H CH 2 CH 2 OCH 2 Ph 1-377 CCl N CH CCl H CH 2 CH 2 NHSO 2 CH 3 1-378 CCl N CH CCl H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-379 CCF 3 N CH CCl H CH 2 CH 2 OH 1-380 CCF 3 N CH CCl H CH 2 CH 2 OCH 3 1-381 CCF 3 N CH CCl H CH 2 CH 2 OCH 2 CH 3 1-382 CCF 3 N CH CCl H CH 2 CH 2 OCH 2 Ph 1-383 CCF 3 N CH CCl H CH 2 CH 2 NHSO 2 CH 3 1-384 CCF 3 N CH CCl H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-385 CCl N CH CBr H CH 2 CH 2 OH 1-386 CCl N CH CBr H CH 2 CH 2 OCH 3 1-387 CCl N CH CBr H CH 2 CH 2 OCH 2 CH 3 1-388 CCl N CH CBr H CH 2 CH 2 OCH 2 Ph 1-389 CCl N CH CBr H CH 2 CH 2 NHSO 2 CH 3 1-390 CCl N CH CBr H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-391 CCl N CH CCH 3 H CH 2 CH 2 OH 1-392 CCl N CH CCH 3 H CH 2 CH 2 OCH 3 1-393 CCl N CH CCH 3 H CH 2 CH 2 OCH 2 CH 3 1-394 CCl N CH CCH 3 H CH 2 CH 2 OCH 2 Ph 1-395 CCl N CH CCH 3 H CH 2 CH 2 NHSO 2 CH 3 1-396 CCl N CH CCH 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-397 CCl N CH CCF2H H CH 2 CH 2 OH 1-398 CCl N CH CCF2H H CH 2 CH 2 OCH 3 1-399 CCl N CH CCF2H H CH 2 CH 2 OCH 2 CH 3 1-400 CCl N CH CCF2H H CH 2 CH 2 OCH 2 Ph 1-401 CCl N CH CCF2H H CH 2 CH 2 NHSO 2 CH 3 1-402 CCl N CH CCF2H H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-403 CCl N CH CCF 2 CH 3 H CH 2 CH 2 OH 1-404 CCl N CH CCF 2 CH 3 H CH 2 CH 2 OCH 3 1-405 CCl N CH CCF 2 CH 3 H CH 2 CH 2 OCH 2 CH 3 1-406 CCl N CH CCF 2 CH 3 H CH 2 CH 2 OCH 2 Ph 1-407 CCl N CH CCF 2 CH 3 H CH 2 CH 2 NHSO 2 CH 3 1-408 CCl N CH CCF 2 CH 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-409 CCl N CH CCF 3 H CH 2 CH 2 OH 1-410 CCl N CH CCF 3 H CH 2 CH 2 OCH 3 1-411 CCl N CH CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-412 CCl N CH CCF 3 H CH 2 CH 2 OCH 2 Ph 1-413 CCl N CH CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-414 CCl N CH CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-415 CH N CH CCF 3 H CH 2 CH 2 OH 1-416 CH N CH CCF 3 H CH 2 CH 2 OCH 3 1-417 CH N CH CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-418 CH N CH CCF 3 H CH 2 CH 2 OCH 2 Ph 1-419 CH N CH CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-420 CH N CH CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-421 CF N CH CCF 3 H CH 2 CH 2 OH 1-422 CF N CH CCF 3 H CH 2 CH 2 OCH 3 1-423 CF N CH CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-424 CF N CH CCF 3 H CH 2 CH 2 OCH 2 Ph 1-425 CF N CH CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-426 CF N CH CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-427 CBr N CH CCF 3 H CH 2 CH 2 OH 1-428 CBr N CH CCF 3 H CH 2 CH 2 OCH 3 1-429 CBr N CH CCF 3 H CH 2 CH 2 OCH 2 CH 3 1-430 CBr N CH CCF 3 H CH 2 CH 2 OCH 2 Ph 1-431 CBr N CH CCF 3 H CH 2 CH 2 NHSO 2 CH 3 1-432 CBr N CH CCF 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-433 CCl N CH CSO 2 CH 3 H CH 2 CH 2 OH 1-434 CCl N CH CSO 2 CH 3 H CH 2 CH 2 OCH 3 1-435 CCl N CH CSO 2 CH 3 H CH 2 CH 2 OCH 2 CH 3 1-436 CCl N CH CSO 2 CH 3 H CH 2 CH 2 OCH 2 Ph 1-437 CCl N CH CSO 2 CH 3 H CH 2 CH 2 NHSO 2 CH 3 1-438 CCl N CH CSO 2 CH 3 H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-439 CH CH N *COCF 2 O CH 2 CH 2 OH 1-440 CH CH N *COCF 2O CH 2 CH 2 OCH 3 1-441 CH CH N *COCF 2 O CH 2 CH 2 OCH 2 CH 3 1-442 CH CH N *COCF 2 O CH 2 CH 2 OCH 2 Ph 1-443 CH CH N *COCF 2 O CH 2 CH 2 NHSO 2 CH 3 1-444 CH CH N *COCF 2 O CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-445 CH CF N CH CF 3 CH 2 CH 2 OH 1-446 CH CF N CH CF 3 CH 2 CH 2 OCH 3 1-447 CH CF N CH CF 3 CH 2 CH 2 OCH 2 CH 3 1-448 CH CF N CH CF 3 CH 2 CH 2 OCH 2 Ph 1-449 CH CF N CH CF 3 CH 2 CH 2 NHSO 2 CH 3 1-450 CH CF N CH CF 3 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-451 CH CCl CCl N H CH 2 CH 2 OH 1-452 CH CCl CCl N H CH 2 CH 2 OCH 3 1-453 CH CCl CCl N H CH 2 CH 2 OCH 2 CH 3 1-454 CH CCl CCl N H CH 2 CH 2 OCH 2 Ph 1-455 CH CCl CCl N H CH 2 CH 2 NHSO 2 CH 3 1-456 CH CCl CCl N H CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-457 CCl CH CH CCH 3 H CH(CH 3 )CH 2 OH 1-458 CCl CH CH CCH 3 H CH(CH 3 )CH 2 OCH 3 1-459 CCl CH CH CCH 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-460 CCl CH CH CCH 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-461 CCl CH CH CCH 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-462 CCl CH CH CCH 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-463 N CH N CCF 3 H CH(CH 3 )CH 2 OH 1-464 N CH N CCF 3 H CH(CH 3 )CH 2 OCH 3 1-465 N CH N CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-466 N CH N CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-467 N CH N CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-468 N CH N CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-469 NO CCl CH CCF 3 H CH(CH 3 )CH 2 OH 1-470 NO CCl CH CCF 3 H CH(CH 3 )CH 2 OCH 3 1-471 NO CCl CH CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-472 NO CCl CH CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-473 NO CCl CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-474 NO CCl CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-475 CF N CH CF H CH(CH 3 )CH 2 OH 1-476 CF N CH CF H CH(CH 3 )CH 2 OCH 3 1-477 CF N CH CF H CH(CH 3 )CH 2 OCH 2 CH 3 1-478 CF N CH CF H CH(CH 3 )CH 2 OCH 2 Ph 1-479 CF N CH CF H CH(CH 3 )CH 2 NHSO 2 CH 3 1-480 CF N CH CF H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-481 CCl N CH CF H CH(CH 3 )CH 2 OH 1-482 CCl N CH CF H CH(CH 3 )CH 2 OCH 3 1-483 CCl N CH CF H CH(CH 3 )CH 2 OCH 2 CH 3 1-484 CCl N CH CF H CH(CH 3 )CH 2 OCH 2 Ph 1-485 CCl N CH CF H CH(CH 3 )CH 2 NHSO 2 CH 3 1-486 CCl N CH CF H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-487 CCl N CH CCl H CH(CH 3 )CH 2 OH 1-488 CCl N CH CCl H CH(CH 3 )CH 2 OCH 3 1-489 CCl N CH CCl H CH(CH 3 )CH 2 OCH 2 CH 3 1-490 CCl N CH CCl H CH(CH 3 )CH 2 OCH 2 Ph 1-491 CCl N CH CCl H CH(CH 3 )CH 2 NHSO 2 CH 3 1-492 CCl N CH CCl H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-493 CCF 3 N CH CCl H CH(CH 3 )CH 2 OH 1-494 CCF 3 N CH CCl H CH(CH 3 )CH 2 OCH 3 1-495 CCF 3 N CH CCl H CH(CH 3 )CH 2 OCH 2 CH 3 1-496 CCF 3 N CH CCl H CH(CH 3 )CH 2 OCH 2 Ph 1-497 CCF 3 N CH CCl H CH(CH 3 )CH 2 NHSO 2 CH 3 1-498 CCF 3 N CH CCl H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-499 CCl N CH CBr H CH(CH 3 )CH 2 OH 1-500 CCl N CH CBr H CH(CH 3 )CH 2 OCH 3 1-501 CCl N CH CBr H CH(CH 3 )CH 2 OCH 2 CH 3 1-502 CCl N CH CBr H CH(CH 3 )CH 2 OCH 2 Ph 1-503 CCl N CH CBr H CH(CH 3 )CH 2 NHSO 2 CH 3 1-504 CCl N CH CBr H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-505 CCl N CH CCH 3 H CH(CH 3 )CH 2 OH 1-506 CCl N CH CCH 3 H CH(CH 3 )CH 2 OCH 3 1-507 CCl N CH CCH 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-508 CCl N CH CCH 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-509 CCl N CH CCH 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-510 CCl N CH CCH 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-511 CCl N CH CCF2H H CH(CH 3 )CH 2 OH 1-512 CCl N CH CCF2H H CH(CH 3 )CH 2 OCH 3 1-513 CCl N CH CCF2H H CH(CH 3 )CH 2 OCH 2 CH 3 1-514 CCl N CH CCF2H H CH(CH 3 )CH 2 OCH 2 Ph 1-515 CCl N CH CCF2H H CH(CH 3 )CH 2 NHSO 2 CH 3 1-516 CCl N CH CCF2H H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-517 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 OH 1-518 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 OCH 3 1-519 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-520 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-521 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-522 CCl N CH CCF 2 CH 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-523 CCl N CH CCF 3 H CH(CH 3 )CH 2 OH 1-524 CCl N CH CCF 3 H CH(CH 3 )CH 2 OCH 3 1-525 CCl N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-526 CCl N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-527 CCl N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-528 CCl N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-529 CH N CH CCF 3 H CH(CH 3 )CH 2 OH 1-530 CH N CH CCF 3 H CH(CH 3 )CH 2 OCH 3 1-531 CH N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-532 CH N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-533 CH N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-534 CH N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-535 CF N CH CCF 3 H CH(CH 3 )CH 2 OH 1-536 CF N CH CCF 3 H CH(CH 3 )CH 2 OCH 3 1-537 CF N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-538 CF N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-539 CF N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-540 CF N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-541 CBr N CH CCF 3 H CH(CH 3 )CH 2 OH 1-542 CBr N CH CCF 3 H CH(CH 3 )CH 2 OCH 3 1-543 CBr N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-544 CBr N CH CCF 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-545 CBr N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-546 CBr N CH CCF 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-547 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 OH 1-548 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 OCH 3 1-549 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 OCH 2 CH 3 1-550 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 OCH 2 Ph 1-551 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 NHSO 2 CH 3 1-552 CCl N CH CSO 2 CH 3 H CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-553 CH CH N *COCF 2 O CH(CH 3 )CH 2 OH 1-554 CH CH N *COCF 2O CH(CH 3 )CH 2 OCH 3 1-555 CH CH N *COCF 2 O CH(CH 3 )CH 2 OCH 2 CH 3 1-556 CH CH N *COCF 2 O CH(CH 3 )CH 2 OCH 2 Ph 1-557 CH CH N *COCF 2 O CH(CH 3 )CH 2 NHSO 2 CH 3 1-558 CH CH N *COCF 2 O CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-559 CH CF N CH CF 3 CH(CH 3 )CH 2 OH 1-560 CH CF N CH CF 3 CH(CH 3 )CH 2 OCH 3 1-561 CH CF N CH CF 3 CH(CH 3 )CH 2 OCH 2 CH 3 1-562 CH CF N CH CF 3 CH(CH 3 )CH 2 OCH 2 Ph 1-563 CH CF N CH CF 3 CH(CH 3 )CH 2 NHSO 2 CH 3 1-564 CH CF N CH CF 3 CH(CH 3 )CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-565 CH CCl CCl N H CH(CH 3 )CH 2 OH 1-566 CH CCl CCl N H CH(CH 3 )CH 2 OCH 3 1-567 CH CCl CCl N H CH(CH 3 )CH 2 OCH 2 CH 3 1-568 CH CCl CCl N H CH(CH 3 )CH 2 OCH 2 Ph 1-569 CH CCl CCl N H CH(CH 3 )CH 2 NHSO 2 CH 3 1-570 CH CCl CCl N H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-571 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) OH 1-572 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) OCH 3 1-573 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-574 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-575 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-576 CCl CH CH CCH 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-577 N CH N CCF 3 H CH 2 CH(CH 3 ) OH 1-578 N CH N CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-579 N CH N CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-580 N CH N CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-581 N CH N CCF 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-582 N CH N CCF 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-583 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) OH 1-584 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-585 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-586 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-587 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-588 NO CCl CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-589 CF N CH CF H CH 2 CH(CH 3 ) OH 1-590 CF N CH CF H CH 2 CH(CH 3 ) OCH 3 1-591 CF N CH CF H CH 2 CH(CH 3 ) OCH 2 CH 3 1-592 CF N CH CF H CH 2 CH(CH 3 ) OCH 2 Ph 1-593 CF N CH CF H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-594 CF N CH CF H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-595 CCl N CH CF H CH 2 CH(CH 3 ) OH 1-596 CCl N CH CF H CH 2 CH(CH 3 ) OCH 3 1-597 CCl N CH CF H CH 2 CH(CH 3 ) OCH 2 CH 3 1-598 CCl N CH CF H CH 2 CH(CH 3 ) OCH 2 Ph 1-599 CCl N CH CF H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-600 CCl N CH CF H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-601 CCl N CH CCl H CH 2 CH(CH 3 ) OH 1-602 CCl N CH CCl H CH 2 CH(CH 3 ) OCH 3 1-603 CCl N CH CCl H CH 2 CH(CH 3 ) OCH 2 CH 3 1-604 CCl N CH CCl H CH 2 CH(CH 3 ) OCH 2 Ph 1-605 CCl N CH CCl H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-606 CCl N CH CCl H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-607 CCF 3 N CH CCl H CH 2 CH(CH 3 ) OH 1-608 CCF 3 N CH CCl H CH 2 CH(CH 3 ) OCH 3 1-609 CCF 3 N CH CCl H CH 2 CH(CH 3 ) OCH 2 CH 3 1-610 CCF 3 N CH CCl H CH 2 CH(CH 3 ) OCH 2 Ph 1-611 CCF 3 N CH CCl H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-612 CCF 3 N CH CCl H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-613 CCl N CH CBr H CH 2 CH(CH 3 ) OH 1-614 CCl N CH CBr H CH 2 CH(CH 3 ) OCH 3 1-615 CCl N CH CBr H CH 2 CH(CH 3 ) OCH 2 CH 3 1-616 CCl N CH CBr H CH 2 CH(CH 3 ) OCH 2 Ph 1-617 CCl N CH CBr H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-618 CCl N CH CBr H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-619 CCl N CH CCH 3 H CH 2 CH(CH 3 ) OH 1-620 CCl N CH CCH 3 H CH 2 CH(CH 3 ) OCH 3 1-621 CCl N CH CCH 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-622 CCl N CH CCH 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-623 CCl N CH CCH 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-624 CCl N CH CCH 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-625 CCl N CH CCF2H H CH 2 CH(CH 3 ) OH 1-626 CCl N CH CCF2H H CH 2 CH(CH 3 ) OCH 3 1-627 CCl N CH CCF2H H CH 2 CH(CH 3 ) OCH 2 CH 3 1-628 CCl N CH CCF2H H CH 2 CH(CH 3 ) OCH 2 Ph 1-629 CCl N CH CCF2H H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-630 CCl N CH CCF2H H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-631 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) OH 1-632 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) OCH 3 1-633 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-634 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-635 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-636 CCl N CH CCF 2 CH 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-637 CCl N CH CCF 3 H CH 2 CH(CH 3 ) OH 1-638 CCl N CH CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-639 CCl N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-640 CCl N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-641 CCl N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-642 CCl N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-643 CH N CH CCF 3 H CH 2 CH(CH 3 ) OH 1-644 CH N CH CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-645 CH N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-646 CH N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-647 CH N CH CCF 3 H CH 2 CHCH 3 NHSO 2 CH 3 1-648 CH N CH CCF 3 H CH 2 CHCH 3 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-649 CF N CH CCF 3 H CH 2 CH(CH 3 ) OH 1-650 CF N CH CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-651 CF N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-652 CF N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-653 CF N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-654 CF N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-655 CBr N CH CCF 3 H CH 2 CH(CH 3 ) OH 1-656 CBr N CH CCF 3 H CH 2 CH(CH 3 ) OCH 3 1-657 CBr N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-658 CBr N CH CCF 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-659 CBr N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-660 CBr N CH CCF 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-661 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) OH 1-662 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) OCH 3 1-663 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) OCH 2 CH 3 1-664 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) OCH 2 Ph 1-665 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-666 CCl N CH CSO 2 CH 3 H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-667 CH CH N *COCF 2 O CH 2 CH(CH 3 ) OH 1-668 CH CH N *COCF 2 O CH 2 CH(CH 3 ) OCH 3 1-669 CH CH N *COCF 2O CH 2 CH(CH 3 ) OCH 2 CH 3 1-670 CH CH N *COCF 2 O CH 2 CH(CH 3 ) OCH 2 Ph 1-671 CH CH N *COCF 2O CH 2 CH(CH 3 ) NHSO 2 CH 3 1-672 CH CH N *COCF 2 O CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-673 CH CF N CH CF 3 CH 2 CH(CH 3 ) OH 1-674 CH CF N CH CF 3 CH 2 CH(CH 3 ) OCH 3 1-675 CH CF N CH CF 3 CH 2 CH(CH 3 ) OCH 2 CH 3 1-676 CH CF N CH CF 3 CH 2 CH(CH 3 ) OCH 2 Ph 1-677 CH CF N CH CF 3 CH 2 CH(CH 3 ) NHSO 2 CH 3 1-678 CH CF N CH CF 3 CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-679 CH CCl CCl N H CH 2 CH(CH 3 ) OH 1-680 CH CCl CCl N H CH 2 CH(CH 3 ) OCH 3 1-681 CH CCl CCl N H CH 2 CH(CH 3 ) OCH 2 CH 3 1-682 CH CCl CCl N H CH 2 CH(CH 3 ) OCH 2 Ph 1-683 CH CCl CCl N H CH 2 CH(CH 3 ) NHSO 2 CH 3 1-684 CH CCl CCl N H CH 2 CH(CH 3 ) NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-685 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 OH 1-686 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 3 1-687 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-688 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-689 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-690 CCl CH CH CCH 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-691 N CH N CCF 3 H C(CH 3 ) 2 CH 2 OH 1-692 N CH N CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-693 N CH N CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-694 N CH N CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-695 N CH N CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-696 N CH N CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-697 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 OH 1-698 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-699 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-700 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-701 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-702 NO CCl CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-703 CF N CH CF H C(CH 3 ) 2 CH 2 OH 1-704 CF N CH CF H C(CH 3 ) 2 CH 2 OCH 3 1-705 CF N CH CF H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-706 CF N CH CF H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-707 CF N CH CF H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-708 CF N CH CF H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-709 CCl N CH CF H C(CH 3 ) 2 CH 2 OH 1-710 CCl N CH CF H C(CH 3 ) 2 CH 2 OCH 3 1-711 CCl N CH CF H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-712 CCl N CH CF H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-713 CCl N CH CF H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-714 CCl N CH CF H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-715 CCl N CH CCl H C(CH 3 ) 2 CH 2 OH 1-716 CCl N CH CCl H C(CH 3 ) 2 CH 2 OCH 3 1-717 CCl N CH CCl H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-718 CCl N CH CCl H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-719 CCl N CH CCl H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-720 CCl N CH CCl H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-721 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 OH 1-722 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 OCH 3 1-723 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-724 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-725 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-726 CCF 3 N CH CCl H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-727 CCl N CH CBr H C(CH 3 ) 2 CH 2 OH 1-728 CCl N CH CBr H C(CH 3 ) 2 CH 2 OCH 3 1-729 CCl N CH CBr H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-730 CCl N CH CBr H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-731 CCl N CH CBr H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-732 CCl N CH CBr H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-733 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 OH 1-734 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 3 1-735 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-736 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-737 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-738 CCl N CH CCH 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-739 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 OH 1-740 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 OCH 3 1-741 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-742 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-743 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-744 CCl N CH CCF2H H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-745 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 OH 1-746 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 3 1-747 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-748 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-749 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-750 CCl N CH CCF 2 CH 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-751 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 OH 1-752 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-753 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-754 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-755 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-756 CCl N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-757 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 OH 1-758 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-759 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-760 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-761 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-762 CH N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-763 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 OH 1-764 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-765 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-766 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-767 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-768 CF N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-769 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 OH 1-770 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 3 1-771 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-772 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-773 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-774 CBr N CH CCF 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-775 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 OH 1-776 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 3 1-777 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-778 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-779 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-780 CCl N CH CSO 2 CH 3 H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-781 CH CH N *COCF 2 O C(CH 3 ) 2 CH 2 OH 1-782 CH CH N *COCF 2O C(CH 3 ) 2 CH 2 OCH 3 1-783 CH CH N *COCF 2 O C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-784 CH CH N *COCF 2 O C(CH 3 ) 2 CH 2 OCH 2 Ph 1-785 CH CH N *COCF 2 O C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-786 CH CH N *COCF 2 O C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-787 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 OH 1-788 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 OCH 3 1-789 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-790 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 OCH 2 Ph 1-791 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-792 CH CF N CH CF 3 C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-793 CH CCl CCl N H C(CH 3 ) 2 CH 2 OH 1-794 CH CCl CCl N H C(CH 3 ) 2 CH 2 OCH 3 1-795 CH CCl CCl N H C(CH 3 ) 2 CH 2 OCH 2 CH 3 1-796 CH CCl CCl N H C(CH 3 ) 2 CH 2 OCH 2 Ph 1-797 CH CCl CCl N H C(CH 3 ) 2 CH 2 NHSO 2 CH 3 1-798 CH CCl CCl N H C(CH 3 ) 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-799 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OH 1-800 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 3 1-801 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-802 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-803 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-804 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-805 N CH N CCF 3 H CH 2 C(CH 3 ) 2 OH 1-806 N CH N CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-807 N CH N CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-808 N CH N CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-809 N CH N CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-810 N CH N CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-811 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 OH 1-812 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-813 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-814 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-815 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-816 NO CCl CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-817 CF N CH CF H CH 2 C(CH 3 ) 2 OH 1-818 CF N CH CF H CH 2 C(CH 3 ) 2 OCH 3 1-819 CF N CH CF H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-820 CF N CH CF H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-821 CF N CH CF H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-822 CF N CH CF H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-823 CCl N CH CF H CH 2 C(CH 3 ) 2 OH 1-824 CCl N CH CF H CH 2 C(CH 3 ) 2 OCH 3 1-825 CCl N CH CF H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-826 CCl N CH CF H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-827 CCl N CH CF H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-828 CCl N CH CF H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-829 CCl N CH CCl H CH 2 C(CH 3 ) 2 OH 1-830 CCl N CH CCl H CH 2 C(CH 3 ) 2 OCH 3 1-831 CCl N CH CCl H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-832 CCl N CH CCl H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-833 CCl N CH CCl H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-834 CCl N CH CCl H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-835 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 OH 1-836 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 OCH 3 1-837 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-838 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-839 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-840 CCF 3 N CH CCl H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-841 CCl N CH CBr H CH 2 C(CH 3 ) 2 OH 1-842 CCl N CH CBr H CH 2 C(CH 3 ) 2 OCH 3 1-843 CCl N CH CBr H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-844 CCl N CH CBr H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-845 CCl N CH CBr H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-846 CCl N CH CBr H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-847 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 OH 1-848 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 3 1-849 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-850 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-851 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-852 CCl N CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-853 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 OH 1-854 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 OCH 3 1-855 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-856 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-857 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-858 CCl N CH CCF2H H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-859 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 OH 1-860 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 3 1-861 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-862 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-863 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-864 CCl N CH CCF 2 CH 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-865 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 OH 1-866 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-867 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-868 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-869 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-870 CCl N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-871 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 OH 1-872 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-873 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-874 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-875 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-876 CH N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-877 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 OH 1-878 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-879 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-880 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-881 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-882 CF N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-883 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 OH 1-884 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 3 1-885 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-886 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-887 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-888 CBr N CH CCF 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-889 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 OH 1-890 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 3 1-891 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-892 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-893 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-894 CCl N CH CSO 2 CH 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-895 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 OH 1-896 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 OCH 3 1-897 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-898 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 OCH 2 Ph 1-899 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-900 CH CH N *COCF 2 O CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-901 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 OH 1-902 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 OCH 3 1-903 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-904 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 OCH 2 Ph 1-905 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-906 CH CF N CH CF 3 CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-907 CH CCl CCl N H CH 2 C(CH 3 ) 2 OH 1-908 CH CCl CCl N H CH 2 C(CH 3 ) 2 OCH 3 1-909 CH CCl CCl N H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-910 CH CCl CCl N H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-911 CH CCl CCl N H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-912 CH CCl CCl N H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-913 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OH 1-914 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 3 1-915 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 CH 3 1-916 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 OCH 2 Ph 1-917 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 CH 3 1-918 CCl CH CH CCH 3 H CH 2 C(CH 3 ) 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-919 N CH N CCF 3 H CH 2 CH 2 CH 2 OH 1-920 N CH N CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-921 N CH N CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-922 N CH N CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-923 N CH N CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-924 N CH N CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-925 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 OH 1-926 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-927 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-928 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-929 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-930 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-931 CF N CH CF H CH 2 CH 2 CH 2 OH 1-932 CF N CH CF H CH 2 CH 2 CH 2 OCH 3 1-933 CF N CH CF H CH 2 CH 2 CH 2 OCH 2 CH 3 1-934 CF N CH CF H CH 2 CH 2 CH 2 OCH 2 Ph 1-935 CF N CH CF H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-936 CF N CH CF H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-937 CCl N CH CF H CH 2 CH 2 CH 2 OH 1-938 CCl N CH CF H CH 2 CH 2 CH 2 OCH 3 1-939 CCl N CH CF H CH 2 CH 2 CH 2 OCH 2 CH 3 1-940 CCl N CH CF H CH 2 CH 2 CH 2 OCH 2 Ph 1-941 CCl N CH CF H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-942 CCl N CH CF H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-943 CCl N CH CCl H CH 2 CH 2 CH 2 OH 1-944 CCl N CH CCl H CH 2 CH 2 CH 2 OCH 3 1-945 CCl N CH CCl H CH 2 CH 2 CH 2 OCH 2 CH 3 1-946 CCl N CH CCl H CH 2 CH 2 CH 2 OCH 2 Ph 1-947 CCl N CH CCl H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-948 CCl N CH CCl H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-949 CCF 3 N CH CCl H CH 2 CH 2 CH 2 OH 1-950 CCF 3 N CH CCl H CH 2 CH 2 CH 2 OCH 3 1-951 CCF 3 N CH CCl H CH 2 CH 2 CH 2 OCH 2 CH 3 1-952 CCF 3 N CH CCl H CH 2 CH 2 CH 2 OCH 2 Ph 1-953 CCF 3 N CH CCl H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-954 CCF 3 N CH CCl H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-955 CCl N CH CBr H CH 2 CH 2 CH 2 OH 1-956 CCl N CH CBr H CH 2 CH 2 CH 2 OCH 3 1-957 CCl N CH CBr H CH 2 CH 2 CH 2 OCH 2 CH 3 1-958 CCl N CH CBr H CH 2 CH 2 CH 2 OCH 2 Ph 1-959 CCl N CH CBr H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-960 CCl N CH CBr H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-961 CCl N CH CCH 3 H CH 2 CH 2 CH 2 OH 1-962 CCl N CH CCH 3 H CH 2 CH 2 CH 2 OCH 3 1-963 CCl N CH CCH 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-964 CCl N CH CCH 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-965 CCl N CH CCH 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-966 CCl N CH CCH 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-967 CCl N CH CCF2H H CH 2 CH 2 CH 2 OH 1-968 CCl N CH CCF2H H CH 2 CH 2 CH 2 OCH 3 1-969 CCl N CH CCF2H H CH 2 CH 2 CH 2 OCH 2 CH 3 1-970 CCl N CH CCF2H H CH 2 CH 2 CH 2 OCH 2 Ph 1-971 CCl N CH CCF2H H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-972 CCl N CH CCF2H H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-973 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 OH 1-974 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 OCH 3 1-975 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-976 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-977 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-978 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-979 CCl N CH CCF 3 H CH 2 CH 2 CH 2 OH 1-980 CCl N CH CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-981 CCl N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-982 CCl N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-983 CCl N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-984 CCl N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-985 CH N CH CCF 3 H CH 2 CH 2 CH 2 OH 1-986 CH N CH CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-987 CH N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-988 CH N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-989 CH N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-990 CH N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-991 CF N CH CCF 3 H CH 2 CH 2 CH 2 OH 1-992 CF N CH CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-993 CF N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-994 CF N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-995 CF N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-996 CF N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-997 CBr N CH CCF 3 H CH 2 CH 2 CH 2 OH 1-998 CBr N CH CCF 3 H CH 2 CH 2 CH 2 OCH 3 1-999 CBr N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-1000 CBr N CH CCF 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-1001 CBr N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1002 CBr N CH CCF 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1003 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 OH 1-1004 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 OCH 3 1-1005 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 OCH 2 CH 3 1-1006 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 OCH 2 Ph 1-1007 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1008 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1009 CH CH N *COCF 2 O CH 2 CH 2 CH 2 OH 1-1010 CH CH N *COCF 2 O CH 2 CH 2 CH 2 OCH 3 1-1011 CH CH N *COCF 2 O CH 2 CH 2 CH 2 OCH 2 CH 3 1-1012 CH CH N *COCF 2 O CH 2 CH 2 CH 2 OCH 2 Ph 1-1013 CH CH N *COCF 2O CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1014 CH CH N *COCF 2 O CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1015 CH CF N CH CF 3 CH 2 CH 2 CH 2 OH 1-1016 CH CF N CH CF 3 CH 2 CH 2 CH 2 OCH 3 1-1017 CH CF N CH CF 3 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1018 CH CF N CH CF 3 CH 2 CH 2 CH 2 OCH 2 Ph 1-1019 CH CF N CH CF 3 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1020 CH CF N CH CF 3 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1021 CH CCl CCl N H CH 2 CH 2 CH 2 OH 1-1022 CH CCl CCl N H CH 2 CH 2 CH 2 OCH 3 1-1023 CH CCl CCl N H CH 2 CH 2 CH 2 OCH 2 CH 3 1-1024 CH CCl CCl N H CH 2 CH 2 CH 2 OCH 2 Ph 1-1025 CH CCl CCl N H CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1026 CH CCl CCl N H CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1027 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1028 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1029 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1030 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1031 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1032 CCl CH CH CCH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1033 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1034 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1035 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1036 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1037 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1038 N CH N CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1039 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1040 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1041 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1042 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1043 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1044 NO CCl CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1045 CF N CH CF H CH 2 CH 2 CH 2 CH 2 OH 1-1046 CF N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1047 CF N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1048 CF N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1049 CF N CH CF H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1050 CF N CH CF H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1051 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 OH 1-1052 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1053 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1054 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1055 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1056 CCl N CH CF H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1057 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 OH 1-1058 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1059 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1060 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1061 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1062 CCl N CH CCl H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1063 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 OH 1-1064 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1065 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1066 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1067 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1068 CCF 3 N CH CCl H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1069 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 OH 1-1070 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1071 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1072 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1073 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1074 CCl N CH CBr H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1075 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1076 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1077 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1078 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1079 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1080 CCl N CH CCH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1081 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 OH 1-1082 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1083 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1084 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1085 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1086 CCl N CH CCF2H H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1087 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1088 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1089 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1090 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1091 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1092 CCl N CH CCF 2 CH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1093 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1094 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1095 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1096 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1097 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1098 CCl N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1099 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1100 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1101 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1102 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1103 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1104 CH N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1105 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1106 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1107 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1108 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1109 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1110 CF N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1111 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1112 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1113 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1114 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1115 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1116 CBr N CH CCF 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1117 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OH 1-1118 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1119 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1120 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1121 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1122 CCl N CH CSO 2 CH 3 H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1123 CH CH N *COCF 2 O CH 2 CH 2 CH 2 CH 2 OH 1-1124 CH CH N *COCF 2O CH 2 CH 2 CH 2 CH 2 OCH 3 1-1125 CH CH N *COCF 2 O CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1126 CH CH N *COCF 2 O CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1127 CH CH N *COCF 2 O CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1128 CH CH N *COCF 2 O CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1129 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 OH 1-1130 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 OCH 3 1-1131 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1132 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1133 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1134 CH CF N CH CF 3 CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 1-1135 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 OH 1-1136 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 OCH 3 1-1137 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 OCH 2 CH 3 1-1138 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 OCH 2 Ph 1-1139 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 NHSO 2 CH 3 1-1140 CH CCl CCl N H CH 2 CH 2 CH 2 CH 2 NHSO 2 N(CH 3 )CH(CH 3 ) 2 *whereX 4Department C-R 19, and R 2and R 19Together with the carbon atoms to which they are attached they form a saturated 5-membered ring containing two oxygen atoms and this ring is replaced by 2 R 16represents a group substitution in which two R 16The groups are all fluorine.

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號2-1至2-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is oxygen, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號3-1至3-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is oxygen, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號4-1至4-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is oxygen, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號5-1至5-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is oxygen, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號6-1至6-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is oxygen, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號7-1至7-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號8-1至8-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號9-1至9-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號10-1至10-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號11-1至11-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號12-1至12-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號13-1至13-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號14-1至14-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號15-1至15-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號16-1至16-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號17-1至17-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係氧，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號18-1至18-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is oxygen, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號19-1至19-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is chlorine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號20-1至20-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號21-1至21-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號22-1至22-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號23-1至23-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係氫，R 21係氫，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號24-1至24-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is hydrogen, R 21 is hydrogen, m is 0, Y is CH and B is NH, and X 1 , X 2 , The values of X3 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號25-1至25-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號26-1至26-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號27-1至27-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號28-1至28-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號29-1至29-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係氫，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號30-1至30-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is hydrogen, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X 2 The values of ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號31-1至31-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號32-1至32-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係氯，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號33-1至33-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is chlorine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氫，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號34-1至34-1140。 1140 compounds of formula (I) (where R 3 is hydrogen, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氟，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號35-1至35-1140。 1140 compounds of formula (I) (where R 3 is fluorine, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

1140種具有式 (I) 的化合物（其中R 3係氯，R 4係溴，R 20係甲基，R 21係甲基，m係0，Y係C-H並且B係N-H，並且X 1、X 2、X 3、X 4、R 2、D和R 8的值係如表1中對於化合物1-1至1-1140給出的）分別被指定為化合物編號36-1至36-1140。 1140 compounds of formula (I) (where R 3 is chlorine, R 4 is bromine, R 20 is methyl, R 21 is methyl, m is 0, Y is CH and B is NH, and X 1 , X The values of 2 ,

本發明之化合物可以藉由有機化學領域的技術人員已知的技術製備。下文描述了用於生產具有式 (I) 的化合物的通用方法。除非在本文中另外說明，否則取代基X 1、X 2、X 3、X 4、m、Y、B、D、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11、R 12、R 13、R 14、R 15、R 16、R 17、R 18、R 19、R 20和R 21係如上文所定義的。 The compounds of the present invention can be prepared by techniques known to those skilled in the art of organic chemistry. General methods for producing compounds of formula (I) are described below. Unless otherwise stated herein, substituents X1 , X2 , X3 , X4 , m, Y, B, D, R1, R2 , R3 , R4 , R5 , R6 , R7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , R 17 , R 18 , R 19 , R 20 and R 21 are as defined above.

用於製備本發明之化合物的起始材料可以購買自通常的商品供應商或者可以藉由已知之方法製備。起始材料以及中間體可以在用於下一步驟之前，藉由先前技術之方法（如層析、結晶、蒸餾和過濾）進行純化。The starting materials used for preparing the compounds of the present invention can be purchased from usual commercial suppliers or can be prepared by known methods. Starting materials as well as intermediates can be purified by prior art methods such as chromatography, crystallization, distillation and filtration before use in the next step.

可以由具有式 (A) 的化合物和具有式 (B) 的化合物製備具有式 (I) 的化合物，如在反應流程1中所示。 反應流程 1 Compounds of formula (I) can be prepared from compounds of formula (A) and compounds of formula (B), as shown in Reaction Scheme 1. Reaction process 1

例如，具有式 (A) 的化合物和具有式 (B) 的化合物的混合物（其中Hal表示鹵素原子，例如氯、溴或碘原子）可以視需要在合適的配位基（如膦配位基，例如S-Phos）或金屬與配位基的預形成錯合物（如dppf二氯化鈀）和鹼（如乙酸鉀）的存在下，在合適的溶劑（如二㗁𠮿）中用金屬催化劑（如乙酸鈀）進行處理。For example, a mixture of a compound of formula (A) and a compound of formula (B), in which Hal represents a halogen atom, such as a chlorine, bromine or iodine atom, may optionally be modified with a suitable ligand, such as a phosphine ligand, For example, S-Phos) or a preformed complex of a metal with a ligand (such as dppf palladium dichloride) and a base (such as potassium acetate), using a metal catalyst in a suitable solvent (such as dichloride) (such as palladium acetate).

具有式 (A) 的硼酸（或對應的硼酸酯）係可獲得的或可以藉由文獻中眾所周知之方法製備。Boronic acids of formula (A) (or corresponding boronic acid esters) are available or can be prepared by methods well known in the literature.

可以由具有式 (C) 的苯胺製備具有式 (B) 的化合物，如在反應流程2中所示。 反應流程 2 Compounds of formula (B) can be prepared from anilines of formula (C) as shown in Reaction Scheme 2. Reaction process 2

例如，具有式 (C) 的化合物可以在合適的溶劑（如水和乙腈的混合物）中用金屬鹵化物（如碘化鉀）和亞硝基化試劑（如亞硝酸鈉和甲苯磺酸）進行處理。For example, compounds of formula (C) can be treated with a metal halide (such as potassium iodide) and a nitrosating agent (such as sodium nitrite and toluenesulfonic acid) in a suitable solvent (such as a mixture of water and acetonitrile).

可以由具有式 (D) 的硝基化合物製備具有式 (C) 的苯胺，如在反應流程3中所示。 反應流程 3 Anilines of formula (C) can be prepared from nitro compounds of formula (D) as shown in Reaction Scheme 3. Reaction process 3

例如，具有式 (D) 的化合物可以在合適的溶劑（如水和乙醇的混合物）中用還原劑（如鐵和氯化銨）進行處理。For example, compounds of formula (D) can be treated with reducing agents such as iron and ammonium chloride in a suitable solvent such as a mixture of water and ethanol.

可以由具有式 (E) 的硫醇和具有式 (F) 的化合物（其中LG表示脫離基，例如鹵素原子，如氯原子）製備具有式 (D) 的硝基化合物（其中m係0），如在反應流程4中所示。 反應流程 4 Nitro compounds of formula (D) (where m is 0) can be prepared from thiols of formula (E) and compounds of formula (F) (where LG represents a leaving group, such as a halogen atom, such as a chlorine atom), such as shown in Reaction Scheme 4. Reaction process 4

例如，具有式 (E) 的硝基化合物可以在鹼（如三乙胺）的存在下在合適的溶劑（如乙腈）中用具有式 (F) 的化合物進行處理。For example, a nitro compound of formula (E) can be treated with a compound of formula (F) in a suitable solvent (such as acetonitrile) in the presence of a base (such as triethylamine).

具有式 (E) 的硝基化合物係可獲得的或可以藉由文獻中眾所周知之方法製備。Nitro compounds of formula (E) are available or can be prepared by methods well known in the literature.

可以由具有式 (G) 的醇或胺和具有式 (H) 的酸製備具有式 (F) 的化合物，如在反應流程5中所示。 反應流程 5 Compounds of formula (F) can be prepared from alcohols or amines of formula (G) and acids of formula (H), as shown in Reaction Scheme 5. Reaction process 5

例如，具有式 (H) 的酸可以在合適的溶劑（如二氯甲烷和二甲基甲醯胺）中用活化劑（如草醯氯）進行處理，並且所得中間體然後在鹼（如三乙胺）的存在下在合適的溶劑（如二氯甲烷）中用具有式 (G) 的醇或胺進行處理。For example, an acid of formula (H) can be treated with an activator (such as oxalic acid chloride) in a suitable solvent (such as dichloromethane and dimethylformamide), and the resulting intermediate is then treated in a base (such as trimethylformamide). Treat with an alcohol or amine of formula (G) in the presence of a suitable solvent such as dichloromethane.

具有式 (G) 的醇和胺以及具有式 (H) 的酸係可獲得的或可以藉由文獻中眾所周知之方法製備。Alcohols and amines of formula (G) and acids of formula (H) are available or can be prepared by methods well known in the literature.

可替代地，可以由具有式 (F) 的化合物和具有式 (J) 的硫醇製備具有式 (I-A) 的化合物（其係具有式 (I) 的化合物，其中m = 0），如在反應流程6中所示。 反應流程 6 Alternatively, a compound of formula (IA) (which is a compound of formula (I) where m = 0) can be prepared from a compound of formula (F) and a thiol of formula (J), as in the reaction As shown in process 6. Reaction process 6

例如，具有式 (J) 的硫醇可以在鹼（如三乙胺）的存在下在合適的溶劑（如乙腈）中用具有式 (F) 化合物進行處理。For example, thiols of formula (J) can be treated with compounds of formula (F) in the presence of a base (such as triethylamine) in a suitable solvent (such as acetonitrile).

可以由具有式 (K) 的磺醯氯製備具有式 (J) 的硫醇，如在反應流程7中所示。 反應流程 7 Thiols of formula (J) can be prepared from sulfonyl chlorides of formula (K) as shown in Reaction Scheme 7. Reaction process 7

例如，具有式 (K) 的磺醯氯可以在合適的溶劑（如水和乙酸的混合物）中用還原劑（如二氯化錫）進行處理。For example, a sulfonyl chloride of formula (K) can be treated with a reducing agent such as tin dichloride in a suitable solvent such as a mixture of water and acetic acid.

可以由具有式 (L) 的化合物製備具有式 (K) 的磺醯氯，如在反應流程8中所示。 反應流程 8 Sulfonyl chlorides of formula (K) can be prepared from compounds of formula (L) as shown in Reaction Scheme 8. Reaction process 8

例如，具有式 (L) 的化合物可以用磺醯化劑（如氯磺酸）進行處理。For example, compounds of formula (L) can be treated with sulfonating agents such as chlorosulfonic acid.

可以由具有式 (M) 的化合物和具有式 (A) 的化合物製備具有式 (L) 的化合物，如在反應流程9中所示。 反應流程 9 Compounds of formula (L) can be prepared from compounds of formula (M) and compounds of formula (A), as shown in Reaction Scheme 9. Reaction process 9

例如，具有式 (A) 的化合物和具有式 (M) 的化合物的混合物（其中Hal表示鹵素原子，例如氯、溴或碘原子）可以視需要在合適的配位基（如膦配位基，例如S-Phos）或金屬與配位基的預形成錯合物（如dppf二氯化鈀）和鹼（如乙酸鉀）的存在下，在合適的溶劑（如二㗁𠮿）中用金屬催化劑（如乙酸鈀）進行處理。For example, a mixture of a compound of formula (A) and a compound of formula (M), in which Hal represents a halogen atom, such as a chlorine, bromine or iodine atom, can optionally be modified with a suitable ligand, such as a phosphine ligand, For example, S-Phos) or a preformed complex of a metal with a ligand (such as dppf palladium dichloride) and a base (such as potassium acetate), using a metal catalyst in a suitable solvent (such as dichloride) (such as palladium acetate).

具有式 (A) 的硼酸（或對應的硼酸酯）係可獲得的或可以藉由文獻中眾所周知之方法製備。Boronic acids of formula (A) (or corresponding boronic acid esters) are available or can be prepared by methods well known in the literature.

具有式 (M) 的化合物係可獲得的或者可以由具有式 (N) 的苯胺製備，如在反應流程10中所示。 反應流程 10 Compounds of formula (M) are available or can be prepared from anilines of formula (N) as shown in Reaction Scheme 10. Reaction process 10

例如，具有式 (N) 的化合物可以在合適的溶劑（如水和乙腈的混合物）中用金屬鹵化物（如碘化鉀）和亞硝基化試劑（如亞硝酸鈉和甲苯磺酸）進行處理。For example, compounds of formula (N) can be treated with a metal halide (such as potassium iodide) and a nitrosating agent (such as sodium nitrite and toluenesulfonic acid) in a suitable solvent (such as a mixture of water and acetonitrile).

還可以由具有式 (P) 的酸和具有式 (G) 的醇或胺製備具有式 (I) 的化合物，如在反應流程11中所示。 反應流程 11 Compounds of formula (I) can also be prepared from acids of formula (P) and alcohols or amines of formula (G), as shown in Reaction Scheme 11. Reaction process 11

例如，具有式 (P) 的酸可以在合適的溶劑（如二氯甲烷和二甲基甲醯胺）中用活化劑（如草醯氯）進行處理，並且所得中間體然後在鹼（如三乙胺）的存在下在合適的溶劑（如二氯甲烷）中用具有式 (G) 的醇或胺進行處理。For example, an acid of formula (P) can be treated with an activator (such as oxalic acid chloride) in a suitable solvent (such as dichloromethane and dimethylformamide), and the resulting intermediate is then treated in a base (such as trimethylformamide). Treat with an alcohol or amine of formula (G) in the presence of a suitable solvent such as dichloromethane.

可以由具有式 (Q) 的酯（其中R表示烷基或類似基團）製備具有式 (P) 的酸，如在反應流程12中所示。 反應流程 12 Acids of formula (P) can be prepared from esters of formula (Q), where R represents an alkyl or similar group, as shown in Reaction Scheme 12. Reaction process 12

例如，具有式 (Q) 的化合物可以在合適的溶劑（如二㗁𠮿）中用鹽酸進行處理。For example, a compound of formula (Q) can be treated with hydrochloric acid in a suitable solvent such as dimethicone.

可以由具有式 (J) 的硫醇和具有式 (R) 的酯（其中LG表示脫離基，例如鹵素原子，如氯原子，並且R表示烷基或類似基團）製備具有式 (Q) 的酯（其中m係0），如在反應流程13中所示。 反應流程 13 The ester of formula (Q) can be prepared from a thiol of formula (J) and an ester of formula (R) (where LG represents a leaving group, such as a halogen atom, such as a chlorine atom, and R represents an alkyl group or a similar group) (where m is 0), as shown in Reaction Scheme 13. Reaction process 13

例如，具有式 (J) 的硫醇可以在合適的溶劑（如乙腈）中在鹼（如三乙胺）的存在下用具有式 (R) 的化合物進行處理。For example, a thiol of formula (J) can be treated with a compound of formula (R) in a suitable solvent (such as acetonitrile) in the presence of a base (such as triethylamine).

具有式 (R) 的酯係可獲得的或可以藉由文獻中眾所周知之方法製備。Esters of formula (R) are available or can be prepared by methods well known in the literature.

可以由具有式 (I-A) 的化合物（其係具有式 (I) 的化合物，其中m係0）製備具有式 (I-B) 的化合物（其係具有式 (I) 的化合物，其中m係1或2），如在反應流程14中所示。 反應流程 14 Compounds of formula (IB), which are compounds of formula (I), where m is 1 or 2, can be prepared from compounds of formula (IA), which are compounds of formula (I), wherein m is 0 ), as shown in Reaction Scheme 14. Reaction process 14

例如，具有式 (I-A) 的化合物可以在合適的溶劑（如乙腈或二氯甲烷）中用氧化劑（例如過氧單磺酸鉀（oxone）或間氯過氧苯甲酸）進行處理。For example, compounds of formula (I-A) can be treated with an oxidizing agent such as potassium peroxymonosulfonate (oxone) or m-chloroperoxybenzoic acid in a suitable solvent such as acetonitrile or dichloromethane.

可以由具有式 (I-D) 的化合物（其係具有式 (I) 的化合物，其中R 8係OR 9）製備具有式 (I-C) 的化合物（其係具有式 (I) 的化合物，其中R 8係OH基團），如在反應流程15中所示。 反應流程 15 Compounds of formula (IC), which are compounds of formula (I), wherein R 8 is OR 9 , can be prepared from compounds of formula (ID), which are compounds of formula (I), wherein R 8 is OR 9 OH group) as shown in Reaction Scheme 15. Reaction process 15

例如，具有式 (I-D) 的化合物可以在合適的溶劑（如二㗁𠮿）中用鹽酸進行處理。For example, compounds of formula (I-D) can be treated with hydrochloric acid in a suitable solvent such as dibenzoethane.

可以由具有式 (I-C) 的化合物製備具有式 (I-E)的化合物（其係具有式 (I) 的化合物，其中R 8係NR 10R 11），如在反應流程16中所示。 反應流程 16 Compounds of formula (IE), which are compounds of formula (I) wherein R 8 is NR 10 R 11 , can be prepared from compounds of formula (IC), as shown in Reaction Scheme 16. Reaction process 16

例如，具有式 (I-C) 的化合物可以在合適的溶劑（如二氯甲烷）中用鹵化試劑（如草醯氯）進行處理以形成醯鹵，該醯鹵可以在鹼（如三乙胺）的存在下在合適的溶劑（如二氯甲烷）中用試劑HNR 10R 11進行處理。 For example, a compound of formula (IC) can be treated with a halogenating reagent (such as oxalyl chloride) in a suitable solvent (such as dichloromethane) to form a chloride halide, which can be dissolved in a base (such as triethylamine) Treat with reagent HNR 10 R 11 in the presence of a suitable solvent such as dichloromethane.

熟悉該項技術者將認識到，經常可以改變進行以上所述之轉化的順序或以可替代的方式將它們組合以製備各種具有式 (I) 的化合物。單個反應中也可以組合多個步驟。預期所有此類變化在本發明之範圍之內。One skilled in the art will recognize that the order in which the above described transformations are performed can often be changed or they can be combined in alternative ways to prepare various compounds of formula (I). Multiple steps can also be combined in a single reaction. All such variations are contemplated to be within the scope of this invention.

技術人員還將意識到一些試劑將與如本文定義的取代基X 1、X 2、X 3、X 4、m、Y、B、D、R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、R 11、R 12、R 13、R 14、R 15、R 16、R 17、R 18、R 19、R 20和R 21的某些值或組合不相容，並且任何附加的步驟，如保護和/或去保護步驟（實現所希望的轉化所必須的）對於技術人員將是清楚的。 The skilled person will also be aware that some reagents will be associated with the substituents X1 , X2 , X3 , X4 , m, Y, B, D, R1 , R2 , R3 , R4 , R5 as defined herein , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , R 17 , R 18 , R 19 , R 20 and some of R 21 These values or combinations are incompatible and any additional steps, such as protection and/or deprotection steps necessary to achieve the desired transformation, will be clear to the skilled person.

根據本發明之化合物可以按未經修飾的形式用作除草劑，但它們通常以多種方式使用配製佐劑（如載體、溶劑和表面活性物質）被配製成組成物。該等配製物可以處於不同的實體形式，例如，處於以下形式：撒粉劑、凝膠、可濕性粉劑、水可分散性顆粒劑、水可分散性片劑、發泡顆粒、可乳化的濃縮物、微可乳化濃縮物、水包油乳液、可流動油、水性分散體、油性分散體、懸乳液、膠囊懸浮液、可乳化的顆粒劑、可溶性液體、水可溶性濃縮物（以水或水混溶性有機溶劑作為載體）、浸漬的聚合物膜或處於已知的其他形式，例如從Manual on Development and Use of FAO and WHO Specifications for Pesticides[關於殺有害生物劑的FAO和WHO標準的發展和使用的手冊]，聯合國，第1版，二次修訂（2010）中已知的。對於水溶性化合物，較佳的是可溶性液體、水溶性濃縮物或水溶性顆粒劑。此類配製物可以直接使用或者可以使用前稀釋再使用。可以用例如水、液體肥料、微量營養素、生物有機體、油或溶劑來進行稀釋。The compounds according to the invention may be used in unmodified form as herbicides, but they are usually formulated into compositions in a variety of ways using formulation adjuvants such as carriers, solvents and surface-active substances. The formulations may be in different physical forms, for example in the following forms: dusting powders, gels, wettable powders, water-dispersible granules, water-dispersible tablets, expanded granules, emulsifiable concentrates Microemulsifiable concentrates, oil-in-water emulsions, flowable oils, aqueous dispersions, oily dispersions, suspoemulsions, capsule suspensions, emulsifiable granules, soluble liquids, water-soluble concentrates (based on water or water miscible organic solvent as carrier), impregnated polymer film or in other forms known, e.g. from Manual on Development and Use of FAO and WHO Specifications for Pesticides [FAO and WHO Specifications for Pesticides] Manual], United Nations, 1st edition, second revision (2010). For water-soluble compounds, soluble liquids, water-soluble concentrates or water-soluble granules are preferred. Such formulations can be used directly or can be diluted before use. Dilution can be carried out with, for example, water, liquid fertilizers, micronutrients, biological organisms, oils or solvents.

可以藉由例如將活性成分與配製佐劑混合來製備該等配製物以便獲得處於精細分散固體、顆粒、溶液、分散體或乳液形式的組成物。該等活性成分還可以與其他佐劑（例如精細分散固體、礦物油、植物或動物來源的油、改性的植物或動物來源的油、有機溶劑、水、表面活性物質或其組合）來一起配製。The formulations may be prepared, for example, by mixing the active ingredient with a formulating adjuvant so as to obtain the composition in the form of finely divided solids, granules, solutions, dispersions or emulsions. The active ingredients may also be combined with other adjuvants such as finely divided solids, mineral oil, oils of vegetable or animal origin, modified oils of vegetable or animal origin, organic solvents, water, surface-active substances or combinations thereof Preparation.

該等活性成分還可以被包含於非常精細的微膠囊中。微膠囊在多孔載體中含有活性成分。這使得活性成分能夠以受控的量釋放（例如，緩慢釋放）到環境中。微膠囊通常具有從0.1至500微米的直徑。它們包含的活性成分的量按重量計係膠囊重量的約從25%至95%。該等活性成分可以處於整體性的固體的形式、處於固體或液體分散體中的精細顆粒的形式或處於適合溶液的形式。包囊的膜可以包含例如天然的或合成的橡膠、纖維素、苯乙烯/丁二烯共聚物、聚丙烯腈、聚丙烯酸酯、聚酯、聚醯胺、聚脲、聚胺酯或化學改性的聚合物以及澱粉黃原酸酯、或熟悉該項技術者已知的其他聚合物。可替代地，可以形成非常精細的微膠囊，其中活性成分在基礎物質的固體基質中是以精細分散顆粒的形式被包含的，但該等微膠囊本身未經包裹。The active ingredients can also be contained in very fine microcapsules. Microcapsules contain the active ingredient in a porous carrier. This allows active ingredients to be released in controlled amounts (e.g., slowly released) into the environment. Microcapsules typically have diameters from 0.1 to 500 microns. They contain the active ingredient in an amount from about 25% to 95% by weight of the capsule. The active ingredients may be in the form of a solid solid, in the form of fine particles in a solid or liquid dispersion, or in a suitable solution. The membrane of the encapsulation may comprise, for example, natural or synthetic rubber, cellulose, styrene/butadiene copolymer, polyacrylonitrile, polyacrylate, polyester, polyamide, polyurea, polyurethane or chemically modified polymers as well as starch xanthate, or other polymers known to those skilled in the art. Alternatively, very fine microcapsules can be formed, in which the active ingredient is contained in the form of finely divided particles in a solid matrix of the base substance, but the microcapsules themselves are not encapsulated.

適合於製備根據本發明之組成物的配製佐劑本身係已知的。作為液體載體可以使用：水、甲苯、二甲苯、石油醚、植物油、丙酮、甲基乙基酮、環己酮、酸酐、乙腈、乙醯苯、乙酸戊酯、2-丁酮、碳酸丁烯酯、氯苯、環己烷、環己醇、乙酸烷基酯、二丙酮醇、1,2-二氯丙烷、二乙醇胺、對-二乙基苯、二甘醇、松脂酸二乙二醇酯、二甘醇丁基醚、二甘醇乙基醚、二甘醇甲醚、 N,N-二甲基甲醯胺、二甲基亞碸、1,4-二㗁𠮿、二丙二醇、二丙二醇甲基醚、雙丙甘醇二苯甲酸酯、二丙二醇、烷基吡咯啶酮、乙酸乙酯、2-乙基己醇、碳酸乙烯酯、1,1,1-三氯乙烷、2-庚酮、α-蒎烯、d-薴烯、乳酸乙酯、乙二醇、乙二醇丁基醚、乙二醇甲基醚、γ-丁內酯、丙三醇、乙酸甘油酯、二乙酸甘油酯、三乙酸甘油酯、十六烷、己二醇、乙酸異戊基酯、乙酸異冰片基(bornyl)酯、異辛烷、異佛爾酮、異丙苯、肉豆蔻酸異丙酯、乳酸、月桂胺、亞異丙基丙酮、甲氧基丙醇、甲基異戊基酮、甲基異丁基酮、月桂酸甲酯、辛酸甲酯、油酸甲酯、二氯甲烷、間二甲苯、正己烷、正辛胺、十八烷酸、辛胺乙酸酯、油酸、油胺、鄰二甲苯、苯酚、聚乙二醇、丙酸、乳酸丙酯、碳酸丙烯酯、丙二醇、丙二醇甲基醚、對-二甲苯、甲苯、磷酸三乙酯、三乙二醇、二甲苯磺酸、石蠟、礦物油、三氯乙烯、全氯乙烯、乙酸乙酯、乙酸戊酯、乙酸丁酯、丙二醇甲基醚、二乙二醇甲基醚、甲醇、乙醇、異丙醇以及更高分子量的醇，例如戊醇、四氫呋喃醇、己醇、辛醇、乙二醇、丙二醇、甘油、 N-甲基-2-吡咯啶酮等。 Formulation adjuvants suitable for the preparation of compositions according to the invention are known per se. As a liquid carrier, water, toluene, xylene, petroleum ether, vegetable oil, acetone, methyl ethyl ketone, cyclohexanone, acid anhydride, acetonitrile, acetobenzene, amyl acetate, 2-butanone, butylene carbonate can be used. Ester, chlorobenzene, cyclohexane, cyclohexanol, alkyl acetate, diacetone alcohol, 1,2-dichloropropane, diethanolamine, p-diethylbenzene, diethylene glycol, rosinic acid diethylene glycol Ester, diethylene glycol butyl ether, diethylene glycol ethyl ether, diethylene glycol methyl ether, N, N-dimethylformamide, dimethyl styrene, 1,4-diethylene glycol ethyl ether, dipropylene glycol, Dipropylene glycol methyl ether, dipropylene glycol dibenzoate, dipropylene glycol, alkylpyrrolidinone, ethyl acetate, 2-ethylhexanol, ethylene carbonate, 1,1,1-trichloroethane , 2-heptanone, α-pinene, d-pinene, ethyl lactate, ethylene glycol, ethylene glycol butyl ether, ethylene glycol methyl ether, γ-butyrolactone, glycerin, glyceryl acetate Ester, glyceryl diacetate, glyceryl triacetate, cetane, hexylene glycol, isopentyl acetate, isobornyl acetate, isooctane, isophorone, cumene, nutmeg Isopropyl acid, lactic acid, laurylamine, isopropylacetone, methoxypropanol, methyl isopentyl ketone, methyl isobutyl ketone, methyl laurate, methyl octanoate, methyl oleate, Dichloromethane, m-xylene, n-hexane, n-octylamine, stearic acid, octylamine acetate, oleic acid, oleylamine, o-xylene, phenol, polyethylene glycol, propionic acid, propyl lactate, Propylene carbonate, propylene glycol, propylene glycol methyl ether, p-xylene, toluene, triethyl phosphate, triethylene glycol, xylene sulfonic acid, paraffin, mineral oil, trichlorethylene, perchlorethylene, ethyl acetate, Amyl acetate, butyl acetate, propylene glycol methyl ether, diethylene glycol methyl ether, methanol, ethanol, isopropyl alcohol and higher molecular weight alcohols such as pentanol, tetrahydrofuranol, hexanol, octanol, ethylene glycol alcohol, propylene glycol, glycerol, N -methyl-2-pyrrolidinone, etc.

合適的固體載體係例如滑石、二氧化鈦、葉蠟石黏土、矽石、厄帖浦石黏土、矽藻土、石灰石、碳酸鈣、膨潤土、鈣蒙脫土、棉籽殼、小麥粉、大豆粉、浮石、木粉、經研磨的胡桃殼、木質素和類似的物質。Suitable solid carrier systems include, for example, talc, titanium dioxide, pyrophyllite clay, silica, etiopite clay, diatomaceous earth, limestone, calcium carbonate, bentonite, calcium montmorillonite, cottonseed hulls, wheat flour, soy flour, pumice. , wood flour, ground walnut shells, lignin and similar substances.

許多表面活性物質可以有利地用在固體和液體配製物兩者中，尤其是在使用前可被載體稀釋的那些配製物中。表面活性物質可以是陰離子的、陽離子的、非離子的或聚合的並且它們可以用作乳化劑、濕潤劑或懸浮劑或用於其他目的。典型的表面活性物質包括例如烷基硫酸酯的鹽，如十二烷基硫酸二乙醇銨；烷基芳基磺酸酯的鹽，如十二烷基苯磺酸鈣；烷基酚/環氧烷加成產物，如乙氧基化壬基苯酚；醇/環氧烷加成產物，如乙氧基化十三烷醇；皂，如硬脂酸鈉；烷基萘磺酸酯的鹽，如二丁基萘磺酸鈉；磺基琥珀酸二烷基酯的鹽，如二(2-乙基己基)磺基琥珀酸鈉；山梨糖醇酯，如山梨糖醇油酸酯；季胺，如氯化十二烷基三甲基銨；脂肪酸的聚乙二醇酯，如聚乙二醇硬脂酸酯；環氧乙烷和環氧丙烷的嵌段共聚物；以及磷酸單烷基酯和二烷基酯的鹽；以及還有另外的物質，例如描述於：McCutcheon's Detergents and Emulsifiers Annual [麥卡琴清潔劑和乳化劑年鑒]，MC出版公司（MC Publishing Corp.），裡奇伍德，新澤西州（Ridgewood New Jersey）（1981）。Many surface-active materials may be advantageously used in both solid and liquid formulations, especially those formulations which can be diluted with a carrier before use. Surface-active substances may be anionic, cationic, nonionic or polymeric and they may act as emulsifiers, wetting agents or suspending agents or for other purposes. Typical surface active substances include, for example, salts of alkyl sulfate esters, such as diethanol ammonium lauryl sulfate; salts of alkyl aryl sulfonates, such as calcium dodecyl benzene sulfonate; alkyl phenols/epoxy Alkane addition products, such as ethoxylated nonylphenol; alcohol/alkylene oxide addition products, such as ethoxylated tridecanol; soaps, such as sodium stearate; salts of alkyl naphthalene sulfonates, Such as sodium dibutylnaphthalene sulfonate; salts of dialkyl sulfosuccinates, such as sodium di(2-ethylhexyl)sulfosuccinate; sorbitol esters, such as sorbitol oleate; quaternary amines , such as dodecyltrimethylammonium chloride; polyethylene glycol esters of fatty acids, such as polyethylene glycol stearate; block copolymers of ethylene oxide and propylene oxide; and monoalkyl phosphates Salts of esters and dialkyl esters; and also others, such as those described in: McCutcheon's Detergents and Emulsifiers Annual, MC Publishing Corp., Ridgewood , Ridgewood New Jersey (1981).

可以用於殺有害生物配製物的另外的佐劑包括結晶抑制劑、黏度調節劑、懸浮劑、染料、抗氧化劑、發泡劑、光吸收劑、混合助劑、消泡劑、錯合劑、中和或改變pH的物質和緩衝液、腐蝕抑制劑、香料、濕潤劑、吸收增強劑、微量營養素、塑化劑、助滑劑、潤滑劑、分散劑、增稠劑、防凍劑、殺微生物劑、以及液體和固體肥料。Additional adjuvants that may be used in pesticidal formulations include crystallization inhibitors, viscosity regulators, suspending agents, dyes, antioxidants, foaming agents, light absorbers, mixing aids, defoaming agents, complexing agents, neutralizing agents, etc. and or pH-changing substances and buffers, corrosion inhibitors, fragrances, wetting agents, absorption enhancers, micronutrients, plasticizers, slip agents, lubricants, dispersants, thickeners, antifreezes, microbicides , and liquid and solid fertilizers.

根據本發明之組成物可以包括添加劑，該添加劑包括植物或動物來源的油、礦物油、此類油的烷基酯或此類油與油衍生物的混合物。在根據本發明之組成物中的油添加劑的量通常是基於該待施用的混合物的從0.01%到10%。例如，可以在噴霧混合物已經製備之後將該油添加劑以所希望的濃度添加到噴霧罐中。較佳的油添加劑包括礦物油或植物來源的油，例如菜籽油、橄欖油或葵花籽油；乳化的植物油；植物來源的油的烷基酯，例如甲基衍生物；或動物來源的油，如魚油或牛脂。較佳的油添加劑包括C 8-C 22脂肪酸的烷基酯，尤其是C 12-C 18脂肪酸的甲基衍生物，例如月桂酸、棕櫚酸以及油酸的甲基酯（分別為月桂酸甲酯、棕櫚酸甲酯和油酸甲酯）。許多油衍生物獲知於Compendium of Herbicide Adjuvants[除草劑佐劑綱要]，第10版，南伊利諾大學，2010。 The compositions according to the invention may comprise additives including oils of vegetable or animal origin, mineral oils, alkyl esters of such oils or mixtures of such oils and oil derivatives. The amount of oil additives in the compositions according to the invention is generally from 0.01% to 10%, based on the mixture to be applied. For example, the oil additive can be added to the spray tank at the desired concentration after the spray mixture has been prepared. Preferred oil additives include mineral oils or oils of vegetable origin, such as rapeseed, olive or sunflower oil; emulsified vegetable oils; alkyl esters of oils of vegetable origin, such as methyl derivatives; or oils of animal origin. , such as fish oil or beef tallow. Preferred oil additives include alkyl esters of C 8 to C 22 fatty acids, especially methyl derivatives of C 12 to C 18 fatty acids, such as the methyl esters of lauric acid, palmitic acid and oleic acid (respectively methyl laurate). esters, methyl palmitate and methyl oleate). Many oil derivatives are known from the Compendium of Herbicide Adjuvants, 10th edition, Southern Illinois University, 2010.

除草組成物總體上包含按重量計從0.1%至99%、尤其是按重量計從0.1%至95%的具有式 (I) 的化合物和按重量計從1%至99.9%的配製佐劑，該配製佐劑較佳的是包括按重量計從0至25%的表面活性物質。本發明組成物總體上包括按重量計從0.1%至99%、尤其是按重量計從0.1%至95%的本發明之化合物以及按重量計從1%至99.9%的配製佐劑，該配製佐劑較佳的是包括按重量計從0至25%的表面活性物質。而商業產品可以較佳的是被配製為濃縮物，最終使用者將通常使用稀釋配製物。Herbicidal compositions generally comprise from 0.1% to 99% by weight, in particular from 0.1% to 95% by weight, of a compound of formula (I) and from 1% to 99.9% by weight of a formulated adjuvant, The formulated adjuvant preferably contains from 0 to 25% by weight of surface active substance. The compositions of the invention generally comprise from 0.1% to 99% by weight of a compound of the invention and in particular from 0.1% to 95% by weight of a formulating adjuvant, the formulation The adjuvant preferably contains from 0 to 25% by weight of surfactant. While commercial products may preferably be formulated as concentrates, end users will typically use dilute formulations.

施用比率在寬範圍之內變化並且取決於土壤的性質、施用方法、作物植物、待控制的有害生物、主要氣候條件、以及受施用方法、施用時間以及目標作物支配的其他因素。一般來講，可以將化合物以從1 l/ha至2000 l/ha、尤其是從10 l/ha到1000 l/ha的比率施用。Application rates vary within wide ranges and depend on the nature of the soil, the application method, the crop plant, the pest to be controlled, the prevailing climatic conditions, and other factors governed by the application method, application time, and target crop. In general, the compounds can be applied at a rate from 1 l/ha to 2000 l/ha, especially from 10 l/ha to 1000 l/ha.

較佳的配製物可以具有以下組成（重量%）： 可乳化的濃縮物： 活性成分：             1%至95%，較佳的是60%至90% 表面活性劑：          1%至30%，較佳的是5%至20% 液體載體：             1%至80%，較佳的是1%至35% 粉塵劑： 活性成分：             0.1%至10%，較佳的是0.1%至5% 固體載體：             99.9%至90%，較佳的是99.9%至99% 懸浮液濃縮物： 活性成分：             5%至75%，較佳的是10%至50% 水：                         94%至24%，較佳的是88%至30% 表面活性劑：          1%至40%，較佳的是2%至30% 可濕性粉劑： 活性成分：             0.5%至90%，較佳的是1%至80% 表面活性劑：          0.5%至20%，較佳的是1%至15% 固體載體：             5%至95%，較佳的是15%至90% 顆粒劑： 活性成分：             0.1%至30%，較佳的是0.1%至15% 固體載體：             99.5%至70%，較佳的是97%至85% A preferred formulation may have the following composition (% by weight): Emulsifiable concentrates: Active ingredients: 1% to 95%, preferably 60% to 90% Surfactant: 1% to 30%, preferably 5% to 20% Liquid carrier: 1% to 80%, preferably 1% to 35% Dust agent: Active ingredient: 0.1% to 10%, preferably 0.1% to 5% Solid carrier: 99.9% to 90%, preferably 99.9% to 99% Suspension concentrate: Active ingredient: 5% to 75%, preferably 10% to 50% Water: 94% to 24%, preferably 88% to 30% Surfactant: 1% to 40%, preferably 2% to 30% Wettable powder: Active ingredients: 0.5% to 90%, preferably 1% to 80% Surfactant: 0.5% to 20%, preferably 1% to 15% Solid carrier: 5% to 95%, preferably 15% to 90% Granules: Active ingredients: 0.1% to 30%, preferably 0.1% to 15% Solid carrier: 99.5% to 70%, preferably 97% to 85%

本發明之組成物可以進一步包含至少一種另外的殺有害生物劑。例如，根據本發明之化合物也可以與其他除草劑或植物生長調節劑組合使用。在較佳的實施方式中，該另外的殺有害生物劑係除草劑和/或除草劑安全劑。The compositions of the present invention may further comprise at least one additional pesticidal agent. For example, the compounds according to the invention can also be used in combination with other herbicides or plant growth regulators. In a preferred embodiment, the additional pesticidal agent is a herbicide and/or a herbicide safener.

因此，具有式 (I) 的化合物可與一種或多種其他除草劑組合使用以提供各種除草混合物。此類混合物的特定實例包括（其中「I」表示具有式 (I) 的化合物）：I + 乙草胺；I + 三氟羧草醚（包括三氟羧草醚-鈉）；I + 苯草醚；I + 甲草胺；I + 禾草滅；I + 莠滅淨（ametryn）；I + 氨唑草酮；I + 醯嘧磺隆；I + 環丙嘧啶酸；I + 氯胺基吡啶酸；I + 殺草強；I + 磺草靈；I + 草脫淨；I + 苄嘧磺隆（包括苄嘧磺隆-甲基）；I + 噻草平；I + 二環哌喃酮；I + 雙丙氨膦；I + 治草醚；I + 雙草醚-鈉；I + 二氯異㗁草酮（bixlozone）；I + 除草定；I + 溴苯腈；I + 丁草胺；I + 氟丙嘧草酯；I + 唑草胺；I + 唑酮草酯（包括唑酮草酯-乙基）；酯磺草胺酸（包括酯磺草胺酸-甲基）；I + 氯嘧磺隆（包括氯嘧磺隆-乙基）；I + 綠麥隆；I + 醚磺隆；I + 氯磺隆；I + 環庚草醚；I + 氯醯草膦（clacyfos）；I + 烯草酮；I + 炔草酸（包括炔草酸-炔丙基）；I + 異㗁草酮；I + 二氯吡啶酸；I + 環吡拉尼（cyclopyranil）；I + 環吡瑞莫（cyclopyrimorate）；I + 環丙嘧磺隆；I + 氰氟草酯（包括氰氟草酯-丁基）；I + 2,4-D（包括其膽鹼鹽和2-乙基己酯）；I + 2,4-DB；I + 殺草隆；I + 甜菜安；I + 麥草畏（包括其鋁、胺基丙基、雙-胺基丙基甲基、膽鹼、二氯丙、二甘醇胺、二甲胺、二甲基銨、鉀鹽和鈉鹽）；I + 禾草靈；I + 雙氯磺草胺；I + 吡氟草胺；I + 野燕枯；I + 吡氟草胺；I + 氟吡草腙；I + 二甲草胺；I + 精二甲吩草胺；I + 敵草快二溴化物；I + 達有龍；I + 禾草畏；I + 丁氟消草；I + 乙氧呋草黃；I + 㗁唑禾草靈（包括精㗁唑禾草靈-乙基）；I + 異㗁苯碸（fenoxasulfone）；I + 芬奎三酮（fenquinotrione）；I + 四唑醯草胺；I + 啶嘧磺隆；I + 雙氟磺草胺；I + 氯氟吡啶酯；I + 吡氟禾草靈（包括精吡氟禾草靈-丁基）；I + 氟酮磺隆（包括氟酮磺隆-鈉）；I + 氟噻草胺；I + 氟節胺；I + 唑嘧磺草胺；I + 丙炔氟草胺；I + 氟啶嘧磺隆（包括氟啶嘧磺隆-甲基-鈉）；I + 氟草煙（包括氟草煙-甲基庚基酯（fluroxypyr-meptyl））；I + 氟噻甲草酯；I + 氟磺胺草醚；I + 甲醯胺磺隆；I + 草銨膦（包括其銨鹽）；I + 草甘膦（包括其二胺、異丙基銨和鉀鹽）；I + 氟氯吡啶酯（halauxifen）（包括氟氯吡啶酯-甲基）；I + 氯吡嘧磺隆；I + 吡氟氯禾靈（包括吡氟氯禾靈-甲基）；I + 環𠯤酮；I + 海當西定（hydantocidin）；I + 甲氧咪草煙；I + 甲基咪草煙；I + 滅草煙；I + 滅草喹；I + 咪草煙；I + 三𠯤茚草胺（indaziflam）；I + 碘甲磺隆（包括碘甲磺隆-甲基-鈉）；I + 異歐芬磺隆（iofensulfuron）；I + 異歐芬磺隆-鈉；I + 碘苯腈；I + 三唑醯草胺（ipfencarbazone）；I + 異丙隆；I + 異惡醯草胺（isoxaben）；I + 異㗁唑草酮；I + 乳氟禾草靈；I + 蘭科三酮（lancotrione）；I + 理有龍；I + MCPA；I + MCPB；I + 高二甲四氯丙酸（mecoprop-P）；I + 苯噻醯草胺；I + 甲基二磺隆；I + 甲基二磺隆-甲基；I + 甲基磺草酮；I + 苯𠯤草酮；I + 吡草胺；I + 異㗁噻草醚（methiozolin）；I + 秀穀隆；I + 異丙甲草胺；I + 磺草唑胺；I + 甲氧隆；I + 𠯤草酮；I + 甲磺隆；I + 草達滅；I + 敵草胺；I + 煙嘧磺隆；I + 達草滅；I + 嘧苯胺磺隆；I + 丙炔㗁草酮；I + 㗁草酮；I + 環氧嘧磺隆；I + 乙氧氟草醚；I + 二氯化巴拉刈；I + 二甲戊樂靈；I + 五氟磺草胺；I + 苯敵草；I + 毒莠定；I + 氟吡醯草胺；I + 唑啉草酯；I + 丙草胺；I + 氟嘧磺隆-甲基；I + 氨氟樂靈；I + 撲草淨；I + 毒草胺；I + 除草寧；I + 喔草酯；I + 苯胺靈；I + 丙𠯤嘧磺隆（propyrisulfuron）、I + 戊炔草胺；I + 苄草丹；I + 氟磺隆；I + 雙唑草腈；I + 吡草醚（包括吡草醚-乙基）：I + 磺醯草吡唑；I + 吡唑特、I + 吡嘧磺隆；I + 嘧啶肟草醚；I + 噠草特；I + 環酯草醚；I + 嘧氟磺草胺（pyrimisulfan）、I + 嘧草硫醚；I + 吡咯磺隆（pyroxasulfone）；I + 啶磺草胺；I + 二氯喹啉酸；I + 氯甲喹啉酸；I + 喹禾靈（包括精喹禾靈-乙基和喹禾糠酯（quizalofop-P-tefuryl））；I + 碸嘧磺隆；I + 苯嘧磺草胺；I + 烯禾啶；I + 西瑪津；I + S-異丙甲草胺；I + 磺草酮；I + 甲磺草胺；I + 磺醯磺隆；I + 特丁噻草隆；I + 特呋三酮；I + 環磺酮；I + 特丁津；I + 特丁淨；I + 噻酮磺隆（thiencarbazone）；I + 噻吩磺隆；I + 地芬納噻（tiafenacil）；I + 托比利特（tolpyralate）；I + 苯吡唑草酮；I + 三甲苯草酮；I + 氟酮磺草胺（triafamone）；I + 野麥畏；I + 醚苯磺隆；I + 苯磺隆（包括苯磺隆-甲基）；I + 綠草定；I + 三氟啶磺隆（包括三氟啶磺隆-鈉）；I + 三氣草嗦（trifludimoxazin）；I + 氟樂靈；I + 氟胺磺隆；I + 三氟甲磺隆；I + 4-羥基-1-甲氧基-5-甲基-3-[4-(三氟甲基)-2-吡啶基]咪唑啶-2-酮；I + 4-羥基-1,5-二甲基-3-[4-(三氟甲基)-2-吡啶基]咪唑啶-2-酮；I + 5-乙氧基-4-羥基-1-甲基-3-[4-(三氟甲基)-2-吡啶基]咪唑啶-2-酮；I + 4-羥基-1-甲基-3-[4-(三氟甲基)-2-吡啶基]咪唑啶-2-酮；I + 4-羥基-1,5-二甲基-3-[1-甲基-5-(三氟甲基)吡唑-3-基]咪唑啶-2-酮；I + (4R)1-(5-三級丁基異㗁唑-3-基)-4-乙氧基-5-羥基-3-甲基-咪唑啶-2-酮；I + 3-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]雙環[3.2.1]辛烷-2,4-二酮；I + 2-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-5-甲基-環己烷-1,3-二酮；I + 2-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]環己烷-1,3-二酮；I + 2-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-5,5-二甲基-環己烷-1,3-二酮；I + 6-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-2,2,4,4-四甲基-環己烷-1,3,5-三酮；I + 2-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-5-乙基-環己烷-1,3-二酮；I + 2-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-4,4,6,6-四甲基-環己烷-1,3-二酮；I + 2-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]-5-甲基-環己烷-1,3-二酮；I + 3-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]雙環[3.2.1]辛烷-2,4-二酮；I + 2-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]-5,5-二甲基-環己烷-1,3-二酮；I + 6-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]-2,2,4,4-四甲基-環己烷-1,3,5-三酮；I + 2-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]環己烷-1,3-二酮；I + 4-[2-(3,4-二甲氧基苯基)-6-甲基-3-側氧基-嗒𠯤-4-羰基]-2,2,6,6-四甲基-四氫哌喃-3,5-二酮和I + 4-[6-環丙基-2-(3,4-二甲氧基苯基)-3-側氧基-嗒𠯤-4-羰基]-2,2,6,6-四甲基-四氫哌喃-3,5-二酮。 Accordingly, compounds of formula (I) can be used in combination with one or more other herbicides to provide various herbicidal mixtures. Specific examples of such mixtures include (where "I" represents a compound of formula (I)): I + acetochlor; I + acifluorfen (including acifluorfen-sodium); I + acifluorfen Ether; I + alachlor; I + carbamid; I + ametryn; I + amethafil; I + sulfosulfuron; I + cypropyridine; I + chloraminopyridine Acid; I + benzosulfuron-methyl; I + sulfentrazone; I + sulfentrazone; I + bensulfuron-methyl (including bensulfuron-methyl); I + thiazepine; I + bicyclopyranone; I + bialaphos; I + bisofen; I + bispfen-sodium; I + bixlozone; I + herbicide; I + bromoxynil; I + butachlor; I + flumefenacet; I + penfentrafen; I + penfentrafen (including penfentrafen-ethyl); sulfentrazone (including sulfentrazone-methyl); I + Chlorsulfuron-methyl (including chlorsulfuron-ethyl); I + chlorosulfuron; I + chlorsulfuron-methyl; I + chlorsulfuron-methyl; I + cyclohepathiofen; I + clacyfos; I + clethodim; I + clopargyl acid (including clopargyl acid - propargyl); I + isopropargil; I + clopyralid; I + cyclopyranil (cyclopyranil); I + cyclopyramid (cyclopyrimorate); I + cyclosulfuron; I + cyhalofop-methyl (including cyhalofop-butyl); I + 2,4-D (including its choline salt and 2-ethylhexyl ester) ; I + 2,4-DB; I + cyclofenac; I + betaine; I + dicamba (including its aluminum, aminopropyl, bis-aminopropylmethyl, choline, dichloropropyl, diglycolamine, dimethylamine, dimethylammonium, potassium and sodium salts); I + closulfonate; I + diclosulam; I + diflufenac; I + dimethochlor; I + flufenac; I + dimethochlor; I + dimethochlor; I + diquat dibromide; I + dayoulong; I + gramin; I + fenoxasulfone; I + ethoxyfenoxal; I + fenoxasulfone (including fenoxafop-ethyl); I + fenoxasulfone; I + fenquintrione (fenquinotrione); I + fenquinotrione; I + pyrosulfuron; I + flusufen; butyl); I + flufensulfuron-methyl (including flufensulfuron-sodium); I + flufenacet; I + flumetrazone; I + flufenacet; I + flufenacet; I + flusulfuron-methyl (including flusulfuron-methyl-sodium); I + fluroxypyr (including fluroxypyr-methyl-meptyl); I + fluroxypyr-methyl ;I + fomesafen; I + methamphetamine; I + glufosinate (including its ammonium salts); I + glyphosate (including its diamine, isopropylammonium and potassium salts); I + Halauxifen (including halauxifen-methyl); I + chlorpyrazofen-methyl; I + halauxifen (including halauxifen-methyl); I + cyclofenone ; I + hydantocidin; I + imazethapyr; I + imazethapyr; I + imazapyr; I + imazapyr; I + imazethapyr; I + indica Indaziflam; I + iofensulfuron-methyl (including iofensulfuron-methyl-sodium); I + isofensulfuron-methyl (iofensulfuron); I + isofensulfuron-sodium; I + iodobenzene Nitrile; I + ipfencarbazone; I + isopropuron; I + isoxaben; I + isoxafencarbazone; I + lactofencarbazone; I + orchidaceae Lancotrione; I + lancotrione; I + MCPA; I + MCPB; I + mecoprop-P; I + benzofen; I + disulfuron methyl; I + disulfuron-methyl-methyl; I + mesotrione; I + benzotrione; I + metazachlor; I + methiozolin; I + mesotrione; I + metolachlor; I + sulfentrazone; I + methoxyfuron; I + cyclosulfuron; I + metsulfuron; I + chloride; I + napropamide; I + nicosulfuron ; I + metasulfuron; I + pyrimisulfuron; I + propynthiotrione; I + ethiotrione; I + oxysulfuron; I + ethoxyfluorfen; I + barbadichloride Lagao; I + pendimethalin; I + penoxsulam; I + bendichlor; I + picloram; I + flumetrachlor; I + pinoxafen; I + pretilachlor ; I + Flusulfuron-methyl; I + Amflunoside; I + Prometrazone; I + Pisochlor; I + Trifenin; I + Oxamethonate; I + Aniline; I + Propyrimidine Propyrisulfuron (propyrisulfuron), I + penclofen; I + probenfenpyr; I + flusulfuron; I + propyrisulfuron; I + metafenpyr (including metafenpyr-ethyl): I + sulfonate pyrimisulfan; I + pyrimisulfan; I + pyrimisulfuron; I + pyrimisulfan; I + pyrimisulfan; I + pyrimisulfan; I + pyrimisulfan, I + pyrosulfuron; I + pyroxasulfone; I + aflafenac; I + quinclorac; I + quinclorac; I + quizalofop (including quizalofop-B and quizalofop-P-tefuryl); I + esosulfuron; I + saflufenacil; I + diplofen; I + simazine; I + S -isopropyl Amine; I + sulfentrione; I + sulfentrazone; I + sulfentrazone; I + terbufuron; I + terfurotrione; I + cyclosulfonate; I + terbuzine; I + terbutin; I + thiencarbazone; I + thiensulfuron; I + tiafenacil; I + tolpyralate; + trimetrione; I + triafamone; I + dicamba; I + trisulfuron-methyl; I + trisulfuron-methyl (including trisulfuron-methyl); I + triclopyr ;I + triflusulfuron-methyl (including triflusulfuron-sodium); I + trifludimoxazin; I + trifluralin; I + flumisulfuron-methyl; I + triflusulfuron-methyl; I + 4-hydroxy-1-methoxy-5-methyl-3-[4-(trifluoromethyl)-2-pyridinyl]imidazolidin-2-one; I + 4-hydroxy-1,5 -Dimethyl-3-[4-(trifluoromethyl)-2-pyridinyl]imidazolidin-2-one; I + 5-ethoxy-4-hydroxy-1-methyl-3-[4 -(Trifluoromethyl)-2-pyridyl]imidazolidin-2-one; I + 4-hydroxy-1-methyl-3-[4-(trifluoromethyl)-2-pyridyl]imidazolidine -2-one; I + 4-hydroxy-1,5-dimethyl-3-[1-methyl-5-(trifluoromethyl)pyrazol-3-yl]imidazolidin-2-one; I + (4R)1-(5-tertiary butylisoethazol-3-yl)-4-ethoxy-5-hydroxy-3-methyl-imidazolidin-2-one; I + 3-[2 -(3,4-dimethoxyphenyl)-6-methyl-3-side-oxy-pyridine-4-carbonyl]bicyclo[3.2.1]octane-2,4-dione; I + 2-[2-(3,4-dimethoxyphenyl)-6-methyl-3-sideoxy-pyridoxine-4-carbonyl]-5-methyl-cyclohexane-1,3- Dione; I + 2-[2-(3,4-dimethoxyphenyl)-6-methyl-3-sideoxy-pyridine-4-carbonyl]cyclohexane-1,3-di Ketone; I + 2-[2-(3,4-dimethoxyphenyl)-6-methyl-3-sideoxy-pyridine-4-carbonyl]-5,5-dimethyl-cyclo Hexane-1,3-dione; I + 6-[2-(3,4-dimethoxyphenyl)-6-methyl-3-sideoxy-pyridine-4-carbonyl]-2 ,2,4,4-tetramethyl-cyclohexane-1,3,5-trione; I + 2-[2-(3,4-dimethoxyphenyl)-6-methyl-3 -Pendant oxy-pyridine-4-carbonyl]-5-ethyl-cyclohexane-1,3-dione; I + 2-[2-(3,4-dimethoxyphenyl)-6 -Methyl-3-side-oxy-pyridin-4-carbonyl]-4,4,6,6-tetramethyl-cyclohexane-1,3-dione; I + 2-[6-cyclopropane Base-2-(3,4-dimethoxyphenyl)-3-side oxy-pyridine-4-carbonyl]-5-methyl-cyclohexane-1,3-dione; I + 3 -[6-Cyclopropyl-2-(3,4-dimethoxyphenyl)-3-side oxy-pyridine-4-carbonyl]bicyclo[3.2.1]octane-2,4-di Ketone; I + 2-[6-cyclopropyl-2-(3,4-dimethoxyphenyl)-3-side oxy-pyridine-4-carbonyl]-5,5-dimethyl- Cyclohexane-1,3-dione; I + 6-[6-cyclopropyl-2-(3,4-dimethoxyphenyl)-3-side oxy-pyridine-4-carbonyl] -2,2,4,4-tetramethyl-cyclohexane-1,3,5-trione; I + 2-[6-cyclopropyl-2-(3,4-dimethoxyphenyl )-3-side oxy-pyridine-4-carbonyl]cyclohexane-1,3-dione; I + 4-[2-(3,4-dimethoxyphenyl)-6-methyl -3-Pendant oxy-pyridine-4-carbonyl]-2,2,6,6-tetramethyl-tetrahydropyran-3,5-dione and I + 4-[6-cyclopropyl- 2-(3,4-dimethoxyphenyl)-3-side oxy-pyridoxine-4-carbonyl]-2,2,6,6-tetramethyl-tetrahydropyran-3,5- diketone.

具有式 (I) 的化合物的混合配伍物還可以呈酯或鹽的形式，如例如在以下文獻中所提到的：The Pesticide Manual [殺有害生物劑手冊], 第十四版, British Crop Protection Council [英國作物保護委員會], 2006。Mixed mixtures of compounds of formula (I) can also be in the form of esters or salts, as mentioned, for example, in: The Pesticide Manual, 14th edition, British Crop Protection Council [UK Crop Protection Council], 2006.

具有式 (I) 的化合物還可以在與其他農用化學品（如殺真菌劑、殺線蟲劑或殺昆蟲劑）的混合物中使用，該等農用化學品的實例在殺有害生物劑手冊中給出。Compounds of formula (I) can also be used in mixtures with other agrochemicals such as fungicides, nematicides or insecticides, examples of which are given in the Handbook of Pesticides .

具有式 (I) 的化合物與混合配伍物的混合比較佳的是從1 : 100至1000 : 1。The mixing ratio of the compound of formula (I) to the mixing partner is preferably from 1:100 to 1000:1.

該等混合物可以有利地用於以上提到的該等配製物中（在這種情況下「活性成分」涉及具有式 (I) 的化合物與混合配伍物的對應混合物）。Such mixtures can be advantageously used in the formulations mentioned above (the "active ingredient" in this case relates to the corresponding mixtures of compounds of formula (I) and mixing partners).

本發明之具有式 (I) 的化合物也可以與除草劑安全劑組合。較佳的組合（其中「I」表示具有式 (I) 的化合物）包括：-I + 解草𠯤、I + 解草酯（包括解草喹）；I + 環丙磺醯胺；I + 二氯丙烯胺；I + 解草唑（包括解草唑乙酯）；I + 解草啶；I + 氟草肟；I + 解草惡唑、I + 雙苯㗁唑酸（包括雙苯㗁唑酸乙酯）；I + 吡唑解草酸（包括吡唑解草酯）；I + 美卡米芬（metcamifen）；I + N-(2-甲氧基苯甲醯基)-4-[(甲基胺基羰基)胺基]苯磺醯胺和I+解草腈。The compounds of formula (I) according to the invention may also be combined with herbicide safeners. Preferred combinations (where "I" represents a compound of formula (I)) include: -I + cyclopropyl, I + cyclopropyl (including cyclopropyl); I + cyclopropyl sulfonamide; I + cyclopropyl Chloropropylamine; I + clofenacet (including clofenacet ethyl); I + clofenacet; I + flufenoxime; I + dipyroxazole, I + dipyroxazole (including dipyroxazole acid ethyl ester); I + pyrazolyl oxalic acid (including pyrazolyl oxalate); I + metcamifen (metcamifen); I + N-(2-methoxybenzyl)-4-[( Methylaminocarbonyl)amino]benzene sulfonamide and I+ oxabenitrile.

特別較佳的是具有式 (I) 的化合物與環丙磺醯胺、雙苯㗁唑酸（包括雙苯㗁唑酸乙酯）、解草酯（包括解草喹）和/或N-(2-甲氧基苯甲醯基)-4-[(甲基-胺基羰基)胺基]苯磺醯胺的混合物。Particularly preferred are compounds of formula (I) in combination with cyclopropanesulfonamide, bisbenzoic acid (including bisbenzoic acid ethyl ester), ethyl bistrizoate (including ethyl bisbenzoate) and/or N-( Mixture of 2-methoxybenzyl)-4-[(methyl-aminocarbonyl)amino]benzenesulfonamide.

具有式 (I) 的化合物的該等安全劑還可以處於酯或鹽的形式，例如像在《殺有害生物劑手冊》（第14版（BCPC），2006）中所提及的。提及解草喹還適用於其鋰、鈉、鉀、鈣、鎂、鋁、鐵、銨、季銨、鋶或鏻鹽（如在WO 02/34048中揭露的），並且對解草唑乙酯的提及還適用於解草唑，等。Such safeners of compounds of formula (I) may also be in the form of esters or salts, as mentioned for example in the Handbook of Pesticides (14th Edition (BCPC), 2006). References to tetraquin also apply to its lithium, sodium, potassium, calcium, magnesium, aluminium, iron, ammonium, quaternary ammonium, sulfonium or phosphonium salts (as disclosed in WO 02/34048), and to cycloquin The mention of esters also applies to oxalazole, etc.

較佳的是，具有式 (I) 的化合物與安全劑的混合比係從100 : 1至1 : 10，尤其是從20 : 1至1 : 1。Preferably, the mixing ratio of the compound of formula (I) to the safener is from 100:1 to 1:10, especially from 20:1 to 1:1.

該等混合物可有利地用於以上提到的配製物中（在這種情況下「活性成分」涉及具有式 (I) 的化合物與安全劑的對應混合物）。Such mixtures can be advantageously used in the formulations mentioned above (the "active ingredient" in this case relates to the corresponding mixture of a compound of formula (I) and a safener).

本發明之具有式 (I) 的化合物作為除草劑係有用的。因此，本發明進一步包括用於控制不想要的植物之方法，包括向該植物或包含它們的場所施用有效量的本發明化合物或含有該化合物的除草組成物。「控制」意指殺死、減少或延遲生長或預防或減少發芽。通常有待控制的植物係不想要的植物（雜草）。「場所」意指植物在其中正生長或將生長的區域。The compounds of formula (I) of the present invention are useful as herbicides. Accordingly, the invention further encompasses a method for controlling unwanted vegetation comprising applying to the plants or a locus containing them an effective amount of a compound of the invention or a herbicidal composition containing the compound. "Control" means to kill, reduce or delay growth or to prevent or reduce germination. Often the flora to be controlled are unwanted plants (weeds). "Place" means the area in which plants are growing or will grow.

具有式 (I) 的化合物的施用比率可以在寬的限度內變化並且取決於土壤的性質、施用之方法（出苗前；出苗後；施用於種子溝；免耕法施用等）、作物植物、待控制的一種或多種雜草、當時的氣候條件和其他受施用方法、施用時間和目標作物支配的因素。根據本發明之具有式 (I) 的化合物通常以從10 g/ha至2000 g/ha，尤其是從50 g/ha到1000 g/ha的比率施用。較佳的範圍為10-200 g/ha。The application rate of the compounds of formula (I) can vary within wide limits and depends on the properties of the soil, the method of application (pre-emergence; post-emergence; application in seed furrows; no-till application, etc.), the crop plant, the treatment The weed or weeds being controlled, prevailing climatic conditions and other factors governed by the method of application, timing of application and target crop. The compounds of formula (I) according to the invention are generally applied at a rate from 10 g/ha to 2000 g/ha, in particular from 50 g/ha to 1000 g/ha. The preferred range is 10-200 g/ha.

通常藉由噴灑該組成物進行施用，典型地是藉由用於大面積的裝在拖拉機上的噴灑機，但是還可以使用其他方法如撒粉（針對粉末）、滴加或浸灌。Application is usually by spraying the composition, typically by a tractor-mounted sprayer for large areas, but other methods such as dusting (for powders), dripping or soaking may also be used.

可以使用根據本發明之組成物的有用植物包括作物如穀物，例如大麥和小麥、棉花、油菜籽油菜、向日葵、玉米、稻、大豆、甜菜、甘蔗以及草皮。Useful plants for which compositions according to the invention may be used include crops such as cereals, such as barley and wheat, cotton, rapeseed, sunflower, corn, rice, soybeans, sugar beet, sugar cane and turf.

作物植物還可以包括樹，如果樹、棕櫚樹、椰子樹或其他堅果。還包括藤本植物（如葡萄）、灌木果樹、果實植物和蔬菜。Crop plants may also include trees such as fruit trees, palm trees, coconut trees, or other nuts. Also included are vines (such as grapes), shrub fruit trees, fruit-bearing plants, and vegetables.

作物應被理解為還包括藉由常規的育種方法或藉由基因工程已經賦予對除草劑或多種類別的除草劑（例如ALS-抑制劑、GS-抑制劑、EPSPS-抑制劑、PPO-抑制劑、ACC酶-抑制劑和HPPD-抑制劑）的耐受性的那些作物。藉由常規的育種方法已經賦予對咪唑啉酮（例如，甲氧咪草煙）的耐受性的作物的實例係Clearfield®夏季油菜（卡諾拉（canola））。藉由基因工程方法已經賦予對除草劑的耐受性的作物的實例包括例如具有草甘膦和草銨膦抗性的玉米品種，該等玉米品種在RoundupReady®和LibertyLink®商標名下是可商購的。Crops are to be understood as also including crops which have been endowed, by conventional breeding methods or by genetic engineering, with resistance to herbicides or classes of herbicides (e.g. ALS-inhibitors, GS-inhibitors, EPSPS-inhibitors, PPO-inhibitors , ACC enzyme-inhibitors and HPPD-inhibitors). An example of a crop that has been conferred tolerance to imidazolinones (eg imazamox) by conventional breeding methods is Clearfield® summer rapeseed (canola). Examples of crops that have been rendered tolerant to herbicides through genetic engineering methods include, for example, corn varieties with resistance to glyphosate and glufosinate, which are commercially available under the trade names Roundup Ready® and LibertyLink® Purchased.

本發明之化合物可以用於控制具有對於原紫質原氧化酶（PPO）抑制劑的耐受性的作物植物中的不希望的植被之方法中。此類植物可以例如藉由用編碼合適的原紫質原氧化酶的核酸轉形作物植物來獲得，所述核酸可以含有突變以便使其對於PPO抑制劑更具抗性。此類核酸和作物植物的實例揭露於WO 95/34659、WO 97/32011、WO 2007/024739、WO 2012/080975、WO 2013/189984、WO 2015/022636、WO 2015/022640、WO 2015/092706、WO 2016/099153、WO 2017/023778、WO 2017/039969、WO 2017/217793、WO 2017/217794、WO 2018/114759、WO 2019/117578、WO 2019/117579和WO 2019/118726中。The compounds of the present invention may be used in methods for controlling undesirable vegetation in crop plants having tolerance to prorhodopsin oxidase (PPO) inhibitors. Such plants can be obtained, for example, by transforming crop plants with a nucleic acid encoding a suitable prorhodopsin oxidase, which nucleic acid may contain mutations to make it more resistant to PPO inhibitors. Examples of such nucleic acids and crop plants are disclosed in WO 95/34659, WO 97/32011, WO 2007/024739, WO 2012/080975, WO 2013/189984, WO 2015/022636, WO 2015/022640, WO 2015/092706, WO 2016/099153, WO 2017/023778, WO 2017/039969, WO 2017/217793, WO 2017/217794, WO 2018/114759, WO 2019/117578, WO 2019/117579 and WO 2019/1187 26 in.

因此，本發明還提供了一種用於控制在植物栽培場所中不希望的植被之方法，該方法包括以下步驟：a) 在所述場所提供包含至少一種核酸的植物，該核酸包含編碼原紫質原氧化酶（PPO）多肽的核苷酸序列，其對「PPO抑制除草劑」具有抗性或耐受性；b) 向所述場所施用有效量的所述除草劑，其中該PPO抑制除草劑係如本文所定義的具有式 (I) 的化合物。Therefore, the present invention also provides a method for controlling undesirable vegetation in a plant cultivation site, the method comprising the steps of: a) providing a plant comprising at least one nucleic acid at said site, the nucleic acid comprising encoding prorhodopsin The nucleotide sequence of a protooxidase (PPO) polypeptide that is resistant or tolerant to a "PPO inhibiting herbicide"; b) applying an effective amount of said herbicide to said locus, wherein the PPO inhibiting herbicide is a compound of formula (I) as defined herein.

農作物還應理解為藉由基因工程方法已經賦予其對有害昆蟲有抗性的那些農作物，例如Bt玉米（對歐洲玉米螟有抗性）、Bt棉花（對棉鈴象鼻蟲有抗性）和還有Bt馬鈴薯（對科羅拉多甲蟲有抗性）。Bt玉米的實例係NK®的Bt 176玉米雜交體（先正達種子公司（Syngenta Seeds））。Bt毒素係由蘇芸金芽孢桿菌（ Bacillus thuringiensis）土壤細菌天然形成的蛋白質。毒素或能夠合成此類毒素的轉基因植物的實例被描述在EP-A-451 878、EP-A-374 753、WO 93/07278、WO 95/34656、WO 03/052073和EP-A-427 529中。包括一個或多個編碼殺昆蟲抗性和表現一種或多種毒素的基因的轉基因植物的實例係KnockOut®（玉米）、Yield Gard®（玉米）、NuCOTIN33B®（棉花）、Bollgard®（棉花）、NewLeaf®（馬鈴薯）、NatureGard®和Protexcta®。植物作物或其種子材料均可以是抗除草劑的並且同時係抗昆蟲攝食的（「疊加的」轉基因結果）。例如，種子可以具有表現殺昆蟲的Cry3蛋白的能力，而同時對草甘膦係耐受的。 Crops are also to be understood as those crops to which resistance to harmful insects has been conferred by genetic engineering methods, such as Bt corn (resistant to the European corn borer), Bt cotton (resistant to the boll weevil) and also There are Bt potatoes (resistant to Colorado beetle). An example of Bt corn is NK®'s Bt 176 corn hybrid (Syngenta Seeds). Bt toxin is a protein naturally produced by the soil bacterium Bacillus thuringiensis . Examples of toxins or transgenic plants capable of synthesizing such toxins are described in EP-A-451 878, EP-A-374 753, WO 93/07278, WO 95/34656, WO 03/052073 and EP-A-427 529 middle. Example lines of transgenic plants including one or more genes encoding insecticidal resistance and expressing one or more toxins KnockOut® (corn), Yield Gard® (corn), NuCOTIN 33B® (cotton), Bollgard® (cotton), NewLeaf ® (potato), NatureGard® and Protexcta®. Either a plant crop or its seed material can be herbicide resistant and at the same time resistant to insect feeding ("stacked" transgenic results). For example, seeds can have the ability to express the insecticidal Cry3 protein while being tolerant to glyphosate.

作物還應被理解為包括藉由常規育種方法或基因工程獲得並且含有所謂輸出性狀（例如改進的儲存穩定性、更高的營養價值以及改進的香味）的那些作物。Crops are also to be understood as including those obtained by conventional breeding methods or genetic engineering and containing so-called output traits such as improved storage stability, higher nutritional value and improved flavour.

其他有用的植物包括例如在高爾夫球場、草地、公園以及路旁的或者商業上種植用於草地的草皮草，以及觀賞植物，如花卉或灌木。Other useful plants include turfgrasses such as those grown on golf courses, lawns, parks and roadsides or commercially for lawns, and ornamental plants such as flowers or shrubs.

本發明之具有式 (I) 的化合物和組成物通常可以用於控制多種單子葉和雙子葉雜草物種。典型地可以被控制的單子葉物種的實例包括大穗看麥娘（ Alopecurus myosuroides）、野燕麥（ Avena fatua）、車前臂形草（ Brachiaria plantaginea）、旱雀麥（ Bromus tectorum）、油莎草（ Cyperus esculentus）、馬唐（ Digitaria sanguinalis）、稗草（ Echinochloa crus-galli）、多年生黑麥草（ Lolium perenne）、多花黑麥草（ Lolium multiflorum）、黍稷（ Panicum miliaceum ）、一年生早熟禾（ Poa annua ）、狗尾草（ Setaria viridis ）、大狗尾草（ Setaria faberi ）和兩色蜀黍（ Sorghum bicolor ）。可以被控制的雙子葉物種的實例包括：苘麻、反枝莧、鬼針草、藜草、白苞猩猩草、豬殃殃、碗仔花、地膚、卷莖蓼、刺金午時花、新疆野生油菜、龍葵、繁縷、波斯婆婆納和蒼耳。 The compounds and compositions of formula (I) of the present invention can generally be used to control a variety of monocotyledonous and dicotyledonous weed species. Examples of monocotyledonous species that can typically be controlled include Alopecurus myosuroides , Avena fatua , Brachiaria plantaginea , Bromus tectorum , sedge ( Cyperus esculentus ), crabgrass ( Digitaria sanguinalis ), barnyardgrass ( Echinochloa crus-galli ), perennial ryegrass ( Lolium perenne ), multifloral ryegrass ( Lolium multiflorum ), millet grass ( Panicum miliaceum ), annual bluegrass ( Poa annua) ), Setaria viridis , Setaria faberi and Sorghum bicolor . Examples of dicotyledonous species that can be controlled include: Amaranth, Amaranthus retroflexus, Amaranth, Pigweed, White-breasted gorilla, Pidgeon, Amaranthus, Kochia, Polygonum, Amaranthus, Xinjiang wild rapeseed, nightshade, chickweed, Persian mother-of-pearl and cocklebur.

不想要的植物應被理解為還包括藉由進化、藉由常規的育種方法或藉由基因工程已經賦予對除草劑或多種類別的除草劑（例如ALS-抑制劑、GS-抑制劑、EPSPS-抑制劑、PPO-抑制劑、ACC酶-抑制劑和HPPD-抑制劑）的耐受性的那些雜草。實例包括已經進化而具有對於草甘膦和/或乙醯乳酸合酶（ALS）抑制除草劑的抗性的長芒莧（Amaranthus palmeri）。Undesirable plants are to be understood as also including plants that have been endowed by evolution, by conventional breeding methods or by genetic engineering with resistance to herbicides or to herbicides of various classes (e.g. ALS-inhibitors, GS-inhibitors, EPSPS- inhibitors, PPO-inhibitors, ACC enzyme-inhibitors and HPPD-inhibitors). Examples include Amaranthus palmeri, which has evolved resistance to glyphosate and/or acetyl lactate synthase (ALS) inhibiting herbicides.

本發明之化合物可以用於控制具有對於原紫質原氧化酶（PPO）抑制劑的抗性的不想要的植物或雜草之方法中。例如，由於PPX2L中的胺基酸取代，如在胺基酸R128（也稱為R98）和G399處發生的取代，或者PPX2L中在密碼子210（Δ210）處的密碼子（甘胺酸）缺失，長芒莧和糙果莧種群已經進化為抗PPO雜草，密碼子編號係基於NCBI參考序列DQ386114。本發明之化合物可以用於控制具有前面提及的密碼子或等效物處的突變或缺失的長芒莧和/或糙果莧之方法中，並且明顯的是嘗試用該等化合物控制可能出現的具有賦予對於PPO抑制劑的耐受性或抗性的其他突變的不想要的植物或雜草。The compounds of the present invention may be used in methods of controlling unwanted plants or weeds that are resistant to prorhodopsin oxidase (PPO) inhibitors. For example, due to amino acid substitutions in PPX2L, such as those occurring at amino acids R128 (also known as R98) and G399, or the codon (glycine) deletion at codon 210 (Δ210) in PPX2L , Amaranthus amaranth and Amaranth amaranth populations have evolved into PPO-resistant weeds, and the codon numbering is based on the NCBI reference sequence DQ386114. The compounds of the present invention may be used in methods of controlling Amaranth amaranth and/or Amaranth having mutations or deletions at the previously mentioned codons or equivalents, and it is obvious that attempts to use these compounds to control possible Undesirable plants or weeds with other mutations that confer tolerance or resistance to PPO inhibitors.

具有式 (I) 的化合物也可用於作物收穫前乾燥，例如但不限於馬鈴薯、大豆、向日葵和棉花。收穫前乾燥用於乾燥作物葉片，而不會對作物本身造成顯著損害，以幫助收穫。Compounds of formula (I) may also be used for pre-harvest drying of crops such as, but not limited to, potatoes, soybeans, sunflowers and cotton. Pre-harvest drying is used to dry crop leaves without causing significant damage to the crop itself to aid harvesting.

本發明之化合物/組成物特別可用於非選擇性燃盡（burn-down）應用，並且因此也可用於控制自生自長（volunteer）或逃逸作物（escape crop）植物。 The compounds/compositions of the present invention are particularly useful in non-selective burn-down applications, and therefore also in the control of volunteer or escape crop plants.

現在將藉由舉例更詳細地說明本發明之不同方面和實施方式。應當理解的是，在不偏離本發明範圍的情況下，可以對細節做出修改。 實施例 Different aspects and embodiments of the invention will now be explained in more detail by way of example. It is to be understood that changes may be made in details without departing from the scope of the invention. Example

以下實施例用來說明但不限制本發明。 合成實施例 實施例 1 ： (3- 甲氧基 -3- 側氧基 - 丙基 )2-[2- 氯 -5-(3,5- 二氯 -2- 吡啶基 )-4- 氟 - 苯基 ] 氫硫基丙酸酯（化合物 8-374 ）的製備 步驟 1 ：3,5-二氯-2-(4-氯-2-氟-苯基)吡啶的合成 The following examples illustrate but do not limit the invention. Synthetic Examples Example 1 : (3- methoxy -3- sideoxy - propyl )2-[2- chloro -5-(3,5- dichloro -2- pyridyl )-4 - fluoro- Preparation step 1 of phenyl ] mercaptopropionate (compound 8-374 ) : Synthesis of 3,5-dichloro-2-(4-chloro-2-fluoro-phenyl)pyridine

將二氯化鈀(dppf)（1.5 g，1.8 mmol）添加至(4-氯-2-氟-苯基)-硼酸（3.2 g，18 mmol）、2-溴-3,5-二氯-吡啶（4.0 g，18 mmol）、碳酸銫（17.4 g，53 mmol）、水（12 ml）和甲苯（60 ml）的攪拌混合物中。將所得混合物在100°C下加熱2小時，然後使其冷卻並添加乙酸乙酯（70 ml）和水（20 ml）。分離相，並用乙酸乙酯（60 ml）萃取水相。將合併的有機相經硫酸鈉乾燥、過濾並在減壓下蒸發，以留下殘餘物，將該殘餘物藉由管柱層析法純化，以提供呈固體的3,5-二氯-2-(4-氯-2-氟-苯基)吡啶（4.1 g）。 1H NMR (400 MHz, CDCl 3) δ 8.6 (d,1H), 7.85 (d,1H), 7.4 (t,1H), 7.25 (dd,1H), 7.2 (dd,1H) ppm。 步驟 2 ：2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯磺醯氯的合成 Palladium dichloride (dppf) (1.5 g, 1.8 mmol) was added to (4-chloro-2-fluoro-phenyl)-boronic acid (3.2 g, 18 mmol), 2-bromo-3,5-dichloro- In a stirred mixture of pyridine (4.0 g, 18 mmol), cesium carbonate (17.4 g, 53 mmol), water (12 ml) and toluene (60 ml). The resulting mixture was heated at 100°C for 2 hours, then allowed to cool and ethyl acetate (70 ml) and water (20 ml) were added. The phases were separated and the aqueous phase was extracted with ethyl acetate (60 ml). The combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to leave a residue which was purified by column chromatography to provide 3,5-dichloro-2 as a solid -(4-Chloro-2-fluoro-phenyl)pyridine (4.1 g). 1 H NMR (400 MHz, CDCl 3 ) δ 8.6 (d,1H), 7.85 (d,1H), 7.4 (t,1H), 7.25 (dd,1H), 7.2 (dd,1H) ppm. Step 2 : Synthesis of 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-benzenesulfonyl chloride

將氯磺酸（1.8 ml，27 mmol）添加至3,5-二氯-2-(4-氯-2-氟-苯基)吡啶（1.5 g，5.4 mmol）中，並將所得混合物加熱至140°C持續3小時。使混合物冷卻然後添加至冰水中，並將所得混合物用添加的乙酸乙酯（2 × 80 ml）萃取。將合併的有機相經硫酸鈉乾燥、過濾並在減壓下蒸發，以提供呈固體的2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯磺醯氯（1.8 g）。 1H NMR (400 MHz, CDCl 3) δ 8.6 (d,1H), 8.3 (d,1H), 7.9 (d,1H), 7.5 (d,1H) ppm。 步驟 3 ：2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯硫酚的合成 Chlorosulfonic acid (1.8 ml, 27 mmol) was added to 3,5-dichloro-2-(4-chloro-2-fluoro-phenyl)pyridine (1.5 g, 5.4 mmol) and the resulting mixture was heated to 140°C for 3 hours. The mixture was allowed to cool and then added to ice water, and the resulting mixture was extracted with added ethyl acetate (2 × 80 ml). The combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to provide 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-benzenesulfonamide as a solid Chlorine (1.8 g). 1 H NMR (400 MHz, CDCl 3 ) δ 8.6 (d,1H), 8.3 (d,1H), 7.9 (d,1H), 7.5 (d,1H) ppm. Step 3 : Synthesis of 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-thiophenol

在室溫下將三苯基膦（4.0 g，15 mmol）分批添加至2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯磺醯氯（1.8 g，4.3 mmol）在四氫呋喃（22 ml）中的攪拌溶液中。添加水（3.6 ml），並將所得混合物在環境溫度下攪拌18小時。添加水（40 ml）和乙酸乙酯（90 ml），並分離相。用乙酸乙酯（50 ml）萃取水相，並將合併的有機相經硫酸鈉乾燥、過濾並在減壓下蒸發，以留下殘餘物，將該殘餘物藉由管柱層析法純化，以提供呈膠狀物的2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯硫酚（1.75 g）。 1H NMR (400 MHz, CDCl 3) δ 8.55 (d,1H), 7.85 (d,1H), 7.45 (d,1H), 7.35 (d,1H), 3.9 (s,1H) ppm。 步驟 4 ：(3-甲氧基-3-側氧基-丙基)2-[2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯基]氫硫基丙酸酯（化合物8-374）的合成 Triphenylphosphine (4.0 g, 15 mmol) was added portionwise to 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-benzenesulfonyl chloride (1.8 g, 4.3 mmol) in a stirred solution of tetrahydrofuran (22 ml). Water (3.6 ml) was added and the resulting mixture was stirred at ambient temperature for 18 hours. Water (40 ml) and ethyl acetate (90 ml) were added and the phases were separated. The aqueous phase was extracted with ethyl acetate (50 ml), and the combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to leave a residue, which was purified by column chromatography. to provide 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-thiophenol (1.75 g) as a gum. 1 H NMR (400 MHz, CDCl 3 ) δ 8.55 (d,1H), 7.85 (d,1H), 7.45 (d,1H), 7.35 (d,1H), 3.9 (s,1H) ppm. Step 4 : (3-methoxy-3-sideoxy-propyl)2-[2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-phenyl]hydrogen Synthesis of thiopropionate (compound 8-374)

將(3-甲氧基-3-側氧基-丙基)2-溴丙酸酯（如在實施例2中所述製備；130 mg，0.53 mmol）添加至2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯硫酚（200 mg，0.49 mmol）、碳酸銫（160 mg，0.50 mmol）和乙腈（14 ml）的攪拌混合物中，並將所得混合物在環境溫度下攪拌2小時。添加乙酸乙酯（50 ml），並將所得混合物用水（2 × 20 ml）清洗、經硫酸鈉乾燥、過濾並蒸發，以留下殘餘物，將該殘餘物藉由管柱層析法純化，以提供呈油狀物的(3-甲氧基-3-側氧基-丙基)2-[2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯基]氫硫基丙酸酯（化合物8-374）（44 mg）。 1H NMR (400 MHz, CDCl 3) δ 8.6 (d,1H), 7.9 (d,1H), 7.7 (d,1H), 7.35 (d, 1H), 4.35 (m, 2H), 3.9 (q, 1H), 3.7 (s, 3H), 2.6 (m, 2H), 1.55 (d, 3H) ppm。 實施例 2 ： (3- 甲氧基 -3- 側氧基 - 丙基 )2- 溴丙酸酯的製備 (3-Methoxy-3-pendantoxy-propyl)2-bromopropionate (prepared as described in Example 2; 130 mg, 0.53 mmol) was added to 2-chloro-5-(3 ,5-dichloro-2-pyridyl)-4-fluoro-thiophenol (200 mg, 0.49 mmol), cesium carbonate (160 mg, 0.50 mmol) and acetonitrile (14 ml) in a stirred mixture, and the resulting The mixture was stirred at ambient temperature for 2 hours. Ethyl acetate (50 ml) was added and the resulting mixture was washed with water (2 × 20 ml), dried over sodium sulfate, filtered and evaporated to leave a residue which was purified by column chromatography. To provide (3-methoxy-3-sideoxy-propyl)2-[2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro- Phenyl]mercaptopropionate (compound 8-374) (44 mg). 1 H NMR (400 MHz, CDCl 3 ) δ 8.6 (d,1H), 7.9 (d,1H), 7.7 (d,1H), 7.35 (d, 1H), 4.35 (m, 2H), 3.9 (q, 1H), 3.7 (s, 3H), 2.6 (m, 2H), 1.55 (d, 3H) ppm. Example 2 : Preparation of (3- methoxy -3- side oxy - propyl ) 2- bromopropionate

將三乙胺（1.3 ml，9.1 mmol）和3-羥基丙酸甲酯（0.48 ml，5.0 mmol）逐滴添加至2-溴丙醯溴（0.49 ml，4.5 mmol）在乙腈（15 ml）中的在0°C下的攪拌溶液中。將所得混合物在0°C下攪拌1小時，然後在環境溫度下攪拌2小時。添加水（20 ml）和乙酸乙酯（60 ml），分離相，並用乙酸乙酯（60 ml）萃取水相。將合併的有機相經硫酸鈉乾燥、過濾並在減壓下蒸發，以留下油狀物，將該油狀物藉由管柱層析法純化，以提供呈油狀物的(3-甲氧基-3-側氧基-丙基)2-溴丙酸酯（440 mg）。 1H NMR (400 MHz, CDCl 3) δ 4.45 (m, 2H), 4.35 (m, 1H), 3.75 (s, 3H), 2.7 (t, 2H), 1.8 (d, 3H) ppm。 實施例 3 ： 3-[2-[2- 氯 -5-(3,5- 二氯 -2- 吡啶基 )-4- 氟 - 苯基 ] 氫硫基丙醯基胺基 ] 丙酸甲酯（化合物 26-374 ）的製備 步驟 1 ：3-(2-溴丙醯基胺基)丙酸甲酯的合成 Triethylamine (1.3 ml, 9.1 mmol) and methyl 3-hydroxypropionate (0.48 ml, 5.0 mmol) were added dropwise to 2-bromopropionyl bromide (0.49 ml, 4.5 mmol) in acetonitrile (15 ml) in a stirred solution at 0°C. The resulting mixture was stirred at 0°C for 1 hour and then at ambient temperature for 2 hours. Water (20 ml) and ethyl acetate (60 ml) were added, the phases were separated and the aqueous phase was extracted with ethyl acetate (60 ml). The combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to leave an oil, which was purified by column chromatography to provide (3-methyl) as an oil. Oxy-3-pentyloxy-propyl)2-bromopropionate (440 mg). 1 H NMR (400 MHz, CDCl 3 ) δ 4.45 (m, 2H), 4.35 (m, 1H), 3.75 (s, 3H), 2.7 (t, 2H), 1.8 (d, 3H) ppm. Example 3 : Methyl 3-[2-[2- chloro- 5-(3,5- dichloro -2- pyridyl )-4- fluoro - phenyl ] mercaptopropionylamine ] propionate (Compound 26-374 ) Preparation step 1 : Synthesis of methyl 3-(2-bromopropionylamine)propionate

將三乙胺（2.6 ml，9.1 mmol）和2-溴丙醯溴（0.97 ml，9.1 mmol）添加至(3-甲氧基-3-側氧基-丙基)氯化銨（1.42 g，10 mmol）在乙腈（30 ml）中的在0°C下的攪拌混合物中。將所得混合物在0°C下攪拌1小時，然後在環境溫度下攪拌2小時。添加水（20 ml）和乙酸乙酯（60 ml），分離相，並用乙酸乙酯（60 ml）萃取水相。將合併的有機相經硫酸鈉乾燥、過濾並在減壓下蒸發，以留下油狀物，將該油狀物藉由管柱層析法純化，以提供呈固體的3-(2-溴丙醯基胺基)丙酸甲酯（560 mg）。 1H NMR (400 MHz, CDCl 3) δ 6.95 (br s, 1H), 4.4 (q, 1H), 3.75 (s, 3H), 3.55 (m, 2H), 2.6 (m, 2H), 1.85 (d, 3H) ppm。 步驟 2 ：3-[2-[2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯基]氫硫基丙醯基胺基]丙酸甲酯（化合物26-374）的合成 Triethylamine (2.6 ml, 9.1 mmol) and 2-bromopropyl bromide (0.97 ml, 9.1 mmol) were added to (3-methoxy-3-pentyloxy-propyl)ammonium chloride (1.42 g, 10 mmol) in acetonitrile (30 ml) in a stirred mixture at 0 °C. The resulting mixture was stirred at 0°C for 1 hour and then at ambient temperature for 2 hours. Water (20 ml) and ethyl acetate (60 ml) were added, the phases were separated and the aqueous phase was extracted with ethyl acetate (60 ml). The combined organic phases were dried over sodium sulfate, filtered and evaporated under reduced pressure to leave an oil, which was purified by column chromatography to provide 3-(2-bromo) as a solid Propionylamine)methyl propionate (560 mg). 1 H NMR (400 MHz, CDCl 3 ) δ 6.95 (br s, 1H), 4.4 (q, 1H), 3.75 (s, 3H), 3.55 (m, 2H), 2.6 (m, 2H), 1.85 (d , 3H) ppm. Step 2 : Methyl 3-[2-[2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-phenyl]mercaptopropionylamine]propionate ( Synthesis of compound 26-374)

將3-(2-溴丙醯基胺基)丙酸甲酯（130 mg，0.53 mmol）添加至2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯硫酚（如在實施例1、步驟3中所述製備；200 mg，0.49 mmol）、碳酸銫（160 mg，0.50 mmol）和乙腈（4 ml）的攪拌混合物中，並將所得混合物在環境溫度下攪拌1小時。添加乙酸乙酯（50 ml），並將所得混合物用水（2 × 20 ml）清洗、經硫酸鈉乾燥、過濾並蒸發，以留下殘餘物，將該殘餘物藉由管柱層析法純化，以提供3-[2-[2-氯-5-(3,5-二氯-2-吡啶基)-4-氟-苯基]氫硫基丙醯基胺基]丙酸甲酯（化合物26-374）（36 mg）。 1H NMR (400 MHz, CDCl 3) δ 8.55 (d,1H), 7.85 (d,1H), 7.45 (d,1H), 7.3 (d, 1H), 7.05 (br t, 1H), 3.85 (q, 1H), 3.6 (s, 3H), 3.5 (m, 1H), 3.45 (m, 1H), 2.45 (t, 2H), 1.55 (d, 3H) ppm。 配製物實施例 可濕性粉劑 a) b) c) 活性成分 [具有式 (I) 的化合物] 25% 50% 75% 木質素磺酸鈉 5% 5% - 月桂基硫酸鈉 3% - 5% 二異丁基萘磺酸鈉 - 6% 10% 苯酚聚乙二醇醚 - 2% - （7-8 mol的環氧乙烷）          高度分散的矽酸 5% 10% 10% 高嶺土 62% 27% - Methyl 3-(2-bromopropylamino)propionate (130 mg, 0.53 mmol) was added to 2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro- of thiophenol (prepared as described in Example 1, step 3; 200 mg, 0.49 mmol), cesium carbonate (160 mg, 0.50 mmol) and acetonitrile (4 ml), and the resulting mixture was Stir at room temperature for 1 hour. Ethyl acetate (50 ml) was added and the resulting mixture was washed with water (2 × 20 ml), dried over sodium sulfate, filtered and evaporated to leave a residue which was purified by column chromatography. To provide methyl 3-[2-[2-chloro-5-(3,5-dichloro-2-pyridyl)-4-fluoro-phenyl]mercaptopropionylamine]propionate (compound 26-374) (36 mg). 1 H NMR (400 MHz, CDCl 3 ) δ 8.55 (d,1H), 7.85 (d,1H), 7.45 (d,1H), 7.3 (d, 1H), 7.05 (br t, 1H), 3.85 (q , 1H), 3.6 (s, 3H), 3.5 (m, 1H), 3.45 (m, 1H), 2.45 (t, 2H), 1.55 (d, 3H) ppm. Formulation Examples wettable powder a) b) c) Active ingredient [compound of formula (I)] 25% 50% 75% Sodium lignosulfonate 5% 5% - sodium lauryl sulfate 3% - 5% Sodium diisobutylnaphthalene sulfonate - 6% 10% Phenol polyglycol ether - 2% - (7-8 mol of ethylene oxide) Highly dispersed silicic acid 5% 10% 10% kaolin 62% 27% -

將該活性成分與佐劑充分混合並且將混合物在適合的研磨機中充分研磨，從而提供可以用水稀釋而給出所希望的濃度的懸浮液的可濕性粉劑。 乾種子處理用的粉劑 a) b) c) 活性成分 [具有式 (I) 的化合物] 25% 50% 75% 輕質礦物油 5% 5% 5% 高度分散的矽酸 5% 5% - 高嶺土 65% 40% - 滑石 -    20% The active ingredient is thoroughly mixed with the adjuvant and the mixture is thoroughly ground in a suitable grinder to provide a wettable powder which can be diluted with water to give a suspension of the desired concentration. Powder for dry seed treatment a) b) c) Active ingredient [compound of formula (I)] 25% 50% 75% light mineral oil 5% 5% 5% Highly dispersed silicic acid 5% 5% - kaolin 65% 40% - talc - 20%

將該活性成分與佐劑充分混合並且將混合物在合適的研磨機中充分研磨，從而提供可以直接用於種子處理的粉劑。 可乳化濃縮物    活性成分 [具有式 (I) 的化合物] 10% 辛基酚聚乙二醇醚 3% （4-5 mol的環氧乙烷）    十二烷基苯磺酸鈣 3% 蓖麻油聚乙二醇醚（35 mol環氧乙烷） 4% 環己酮 30% 二甲苯混合物 50% The active ingredient is thoroughly mixed with the adjuvant and the mixture is thoroughly ground in a suitable grinder to provide a powder which can be used directly for seed treatment. emulsifiable concentrate Active ingredient [compound of formula (I)] 10% Octylphenol polyglycol ether 3% (4-5 mol of ethylene oxide) Calcium dodecyl benzene sulfonate 3% Castor oil polyglycol ether (35 mol ethylene oxide) 4% cyclohexanone 30% xylene mixture 50%

在植物保護中可以使用的具有任何所要求的稀釋的乳液可以藉由用水稀釋由這種濃縮物中獲得。 粉塵劑 a) b) c) 活性成分 [具有式 (I) 的化合物] 5% 6% 4% 滑石 95% - - 高嶺土 - 94% - 礦物填料 - - 96% Emulsions with any desired dilution which can be used in plant protection can be obtained from such concentrates by diluting with water. dust agent a) b) c) Active ingredient [compound of formula (I)] 5% 6% 4% talc 95% - - kaolin - 94% - mineral fillers - - 96%

藉由將該活性成分與載體混合並且將混合物在適合的研磨機中研磨而獲得即用型粉塵劑。此類粉劑還可以用於種子的乾拌種。 擠出機顆粒劑    活性成分 [具有式 (I) 的化合物] 15% 木質素磺酸鈉 2% 羧甲基纖維素 1% 高嶺土 82% Ready-to-use dusts are obtained by mixing the active ingredient with the carrier and grinding the mixture in a suitable grinder. This type of powder can also be used for dry seed dressing of seeds. extruder granules Active ingredient [compound of formula (I)] 15% Sodium lignosulfonate 2% carboxymethyl cellulose 1% kaolin 82%

將該活性成分與佐劑混合並且研磨，並且將該混合物用水潤濕。將混合物擠出並且然後在空氣流中乾燥。 包衣顆粒劑    活性成分 [具有式 (I) 的化合物] 8% 聚乙二醇（分子量200） 3% 高嶺土 89% The active ingredient is mixed with the adjuvant and triturated, and the mixture is moistened with water. The mixture was extruded and then dried in a stream of air. coated granules Active ingredient [compound of formula (I)] 8% Polyethylene glycol (molecular weight 200) 3% kaolin 89%

將精細研磨的活性成分在混合器中均勻地施用到用聚乙二醇濕潤的高嶺土上。以此方式獲得無塵的包衣顆粒劑。 懸浮液濃縮物 活性成分 [具有式 (I) 的化合物] 40% 丙二醇 10% 壬基酚聚乙二醇醚（15 mol的環氧乙烷） 6% 木質素磺酸鈉 10% 羧甲基纖維素 1% 矽油（處於在水中75%的乳液的形式） 1% 水 32% The finely ground active ingredient is applied evenly in a mixer to kaolin moistened with polyethylene glycol. In this way dust-free coated granules are obtained. suspension concentrate Active ingredient [compound of formula (I)] 40% propylene glycol 10% Nonylphenol glycol ether (15 mol of ethylene oxide) 6% Sodium lignosulfonate 10% carboxymethyl cellulose 1% Silicone oil (in the form of a 75% emulsion in water) 1% water 32%

將精細研磨的活性成分與佐劑緊密地混合，得到懸浮液濃縮物，從該懸浮液濃縮物可以藉由用水稀釋獲得任何所希望的稀釋度的懸浮液。使用此類稀釋物，可以對活的植物連同植物繁殖材料進行處理並且藉由噴灑、傾倒或浸漬保護其對抗微生物的侵染。 種子處理用的可流動性濃縮物 活性成分 [具有式 (I) 的化合物] 40% 丙二醇 5% 共聚物丁醇PO/EO 2% 三苯乙烯酚，具有10-20莫耳EO 2% 1,2-苯并異噻唑啉-3-酮（處於在水中20%的溶液形式） 0.5% 單偶氮-顏料鈣鹽 5% 矽油（處於在水中75%的乳液的形式） 0.2% 水 45.3% The finely ground active ingredient is intimately mixed with the adjuvant to obtain a suspension concentrate from which a suspension at any desired dilution can be obtained by dilution with water. Using such dilutions, living plants together with plant propagation material can be treated and protected against microbial contamination by spraying, pouring or dipping. Flowable concentrates for seed treatment Active ingredient [compound of formula (I)] 40% propylene glycol 5% Copolymer butanol PO/EO 2% Tristyrylphenol, with 10-20 moles EO 2% 1,2-Benzisothiazolin-3-one (as a 20% solution in water) 0.5% Monoazo-Pigment Calcium Salt 5% Silicone oil (in the form of a 75% emulsion in water) 0.2% water 45.3%

將精細研磨的活性成分與佐劑緊密地混合，得到懸浮液濃縮物，從該懸浮液濃縮物可以藉由用水稀釋獲得任何所希望的稀釋度的懸浮液。使用此類稀釋物，可以對活的植物連同植物繁殖材料進行處理並且藉由噴灑、傾倒或浸漬保護其對抗微生物的侵染。 緩釋的膠囊懸浮液 The finely ground active ingredient is intimately mixed with the adjuvant to obtain a suspension concentrate from which a suspension at any desired dilution can be obtained by dilution with water. Using such dilutions, living plants together with plant propagation material can be treated and protected against microbial contamination by spraying, pouring or dipping. Extended release capsule suspension

將28份的具有式 (I) 的化合物的組合與2份的芳香族溶劑以及7份的甲苯二異氰酸酯/聚甲烯（polymethylene）-聚苯基異氰酸酯-混合物（8 : 1）進行混合。將此混合物在1.2份的聚乙烯醇、0.05份的消泡劑以及51.6份的水的混合物中進行乳化直至達到所希望的粒度。向此乳液中添加在5.3份的水中的2.8份的1,6-己二胺混合物。將混合物攪拌直至聚合反應完成。將獲得的膠囊懸浮液藉由添加0.25份的增稠劑以及3份的分散劑進行穩定。該膠囊懸浮液配製物包含28%的活性成分。該介質膠囊的直徑係8-15微米。將所得配製物作為在適合於此目的的裝置中的水性懸浮液施用至種子上。 生物學實施例 出苗前生物學功效 28 parts of a combination of compounds of formula (I) are mixed with 2 parts of aromatic solvent and 7 parts of toluene diisocyanate/polymethylene-polyphenylisocyanate mixture (8:1). This mixture was emulsified in a mixture of 1.2 parts polyvinyl alcohol, 0.05 parts antifoam agent and 51.6 parts water until the desired particle size was achieved. To this emulsion was added a mixture of 2.8 parts of 1,6-hexanediamine in 5.3 parts of water. The mixture was stirred until polymerization was complete. The obtained capsule suspension was stabilized by adding 0.25 parts of thickening agent and 3 parts of dispersing agent. This capsule suspension formulation contains 28% active ingredient. The diameter of the media capsule ranges from 8 to 15 microns. The resulting formulation is applied to the seeds as an aqueous suspension in a device suitable for this purpose. Biological Examples Pre-emergence Biological Efficacy

將雜草和/或作物的種子播種在盆中的標準土壤中（長芒莧（ Amaranthus palmeri，AMAPA）、多年生黑麥草（ Lolium perenne，LOLPE）、白苞猩猩草（ Euphorbia heterophylla，EPHHL）、碗仔花（ Ipomoea hederacea，IPOHE）、大狗尾草（ Setaria faberi，SETFA）、稗草（ Echinochloa crus-galli，ECHCG））。在溫室中的受控條件（在24°C/19°C下，白天/夜晚；16小時光照）下培養一天之後，用如下得到的水性噴霧溶液噴灑植物：將工業活性成分在少量丙酮和稱為IF50（11.12% Emulsogen EL360 TM + 44.44% N-甲基吡咯啶酮 + 44.44% Dowanol DPM乙二醇醚）的特殊溶劑和乳化劑混合物中配製，以產生50 g/l溶液，然後使用0.2% Genapol XO80作為稀釋劑將其稀釋以得到所需最終劑量的測試化合物。 Sow weed and/or crop seeds in pots in standard soil ( Amaranthus palmeri (AMAPA), perennial ryegrass ( Lolium perenne , LOLPE), white bract gorilla grass ( Euphorbia heterophylla , EPHHL), bowl Ipomoea hederacea , IPOHE, Setaria faberi , SETFA, Echinochloa crus-galli , ECHCG). After one day of cultivation in the greenhouse under controlled conditions (at 24°C/19°C, day/night; 16 hours of light), the plants are sprayed with an aqueous spray solution obtained as follows: add the industrial active ingredient in a small amount of acetone and weigh Formulated in a special mixture of solvents and emulsifiers for IF50 (11.12% Emulsogen EL360 TM + 44.44% N-methylpyrrolidone + 44.44% Dowanol DPM glycol ether) to produce a 50 g/l solution, then use 0.2% Genapol XO80 is used as a diluent to dilute it to give the desired final dose of test compound.

該等測試植物然後在溫室中的受控條件（在24°C/18°C下，白天/夜晚；15小時光照；50%濕度）下生長，並且每日澆水兩次。13天後，評估測試（100 = 對植物的完全損害；0 = 無植物損害）。結果在下表2中示出。 [ 表 2 ] 化合物編號 比率 （ g/ha ） 種 AMAPA LOLPE EPHHL IPOHE SETFA ECHCG 8-374 250 100 0 40 80 0 0 26-374 250 100 0 100 80 100 10 出苗後生物學功效 The test plants were then grown in a greenhouse under controlled conditions (day/night at 24°C/18°C; 15 hours of light; 50% humidity) and watered twice daily. After 13 days, the test is evaluated (100 = complete damage to the plant; 0 = no damage to the plant). The results are shown in Table 2 below. [ Table 2 ] Compound number Ratio ( g/ha ) kind AMAPA LOLPE EPHHL IPOHE SETFA ECHCG 8-374 250 100 0 40 80 0 0 26-374 250 100 0 100 80 100 10 Post-emergence biological efficacy

將雜草和/或作物的種子播種在盆中的標準土壤中（長芒莧（AMAPA）、藜草（ Chenopodium album，CHEAL）、白苞猩猩草（EPHHL）、碗仔花（ IPOHE）、 牛筋草（ Eleusine indica，ELEIN ）、多年生黑麥草（LOLPE）、馬唐（ Digitaria sanguinalis，DIGSA）、大狗尾草（SETFA）、稗草（ECHCG））。在溫室中的受控條件（在24°C/19°C下，白天/夜晚；16小時光照）下培養14天之後，用如下得到的水性噴霧溶液噴灑植物：將技術活性成分在少量丙酮和稱為IF50（11.12% Emulsogen EL360 TM + 44.44% N-甲基吡咯啶酮 + 44.44% Dowanol DPM乙二醇醚）的特殊溶劑和乳化劑混合物中配製，以產生50 g/l溶液，然後使用0.2% Genapol XO80作為稀釋劑將其稀釋以得到所需最終劑量的測試化合物。 Sow seeds of weeds and/or crops in pots in standard soil (Amaranth amaranth (AMAPA), Chenopodium album (CHEAL), White bract orangutan grass (EPHHL), Ipohe ( IPOHE ), Cowgrass Eleusine indica ( ELEIN ) , perennial ryegrass (LOLPE), crabgrass ( Digitaria sanguinalis , DIGSA), giant setaria (SETFA), barnyard grass (ECCHG)). After 14 days of cultivation in the greenhouse under controlled conditions (at 24°C/19°C, day/night; 16 hours of light), the plants are sprayed with an aqueous spray solution obtained as follows: the technically active ingredient is mixed with a small amount of acetone and Prepared in a special mixture of solvents and emulsifiers called IF50 (11.12% Emulsogen EL360 TM + 44.44% N-methylpyrrolidone + 44.44% Dowanol DPM glycol ether) to produce a 50 g/l solution, then use 0.2 % Genapol XO80 as diluent to obtain the desired final dose of test compound.

該等測試植物然後在溫室中的受控條件（在24°C/18°C下，白天/夜晚；15小時光照；50%濕度）下生長，並且每日澆水兩次。13天後，評估測試（100 = 對植物的完全損害；0 = 無植物損害）。結果在下表3中示出。 [ 表 3 ] 化合物編號 比率 （ g/ha ） 種 AMAPA CHEAL EPHHL IPOHE ELEIN LOLPE DIGSA SETFA ECHCG 8-374 250 100 100 80 100 60 80 50 50 20 26-374 250 90 100 90 100 60 100 50 30 20 The test plants were then grown in a greenhouse under controlled conditions (day/night at 24°C/18°C; 15 hours of light; 50% humidity) and watered twice daily. After 13 days, the test is evaluated (100 = complete damage to the plant; 0 = no damage to the plant). The results are shown in Table 3 below. [ table 3 ] Compound number Ratio ( g/ha ) kind AMAPA CHEAL EPHHL IPOHE ELEIN LOLPE DIGSA SETFA ECHCG 8-374 250 100 100 80 100 60 80 50 50 20 26-374 250 90 100 90 100 60 100 50 30 20

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Claims (15)

一種具有式 (I) 的化合物或其農藝學上可接受的鹽： (I) X 1係C-R 1、氮或N +-O -； X 2係C-R 17或氮； X 3係C-R 18或氮； X 4係C-R 19或氮； 前提係X 1、X 2、X 3和X 4中最多兩個係氮，並且X 3和X 4兩者不皆為氮； Y係C-H或氮； B係O、S或NR 5； D係-[C(R 6)(R 7)] n-； m係從0至2的整數； n係從1至4的整數； R 1係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基(alkylsulfonyloxy)、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基(alkylthio)、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基(alkylamino)、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 2係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、CO 2R 9或CONR 10R 11；或者 R 1和R 2與它們所附接的碳原子一起形成5員或6員環，其可以是飽和的或部分或完全不飽和的，並且可以視需要含有一個或兩個選自氮、氧和硫的雜原子，並且可以被1至4個由R 16表示的基團取代；或者 R 2和R 19與它們所附接的碳原子一起形成5員或6員環，其可以是飽和的或部分或完全不飽和的，並且可以視需要含有一個或兩個選自氮、氧和硫的雜原子，並且可以被1至4個由R 16表示的基團取代； R 3係氫、鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷硫基或C 1-C 4烷基磺醯基； R 4係氫、鹵素、氰基、硝基、胺基羰基、胺基硫代羰基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基或C 1-C 4烷基磺醯基； R 5係氫、羥基、C 1-C 6烷基或C 1-C 4烷氧基； R 6和R 7各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、羥基、C 1-C 4烷氧基、C 1-C 4烷氧基羰基或-CH 2OR 12；前提係R 6和R 7在同一碳原子上不皆為羥基； 或者，在同一碳原子或不同碳原子上的兩個R 6和R 7基團一起形成C 1-C 5伸烷基鏈，該鏈含有0、1或2個氧原子，被1至3個由R 15表示的基團取代； 或者，在同一碳原子上的兩個R 6和R 7基團一起形成C 2-C 3烯烴； R 8係OR 9、SR 9或NR 10R 11； R 9係氫、C 1-C 10烷基、C 1-C 10鹵代烷基、C 3-C 6烯基、C 3-C 6鹵代烯基、C 3-C 6炔基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 6-C 10芳基C 1-C 3烷基、被1至4個由R 13表示的基團取代的C 6-C 10芳基C 1-C 3烷基、雜芳基C 1-C 3烷基、或被1至3個由R 13表示的基團取代的雜芳基C 1-C 3烷基； R 10係氫、C 1-C 6烷基、SO 2R 14； R 11係氫或C 1-C 6烷基；或者 R 10和R 11與它們所附接的氮一起形成3員至6員雜環基環； R 12係氫、C 1-C 4烷基或C 1-C 4烷基羰基； R 13係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基； R 14係C 1-C 4烷基、C 1-C 4鹵代烷基或C 1-C 4烷基(C 1-C 4烷基)胺基； R 15係氫、鹵素、C 1-C 4烷基或C 1-C 4鹵代烷基； R 16係鹵素、C 1-C 4烷基、C 1-C 4鹵代烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、氰基或C 1-C 4烷基磺醯基； R 17係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 18係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 19係氫、鹵素、氰基、硝基、C 1-C 4烷基、C 1-C 4鹵代烷基、C 3-C 6環烷基、C 1-C 4烷氧基C 1-C 6烷基、C 1-C 4鹵代烷氧基C 1-C 6烷基、C 1-C 4烷氧基、C 1-C 4鹵代烷氧基、C 1-C 4烷氧基C 1-C 4烷氧基、C 1-C 4烷基磺醯氧基、C 1-C 4鹵代烷基磺醯氧基、C 1-C 4烷硫基、C 1-C 4烷基亞磺醯基、C 1-C 4烷基磺醯基、C 1-C 4鹵代烷硫基、C 1-C 4鹵代烷基亞磺醯基、C 1-C 4鹵代烷基磺醯基、胺基、C 1-C 4烷基胺基、二(C 1-C 4烷基)胺基、C 1-C 4烷基羰基胺基、C 1-C 4烷基羰基(C 1-C 4烷基)胺基、C 1-C 4烷氧基羰基胺基、胺基羰基胺基、C 1-C 4烷基胺基羰基胺基、C 1-C 4烷基磺醯基胺基、C 1-C 4鹵代烷基磺醯基胺基、-CO 2R 9或-CONR 10R 11； R 20和R 21各自獨立地是氫、鹵素、C 1-C 6烷基、C 1-C 6鹵代烷基、C 1-C 4烷氧基或-CH 2OR 12； 或者兩個R 20和R 21基團與它們所附接的碳原子一起形成C 2-C 5伸烷基鏈，其中所述C 2-C 5伸烷基鏈包含0、1或2個氧原子，並且其中所述C 2-C 5伸烷基鏈被1至3個由R 15表示的基團取代； 或者兩個R 20和R 21基團與它們所附接的碳原子一起形成C 2-C 3烯烴；並且 前提係R 1、R 2、R 17、R 18和R 19不全係氫。 A compound of formula (I) or an agronomically acceptable salt thereof: (I) X 1 is CR 1 , nitrogen or N + -O - ; X 2 is CR 17 or nitrogen; X 3 is CR 18 or nitrogen; X 4 is CR 19 or nitrogen; provided that X 1 , X 2 , X At most two of 3 and X 4 are nitrogen, and both X 3 and 7 )] n -; m is an integer from 0 to 2; n is an integer from 1 to 4; R 1 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 Haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkyl Oxygen group, C 1 -C 4 haloalkoxy group, C 1 -C 4 alkoxy group, C 1 -C 4 alkoxy group, C 1 -C 4 alkylsulfonyloxy group (alkylsulfonyloxy), C 1 -C 4 haloalkyl group Alkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio, C 1 -C 4 haloalkylsulfenyl, C 1 -C 4 haloalkylsulfonyl, amine, C 1 -C 4 alkylamino, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group , C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkylsulfonylamine, -CO 2 R 9 or -CONR 10 R 11 ; R 2 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy, C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfenyl Base, C 1 -C 4 alkylsulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkylsulfinyl group, C 1 -C 4 haloalkylsulfonyl group, amino group, C 1 -C 4 alkylamino, di(C 1 -C 4 alkyl)amine, C 1 -C 4 alkylcarbonylamino, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkylamine carbonylamino group, C 1 -C 4 alkylsulfonylamine group, C 1 -C 4 haloalkylsulfonamide, CO 2 R 9 or CONR 10 R 11 ; or R 1 and R 2 together with the carbon atoms to which they are attached form a 5- or 6-membered ring, which may be saturated or partially or Completely unsaturated, and may optionally contain one or two heteroatoms selected from nitrogen, oxygen and sulfur, and may be substituted by 1 to 4 groups represented by R 16 ; or R 2 and R 19 are identical to the The attached carbon atoms together form a 5- or 6-membered ring, which may be saturated or partially or fully unsaturated, and may optionally contain one or two heteroatoms selected from nitrogen, oxygen, and sulfur, and may be 1 to 4 groups represented by R 16 are substituted; R 3 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 Haloalkoxy, C 1 -C 4 alkylthio or C 1 -C 4 alkylsulfonyl; R 4 is hydrogen, halogen, cyano, nitro, aminocarbonyl, aminothiocarbonyl, C 1 - C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy or C 1 -C 4 alkylsulfonyl group; R 5 is hydrogen, hydroxyl, C 1 -C 6 alkyl or C 1 -C 4 alkoxy; R 6 and R 7 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, hydroxyl, C 1 - C 4 alkoxy, C 1 -C 4 alkoxycarbonyl or -CH 2 OR 12 ; provided that R 6 and R 7 are not both hydroxyl groups on the same carbon atom; or, on the same carbon atom or different carbon atoms The two R 6 and R 7 groups together form a C 1 -C 5 alkylene chain containing 0, 1 or 2 oxygen atoms substituted by 1 to 3 groups represented by R 15 ; or, Two R 6 and R 7 groups on the same carbon atom together form a C 2 -C 3 alkene; R 8 is OR 9 , SR 9 or NR 10 R 11 ; R 9 is hydrogen, C 1 -C 10 alkyl , C 1 -C 10 haloalkyl, C 3 -C 6 alkenyl, C 3 -C 6 haloalkenyl, C 3 -C 6 alkynyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl , C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 6 -C 10 aryl C 1 -C 3 alkyl, C 6 -C substituted by 1 to 4 groups represented by R 13 10 Aryl C 1 -C 3 alkyl, heteroaryl C 1 -C 3 alkyl, or heteroaryl C 1 -C 3 alkyl substituted by 1 to 3 groups represented by R 13 ; R 10 is hydrogen, C 1 -C 6 alkyl, SO 2 R 14 ; R 11 is hydrogen or C 1 -C 6 alkyl; or R 10 and R 11 together with the nitrogen to which they are attached form a 3- to 6-membered heterogeneous Ring base ring; R 12 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkylcarbonyl; R 13 is halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 - C 4 alkoxy group, C 1 -C 4 haloalkoxy group, cyano group or C 1 -C 4 alkylsulfonyl group; R 14 is C 1 -C 4 alkyl group, C 1 -C 4 haloalkyl group or C 1 -C 4 alkyl (C 1 -C 4 alkyl) amino group; R 15 is hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl; R 16 is halogen, C 1 -C 4 Alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, cyano or C 1 -C 4 alkylsulfonyl; R 17 is hydrogen, halogen, Cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy, C 1 -C 6 alkyl, C 1 - C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy C 1 -C 4 alkoxy , C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkyl Sulfonyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4 alkylamino group, di (C 1 -C 4 alkyl)amine, C 1 -C 4 alkylcarbonylamino, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine, C 1 -C 4 alkoxy basecarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkylaminocarbonylamino group, C 1 -C 4 alkylsulfonylamine group, C 1 -C 4 haloalkylsulfonylamine group, -CO 2 R 9 or -CONR 10 R 11 ; R 18 is hydrogen, halogen, cyano, nitro, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl group, C 1 -C 4 alkylsulfinyl group, C 1 -C 4 haloalkylthio group, C 1 -C 4 haloalkyl sulfinyl group, C 1 -C 4 haloalkyl group Sulfonyl group, amine group, C 1 -C 4 alkylamino group, di(C 1 -C 4 alkyl)amine group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl group (C 1 -C 4 alkyl)amine, C 1 -C 4 alkoxycarbonylamino, aminocarbonylamino, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkyl Sulfonylamine group, C 1 -C 4 haloalkylsulfonylamine group, -CO 2 R 9 or -CONR 10 R 11 ; R 19 is hydrogen, halogen, cyano group, nitro group, C 1 -C 4 alkane base, C 1 -C 4 haloalkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxy C 1 -C 6 alkyl, C 1 -C 4 haloalkoxy C 1 -C 6 alkyl , C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy, C 1 -C 4 alkylsulfonyloxy, C 1 -C 4 haloalkylsulfonyloxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylthio , C 1 -C 4 haloalkyl sulfonyl group, C 1 -C 4 haloalkyl sulfonyl group, amino group, C 1 -C 4 alkylamino group, di(C 1 -C 4 alkyl) amino group, C 1 -C 4 alkylcarbonylamino group, C 1 -C 4 alkylcarbonyl (C 1 -C 4 alkyl)amine group, C 1 -C 4 alkoxycarbonylamino group, aminocarbonylamino group, C 1 -C 4 alkylaminocarbonylamino, C 1 -C 4 alkylsulfonylamine, C 1 -C 4 haloalkylsulfonylamine, -CO 2 R 9 or -CONR 10 R 11 ; R 20 and R 21 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 4 alkoxy, or -CH 2 OR 12 ; or two R 20 and The R 21 groups together with the carbon atoms to which they are attached form a C 2 -C 5 alkylene chain, wherein said C 2 -C 5 alkylene chain contains 0, 1 or 2 oxygen atoms, and wherein said The C 2 -C 5 alkyl chain is substituted by 1 to 3 groups represented by R 15 ; or the two R 20 and R 21 groups together with the carbon atoms to which they are attached form a C 2 -C 3 alkene; And the premise is that R 1 , R 2 , R 17 , R 18 and R 19 are not all hydrogen. 如請求項1所述之化合物，其中，X 1係C-R 1。 The compound of claim 1, wherein X 1 is CR 1 . 如請求項1或請求項2所述之化合物，其中，X 2係氮。 The compound of claim 1 or claim 2, wherein X 2 is nitrogen. 如請求項1或請求項2所述之化合物，其中，X 3係C-R 18。 The compound of claim 1 or claim 2, wherein X 3 is CR 18 . 如請求項1或請求項2所述之化合物，其中，X 4係C-R 19。 The compound of claim 1 or claim 2, wherein X 4 is CR 19 . 如請求項1或請求項2所述之化合物，其中，Y係C-H。The compound of claim 1 or claim 2, wherein Y is C-H. 如請求項1或請求項2所述之化合物，其中，B係O、NH和NCH 3。 The compound of claim 1 or claim 2, wherein B is O, NH and NCH 3 . 如請求項1或請求項2所述之化合物，其中，n係2。The compound of claim 1 or claim 2, wherein n is 2. 如請求項1或請求項2所述之化合物，其中，R 2係氫、氟、氯、甲基或三氟甲基。 The compound of claim 1 or claim 2, wherein R 2 is hydrogen, fluorine, chlorine, methyl or trifluoromethyl. 如請求項1或請求項2所述之化合物，其中，R 3係氫、氯或氟。 The compound of claim 1 or claim 2, wherein R 3 is hydrogen, chlorine or fluorine. 如請求項1或請求項2所述之化合物，其中，R 4係氫、氯、溴、氰基或胺基硫代羰基，較佳的是氯、溴或氰基。 The compound of claim 1 or claim 2, wherein R 4 is hydrogen, chlorine, bromine, cyano or aminothiocarbonyl, preferably chlorine, bromine or cyano. 如請求項1或請求項2所述之化合物，其中，R 8係OR 9。 The compound according to claim 1 or claim 2, wherein R 8 is OR 9 . 一種農用化學組成物，其包含除草有效量的如請求項1至12中任一項中所定義的具有式 (I) 的化合物、以及農用化學上可接受的稀釋劑或載體。An agrochemical composition comprising a herbicidal effective amount of a compound of formula (I) as defined in any one of claims 1 to 12, and an agrochemically acceptable diluent or carrier. 一種控制或預防不希望的植物生長之方法，其中將除草有效量的如請求項1至12中任一項所定義的具有式 (I) 的化合物、或如請求項13所述之組成物施用至該等植物、其部分或其場所。A method of controlling or preventing undesired plant growth, wherein a herbicidally effective amount of a compound of formula (I) as defined in any one of claims 1 to 12, or a composition as described in claim 13 is applied to such plants, parts or places thereof. 一種用於控制在植物栽培場所中不希望的植被之方法，該方法包括以下步驟：a) 在所述場所提供包含至少一種核酸的植物，該核酸包含編碼原紫質原氧化酶（PPO）多肽的核苷酸序列，其對「PPO抑制除草劑」具有抗性或耐受性；b) 向所述場所施用有效量的所述除草劑，其中該PPO抑制除草劑係如請求項1至12中任一項所述之化合物。A method for controlling undesirable vegetation in a plant cultivation site, the method comprising the steps of: a) providing at the site a plant comprising at least one nucleic acid comprising a polypeptide encoding protorhodopsin oxidase (PPO) A nucleotide sequence that is resistant or tolerant to a "PPO inhibiting herbicide"; b) applying an effective amount of said herbicide to said location, wherein the PPO inhibiting herbicide is as claimed in claims 1 to 12 The compound described in any one of them.
TW112118446A 2022-05-20 2023-05-18 Herbicidal compounds TW202404935A (en)

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