CN1121510A - 取代的苯氧基甲基苯基衍生物和其制备方法及其作为抑制害虫和真菌的应用 - Google Patents
取代的苯氧基甲基苯基衍生物和其制备方法及其作为抑制害虫和真菌的应用 Download PDFInfo
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- CN1121510A CN1121510A CN95105106A CN95105106A CN1121510A CN 1121510 A CN1121510 A CN 1121510A CN 95105106 A CN95105106 A CN 95105106A CN 95105106 A CN95105106 A CN 95105106A CN 1121510 A CN1121510 A CN 1121510A
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- -1 phenoxymethylphenyl Chemical class 0.000 title claims description 615
- 238000002360 preparation method Methods 0.000 title claims description 29
- 241000233866 Fungi Species 0.000 title claims description 17
- 241000607479 Yersinia pestis Species 0.000 title description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 466
- 239000000460 chlorine Substances 0.000 claims description 460
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 112
- 229910052760 oxygen Inorganic materials 0.000 claims description 106
- 239000001301 oxygen Substances 0.000 claims description 106
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 98
- 239000000203 mixture Substances 0.000 claims description 55
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 42
- 229910052801 chlorine Inorganic materials 0.000 claims description 35
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 238000000034 method Methods 0.000 claims description 29
- 125000003118 aryl group Chemical group 0.000 claims description 26
- 229910052731 fluorine Inorganic materials 0.000 claims description 26
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 24
- 239000011737 fluorine Substances 0.000 claims description 21
- 239000002253 acid Substances 0.000 claims description 20
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 19
- 229910052794 bromium Inorganic materials 0.000 claims description 19
- 229910052736 halogen Inorganic materials 0.000 claims description 19
- 229910052739 hydrogen Inorganic materials 0.000 claims description 19
- 239000001257 hydrogen Substances 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 18
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 17
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 16
- 125000005843 halogen group Chemical group 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 13
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 12
- 241000238631 Hexapoda Species 0.000 claims description 12
- 229940031815 mycocide Drugs 0.000 claims description 12
- 239000000463 material Substances 0.000 claims description 11
- 230000000855 fungicidal effect Effects 0.000 claims description 10
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 9
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 9
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 9
- 125000004432 carbon atom Chemical group C* 0.000 claims description 9
- 239000007787 solid Substances 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- 125000004104 aryloxy group Chemical group 0.000 claims description 7
- 125000001544 thienyl group Chemical group 0.000 claims description 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 5
- 125000005377 alkyl thioxy group Chemical group 0.000 claims description 4
- 125000005110 aryl thio group Chemical group 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- QFXZANXYUCUTQH-UHFFFAOYSA-N ethynol Chemical group OC#C QFXZANXYUCUTQH-UHFFFAOYSA-N 0.000 claims description 4
- 230000000749 insecticidal effect Effects 0.000 claims description 4
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Natural products C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 claims description 4
- 150000003254 radicals Chemical class 0.000 claims description 4
- 239000002689 soil Substances 0.000 claims description 4
- 125000002837 carbocyclic group Chemical group 0.000 claims description 3
- 239000000417 fungicide Substances 0.000 claims description 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 2
- 238000005911 haloform reaction Methods 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims 5
- KWOLFJPFCHCOCG-UHFFFAOYSA-N Acetophenone Chemical compound CC(=O)C1=CC=CC=C1 KWOLFJPFCHCOCG-UHFFFAOYSA-N 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- GCUHRCUNPDMAIX-UHFFFAOYSA-N 3-phenoxy-2-phenylpropanoic acid Chemical class C=1C=CC=CC=1C(C(=O)O)COC1=CC=CC=C1 GCUHRCUNPDMAIX-UHFFFAOYSA-N 0.000 claims 1
- BOTNYLSAWDQNEX-UHFFFAOYSA-N phenoxymethylbenzene Chemical compound C=1C=CC=CC=1COC1=CC=CC=C1 BOTNYLSAWDQNEX-UHFFFAOYSA-N 0.000 claims 1
- FAQJJMHZNSSFSM-UHFFFAOYSA-N phenylglyoxylic acid Chemical class OC(=O)C(=O)C1=CC=CC=C1 FAQJJMHZNSSFSM-UHFFFAOYSA-N 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1155
- 239000002585 base Substances 0.000 description 510
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 description 307
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 description 280
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 227
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 200
- 150000001875 compounds Chemical class 0.000 description 90
- 125000006180 3-methyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1[H])C([H])([H])[H])C([H])([H])* 0.000 description 76
- BKOOMYPCSUNDGP-UHFFFAOYSA-N 2-methylbut-2-ene Chemical compound CC=C(C)C BKOOMYPCSUNDGP-UHFFFAOYSA-N 0.000 description 43
- XNMQEEKYCVKGBD-UHFFFAOYSA-N 2-butyne Chemical compound CC#CC XNMQEEKYCVKGBD-UHFFFAOYSA-N 0.000 description 42
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 description 42
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 description 39
- 238000006243 chemical reaction Methods 0.000 description 37
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 29
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 28
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 27
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 25
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 25
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 23
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 22
- 125000006022 2-methyl-2-propenyl group Chemical group 0.000 description 21
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 21
- 125000006506 3-phenyl benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])* 0.000 description 21
- 125000006495 3-trifluoromethyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1[H])C([H])([H])*)C(F)(F)F 0.000 description 21
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 description 21
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 21
- 229940073608 benzyl chloride Drugs 0.000 description 21
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 19
- 238000005160 1H NMR spectroscopy Methods 0.000 description 18
- 241000196324 Embryophyta Species 0.000 description 18
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 18
- 239000000047 product Substances 0.000 description 18
- 239000003795 chemical substances by application Substances 0.000 description 16
- 239000000243 solution Substances 0.000 description 16
- 239000002904 solvent Substances 0.000 description 16
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 15
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 14
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 14
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 12
- 239000006185 dispersion Substances 0.000 description 12
- 229910052757 nitrogen Inorganic materials 0.000 description 12
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 11
- 230000000694 effects Effects 0.000 description 11
- 239000000843 powder Substances 0.000 description 11
- 239000002243 precursor Substances 0.000 description 11
- 241000254032 Acrididae Species 0.000 description 10
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 10
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 description 10
- 125000000217 alkyl group Chemical group 0.000 description 9
- 230000002140 halogenating effect Effects 0.000 description 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 9
- 239000011541 reaction mixture Substances 0.000 description 9
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 9
- 239000007921 spray Substances 0.000 description 9
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 9
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 8
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 8
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- HJUGFYREWKUQJT-UHFFFAOYSA-N tetrabromomethane Chemical compound BrC(Br)(Br)Br HJUGFYREWKUQJT-UHFFFAOYSA-N 0.000 description 8
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- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 7
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- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- KUAZQDVKQLNFPE-UHFFFAOYSA-N thiram Chemical compound CN(C)C(=S)SSC(=S)N(C)C KUAZQDVKQLNFPE-UHFFFAOYSA-N 0.000 description 1
- 229960002447 thiram Drugs 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- BAZVSMNPJJMILC-UHFFFAOYSA-N triadimenol Chemical class C1=NC=NN1C(C(O)C(C)(C)C)OC1=CC=C(Cl)C=C1 BAZVSMNPJJMILC-UHFFFAOYSA-N 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
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- DUBNHZYBDBBJHD-UHFFFAOYSA-L ziram Chemical compound [Zn+2].CN(C)C([S-])=S.CN(C)C([S-])=S DUBNHZYBDBBJHD-UHFFFAOYSA-L 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract
取代的苯氧基甲基苯基衍生物I,式中X,R1,R2,R3,R4,R5,R6,Y和n的定义如说明书中所述。
Description
X为=CH-OCH3,=CH-CH3或=N-OCH3;
R1为C1-C6烷基,C2-C6链烯基,C3-C6链炔基,C1-C6卤代烷基,C3-C6卤代链烯基,C1-C4烷氧基-C1-C6烷基,氰基-C1-C6烷基,C1-C6-烷氧基羰基-C1-C6烷基,C3-C6环烷基或C3-C6环烷基-C1-C4烷基,芳基-C1-C6烷基或芳基-C3-C6链烯基或芳氧基-C1-C6烷基,饱和或未饱和的4至6元杂环基或杂环-C1-C4烷基或杂芳基-C1-C6烷基,所说的杂环除了含有碳原子以外,还含有一个或二个选自如下的杂原子基团:氧原子或硫原子,一个或二个氮原子和一个或二个-N(CH3)-基团,
对于上述碳环和苯环来说,其还可能含有一个或多个选自下述的基团:卤素,C1-C4烷基,C1-C2卤代烷基,C3-C6环烷基,C1-C4烷氧基,C1-C2卤代烷氧基,芳基和芳氧基;
R2和R3为氢,卤素,氰基,硝基,C1-C4烷基,C1-C2-卤代烷基,C1-C4烷氧基,C1-C2卤代烷氧基,如果R2和R3彼此相邻则R2和R3可以构成氧亚甲基氧桥或氧亚乙基氧桥,对于这些桥键中的每个碳原子来说,还可以含有一个或二个卤原子和/或甲基;
R4为氰基,氯,溴,C1-C6烷氧基,C1-C6烷硫基,C1-C4卤代烷氧基,C1-C4烷氧基-C1-C4烷氧基,C3-C6环烷基-C1-C2烷氧基,C1-C6烷基氨基,=(C1-C6烷基)氨基,C3-C6链烯氧基,C3-C6链炔氧基,芳氧基,芳硫基,对于芳族环还可能含有一至三个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中可能还进一步带有足够的卤原子以使取代基的总数达到4或5个;
R5为硝基,氰基,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷硫基,苯基或苯氧基,其中芳环可能含有1至3个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中可能还进一步含有足够的卤原子以使取代基的总数达到4或5个;或如果n是2,3,或4,则R5是与母体结构的二个相邻碳原子稠合的1,3-丁二烯-1,4-二基或单-或二卤代的1,3-丁二烯-1,4-二基,这些稠合环还可能含有一或二个选自下述的基团:硝基,氰基,卤素,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基;
n是0,1,2,3或4,如果n为2,3或4时,R5基团可以相同或不同;
Y是氧,-NH-或-N(CH3)-;
R6是氢或C1-C4烷基。
本发明还涉及制备化合物I和化合物I的中间体的方法, 它们用作杀真菌剂和用于杀虫的应用,含有这些化合物作为活性物质的杀真菌组合物和杀虫组合物,抑制有害真菌和害虫的方法。
苯氧基甲基苯基衍生物I类化合物已公开在下述的公开文献中。
EP-A386561描述了具有杀虫和杀真菌特性的式I′的[(亚氨基甲基)苯氧基甲基]苯基乙酸酯衍生物:
其中Ra是氢,烷基或芳基。
其中Rb是氢,烷基,环烷基,卤代烷基或芳基和Z是氨基,烷基氨基或二烷基氨基。
EP-A513580公开了一些通常具有某一基本结构的α-苯基丙烯酸衍生物,这些化合物具有杀虫和杀真菌活性。通过适当地选取各个取代基可形成式I的化合物。其中,Rc是氢,硝基,氰基,卤素,C1-C4烷基,C1-C4烷氧基,C1-C4卤代烷基,C1-C4卤代烷氧基或C1-C4烷硫基,或在n为2,3或4的情况下,二个相邻的取代基Rc一起构成未取代的或取代的1,3-丁二烯-1,4-二基。
当Ph为苯环时,除了其它各种取代基之外,其尤其可含有-C(Rd)=NORe,其中Rd是氢,C1-C6烷基或未取代的或取代的芳基,和Re是未取代的或取代的C1-C6烷基,C2-C6链烯基或C2-C6链炔基,或Ph也可为5元或6元芳环或杂芳环。
在EP-A513580中强调了用式Ib表示的这类化合物作为优选的杀真菌剂,这类化合物在苯环上最多只含一个Rc基团,Ph上除了含有-C(Rd)=NORe基团之外,还可能进一步包含一至二个氰基,卤素,C1-C4烷基,C1-C4卤代烷基和/或C1-C4烷氧基取代基。
最后,EP-A-398692特别地公开了具有杀真菌特性的取代的2-[2-(苯氧基甲基)苯基]-2-烷氧基亚氨基乙酰胺。
但是上述已知化合物的杀虫或杀真菌作用仅在一定程度上令人满意,特别是当它们以低应用率和低浓度使用时。
本发明的目的是提供具有改进的杀真菌和/或杀虫活性的新化合物。
我们发现本发明的目的可以通过如上述定义的取代的苯氧基甲基苯基衍生物I来实现。另外还发现了制备这些化合的方法和中间体,含有这些化合物的组合物及它们用于抑制有害真菌和害虫的方法。
以上所列的取代基R1至R6的定义是分别单列的各个基团的集合术语。所有碳原子,即所有烷基,链烯基,链炔基,卤代烷基,卤代链烯基,烷氧基,卤代烷氧基,链烯氧基,链炔氧基,烷氧基羰基,烷硫基和烷基氨基部分可以是直链或支链的。卤化的取代基优选含有1至5个相同或不同的卤原子。
具体的实例是:
-卤素:氟,氯,溴或碘,优选氟或氯;
-C1-C4烷基:甲基,乙基,正丙基,1-甲基乙基,正丁基,1-甲基丙基,2-甲基丙基,1,1-二甲基乙基,优选甲基;
-C1-C6烷基:如上述定义的C1-C4烷基,正戊基,1-甲基丁基,2-甲基丁基,3-甲基丁基,2,2-二甲基丙基,1-乙基丙基,正己基,1,1-二甲基丙基,1,2-二甲基丙基,1-甲基戊基,2-甲基戊基,3-甲基戊基,4-甲基戊基,1,1-二甲基丁基,1,2-二甲基丁基,1,3-二甲基丁基,2,2-二甲基丁基,2,3-二甲基丁基,3,3-二甲基丁基,1-乙基丁基,2-乙基丁基,1,1,2-三甲基丙基,1,2,2-三甲基丙基,1-乙基-1-甲基丙基,1-乙基-2-甲基丙基,优选甲基,乙基,正丙基,1-甲基乙基,正丁基或1,1-二甲基乙基;
-C2-C6链烯基:乙烯基,丙-1-烯-1-基,丙-2-烯-1-基,1-甲基乙烯基,正丁烯-1-基,正丁烯-2-基,正丁基-3-基,1-甲基丙-1-烯-1-基,2-甲基丙-1-烯-1-基,1-甲基丙-2-烯-1-基,2-甲基丙-2-烯-1-基,正戊烯-1-基,正戊烯-2-基,正戊烯-3-基,正戊烯-4-基,1-甲基丁-1-烯-1-基,2-甲基丁1-烯-1-基,3-甲基丁-1-烯-1-基,1-甲基丁-2-烯-1-基,2-甲基丁-2-烯-1-基,3-甲基丁-2-烯-1-基,1-甲基丁-3-烯-1-基,2-甲基丁-3-烯-1-基,3-甲基丁-3-烯-1-基,1,1-二甲基-丙-2-烯-1-基,1,2-二甲基丙-1-烯-1-基,1,2-二甲基丙-2-烯-1-基,1-乙基丙-1-基-2-基,1-乙基丙-2-烯-1-基,正己-1-烯-1-基,正己-2-烯-1-基,正己-3-烯-1-基,正己-4-烯-1-基,正己-5-烯-1-基,1-甲基戊-1-烯-1-基,2-甲基戊-1-烯-1-基,3-甲基戊-1-烯-1-基,4-甲基戊-1-烯-1-基,1-甲基戊-2-烯-1-基,2-甲基戊-2-烯-1-基,3-甲基戊-2-烯-1-基,4-甲基戊-2-烯-1-基,1-甲基戊-3-烯-1-基,2-甲基戊-3-烯-1-基,3-甲基戊-3-基-1-基,4-甲基戊-3-烯-1-基,1-甲基戊-4-烯-1-基,2-甲基戊-4-烯-1-基,3-甲基戊-4-烯-1-基,4-甲基戊-4-烯-1-基,1,1-二甲基丁-2-烯-1-基,1,1-二甲基丁-3-烯-1-基,1,2-二甲基丁-1-烯-1-基,1,2-二甲基丁-2-烯-1-基,1,2-二甲基丁-3-烯-1-基,1,3-二甲基丁-1-烯-1-基,1,3-二甲基丁-2-烯-1-基,1,3-二甲基丁-3-烯-1-基,2,2-二甲基丁-3-烯-1-基,2,3-二甲基丁-1-烯-1-基,2,3-二甲基丁-2-烯-1-基,2,3-二甲基丁-3-烯-1-基,3,3-二甲基丁-1-烯-1-基,3,3-二甲基丁-2-烯-1-基,1-乙基丁-1-烯-1-基,1-乙基丁-2-烯-1-基,1-乙基丁-3-烯-1-基,2-乙基丁-1-烯-1-基,2-乙基丁-2-烯-1-基,2-乙基丁-3-烯-1-基,1,1,2-三甲基丙-2-烯-1-基,1-乙基-1-甲基丙-2-烯-1-基,1-乙基-2-甲基丙-1-烯-1-基,1-乙基-2-甲基丙-2-烯-1-基,优选乙烯基或丙-2-烯-1-基;
-C3-C6链炔基:丙-1-炔-1-基,丙-2-炔-3-基,正丁-1-炔-1-基,正丁-1-炔-4-基,正丁-2-炔-1-基,正戊-1-炔-1-基,正戊-1-炔-3-基,正戊-1-炔-4-基,正戊-1-炔-5-基,正戊-2-炔-1-基,正戊-2-炔-4-基,正戊-2-炔-5-基,3-甲基丁-1-炔-1-基,3-甲基丁-1-炔-3-基,3-甲基丁-1-炔-4-基,正己-1-炔-1-基,正己-1-炔-3-基,正己-1-炔-4-基,正己-1-炔-5-基,正己-1-炔-6-基,正己-2-炔-1-基,正己-2-炔-4-基,正己-2-炔-5-基,正己-2-炔-6-基,正己-3-炔-1-基,正己-3-炔-2-基,3-甲基戊-1-炔-1-基,3-甲基戊-1-炔-3-基,3-甲基戊-1-炔-4-基,3-甲基戊-1-炔-5-基,4-甲基戊-1-炔-1-基,4-甲基戊-2-炔-4-基,4-甲基戊-2-炔-5-基,优选丙-2-炔-1-基;
-C1-C2卤代烷基:如氯代甲基,二氯甲基,三氯甲基,氟代甲基,二氟甲基,三氟甲基,氯氟甲基,二氯一氟甲基,一氯二氟甲基,1-氟代乙基,2-氟代乙基,2,2-二氟乙基,2,2,2-三氟乙基,2-氯-2-氟乙基,2-氯-2,2-二氟乙基,2,2-二氯-2-氟乙基,2,2,2-三氯乙基,五氟乙基,优选二氟甲基或三氟甲基;
-C1-C6卤代烷基:被氟,氯和/或溴部分或全部取代的如上所述的C1-C6烷基,例如,如上所述的C1-C2卤代烷基,和3-氯丙基或七氟丙基,优选三氟甲基,五氟乙基或七氟丙基;
-C3-C6卤代链烯基:被氟,氯和/或溴部分或全部取代的如上所述的C3-C6链烯基,如2-氯烯丙基,3-氯烯丙基或3,3-二氯烯丙基;
-C1-C4烷氧基:甲氧基,乙氧基,正丙氧基,1-甲基乙氧基,正丁氧基,1-甲基丙氧基,2-甲基丙氧基,1,1-二甲基乙氧基,优选甲氧基或乙氧基;
-C1-C6烷氧基:如上所述的C1-C4烷氧基,和正戊氧基,1-甲基丁氧基,2-甲基丁氧基,3-甲基丁氧基,2,2-二甲基丙氧基,1-乙基丙氧基,正己氧基,1,1-二甲基丙氧基,1,2-二甲基丙氧基,1-甲基戊氧基,2-甲基戊氧基,3-甲基戊氧基,4-甲基戊氧基,1,1-二甲基丁氧基,1,2-二甲基丁氧基,1,3-二甲基丁氧基,2,2-二甲基丁氧基,2,3-二甲基丁氧基,3,3-二甲基丁氧基,1-乙基丁氧基,2-乙基丁氧基,1,1,2-三甲基丙氧基,1,2,2-三甲基丙氧基,1-乙基-1-甲基丙氧基,1-乙基-2-甲基丙氧基,优选的是如上所述的C1-C4烷氧基;
-C1-C4卤代烷氧基:被氟,氯和/或溴部分或全部取代的上述C1-C4烷氧基,如氯代甲氧基,二氯甲氧基,三氯甲氧基,氟代甲氧基,二氟甲氧基,三氟甲氧基,氯氟甲氧基,二氯一氟甲氧基,一氯二氟甲氧基,1-氟乙氧基,2-氟乙氧基,2,2-二氟乙氧基,2,2,2-三氟乙氧基,2-氯-2-氟乙氧基,2-氯-2,2-二氟乙氧基,2,2-二氯-2-氟乙氧基,2,2,2-三氯乙氧基,戊氟乙氧基,3-氯丙氧基,优选二氟甲氧基,三氟甲氧基,2,2,2-三氟乙氧基或五氟乙氧基;
-在取代基C1-C6烷氧基羰基-C1-C6烷基中的C1-C6烷氧基羰基:甲氧基羰基,乙氧基羰基,正丙氧基羰基,1-甲基乙氧基羰基,正丁氧基羰基,1-甲基丙氧基羰基,2-甲基丙氧基羰基,和1,1-二甲基乙氧基羰基,正戊氧基羰基,1-甲基丁氧基羰基,2-甲基丁氧基羰基,3-甲基丁氧基羰基,2,2-二甲基丙氧基羰基,1-乙基丙氧基羰基,正己氧基羰基,1,1-二甲基丙氧基羰基,1,2-二甲基丙氧基羰基,1-甲基戊氧基羰基,2-甲基戊氧基羰基,3-甲基戊氧基羰基,4-甲基戊氧基羰基,1,1-二甲基丁氧基羰基,1,2-二甲基丁氧基羰基,1,3-二甲基丁氧基羰基,2,2-二甲基丁氧基羰基,2,3-二甲基丁氧基羰基,3,3-二甲基丁氧基羰基,1-乙基丁氧基羰基,2-乙基丁氧基羰基,1,1,2-三甲基丙氧基羰基,1,2,2-三甲基丙氧基碳基,1-乙基-1-甲基丙氧基羰基,1-乙基-2-甲基丙氧基羰基,优选C1-C4烷氧基羰基;C1-C6烷氧基羰基-C1-C6-烷基的实例是乙氧基羰基甲基,叔丁氧基羰基甲基和叔丁氧基羰基丙基;
-C3-C6环烷基:环丙基,环丁基,环戊基,环己基,优选环丙基,环戊基或环己基;
-C3-C6环烷基-C1-C4-烷基:如环丙基甲基,环丁基甲基,环戊基甲基,环己基甲基,2-(环丙基)乙基,2-(环丁基)乙基,2-(环戊基)乙基,2-(环己基)乙基,3-(环丙基)丙基,3-(环丁基)丙基,3-(环戊基)丙基,3-(环己基)丙基,4-(环丙基)丁基,4-(环丁基)丁基,4-(环戊基)丁基,4-(环己基)丁基,优选环丙基甲基或环戊基甲基;
-氰基-C1-C6烷基:如氰基甲基,1-氰基乙-1-基,2-氰基乙-1-基,1-氰基丙-1-基,2-氰基丙-1-基,3-氰基丙-1-基,1-氰基丙-2-基,2-氰基丙-2-基,1-氰基丁-1-基,2-氰基丁-1-基,3-氰基丁-1-基,4-氰基丁-1-基,1-氰基丁-2-基,2-氰基丁-2-基,1-氰基丁-3-基,2-氰基丁-3-基,1-氰基-2-甲基丙-3-基,2-氰基-2-甲基丙-3-基,3-氰基-2-甲基丙-3-基,2-氰基甲基丙-2-基,优选氰基甲基;
-芳基-C1-C6烷基:芳基甲基,1-芳基乙基,2-芳基乙基,1-芳基丙-1-基,2-芳基丙-1-基,3-芳基丙-1-基,1-芳基丁-1-基,2-芳基丁-1-基,3-芳基丁-1-基,4-芳基丁-1-基,1-芳基丁-2-基,2-芳基丁-2-基,3-芳基丁-2-基,3-芳基丁-2-基,4-芳基丁-2-基,1-(芳基甲基)乙-1-基,1-(芳基甲基)-1-(甲基)乙-1-基,1-(芳基甲基)丙-1-基,优选芳基甲基或1-芳基乙基;
-杂芳基-C1-C6烷基:杂芳基甲基,1-(杂芳基)乙基,2-(杂芳基)乙基,1-(杂芳基)丙-1-基,2-(杂芳基)丙-1-基,3-(杂芳基)丙-1-基,1-(杂芳基)丁-1-基,2-(杂芳基)丁-1-基,3-(杂芳基)丁-1-基,4-(杂芳基)丁-1-基,1-(杂芳基)丁-2-基,2-(杂芳基)丁-2-基,3-(杂芳基)丁-2-基,4-(杂芳基)丁-2-基,1-(杂芳基甲基)乙-1-基,1-(杂芳基甲基)-1-(甲基)乙-1-基,1-(杂芳基甲基)丙-1-基,优先杂芳基甲基;
-C1-C4烷硫基:甲硫基,乙硫基,正丙硫基,1-甲基乙硫基,正丁硫基,1-甲基丙硫基,2-甲基丙硫基,1,1-二甲基乙硫基,优选甲硫基或乙硫基;
-C1-C6烷硫基:如上所述的C1-C4烷硫基,和正戊硫基,1-甲基丁硫基,2-甲基丁硫基,3-甲基丁硫基,2,2-二甲基丙硫基,1-乙基丙硫基,正己硫基,1,1-二甲基丙硫基,1,2-二甲基丙硫基,1-甲基戊硫基,2-甲基戊硫基,3-甲基戊硫基,4-甲基戊硫基,1,1-二甲基丁硫基,1,2-二甲基丁硫基,1,3-二甲基丁硫基,2,2-二甲基丁硫基,2,3-二甲基丁硫基,3,3-二甲基丁硫基,1-乙基丁硫基,2-乙基丁硫基,1,1,2-三甲基丙硫基,1,2,2-三甲基丙硫基,1-乙基-1-甲基丙硫基,1-乙基-2-甲基丙硫基,优选上述的C1-C4烷硫基;
-C1-C4烷氧基-C1-C6烷基;甲氧基甲基,乙氧基甲基,正丙氧基甲基,(1-甲基乙氧基)甲基,正丁氧基甲基,(1-甲基丙氧基)甲基,(2-甲基丙氧基)甲基,(1,1-二甲基乙氧基)甲基,2-甲氧基乙基,2-乙氧基乙基,2-(正丙氧基)乙基,2-(1-甲基乙氧基)乙基,2-(正丁氧基)乙基,2-(1-甲基丙氧基)乙基,2-(2-甲基丙氧基)乙基,2-(1,1-二甲基乙氧基)乙基,2-(甲氧基)丙基,3-(甲氧基)丙基,2-(乙氧基)丙基,3-(乙氧基)丙基,3-丙氧基丙基,3-丁氧基丙基,4-(甲氧基)丁基,4-(乙氧基)丁基,4-(正丙氧基)丁基,4-(正丁氧基)丁基,5-(甲氧基)戊基,5-(乙氧基)戊基,5-(正丙氧基)戊基,5-(正丁氧基)戊基,6-(甲氧基)己基,6-(乙氧基)己基,6-(正丙氧基)己基,6-(正丁氧基)己基,优选甲氧基甲基,乙氧基甲基,(1,1-二甲基乙氧基)甲基或2-甲氧基乙基;
-C1-C6烷基氨基;甲氨基,乙氨基,正丙氨基,1-甲基乙氨基,正丁氨基,1-甲基丙氨基,2-甲基丙氨基,1,1-二甲基乙氨基,正戊氨基,1-甲基丁氨基,2-甲基丁氨基,3-甲基丁氨基,2,2-二甲基丙氨基,1-乙基丙氨基,正己氨基,1,1-二甲基丙氨基,1,2-二甲基丙氨基,1-甲基戊氨基,2-甲基戊氨基,3-甲基戊氨基,4-甲基戊氨基,1,1-二甲基丁氨基,1,2-二甲基丁氨基,1,3-二甲基丁氨基,2,2-二甲基丁氨基,2,3-二甲基丁氨基,3,3-二甲基丁氨基,1-乙基丁氨基,2-乙基丁氨基,1,1,2-三甲基丙氨基,1,2,2-三甲基丙氨基,1-乙基-1-甲基丙氨基,1-乙基-2-甲基丙氨基,优选的是C1-C4烷基氨基如甲氨基,乙氨基,正丙氨基和正丁氨基;
-二(C1-C6烷基)氨基:如N,N-二甲基氨基,N,N-二乙基氨基,N,N-二丙基氨基,N,N-二(1-甲基乙基)氨基,N,N-二丁基氨基,N,N-二(1-甲基丙基)氨基,N,N-二(2-甲基丙基)氨基,N,N-二(1,1-二甲基乙基)氨基,N-乙基-N-甲基氨基,N-甲基-N-丙基氨基,N-甲基-N-(1-甲基乙基)氨基,N-丁基-N-甲基氨基,N-甲基-N-(1-甲基丙基)氨基,N-甲基-N-(2-甲基丙基)氨基,N-(1,1-二甲基乙基)-N-甲基氨基,N-乙基-N-丙基氨基,N-乙基-N-(1-甲基乙基)氨基,N-丁基-N-乙基氨基,N-乙基-N-(1-甲基丙基)氨基,N-乙基-N-(2-甲基丙基)氨基,N-乙基-N-(1,1-二甲基乙基)氨基,N-(1-甲基乙基)-N-丙基氨基,N-丁基-N-丙基氨基,N-(1-甲基丙基)-N-丙基氨基,N-(2-甲基丙基)-N-丙基氨基,N-(1,1-二甲基乙基)-N-丙基氨基,N-丁基-N-(1-甲基乙基)氨基,N-(1-甲基乙基)-N-(1-甲基丙基)氨基,N-(1-甲基乙基)-N-(2-甲基丙基)氨基,N-(1,1-二甲基乙基)-N-(1-甲基乙基)氨基,N-丁基-N-(1-甲基丙基)氨基,N-丁基-N-(2-甲基丙基)氨基,N-丁基-N-(1,1-二甲基乙基)氨基,N-(1-甲基丙基)-N-(2-甲基丙基)氨基,N-(1,1-二甲基乙基)-N-(1-甲基丙基)氨基,N-(1,1-二甲基乙基)-N-(2-甲基丙基)氨基,优选的是二-(C1-C4烷基)氨基如N,N-二甲基氨基和N,N-二乙基氨基;
-C3-C6链烯氧基;丙-2-烯-1-基氧基,正丁烯-2-基氧基,正丁烯-3-基氧基,1-甲基丙-2-烯-1-基氧基,2-甲基丙-2-烯-1-基氧基,正戊烯-2-基氧基,正戊烯-3-基氧基,正戊烯-4-基氧基,1-甲基丁-2-烯-1-基氧基,2-甲基丁-2-烯-1-基氧基,3-甲基-丁-2-烯基-1-基氧基,1-甲基丁-3-烯-1-基氧基,2-甲基丁-3-烯-1-基氧基,3-甲基丁-3-烯-1-基氧基,1,1-二甲基丙-2-烯-1-基氧基,1,2-二甲基丙-2-烯-1-基氧基,1-乙基丙-2-烯-1-基氧基,正己-2-烯-1-基氧基,正己-3-烯-1-基氧基,正己-4-烯-1-基氧基,正己-5-烯-1-基氧基,3-甲基戊-1-烯-1-基氧基,4-甲基戊-1-烯-1-基氧基,1-甲基戊-2-烯-1-基氧基,2-甲基戊-2-烯-1-基氧基,3-甲基戊-2-烯-1-基氧基,4-甲基戊-2-烯-1-基氧基,1-甲基戊-3-烯-1-基氧基,2-甲基戊-3-烯-1-基氧基,3-甲基戊-3-烯-1-基氧基,4-甲基戊-3-烯-1-基氧基,1-甲基戊-4-烯-1-基氧基,2-甲基戊-4-烯-1-基氧基,3-甲基戊-4-烯-1-基氧基,4-甲基戊-4-烯-1-基氧基,1,1-二甲基丁-2-烯-1-基氧基,1,1-二甲基丁-3-烯-1-基氧基,1,2-二甲基丁-2-烯-1-基氧基,1,2-二甲基丁-3-烯-1-基氧基,1,3-二甲基丁-2-烯-1-基氧基,1,3-二甲基丁-3-烯-1-基氧基,2,2-二甲基丁-3-烯-1-基氧基,2,3-二甲基丁-2-烯-1-基氧基,2,3-二甲基丁-3-烯-1-基氧基,3,3-二甲基丁-2-烯-1-基氧基,1-乙基丁-2-烯-1-基氧基,1-乙基丁-3-烯-1-基氧基,2-乙基丁-2-烯-1-基氧基,2-乙基丁-3-烯-1-基氧基,1,1,2-三甲基丙-2-烯-1-基氧基,1-乙基-1-甲基丙-2-烯-1-基氧基,1-乙基-2-甲基丙-1-烯-1-基氧基,1-乙基-2-甲基丙-2-烯-1-基氧基,优选的是丙-2-烯-1-基氧基;
-C3-C6链炔氧基:丙-2-炔-3-基氧基,正丁-1-炔-4-基氧基,正丁-2-炔-1-基氧基,正戊-1-炔-3-基氧基,正戊-1-炔-4-基氧基,正戊-1-炔-5-基氧基,正戊-2-炔-1-基氧基,正戊-2-炔-4-基氧基,正戊-2-炔-5-基氧基,3-甲基丁-1-炔-3-基氧基,3-甲基丁-1-炔-4-基氧基,正己-1-炔-3-基氧基,正己-1-炔-4-基氧基,正己-1-炔-5-基氧基,正己-1-炔-6-基氧基,正己-2-炔-1-基氧基,正己-2-炔-4-基氧基,正己-2-炔-5-基氧基,正己-2-炔-6-基氧基,正己-3-炔-1-基氧基,正己-3-炔-2-基氧基,3-甲基戊-1-炔-3-基氧基,3-甲基戊-1-炔-4-基氧基,3-甲基戊-1-炔-5-基氧基,4-甲基戊-2-炔-4-基氧基,4-甲基戊-2-炔-5-基氧基,优选的是丙-2-炔-1-基氧基;
-芳氧基-C1-C6烷基;芳氧基甲基,1-(芳氧基)乙基,2-(芳氧基)乙基,1-(芳氧基)丙-1-基,2-(芳氧基)丙-1-基,3-(芳氧基)丙-1-基,1-(芳氧基)丁-1-基,2-(芳氧基)丁-1-基,3-(芳氧基)丁-1-基,4-(芳氧基)丁-1-基,1-(芳氧基)丁-2-基,2-(芳氧基)丁-2-基,3-(芳氧基)丁-2-基,4-(芳氧基)丁-2-基,1-(芳氧基甲基)乙-1-基,1-(芳氧基甲基)-1-(甲基)乙-1-基,1-(芳氧基甲基)丙-1-基,优选的是芳氧基甲基和1-(芳氧基)乙基;
-芳基-C3-C6链烯基:如3-芳基烯丙基,4-芳基丁-2-烯基,4-芳基丁-3-烯基,5-芳基戊-4-烯基,优选的是3-芳基烯丙基或4-芳基丁-2-烯基;
-饱和或未饱和的4元至6元杂环-C1-C4烷基:(杂环基)甲基,1-(杂环基)乙基,2-(杂环基)乙基,1-(杂环基)丙-1-基,2-(杂环基)丙-1-基,3-(杂环基)丙-1-基,1-(杂环基)丁-1-基,2-(杂环基)丁-1-基,3-(杂环基)丁-1-基,4-(杂环基)丁-1-基,1-(杂环基)丁-2-基,2-(杂环基)丁-2-基,3-(杂环基)丁-2-基,3-(杂环基)丁-2-基,4-(杂环基)丁-2-基,1-[(杂环基)甲基]乙-1-基,1-[(杂环基)甲基]环基)丁-2-基,1-[(杂环基)甲基]乙-1-基,1-[(杂环基)甲基]1-(甲基)乙-1-基,1-[(杂环基)甲基]丙-1-基,优选的是(杂环基)甲基和1-(杂环基)乙基。
芳基优选的是苯基或萘基,特别是苯基;
芳氧基优选的是苯氧基,1-萘氧基或2-萘氧基,特别是苯氧基;
芳硫基优选的是苯硫基,1-萘硫基或2-萘硫基,特别是苯硫基;
杂芳基优选的是含有氧原子和硫原子的5元或6元芳族杂环或含有1个或2个下述杂原子的5元或6元芳族杂环:2个氮原子和1个氧原子或硫原子:如2-呋喃基,3-呋喃基,2-噻吩基,3-噻吩基,2-吡咯基,3-吡咯基,3-异噁唑基,4-异噁唑基,5-噁唑基,3-异噻唑基,4-异噻唑基,5-异噻唑基,3-吡唑基,4-吡唑基,5-吡唑基,2-噁唑基,4-噁唑基,5-噁唑基,2-噻唑基,4-噻唑基,5-噻唑基,2-咪唑基,4-咪唑基,1,2,4-噁二唑-3-基,1,2,4-噁二唑-5-基,1,2,4-噻二唑-3-基,1,2,4-噻二唑-5-基,1,2,4-三唑-3-基,1,3,4-噁二唑-2-基,1,3,4-噻二唑-2-基,1,3,4-三唑-2-基,2-吡啶基,3-吡啶基,4-吡啶基,3-哒嗪基,4-哒嗪基,2-嘧啶基,4-嘧啶基,5-嘧啶基,2-吡嗪基,1,3,5-三嗪-2-基和1,2,4-三嗪-3基,特别是吡啶基,嘧啶基,呋喃基和噻吩基。
饱和或不饱和4元至6元杂环除含C原子外还包含选自一个氧或硫原子、一或二个氮原子及一或二个-N(CH3)-基团的一个或二个环成员,这些杂环中特别优选的是;氧杂环丁基、四氢呋喃基、四氢噻吩基、吡咯烷基、异噁唑烷基、异噻唑烷基、吡唑烷基、噁唑烷基、噻唑烷基、咪唑烷基、1,2,4-噁二唑烷基、1,3,4-噁二唑烷基、1,2,4-噻二唑烷基、1,3,4-噻二唑烷基、1,2,4-三唑烷基、1,3,4-三唑烷基、2,3-二氢呋喃基、2,4-二氢呋喃基、2,3-二氢噻吩基、2,4-二氢噻吩基、2,3-吡咯啉基、2,4-吡咯啉基、2,3-异噁唑啉基、3,4-异噁唑啉基、4,5-异噁唑啉基、2,3-异噻唑啉基、3,4-异噻唑啉基、4,5-异噻唑啉基、2,3-二氢吡唑基、3,4-二氢吡唑基、4,5-二氢吡唑基、2,3-二氢噁唑基、 3,4-二氢噁唑基、噻唑基、咪唑基、1,2,4-噁二唑基、1,3,4-噁二唑基、1,2,4-噻二唑基、1,3,4-噻二唑基、1,2,4-三唑基和1,3,4-三唑基、1,3-二氧杂环戊基、哌啶基、四氢哒嗪基、四氢嘧啶基、四氢吡嗪基、1,3,5-四氢三嗪基和1,2,4-四氢三嗪基。
如果需要的话,芳环和所有的饱和、不饱和或芳杂环的每一个可取代的C原子上可包含下述基团之一:-卤原子,优选氟或氯原子;-C1-C4烷基,优选甲基;-C1或C2卤代烷基,优选三氟甲基;-C3-C6环烷基,优选环丙基;-C1-C4烷氧基,优选甲氧基;-C1或C2卤代烷氧基,优选二氟甲氧基。
芳环和杂环优选未被取代或含1-3个上述基团。
当n为2、3或4时,两个相邻的R5可一起形成稠合的1,3-丁二烯-1,4-二基桥或者单一或二卤代的1,3-丁二烯-1,4-二基桥,其中特别优选的卤原子为氟、氯和溴原子。
基团-C(R4)=N-O-R1相对于1位的桥-O-CH2-可在苯基的2位上,或优选在3或4位上。
在X为=CH-OCH3的化合物I中,特别优选基团如下的那些化合物;其中,Y为氧原子,R1为C1-C6烷基、C2-C6链烯基、C3-C6链炔基、C1-C6卤代烷基或C3-C6卤代烯基;R2为氰基、氯原子、氟原子、甲基、三氟甲基或甲氧基;R3为氢原子、氰基、氯原子、氟原子、甲基或甲氧基;R4为氰基、氯原子、溴原子、C1-C6烷氧基、C1-C6烷硫基、C3-C6链烯氧基、苯氧基或苯硫基;R5为氰基、卤原子、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或苯基。
在X为=CH-CH3的化合物I中,特别优选基团如下的那些化合物,其中,Y为氧原子,R1为C1-C6烷基、C2-C6链烯基、C3-C6链炔基、C1-C6卤代烷基或C3-C6卤代烯基;R2为氰基、氯原子、氟原子、甲基、三氟甲基或甲氧基;R3是氢、氰基、氯、氟、甲基或甲氧基;R4是氰基、氯、溴、C1-C6烷氧基、C1-C6烷硫基、C3-C6链烯氧基、苯氧基或苯硫基和R5是氰基、卤素、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或苯基。
在X为=N-OCH3的化合物I中,特别优选基团如下的那些化合物,其中Y为氧原子或-NH-,R1为C1-C6烷基、C2-C6链烯基、C3-C6链炔基、C1-C6卤代烷基或C3-C6卤代烯基;R2为氰基、氯原子、氟原子、甲基、三氟甲基或甲氧基;R3为氢原子、氰基、氯原子、氟原子、甲基或甲氧基;R4为氰基、氯原子、溴原子、C1-C6烷氧基、C1-C6烷硫基、C3-C6链烯氧基、苯氧基或苯硫基;R5为氰基、卤原子、C1-C6烷基、C1-C6卤代烷基、C1-C6烷氧基或苯基。
就中间体IVb′和XI′而言,各基团的定义优选其在化合物I中被优选的定义。
在制备过程中,可以得到作为关于C=X键的E/Z异构体混合物的式I、IVb′和XI′的新化合物及关于(R1O)N=C(R4)键的E/Z异构体混合物的化合物I。如果需要的话,可以按常规方法如结晶法或色谱法将异构体混合物分离成基本纯的异构体。
纯异构体和各种异构体的混合物均属于本发明保护范围之列,它们均可用作杀真菌剂或杀虫剂。
特别优选的化合物I是C=X基团为E构型即-CO-Y-R6与基团-OCH3或-CH3为反式的那些化合物。
这种结构类型的代表为化合物D.0001-D.1958,它们可被表A中相应的化合物A.0001-A.1958取代。-式I-4化合物:
这种结构类型的代表为化合物E.0001-E.1958,它们可被表A中相应的化合物A.0001-A.1958取代-式I-5化合物;
这种结构类型的代表为表B列出的化合物B.001-B.544。-式I-6化合物
这种结构类型的代表为化合物F.001-F.544,它们可被表B的相应化合物B.001-B.544取代。-式I-7化合物:
这种结构类型的代表为化合物H.001-H.544,它们可被表B的相应化合物B.001-B.544取代。表A
Table B
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0001 | 甲基 | 2-CH3 | H | OCH3 | H |
| A.0002 | 甲基 | 2-CH3 | H | OCH3 | 3-Cl |
| A.0003 | 甲基 | 2-CH3 | H | OCH3 | 4-Cl |
| A.0004 | 甲基 | 2-CH3 | H | OCH3 | 6-Cl |
| A.0005 | 甲基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| A.0006 | 甲基 | 2-CH3 | H | OCH3 | 4-OCH3 |
| A.0007 | 甲基 | 2-CH3 | H | OCH3 | 3-CF3 |
| A.0008 | 甲基 | 2-CH3 | H | OCH3 | 6-CH3 |
| A.0009 | 甲基 | 2-CH3 | H | OCH3 | 6-C6H5 |
| A.0010 | 乙基 | 2-CH3 | H | OCH3 | H |
| A.0011 | 正丙基 | 2-CH3 | H | 0CH3 | H |
| A.0012 | 异丙基 | 2-CH3 | H | OCH3 | H |
| A.0013 | 正丁基 | 2-CH3 | H | OCH3 | H |
| A.0014 | 异丁基 | 2-CH3 | H | OCH3 | H |
| A.0015 | 仲丁基 | 2-CH3 | H | OCH3 | H |
| A.0016 | 叔丁基 | 2-CH3 | H | OCH3 | H |
| A.0017 | 正戊基 | 2-CH3 | H | OCH3 | H |
| A.0018 | 正己基 | 2-CH3 | H | OCH3 | H |
| A.0019 | 2-丙烯基 | 2-CH3 | H | OCH3 | H |
| A.0020 | 2-丙烯基 | 2-CH3 | H | OCH3 | 3-Cl |
| A.0021 | 2-丙烯基 | 2-CH3 | H | OCH3 | 4-Cl |
| A.0022 | 2-丙烯基 | 2-CH3 | H | OCH3 | 6-Cl |
| A.0023 | 2-丙烯基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| A.0024 | 2-丙烯基 | 2-CH3 | H | OCH3 | 4-OCH3 |
| A.0025 | 2-丙烯基 | 2-CH3 | H | OCH3 | 3-CF3 |
| A.0026 | 2-丙烯基 | 2-CH3 | H | OCH3 | 6-CH3 |
| A.0027 | 2-丙烯基 | 2-CH3 | H | OCH3 | 6-C6H5 |
| A.0028 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | OCH3 | H |
| A.0029 | 2-氯-2-丙烯基 | 2-CH3 | H | OCH3 | H |
| A.0030 | (E)-2-丁烯基 | 2-CH3 | H | OCH3 | H |
| A.0031 | 2-甲基-2-丙烯基 | 2-CH3 | H | OCH3 | H |
| A.0032 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | OCH3 | H |
| A.0033 | 3-甲基-2-丁烯基 | 2-CH3 | H | OCH3 | H |
| A.0034 | 2-丙炔基 | 2-CH3 | H | OCH3 | H |
| A.0035 | 2-丙炔基 | 2-CH3 | H | OCH3 | 3-Cl |
| A.0036 | 2-丙炔基 | 2-CH3 | H | OCH3 | 4-Cl |
| A.0037 | 2-丙炔基 | 2-CH3 | H | OCH3 | 6-Cl |
| A.0038 | 2-丙炔基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| A.0039 | 2-丙炔基 | 2-CH3 | H | OCH3 | 4-OCH3 |
| A.0040 | 2-丙炔基 | 2-CH3 | H | OCH3 | 3-CF3 |
| A.0041 | 2-丙炔基 | 2-CH3 | H | OCH3 | 6-CH3 |
| A.0042 | 2-丙炔基 | 2-CH3 | H | OCH3 | 6-C6H5 |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0043 | 2-丁炔基 | 2-CH3 | H | OCH3 | H |
| A.0044 | 3-丁炔-2-基 | 2-CH3 | H | OCH3 | H |
| A.0045 | 氰基甲基 | 2-CH3 | H | OCH3 | H |
| A.0046 | 甲氧基羰基甲基 | 2-CH3 | H | OCH3 | H |
| A.0047 | 叔丁氧基羰基甲基 | 2-CH3 | H | OCH3 | H |
| A.0048 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OCH3 | H |
| A.0049 | 环丙基甲基 | 2-CH3 | H | OCH3 | H |
| A.0050 | 1-甲基环戊基 | 2-CH3 | H | OCH3 | H |
| A.0051 | 环己基 | 2-CH3 | H | OCH3 | H |
| A.0052 | 1-甲氧基丙-2-基 | 2-CH3 | H | OCH3 | H |
| A.0053 | 苄基 | 2-CH3 | H | OCH3 | H |
| A.0054 | 苄基 | 2-CH3 | H | OCH3 | 3-Cl |
| A.0055 | 苄基 | 2-CH3 | H | OCH3 | 4-Cl |
| A.0056 | 苄基 | 2-CH3 | H | OCH3 | 6-Cl |
| A.0057 | 苄基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| A.0058 | 苄基 | 2-CH3 | H | OCH3 | 4-OCH3 |
| A.0059 | 苄基 | 2-CH3 | H | OCH3 | 3-CF3 |
| A.0060 | 苄基 | 2-CH3 | H | OCH3 | 6-CH3 |
| A.0061 | 苄基 | 2-CH3 | H | OCH3 | 6-C6H5 |
| A.0062 | 3-甲基苄基 | 2-CH3 | H | OCH3 | H |
| A.0063 | 2-氟苄基 | 2-CH3 | H | OCH3 | H |
| A.0064 | 3-氟苄基 | 2-CH3 | H | OCH3 | H |
| A.0065 | 4-氯苄基 | 2-CH3 | H | OCH3 | H |
| A.0066 | 3,4-二氯苄基 | 2-CH3 | H | OCH3 | H |
| A.0067 | 2,6-二氟苄基 | 2-CH3 | H | OCH3 | H |
| A.0068 | 3-三氟甲基苄基 | 2-CH3 | H | OCH3 | H |
| A.0069 | 3-氰基苄基 | 2-CH3 | H | OCH3 | H |
| A.0070 | 4-甲氧基苄基 | 2-CH3 | H | OCH3 | H |
| A.0071 | 4-甲氧基羰基苄基 | 2-CH3 | H | OCH3 | H |
| A.0072 | 3-苯基苄基 | 2-CH3 | H | OCH3 | H |
| A.0073 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | OCH3 | H |
| A.0074 | (2.5-二氯-3-噻吩基)甲基 | 2-CH3 | H | OCH3 | H |
| A.0075 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | OCH3 | H |
| A.0076 | 1-苯基乙基 | 2-CH3 | H | OCH3 | H |
| A.0077 | 1-(4-甲苯基)乙基 | 2-CH3 | H | OCH3 | H |
| A.0078 | 1-(4-氯苯基)乙基 | 2-CH3 | H | OCH3 | H |
| A.0079 | 1(3-三氟甲基苯基)乙基 | 2-CH3 | H | OCH3 | H |
| A.0080 | 2-苯基乙基 | 2-CH3 | H | OCH3 | H |
| A.0081 | 3-苯基丙-1-基 | 2-CH3 | H | OCH3 | H |
| A.0082 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | OCH3 | H |
| A.0083 | 甲基 | 2-CH3 | H | OC2H5 | H |
| A.0084 | 甲基 | 2-CH3 | H | OC2H5 | 3-Cl |
| A.0085 | 甲基 | 2-CH3 | H | OC2H5 | 4-Cl |
| A.0086 | 甲基 | 2-CH3 | H | OC2H5 | 6-Cl |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0087 | 甲基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| A.0088 | 甲基 | 2-CH3 | H | OC2H5 | 4-OCH3 |
| A.0089 | 甲基 | 2-CH3 | H | OC2H5 | 3-CF3 |
| A.0090 | 甲基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| A.0091 | 甲基 | 2-CH3 | H | OC2H5 | 6-C6H5 |
| A.0092 | 乙基 | 2-CH3 | H | OC2H5 | H |
| A.0093 | 正丙基 | 2-CH3 | H | OC2H5 | H |
| A.0094 | 异丙基 | 2-CH3 | H | OC2H5 | H |
| A.0095 | 正丁基 | 2-CH3 | H | OC2H5 | H |
| A.0096 | 异丁基 | 2-CH3 | H | OC2H5 | H |
| A.0097 | 仲丁基 | 2-CH3 | H | OC2H5 | H |
| A.0098 | 叔丁基 | 2-CH3 | H | OC2H5 | H |
| A.0099 | 正戊基 | 2-CH3 | H | OC2H5 | H |
| A.0100 | 正己基 | 2-CH3 | H | OC2H5 | H |
| A.0101 | 2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| A.0102 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 3-Cl |
| A.0103 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 6-Cl |
| A.0104 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 6-Cl |
| A.0105 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| A.0106 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 4-OCH3 |
| A.0107 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 3-CF3 |
| A.0108 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| A.0109 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 6-C6H5 |
| A.0110 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| A.0111 | 2-氯-2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| A.0112 | (E)-2-丁烯基 | 2-CH3 | H | OC2H5 | H |
| A.0113 | 2-甲基-2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| A.0114 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | OC2H5 | H |
| A.0115 | 3-甲基-2-丁烯基 | 2-CH3 | H | OC2H5 | H |
| A.0116 | 2-丙炔基 | 2-CH3 | H | OC2H5 | H |
| A.0117 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 3-Cl |
| A.0118 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 4-Cl |
| A.0119 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 6-Cl |
| A.0120 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| A.0121 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 4-OCH3 |
| A.0122 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 3-CF3 |
| A.0123 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| A.0124 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 6-C6H5 |
| A.0125 | 2-丁炔基 | 2-CH3 | H | OC2H5 | H |
| A.0126 | 3-丁炔-2-基 | 2-CH3 | H | OC2H5 | H |
| A.0127 | 氰基甲基 | 2-CH3 | H | OC2H5 | H |
| A.0128 | 甲氧基羰基甲基 | 2-CH3 | H | OC2H5 | H |
| A.0129 | 叔丁氧基羰基甲基 | 2-CH3 | H | OC2H5 | H |
| A.0130 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OC2H5 | H |
| NO. | R1 | R2 | R3 | R4 | R5 n |
| A.0131 | 环丙基甲基 | 2-CH3 | H | OC2H5 | H |
| A.0132 | 1-甲基环戊基 | 2-CH3 | H | OC2H5 | H |
| A.0133 | 环己基 | 2-CH3 | H | OC2H5 | H |
| A.0134 | 1-甲氧基丙-2-基 | 2-CH3 | H | OC2H5 | H |
| A.0135 | 苄基 | 2-CH3 | H | OC2H5 | H |
| A.0136 | 苄基 | 2-CH3 | H | OC2H5 | 3-Cl |
| A.0137 | 苄基 | 2-CH3 | H | OC2H5 | 4-Cl |
| A.0138 | 苄基 | 2-CH3 | H | OC2H5 | 6-Cl |
| A.0139 | 苄基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| A.0140 | 苄基 | 2-CH3 | H | OC2H5 | 4-OCH3 |
| A.0141 | 苄基 | 2-CH3 | H | OC2H5 | 3-CF3 |
| A.0142 | 苄基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| A.0143 | 苄基 | 2-CH3 | H | OC2H5 | 6-C6H5 |
| A.0144 | 3-甲基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0145 | 2-氟苄基 | 2-CH3 | H | OC2H5 | H |
| A.0146 | 3-氟苄基 | 2-CH3 | H | OC2H5 | H |
| A.0147 | 4-氯苄基 | 2-CH3 | H | OC2H5 | H |
| A.0148 | 3,4-二氯苄基 | 2-CH3 | H | OC2H5 | H |
| A.0149 | 2,6-二氟苄基 | 2-CH3 | H | OC2H5 | H |
| A.0150 | 3-三氟甲基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0151 | 3-氰基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0152 | 4-甲氧基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0153 | 4-甲氧基羰基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0154 | 3-苯基苄基 | 2-CH3 | H | OC2H5 | H |
| A.0155 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | OC2H5 | H |
| A.0156 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | OC2H5 | H |
| A.0157 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | OC2H5 | H |
| A.0158 | 1-苯基乙基 | 2-CH3 | H | OC2H5 | H |
| A.0159 | 1-(4-甲苯基)乙基 | 2-CH3 | H | OC2H5 | H |
| A.0160 | 1-(4-氯苯基)乙基 | 2-CH3 | H | OC2H5 | H |
| A.0161 | 1-(3-三氟甲基苯基)乙基 | 2-CH3 | H | OC2H5 | H |
| A.0162 | 2-苯基乙基 | 2-CH3 | H | OC2H5 | H |
| A.0163 | 3-苯基丙-1-基 | 2-CH3 | H | OC2H5 | H |
| A.0164 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | OC2H5 | H |
| A.0165 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0166 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 3-Cl |
| A.0167 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 4-Cl |
| A.0168 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 6-Cl |
| A.0169 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 3-OCH3 |
| A.0170 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 4-OCH3 |
| A.0171 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 3-CF3 |
| A.0172 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 6-CH3 |
| A.0173 | 甲基 | 2-CH3 | H | OCH2CH=CH2 | 6-C6H5 |
| A.0174 | 乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0175 | 正丙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0176 | 异丙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0177 | 正丁基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0178 | 异丁基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0179 | 仲丁基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0180 | 叔丁基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0181 | 正戊基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0182 | 正己基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0183 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0184 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 3-Cl |
| A.0185 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 4-Cl |
| A.0186 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 6-Cl |
| A.0187 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 3-OCH3 |
| A.0188 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 4-OCH3 |
| A.0189 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 3-CF3 |
| A.0190 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 6-CH3 |
| A.0191 | 2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | 6-C6H5 |
| A.0192 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0193 | 2-氯-2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0194 | (E)-2-丁烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0195 | 2-甲基-2-丙烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0196 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0197 | 3-甲基-2-丁烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0198 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0199 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 3-Cl |
| A.0200 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 4-Cl |
| A.0201 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 6-Cl |
| A.0202 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 3-OCH3 |
| A.0203 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 4-OCH3 |
| A.0204 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 3-CF3 |
| A.0205 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 6-CH3 |
| A.0206 | 2-丙炔基 | 2-CH3 | H | OCH2CH=CH2 | 6-C6H5 |
| A.0207 | 2-丁炔基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0208 | 3-丁炔-2-基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0209 | 氰基甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0210 | 甲氧基羰基甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0211 | 叔丁氧基羰基甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0212 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0213 | 环丙基甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0214 | 1-甲基环戊基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0215 | 环己基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0216 | 1-甲氧基丙-2-基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0217 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0218 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 3-Cl |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0219 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 4-Cl |
| A.0220 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 6-Cl |
| A.0221 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 3-OCH3 |
| A.0222 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 4-OCH3 |
| A.0223 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 3-CF3 |
| A.0224 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 6-CH3 |
| A.0225 | 苄基 | 2-CH3 | H | OCH2CH=CH2 | 6-C6H5 |
| A.0226 | 3-甲基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0227 | 2-氟苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0228 | 3-氟苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0229 | 4-氯苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0230 | 3,4-二氯苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0231 | 2,6-二氟苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0232 | 3-三氟甲基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0233 | 3-氰基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0234 | 4-甲氧基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0235 | 4-甲氧基羰基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0236 | 3-苯基苄基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0237 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0238 | (1,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0239 | 1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0240 | 1-苯基乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0241 | 1-(4-甲基苯基)乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0242 | 1-(4-氯苯基)乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0243 | 1-(3-三氟甲基苯基)乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0244 | 2-苯基乙基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0245 | 3-苯基丙-1-基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0246 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | OCH2CH=CH2 | H |
| A.0247 | 甲基 | 2-CH3 | H | SCH3 | H |
| A.0248 | 甲基 | 2-CH3 | H | SCH3 | 3-Cl |
| A.0249 | 甲基 | 2-CH3 | H | SCH3 | 4-Cl |
| A.0250 | 甲基 | 2-CH3 | H | SCH3 | 6-Cl |
| A.0251 | 甲基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| A.0252 | 甲基 | 2-CH3 | H | SCH3 | 4-OCH3 |
| A.0253 | 甲基 | 2-CH3 | H | SCH3 | 3-CF3 |
| A.0254 | 甲基 | 2-CH3 | H | SCH3 | 6-CH3 |
| A.0255 | 甲基 | 2-CH3 | H | SCH3 | 6-C6H5 |
| A.0256 | 乙基 | 2-CH3 | H | SCH3 | H |
| A.0257 | 正丙基 | 2-CH3 | H | SCH3 | H |
| A.0258 | 异丙基 | 2-CH3 | H | SCH3 | H |
| A.0259 | 正丁基 | 2-CH3 | H | SCH3 | H |
| A.0260 | 异丁基 | 2-CH3 | H | SCH3 | H |
| A.0261 | 仲丁基 | 2-CH3 | H | SCH3 | H |
| A.0262 | 叔丁基 | 2-CH3 | H | SCH3 | H |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0263 | 正戊基 | 2-CH3 | H | SCH3 | H |
| A.0264 | 正己基 | 2-CH3 | H | SCH3 | H |
| A.0265 | 2-丙烯基 | 2-CH3 | H | SCH3 | H |
| A.0266 | 2-丙烯基 | 2-CH3 | H | SCH3 | 3-Cl |
| A.0267 | 2-丙烯基 | 2-CH3 | H | SCH3 | 4-Cl |
| A.0268 | 2-丙烯基 | 2-CH3 | H | SCH3 | 6-Cl |
| A.0269 | 2-丙烯基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| A.0270 | 2-丙烯基 | 2-CH3 | H | SCH3 | 4-OCH3 |
| A.0271 | 2-丙烯基 | 2-CH3 | H | SCH3 | 3-CF3 |
| A.0272 | 2-丙烯基 | 2-CH3 | H | SCH3 | 6-CH3 |
| A.0273 | 2-丙烯基 | 2-CH3 | H | SCH3 | 6-C6H5 |
| A.0274 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | SCH3 | H |
| A.0275 | 2-氯-2-丙烯基 | 2-CH3 | H | SCH3 | H |
| A.0276 | (E)-2-丁烯基 | 2-CH3 | H | SCH3 | H |
| A.0277 | 2-甲基-2-丙烯基 | 2-CH3 | H | SCH3 | H |
| A.0278 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | SCH3 | H |
| A.0279 | 3-甲基-2-丁烯基 | 2-CH3 | H | SCH3 | H |
| A.0280 | 2-丙炔基 | 2-CH3 | H | SCH3 | H |
| A.0281 | 2-丙炔基 | 2-CH3 | H | SCH3 | 3-Cl |
| A.0282 | 2-丙炔基 | 2-CH3 | H | SCH3 | 4-Cl |
| A.0283 | 2-丙炔基 | 2-CH3 | H | SCH3 | 6-Cl |
| A.0284 | 2-丙炔基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| A.0285 | 2-丙炔基 | 2-CH3 | H | SCH3 | 4-OCH3 |
| A.0286 | 2-丙炔基 | 2-CH3 | H | SCH3 | 3-CF3 |
| A.0287 | 2-丙炔基 | 2-CH3 | H | SCH3 | 6-CH3 |
| A.0288 | 2-丙炔基 | 2-CH3 | H | SCH3 | 6-C6H5 |
| A.0289 | 2-丁炔基 | 2-CH3 | H | SCH3 | H |
| A.0290 | 3-丁炔-2-基 | 2-CH3 | H | SCH3 | H |
| A.0291 | 氰基甲基 | 2-CH3 | H | SCH3 | H |
| A.0292 | 甲氧基羰基甲基 | 2-CH3 | H | SCH3 | H |
| A.0293 | 叔丁氧基羰基甲基 | 2-CH3 | H | SCH3 | H |
| A.0294 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | SCH3 | H |
| A.0295 | 环丙基甲基 | 2-CH3 | H | SCH3 | H |
| A.0296 | 1-甲基环戊基 | 2-CH3 | H | SCH3 | H |
| A.0297 | 环己基 | 2-CH3 | H | SCH3 | H |
| A.0298 | 1-甲氧基丙-2-基 | 2-CH3 | H | SCH3 | H |
| A.0299 | 苄基 | 2-CH3 | H | SCH3 | H |
| A.0300 | 苄基 | 2-CH3 | H | SCH3 | 3-Cl |
| A.0301 | 苄基 | 2-CH3 | H | SCH3 | 4-Cl |
| A.0302 | 苄基 | 2-CH3 | H | SCH3 | 6-Cl |
| A.0303 | 苄基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| A.0304 | 苄基 | 2-CH3 | H | SCH3 | 4-OCH3 |
| A.0305 | 苄基 | 2-CH3 | H | SCH3 | 3-CF3 |
| A.0306 | 苄基 | 2-CH3 | H | SCH3 | 6-CH3 |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0307 | 苄基 | 2-CH3 | H | SCH3 | 6-C6H5 |
| A.0308 | 3-甲基苄基 | 2-CH3 | H | SCH3 | H |
| A.0309 | 2-氟苄基 | 2-CH3 | H | SCH3 | H |
| A.0310 | 3-氟苄基 | 2-CH3 | H | SCH3 | H |
| A.0311 | 4-氯苄基 | 2-CH3 | H | SCH3 | H |
| A.0312 | 3,4-二氯苄基 | 2-CH3 | H | SCH3 | H |
| A.0313 | 2,6-二氟苄基 | 2-CH3 | H | SCH3 | H |
| A.0314 | 3-三氟甲基苄基 | 2-CH3 | H | SCH3 | H |
| A.0315 | 3-氰基苄基 | 2-CH3 | H | SCH3 | H |
| A.0316 | 4-甲氧基苄基 | 2-CH3 | H | SCH3 | H |
| A.0317 | 4-甲氧基羰基苄基 | 2-CH3 | H | SCH3 | H |
| A.0318 | 3-苯基苄基 | 2-CH3 | H | SCH3 | H |
| A.0319 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | SCH3 | H |
| A.0320 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | SCH3 | H |
| A.0321 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | SCH3 | H |
| A.0322 | 1-苯乙基 | 2-CH3 | H | SCH3 | H |
| A.0323 | 1-(4-甲苯基)乙基 | 2-CH3 | H | SCH3 | H |
| A.0324 | 1-(4-氯苯基)乙基 | 2-CH3 | H | SCH3 | H |
| A.0325 | 1-(3-三氟甲基苯基)乙基 | 2-CH3 | H | SCH3 | H |
| A.0326 | 2-苯基乙基 | 2-CH3 | H | SCH3 | H |
| A.0327 | 3-苯基丙-1-基 | 2-CH3 | H | SCH3 | H |
| A.0328 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | SCH3 | H |
| A.0329 | 甲基 | 2-CH3 | H | Cl | H |
| A.0330 | 甲基 | 2-CH3 | H | Cl | 3-Cl |
| A.0331 | 甲基 | 2-CH3 | H | Cl | 4-Cl |
| A.0332 | 甲基 | 2-CH3 | H | Cl | 6-Cl |
| A.0333 | 甲基 | 2-CH3 | H | Cl | 3-OCH3 |
| A.0334 | 甲基 | 2-CH3 | H | Cl | 4-OCH3 |
| A.0335 | 甲基 | 2-CH3 | H | Cl | 3-CF3 |
| A.0336 | 甲基 | 2-CH3 | H | Cl | 6-CH3 |
| A.0337 | 甲基 | 2-CH3 | H | Cl | 6-C6H5 |
| A.0338 | 乙基 | 2-CH3 | H | Cl | H |
| A.0339 | 正丙基 | 2-CH3 | H | Cl | H |
| A.0340 | 异丙基 | 2-CH3 | H | Cl | H |
| A.0341 | 正丁基 | 2-CH3 | H | Cl | H |
| A.0342 | 异丁基 | 2-CH3 | H | Cl | H |
| A.0343 | 仲丁基 | 2-CH3 | H | Cl | H |
| A.0344 | 叔丁基 | 2-CH3 | H | Cl | H |
| A.0345 | 正戊基 | 2-CH3 | H | Cl | H |
| A.0346 | 正己基 | 2-CH3 | H | Cl | H |
| A.0347 | 2-丙烯基 | 2-CH3 | H | Cl | H |
| A.0348 | 2-丙烯基 | 2-CH3 | H | Cl | 3-Cl |
| A.0349 | 2-丙烯基 | 2-CH3 | H | Cl | 4-Cl |
| A.0350 | 2-丙烯基 | 2-CH3 | H | Cl | 6-Cl |
| 序号 | R1 | R2 | R3 | R4 | R5 n |
| A.0351 | 2-丙烯基 | 2-CH3 | H | Cl | 3-OCH3 |
| A.0352 | 2-丙烯基 | 2-CH3 | H | Cl | 4-OCH3 |
| A.0353 | 2-丙烯基 | 2-CH3 | H | Cl | 3-CF3 |
| A.0354 | 2-丙烯基 | 2-CH3 | H | Cl | 6-CH3 |
| A.0355 | 2-丙烯基 | 2-CH3 | H | Cl | 6-C6H5 |
| A.0356 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | Cl | H |
| A.0357 | 2-氯-2-丙烯基 | 2-CH3 | H | Cl | H |
| A.0358 | (E)-2-丁烯基 | 2-CH3 | H | Cl | H |
| A.0359 | 2-甲基-2-丙烯基 | 2-CH3 | H | Cl | H |
| A.0360 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | Cl | H |
| A.0361 | 3-甲基-2-丁烯基 | 2-CH3 | H | Cl | H |
| A.0362 | 2-丙炔基 | 2-CH3 | H | Cl | H |
| A.0363 | 2-丙炔基 | 2-CH3 | H | Cl | 3-Cl |
| A.0364 | 2-丙炔基 | 2-CH3 | H | Cl | 4-Cl |
| A.0365 | 2-丙炔基 | 2-CH3 | H | Cl | 6-Cl |
| A.0366 | 2-丙炔基 | 2-CH3 | H | Cl | 3-OCH3 |
| A.0367 | 2-丙炔基 | 2-CH3 | H | Cl | 4-OCH3 |
| A.0368 | 2-丙炔基 | 2-CH3 | H | Cl | 3-CF3 |
| A.0369 | 2-丙炔基 | 2-CH3 | H | Cl | 6-CH3 |
| A.0370 | 2-丙炔基 | 2-CH3 | H | Cl | 6-C6H5 |
| A.0371 | 2-丁炔基 | 2-CH3 | H | Cl | H |
| A.0372 | 3-丁炔-2-基 | 2-CH3 | H | Cl | H |
| A.0373 | 氰基甲基 | 2-CH3 | H | Cl | H |
| A.0374 | 甲氧基羰基甲基 | 2-CH3 | H | Cl | H |
| A.0375 | 叔丁氧基羰基甲基 | 2-CH3 | H | Cl | H |
| A.0376 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | Cl | H |
| A.0377 | 环丙基甲基 | 2-CH3 | H | Cl | H |
| A.0378 | 1-甲基环戊基 | 2-CH3 | H | Cl | H |
| A.0379 | 环己基 | 2-CH3 | H | Cl | H |
| A.0380 | 1-甲氧基丙-2-基 | 2-CH3 | H | Cl | H |
| A.0381 | 苄基 | 2-CH3 | H | Cl | H |
| A.0382 | 苄基 | 2-CH3 | H | Cl | 3-Cl |
| A.0383 | 苄基 | 2-CH3 | H | Cl | 4-Cl |
| A.0384 | 苄基 | 2-CH3 | H | Cl | 6-Cl |
| A.0385 | 苄基 | 2-CH3 | H | Cl | 3-OCH3 |
| A.0386 | 苄基 | 2-CH3 | H | Cl | 4-OCH3 |
| A.0387 | 苄基 | 2-CH3 | H | Cl | 3-CF3 |
| A.0388 | 苄基 | 2-CH3 | H | Cl | 6-CH3 |
| A.0389 | 苄基 | 2-CH3 | H | Cl | 6-C6H5 |
| A.0390 | 3-甲基苄基 | 2-CH3 | H | Cl | H |
| A.0391 | 2-氟苄基 | 2-CH3 | H | Cl | H |
| A.0392 | 3-氟苄基 | 2-CH3 | H | Cl | H |
| A.0393 | 4-氯苄基 | 2-CH3 | H | Cl | H |
| A.0394 | 3,4-二氯苄基 | 2-CH3 | H | Cl | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0395 | 2,6-二氟苄基 | 2-CH3 | H | Cl | H |
| A.0396 | 3-三氟甲基苄基 | 2-CH3 | H | Cl | H |
| A.0397 | 3-氰基苄基 | 2-CH3 | H | Cl | H |
| A.0398 | 4-甲氧基苄基 | 2-CH3 | H | Cl | H |
| A.0399 | 4-甲氧基羰基苄基 | 2-CH3 | H | Cl | H |
| A.0400 | 3-苯基苄基 | 2-CH3 | H | Cl | H |
| A.0401 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | Cl | H |
| A.0402 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | Cl | H |
| A.0403 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | Cl | H |
| A.0404 | 1-苯基乙基 | 2-CH3 | H | Cl | H |
| A.0405 | 1-(4-甲基苯基)乙基 | 2-CH3 | H | Cl | H |
| A.0406 | 1-(4-氯苯基)乙基 | 2-CH3 | H | Cl | H |
| A.0407 | 1-(3-三氟甲苯基)乙基 | 2-CH3 | H | Cl | H |
| A.0408 | 2-苯基乙基 | 2-CH3 | H | Cl | H |
| A.0409 | 3-苯基丙-1-基 | 2-CH3 | H | Cl | H |
| A.0410 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | Cl | H |
| A.0411 | 甲基 | 2-CH3 | H | Br | H |
| A.0412 | 甲基 | 2-CH3 | H | Br | 3-Cl |
| A.0413 | 甲基 | 2-CH3 | H | Br | 4-Cl |
| A.0414 | 甲基 | 2-CH3 | H | Br | 6-Cl |
| A.0415 | 甲基 | 2-CH3 | H | Br | 3-OCH3 |
| A.0416 | 甲基 | 2-CH3 | H | Br | 4-OCH3 |
| A.0417 | 甲基 | 2-CH3 | H | Br | 3-CF3 |
| A.0418 | 甲基 | 2-CH3 | H | Br | 6-CH3 |
| A.0419 | 甲基 | 2-CH3 | H | Br | 6-C6H5 |
| A.0420 | 乙基 | 2-CH3 | H | Br | H |
| A.0421 | 正丙基 | 2-CH3 | H | Br | H |
| A.0422 | 异丙基 | 2-CH3 | H | Br | H |
| A.0423 | 正丁基 | 2-CH3 | H | Br | H |
| A.0424 | 异丁基 | 2-CH3 | H | Br | H |
| A.0425 | 仲丁基 | 2-CH3 | H | Br | H |
| A.0426 | 叔丁基 | 2-CH3 | H | Br | H |
| A.0427 | 正戊基 | 2-CH3 | H | Br | H |
| A.0428 | 正己基 | 2-CH3 | H | Br | H |
| A.0429 | 2-丙烯基 | 2-CH3 | H | Br | H |
| A.0430 | 2-丙烯基 | 2-CH3 | H | Br | 3-Cl |
| A.0431 | 2-丙烯基 | 2-CH3 | H | Br | 4-Cl |
| A.0432 | 2-丙烯基 | 2-CH3 | H | Br | 6-Cl |
| A.0433 | 2-丙烯基 | 2-CH3 | H | Br | 3-OCH3 |
| A.0434 | 2-丙烯基 | 2-CH3 | H | Br | 4-OCH3 |
| A.0435 | 2-丙烯基 | 2-CH3 | H | Br | 3-CF3 |
| A.0436 | 2-丙烯基 | 2-CH3 | H | Br | 6-CH3 |
| A.0437 | 2-丙烯基 | 2-CH3 | H | Br | 6-C6H5 |
| A.0438 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | Br | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0439 | 2-氯-2-丙烯基 | 2-CH3 | H | Br | H |
| A.0440 | (E)-2-丁烯基 | 2-CH3 | H | Br | H |
| A.0441 | 2-甲基-2-丙烯基 | 2-CH3 | H | Br | H |
| A.0442 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | Br | H |
| A.0443 | 3-甲基-2-丁烯基 | 2-CH3 | H | Br | H |
| A.0444 | 2-丙炔基 | 2-CH3 | H | Br | H |
| A.0445 | 2-丙炔基 | 2-CH3 | H | Br | 3-Cl |
| A.0446 | 2-丙炔基 | 2-CH3 | H | Br | 4-Cl |
| A.0447 | 2-丙炔基 | 2-CH3 | H | Br | 6-Cl |
| A.0448 | 2-丙炔基 | 2-CH3 | H | Br | 3-OCH3 |
| A.0449 | 2-丙炔基 | 2-CH3 | H | Br | 4-OCH3 |
| A.0450 | 2-丙炔基 | 2-CH3 | H | Br | 3-CF3 |
| A.0451 | 2-丙炔基 | 2-CH3 | H | Br | 6-CH3 |
| A.0452 | 2-丙炔基 | 2-CH3 | H | Br | 6-C6H5 |
| A.0453 | 2-丁炔基 | 2-CH3 | H | Br | H |
| A.0454 | 3-丁炔-2-基 | 2-CH3 | H | Br | H |
| A.0455 | 氰基甲基 | 2-CH3 | H | Br | H |
| A.0456 | 甲氧基羰基甲基 | 2-CH3 | H | Br | H |
| A.0457 | 叔丁氧基羰基甲基 | 2-CH3 | H | Br | H |
| A.0458 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | Br | H |
| A.0459 | 环丙基甲基 | 2-CH3 | H | Br | H |
| A.0460 | 1-甲基环戊基 | 2-CH3 | H | Br | H |
| A.0461 | 环己基 | 2-CH3 | H | Br | H |
| A.0462 | 1-甲氧基丙-2-基 | 2-CH3 | H | Br | H |
| A.0463 | 苄基 | 2-CH3 | H | Br | H |
| A.0464 | 苄基 | 2-CH3 | H | Br | 3-Cl |
| A.0465 | 苄基 | 2-CH3 | H | Br | 4-Cl |
| A.0466 | 苄基 | 2-CH3 | H | Br | 6-Cl |
| A.0467 | 苄基 | 2-CH3 | H | Br | 3-OCH3 |
| A.0468 | 苄基 | 2-CH3 | H | Br | 4-OCH3 |
| A.0469 | 苄基 | 2-CH3 | H | Br | 3-CF3 |
| A.0470 | 苄基 | 2-CH3 | H | Br | 6-CH3 |
| A.0471 | 苄基 | 2-CH3 | H | Br | 6-C6H5 |
| A.0472 | 3-甲基苄基 | 2-CH3 | H | Br | H |
| A.0473 | 2-氟苄基 | 2-CH3 | H | Br | H |
| A.0474 | 3-氟苄基 | 2-CH3 | H | Br | H |
| A.0475 | 4-氯苄基 | 2-CH3 | H | Br | H |
| A.0476 | 3,4-二氯苄基 | 2-CH3 | H | Br | H |
| A.0477 | 2,6-二氟苄基 | 2-CH3 | H | Br | H |
| A.0478 | 3-三氟甲基苄基 | 2-CH3 | H | Br | H |
| A.0479 | 3-氰基苄基 | 2-CH3 | H | Br | H |
| A.0480 | 4-甲氧基苄基 | 2-CH3 | H | Br | H |
| A.0481 | 4-甲氧基羰基苄基 | 2-CH3 | H | Br | H |
| A.0482 | 3-苯基苄基 | 2-CH3 | H | Br | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0483 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | Br | H |
| A.0484 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | Br | H |
| A.0485 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | H | Br | H |
| A.0486 | 1-苯基乙基 | 2-CH3 | H | Br | H |
| A.0487 | 1-(4-甲基苯基)乙基 | 2-CH3 | H | Br | H |
| A.0488 | 1-(4-氯苯基)乙基 | 2-CH3 | H | Br | H |
| A.0489 | 1-(3-三氟甲基苯基)乙基 | 2-CH3 | H | Br | H |
| A.0490 | 2-苯基乙基 | 2-CH3 | H | Br | H |
| A.0491 | 3-苯基丙-1-基 | 2-CH3 | H | Br | H |
| A.0492 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | Br | H |
| A.0493 | 甲基 | 2-CH3 | H | CN | H |
| A.0494 | 甲基 | 2-CH3 | H | CN | 3-Cl |
| A.0495 | 甲基 | 2-CH3 | H | CN | 4-Cl |
| A.0496 | 甲基 | 2-CH3 | H | CN | 6-Cl |
| A.0497 | 甲基 | 2-CH3 | H | CN | 3-OCH3 |
| A.0498 | 甲基 | 2-CH3 | H | CN | 4-OCH3 |
| A.0499 | 甲基 | 2-CH3 | H | CN | 3-CF3 |
| A.0500 | 甲基 | 2-CH3 | H | CN | 6-CH3 |
| A.0501 | 甲基 | 2-CH3 | H | CN | 6-C6H5 |
| A.0502 | 乙基 | 2-CH3 | H | CN | H |
| A.0503 | 正丙基 | 2-CH3 | H | CN | H |
| A.0504 | 异丙基 | 2-CH3 | H | CN | H |
| A.0505 | 正丁基 | 2-CH3 | H | CN | H |
| A.0506 | 异丁基 | 2-CH3 | H | CN | H |
| A.0507 | 仲丁基 | 2-CH3 | H | CN | H |
| A.0508 | 叔丁基 | 2-CH3 | H | CN | H |
| A.0509 | 正戊基 | 2-CH3 | H | CN | H |
| A.0510 | 正己基 | 2-CH3 | H | CN | H |
| A.0511 | 2-丙烯基 | 2-CH3 | H | CN | H |
| A.0512 | 2-丙烯基 | 2-CH3 | H | CN | 3-Cl |
| A.0513 | 2-丙烯基 | 2-CH3 | H | CN | 4-Cl |
| A.0514 | 2-丙烯基 | 2-CH3 | H | CN | 6-Cl |
| A.0515 | 2-丙烯基 | 2-CH3 | H | CN | 3-OCH3 |
| A.0516 | 2-丙烯基 | 2-CH3 | H | CN | 4-OCH3 |
| A.0517 | 2-丙烯基 | 2-CH3 | H | CN | 3-CF3 |
| A.0518 | 2-丙烯基 | 2-CH3 | H | CN | 6-CH3 |
| A.0519 | 2-丙烯基 | 2-CH3 | H | CN | 6-C6H5 |
| A.0520 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | CN | H |
| A.0521 | 2-氯-2-丙烯基 | 2-CH3 | H | CN | H |
| A.0522 | (E)-2-丁烯基 | 2-CH3 | H | CN | H |
| A.0523 | 2-甲基-2-丙烯基 | 2-CH3 | H | CN | H |
| A.0524 | (Z)-3-氯-2-丁烯基 | 2-CH3 | H | CN | H |
| A.0525 | 3-甲基-2-丁烯基 | 2-CH3 | H | CN | H |
| A.0526 | 2-丙炔基 | 2-CH3 | H | CN | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0527 | 2-丙炔基 | 2-CH3 | H | CN | 3-Cl |
| A.0528 | 2-丙炔基 | 2-CH3 | H | CN | 4-Cl |
| A.0529 | 2-丙炔基 | 2-CH3 | H | CN | 6-Cl |
| A.0530 | 2-丙炔基 | 2-CH3 | H | CN | 3-OCH3 |
| A.0531 | 2-丙炔基 | 2-CH3 | H | CN | 4-OCH3 |
| A.0532 | 2-丙炔基 | 2-CH3 | H | CN | 3-CF3 |
| A.0533 | 2-丙炔基 | 2-CH3 | H | CN | 6-CH3 |
| A.0534 | 2-丙炔基 | 2-CH3 | H | CN | 6-C6H5 |
| A.0535 | 2-丁炔基 | 2-CH3 | H | CN | H |
| A.0536 | 3-丁炔-2-基 | 2-CH3 | H | CN | H |
| A.0537 | 氰基甲基 | 2-CH3 | H | CN | H |
| A.0538 | 甲氧基羰基甲基 | 2-CH3 | H | CN | H |
| A.0539 | 叔丁氧基羰基甲基 | 2-CH3 | H | CN | H |
| A.0540 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | CN | H |
| A.0541 | 环丙基甲基 | 2-CH3 | H | CN | H |
| A.0542 | 1-甲基环戊基 | 2-CH3 | H | CN | H |
| A.0543 | 环己基 | 2-CH3 | H | CN | H |
| A.0544 | 1-甲氧基丙-2-基 | 2-CH3 | H | CN | H |
| A.0545 | 苄基 | 2-CH3 | H | CN | H |
| A.0546 | 苄基 | 2-CH3 | H | CN | 3-Cl |
| A.0547 | 苄基 | 2-CH3 | H | CN | 4-Cl |
| A.0548 | 苄基 | 2-CH3 | H | CN | 6-Cl |
| A.0549 | 苄基 | 2-CH3 | H | CN | 3-OCH3 |
| A.0550 | 苄基 | 2-CH3 | H | CN | 4-OCH3 |
| A.0551 | 苄基 | 2-CH3 | H | CN | 3-CF3 |
| A.0552 | 苄基 | 2-CH3 | H | CN | 6-CH3 |
| A.0553 | 苄基 | 2-CH3 | H | CN | 6-C6H5 |
| A.0554 | 3-甲基苄基 | 2-CH3 | H | CN | H |
| A.0555 | 2-氟苄基 | 2-CH3 | H | CN | H |
| A.0556 | 3-氟苄基 | 2-CH3 | H | CN | H |
| A.0557 | 4-氯苄基 | 2-CH3 | H | CN | H |
| A.0558 | 3,4-二氯苄基 | 2-CH3 | H | CN | H |
| A.0559 | 2,6-二氟苄基 | 2-CH3 | H | CN | H |
| A.0560 | 3-三氟甲基苄基 | 2-CH3 | H | CN | H |
| A.0561 | 3-氰基苄基 | 2-CH3 | H | CN | H |
| A.0562 | 4-甲氧基苄基 | 2-CH3 | H | CN | H |
| A.0563 | 4-甲氧基羰基苄基 | 2-CH3 | H | CN | H |
| A.0564 | 3-苯基苄基 | 2-CH3 | H | CN | H |
| A.0565 | (5-氯-3-噻吩基)甲基 | 2-CH3 | H | CN | H |
| A.0566 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | H | CN | H |
| A.0567 | (1,3)-二氧杂环戊-2-基)甲基 | 2-CH3 | H | CN | H |
| A.0568 | 1-苯基乙基 | 2-CH3 | H | CN | H |
| A.0569 | 1-(4-甲基苯基)乙基 | 2-CH3 | H | CN | H |
| A.0570 | 1-(4-氯苯基)乙基 | 2-CH3 | H | CN | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0571 | 1-( 3-三氟甲基苯基)乙基 | 2-CH3 | H | CN | H |
| A.0572 | 2-苯基乙基 | 2-CH3 | H | CN | H |
| A.0573 | 3-苯基丙-1-基 | 2-CH3 | H | CN | H |
| A.0574 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | CN | H |
| A.0575 | 甲基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0576 | 乙基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0577 | 2-丙烯基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0578 | 2-丙炔基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0579 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0580 | 3-甲基苄基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0581 | 1-苯基乙基 | 2-CH3 | H | OCH2C≡CH | H |
| A.0582 | 甲基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0583 | 乙基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0584 | 2-丙烯基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0585 | 2-丙炔基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0586 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0587 | 3-甲基苄基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0588 | 1-苯基乙基 | 2-CH3 | H | OCH2CH2C6H5 | H |
| A.0589 | 甲基 | 2-CH3 | H | SCH2CH3 | H |
| A.0590 | 乙基 | 2-CH3 | H | SCH2CH3 | H |
| A.0591 | 2-丙烯基 | 2-CH3 | H | SCH2CH3 | H |
| A.0592 | 2-丙炔基 | 2-CH3 | H | SCH2CH3 | H |
| A.0593 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | SCH2CH3 | H |
| A.0594 | 3-甲基苄基 | 2-CH3 | H | SCH2CH3 | H |
| A.0595 | 1-苯基乙基 | 2-CH3 | H | SCH2CH3 | H |
| A.0596 | 甲基 | 2-CH3 | H | NHCH3 | H |
| A.0597 | 乙基 | 2-CH3 | H | NHCH3 | H |
| A.0598 | 2-丙烯基 | 2-CH3 | H | NHCH3 | H |
| A.0599 | 2-丙炔基 | 2-CH3 | H | NHCH3 | H |
| A.0600 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | NHCH3 | H |
| A.0601 | 3-甲基苄基 | 2-CH3 | H | NHCH3 | H |
| A.0602 | 1-苯基乙基 | 2-CH3 | H | NHCH3 | H |
| A.0603 | 甲基 | 2-CH3 | H | N(CH3)2 | H |
| A.0604 | 乙基 | 2-CH3 | H | N(CH3)2 | H |
| A.0605 | 2-丙烯基 | 2-CH3 | H | N(CH3)2 | H |
| A.0606 | 2-丙炔基 | 2-CH3 | H | N(CH3)2 | H |
| A.0607 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | N(CH3)2 | H |
| A.0608 | 3-甲基苄基 | 2-CH3 | H | N(CH3)2 | H |
| A.0609 | 1-苯基乙基 | 2-CH3 | H | N(CH3)2 | H |
| A.0610 | 甲基 | 2-CH3 | H | OC6H5 | H |
| A.0611 | 乙基 | 2-CH3 | H | OC6H5 | H |
| A.0612 | 2-丙烯基 | 2-CH3 | H | OC6H5 | H |
| A.0613 | 2-丙炔基 | 2-CH3 | H | OC6H5 | H |
| A.0614 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OC6H5 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0615 | 3-甲基丁基 | 2-CH3 | H | OC6H5 | H |
| A.0616 | 1-苯乙基 | 2-CH3 | H | OC6H5 | H |
| A.0617 | 甲基 | 2-CH3 | H | SC6H5 | H |
| A.0618 | 乙基 | 2-CH3 | H | SC6H5 | H |
| A.0619 | 2-丙烯基 | 2-CH3 | H | SC6H5 | H |
| A.0620 | 2-丙炔基 | 2-CH3 | H | SC6H5 | H |
| A.0621 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | SC6H5 | H |
| A.0622 | 3-甲基苄基 | 2-CH3 | H | SC6H5 | H |
| A.0623 | 1-苯基乙基 | 2-CH3 | H | SC6H5 | H |
| A.0624 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0625 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 3-Cl |
| A.0626 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 4-Cl |
| A.0627 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 6-Cl |
| A.0628 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 3-OCH3 |
| A.0629 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 4-OCH3 |
| A.0630 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 3-CF3 |
| A.0631 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 6-CH3 |
| A.0632 | 甲基 | 2-CH3 | 5-CH3 | OCH3 | 6-C6H5 |
| A.0633 | 乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0634 | 正丙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0635 | 异丙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0636 | 正丁基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0637 | 异丁基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0638 | 仲丁基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0639 | 叔丁基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0640 | 正戊基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0641 | 正己基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0642 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0643 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 3-Cl |
| A.0644 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 4-Cl |
| A.0645 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 6-Cl |
| A.0646 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 3-OCH3 |
| A.0647 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 4-OCH3 |
| A.0648 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 3-CF3 |
| A.0649 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 6-CH3 |
| A.0650 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 6-C6H5 |
| A.0651 | (E)-3-氯-2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0652 | 2-氯-2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0653 | (E)-2-丁烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0654 | 2-甲基-2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0655 | (Z)-3-氯-2-丁烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0656 | 3-甲基-2-丁烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0657 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0658 | 2-丙烯基 | 2-CH3 | 5-CH3 | OCH3 | 3-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0659 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 4-Cl |
| A.0660 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 6-Cl |
| A.0661 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 3-OCH3 |
| A.0662 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 4-OCH3 |
| A.0663 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 3-CF3 |
| A.0664 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 6-CH3 |
| A.0665 | 2-丙炔基 | 2-CH3 | 5-CH3 | OCH3 | 6-C6H5 |
| A.0666 | 2-丁炔基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0667 | 2-丁炔-2-基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0668 | 氰基甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0669 | 甲氧基羰基甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0670 | 叔丁氧基羰基甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0671 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0672 | 环丙基甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0673 | 1-甲基环戊基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0674 | 环己基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0675 | 1-甲氧基丙-2-基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0676 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0677 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 3-Cl |
| A.0678 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 4-Cl |
| A.0679 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 6-Cl |
| A.0680 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 3-OCH3 |
| A.0681 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 4-OCH3 |
| A.0682 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 3-CF3 |
| A.0683 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 6-CH3 |
| A.0684 | 苄基 | 2-CH3 | 5-CH3 | OCH3 | 6-C6H5 |
| A.0685 | 3-甲基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0686 | 2-氟苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0687 | 3-氟苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0688 | 4-氯苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0689 | 3,4-二氯苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0690 | 2,6-二氟苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0691 | 3-三氟甲基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0692 | 3-氰基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0693 | 4-甲氧基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0694 | 4-甲氧基羰基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0695 | 3-苯基苄基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0696 | (5-氯-3-噻吩基)甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0697 | (2,5-二氯-3-噻吩基)甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0698 | (1,3-二氧杂环戊-2-基)甲基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0699 | 1-苯基乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0700 | 1-(4-甲基苯基)乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0701 | 1-(4-氯苯基)乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0702 | 1-(3-三氟甲基苯基)乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0703 | 2-苯基乙基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0704 | 3-苯基丙-1-基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0705 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | 5-CH3 | OCH3 | H |
| A.0706 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0707 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 3-Cl |
| A.0708 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 4-Cl |
| A.0709 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 6-Cl |
| A.0710 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 3-OCH3 |
| A.0711 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 4-OCH3 |
| A.0712 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 3-CF3 |
| A.0713 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 6-CH3 |
| A.0714 | 甲基 | 2-CH3 | 5-CH3 | OC2H5 | 6-C6H5 |
| A.0715 | 乙基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0716 | 正丙基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0717 | 异丙基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0718 | 正丁基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0719 | 异丁基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0720 | 仲丁基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0721 | 叔丁基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0722 | 仲戊基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0723 | 正己基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0724 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0725 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 3-Cl |
| A.0726 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 4-Cl |
| A.0727 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 6-Cl |
| A.0728 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 3-OCH3 |
| A.0729 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 4-OCH3 |
| A.0730 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 3-CF3 |
| A.0731 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 6-CH3 |
| A.0732 | 2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | 6-C6H5 |
| A.0733 | (E)-3-氯-2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0734 | 2-氯-2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0735 | (E)-2-丁烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0736 | 2-甲基-2-丙烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0737 | (Z)-3-氯-2-丁烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0738 | 3-甲基-2-丁烯基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0739 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0740 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 3-Cl |
| A.0741 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 4-Cl |
| A.0742 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 6-Cl |
| A.0743 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 3-OCH3 |
| A.0744 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 4-OCH3 |
| A.0745 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 3-CF3 |
| A.0746 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 6-CH3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0747 | 2-丙炔基 | 2-CH3 | 5-CH3 | OC2H5 | 6-C6H5 |
| A.0748 | 2-丁炔基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0749 | 3-丁炔-2-基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0750 | 氰基甲基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0751 | 甲氧基羰基甲基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0752 | 叔丁氧基羰基甲基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0753 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0754 | 环丙基甲基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0755 | 1-甲基环戊基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0756 | 环己基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0757 | 1-甲氧基丙-2-基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0758 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | H |
| A.0759 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 3-Cl |
| A.0760 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 4-Cl |
| A.0761 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 6-Cl |
| A.0762 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 3-OCH3 |
| A.0763 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 4-OCH3 |
| A.0764 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 3-CF3 |
| A.0765 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 6-CH3 |
| A.0766 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 6-C6H5 |
| A.0767 | 苄基 | 2-CH3 | 5-CH3 | OC2H5 | 5-Cl |
| A.0768 | 3-甲基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0769 | 2-氟苄基 | CH3 | CH3 | OC2H5 | H |
| A.0770 | 3-氟苄基 | CH3 | CH3 | OC2H5 | H |
| A.0771 | 4-氯苄基 | CH3 | CH3 | OC2H5 | H |
| A.0772 | 3,4-二氯苄基 | CH3 | CH3 | OC2H5 | H |
| A.0773 | 2,6-二氟苄基 | CH3 | CH3 | OC2H5 | H |
| A.0774 | 3-三氟甲基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0775 | 3-氰基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0776 | 4-甲氧基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0777 | 4-甲氧基羰基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0778 | 3-苯基苄基 | CH3 | CH3 | OC2H5 | H |
| A.0779 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | OC2H5 | H |
| A.0780 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | OC2H5 | H |
| A.0781 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | OC2H5 | H |
| A.0782 | 1-苯基乙基 | CH3 | CH3 | OC2H5 | H |
| A.0783 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | OC2H5 | H |
| A.0784 | 1-(4-氯苯基)乙基 | CH3 | CH3 | OC2H5 | H |
| A.0785 | 1-(3-三氟甲基苯基)乙基 | CH3 | CH3 | OC2H5 | H |
| A.0786 | 2-苯基乙基 | CH3 | CH3 | OC2H5 | H |
| A.0787 | 3-苯基丙-1-基 | CH3 | CH3 | OC2H5 | H |
| A.0788 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | OC2H5 | H |
| A.0789 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0790 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 3-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0791 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 4-Cl |
| A.0792 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 6-Cl |
| A.0793 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 3-OCH3 |
| A.0794 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 4-OCH3 |
| A.0795 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 3-CF3 |
| A.0796 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 6-CH3 |
| A.0797 | 甲基 | CH3 | CH3 | OCH2CH=CH2 | 6-C6H5 |
| A.0798 | 乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0799 | 正丙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0800 | 异丙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0801 | 正丁基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0802 | 异丁基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0803 | 仲丁基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0804 | 叔丁基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0805 | 正戊基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0806 | 正己基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0807 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0808 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 3-Cl |
| A.0809 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 4-Cl |
| A.0810 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 6-Cl |
| A.0811 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 3-OCH3 |
| A.0812 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 4-OCH3 |
| A.0813 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 3-CF3 |
| A.0814 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 6-CH3 |
| A.0815 | 2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | 6-C6H5 |
| A.0816 | (E)-3-氯-2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0817 | 2-氯-2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0818 | (E)-2-丁烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0819 | 2-甲基-2-丙烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0820 | (Z)-3-氯-2-丁烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0821 | 3-甲基-2-丁烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0822 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0823 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 3-Cl |
| A.0824 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 4-Cl |
| A.0825 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 6-Cl |
| A.0826 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 3-OCH3 |
| A.0827 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 4-OCH3 |
| A.0828 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 3-CF3 |
| A.0829 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 6-CH3 |
| A.0830 | 2-丙炔基 | CH3 | CH3 | OCH2CH=CH2 | 6-C6H5 |
| A.0831 | 2-丁炔基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0832 | 3-丁炔-2-基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0833 | 氰基甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0834 | 甲氧基羰基甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0835 | 叔丁氧基羰基甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0836 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0837 | 环丙基甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0838 | 1-甲基环戊基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0839 | 环己基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0840 | 1-甲氧基丙-2-基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0841 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0842 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 3-Cl |
| A.0843 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 4-Cl |
| A.0844 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 6-Cl |
| A.0845 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 3-OCH3 |
| A.0846 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 4-OCH3 |
| A.0847 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 3-CF3 |
| A.0848 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 6-CH3 |
| A.0849 | 苄基 | CH3 | CH3 | OCH2CH=CH2 | 6-C6H5 |
| A.0850 | 3-甲基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0851 | 2-氟苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0852 | 3-氟苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0853 | 4-氯苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0854 | 3,4-二氯苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0855 | 2,6-二氟苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0856 | 3-三氟甲基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0857 | 3-氰基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0858 | 4-甲氧基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0859 | 4-甲氧基羰基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0860 | 3-苯基苄基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0861 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0862 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0863 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0864 | 1-苯基乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0865 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0866 | 1-(4-氯苯基)乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0867 | 1-(3-三氟甲基苯基)乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0868 | 2-苯基乙基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0869 | 3-苯基丙-1-基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0870 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | OCH2CH=CH2 | H |
| A.0871 | 甲基 | CH3 | CH3 | SCH3 | H |
| A.0872 | 甲基 | CH3 | CH3 | SCH3 | 3-Cl3 |
| A.0873 | 甲基 | CH3 | CH3 | SCH3 | 4-Cl |
| A.0874 | 甲基 | CH3 | CH3 | SCH3 | 6-Cl |
| A.0875 | 甲基 | CH3 | CH3 | SCH3 | 3-OCH3 |
| A.0876 | 甲基 | CH3 | CH3 | SCH3 | 4-OCH3 |
| A.0877 | 甲基 | CH3 | CH3 | SCH3 | 3-CF3 |
| A.0878 | 甲基 | CH3 | CH3 | SCH3 | 6-CH3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0879 | 甲基 | CH3 | CH3 | SCH3 | 6-C6H5 |
| A.0880 | 乙基 | CH3 | CH3 | SCH3 | H |
| A.0881 | 正丙基 | CH3 | CH3 | SCH3 | H |
| A.0882 | 异丙基 | CH3 | CH3 | SCH3 | H |
| A.0883 | 正丁基 | CH3 | CH3 | SCH3 | H |
| A.0884 | 异丁基 | CH3 | CH3 | SCH3 | H |
| A.0885 | 仲丁基 | CH3 | CH3 | SCH3 | H |
| A.0886 | 叔丁基 | CH3 | CH3 | SCH3 | H |
| A.0887 | 正戊基 | CH3 | CH3 | SCH3 | H |
| A.0888 | 正己基 | CH3 | CH3 | SCH3 | H |
| A.0889 | 2-丙烯基 | CH3 | CH3 | SCH3 | H |
| A.0890 | 2-丙烯基 | CH3 | CH3 | SCH3 | 3-Cl |
| A.0891 | 2-丙烯基 | CH3 | CH3 | SCH3 | 4-Cl |
| A.0892 | 2-丙烯基 | CH3 | CH3 | SCH3 | 6-Cl |
| A.0893 | 2-丙烯基 | CH3 | CH3 | SCH3 | 3-OCH3 |
| A.0894 | 2-丙烯基 | CH3 | CH3 | SCH3 | 4-OCH3 |
| A.0895 | 2-丙烯基 | CH3 | CH3 | SCH3 | 3-CF3 |
| A.0896 | 2-丙烯基 | CH3 | CH3 | SCH3 | 6-CH3 |
| A.0897 | 2-丙烯基 | CH3 | CH3 | SCH3 | 6-C6H5 |
| A.0898 | (E)-3-氯-2-丙烯基 | CH3 | CH3 | SCH3 | H |
| A.0899 | 2-氯-2-丙烯基 | CH3 | CH3 | SCH3 | H |
| A.0900 | (E)-2-丁烯基 | CH3 | CH3 | SCH3 | H |
| A.0901 | 2-甲基-2-丙烯基 | CH3 | CH3 | SCH3 | H |
| A.0902 | (Z)-3-氯-2-丁烯基 | CH3 | CH3 | SCH3 | H |
| A.0903 | 3-甲基-2-丁烯基 | CH3 | CH3 | SCH3 | H |
| A.0904 | 2-丙炔基 | CH3 | CH3 | SCH3 | H |
| A.0905 | 2-丙炔基 | CH3 | CH3 | SCH3 | 3-Cl |
| A.0906 | 2-丙炔基 | CH3 | CH3 | SCH3 | 4-Cl |
| A.0907 | 2-丙炔基 | CH3 | CH3 | SCH3 | 6-Cl |
| A.0908 | 2-丙炔基 | CH3 | CH3 | SCH3 | 3-OCH3 |
| A.0909 | 2-丙炔基 | CH3 | CH3 | SCH3 | 4-OCH3 |
| A.0910 | 2-丙炔基 | CH3 | CH3 | SCH3 | 3-CF3 |
| A.0911 | 2-丙炔基 | CH3 | CH3 | SCH3 | 6-CH3 |
| A.0912 | 2-丙炔基 | CH3 | CH3 | SCH3 | 6-C6H5 |
| A.0913 | 2-丁炔基 | CH3 | CH3 | SCH3 | H |
| A.0914 | 3-丁炔-2-基 | CH3 | CH3 | SCH3 | H |
| A.0915 | 氰基甲基 | CH3 | CH3 | SCH3 | H |
| A.0916 | 甲氧基羰基甲基 | CH3 | CH3 | SCH3 | H |
| A.0917 | 叔丁氧基羰基甲基 | CH3 | CH3 | SCH3 | H |
| A.0918 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | SCH3 | H |
| A.0919 | 环丙基甲基 | CH3 | CH3 | SCH3 | H |
| A.0920 | 1-甲基环戊基 | CH3 | CH3 | SCH3 | H |
| A.0921 | 环己基 | CH3 | CH3 | SCH3 | H |
| A.0922 | 1-甲氧基丙-2-基 | CH3 | CH3 | SCH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0923 | 苄基 | CH3 | CH3 | SCH3 | H |
| A.0924 | 苄基 | CH3 | CH3 | SCH3 | 3-Cl |
| A.0925 | 苄基 | CH3 | CH3 | SCH3 | 4-Cl |
| A.0926 | 苄基 | CH3 | CH3 | SCH3 | 6-Cl |
| A.0927 | 苄基 | CH3 | CH3 | SCH3 | 3-OCH3 |
| A.0928 | 苄基 | CH3 | CH3 | SCH3 | 4-OCH3 |
| A.0929 | 苄基 | CH3 | CH3 | SCH3 | 3-CF3 |
| A.0930 | 苄基 | CH3 | CH3 | SCH3 | 6-CH3 |
| A.0931 | 苄基 | CH3 | CH3 | SCH3 | 6-C6H5 |
| A.0932 | 3-甲基苄基 | CH3 | CH3 | SCH3 | H |
| A.0933 | 2-氟苄基 | CH3 | CH3 | SCH3 | H |
| A.0934 | 3-氟苄基 | CH3 | CH3 | SCH3 | H |
| A.0935 | 4-氯苄基 | CH3 | CH3 | SCH3 | H |
| A.0936 | 3,4-二氯苄基 | CH3 | CH3 | SCH3 | H |
| A.0937 | 2,6-二氟苄基 | CH3 | CH3 | SCH3 | H |
| A.0938 | 3-三氟甲基苄基 | CH3 | CH3 | SCH3 | H |
| A.0939 | 3-氰基苄基 | CH3 | CH3 | SCH3 | H |
| A.0940 | 4-甲氧基苄基 | CH3 | CH3 | SCH3 | H |
| A.0941 | 4-甲氧基羰基苄基 | CH3 | CH3 | SCH3 | H |
| A.0942 | 3-苯基苄基 | CH3 | CH3 | SCH3 | H |
| A.0943 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | SCH3 | H |
| A.0944 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | SCH3 | H |
| A.0945 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | SCH3 | H |
| A.0946 | 1-苯基乙基 | CH3 | CH3 | SCH3 | H |
| A.0947 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | SCH3 | H |
| A.0948 | 1-(4-氯苯基)乙基 | CH3 | CH3 | SCH3 | H |
| A.0949 | 1-(3-三氟甲基苯基)乙基) | CH3 | CH3 | SCH3 | H |
| A.0950 | 2-苯基乙基 | CH3 | CH3 | SCH3 | H |
| A.0951 | 3-苯基丙-1-基 | CH3 | CH3 | SCH3 | H |
| A.0952 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | SCH3 | H |
| A.0953 | 甲基 | CH3 | CH3 | Cl | H3 |
| A.0954 | 甲基 | CH3 | CH3 | Cl | 3-Cl |
| A.0955 | 甲基 | CH3 | CH3 | Cl | 4-Cl |
| A.0956 | 甲基 | CH3 | CH3 | Cl | 6-Cl |
| A.0957 | 甲基 | CH3 | CH3 | Cl | 3-OCH3 |
| A.0958 | 甲基 | CH3 | CH3 | Cl | 4-OCH3 |
| A.0959 | 甲基 | CH3 | CH3 | Cl | 3-CF3 |
| A.0960 | 甲基 | CH3 | CH3 | Cl | 6-CH3 |
| A.0961 | 甲基 | CH3 | CH3 | Cl | 6-C6H5 |
| A.0962 | 乙基 | CH3 | CH3 | Cl | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.0963 | 正丙基 | CH3 | CH3 | Cl | H |
| A.0964 | 异丙基 | CH3 | CH3 | Cl | H |
| A.0965 | 正丁基 | CH3 | CH3 | Cl | H |
| A.0966 | 异丁基 | CH3 | CH3 | Cl | H |
| A.0967 | 仲丁基 | CH3 | CH3 | Cl | H |
| A.0968 | 叔丁基 | CH3 | CH3 | Cl | H |
| A.0969 | 正戊基 | CH3 | CH3 | Cl | H |
| A.0970 | 正己基 | CH3 | CH3 | Cl | H |
| A.0971 | 2-丙烯基 | CH3 | CH3 | Cl | H |
| A.0972 | 2-丙烯基 | CH3 | CH3 | Cl | 3-Cl |
| A.0973 | 2-丙烯基 | CH3 | CH3 | Cl | 4-Cl |
| A.0974 | 2-丙烯基 | CH3 | CH3 | Cl | 6-Cl |
| A.0975 | 2-丙烯基 | CH3 | CH3 | Cl | 3-OCH3 |
| A.0976 | 2-丙烯基 | CH3 | CH3 | Cl | 4-OCH3 |
| A.0977 | 2-丙烯基 | CH3 | CH3 | Cl | 3-CF3 |
| A.0978 | 2-丙烯基 | CH3 | CH3 | Cl | 6-CH3 |
| A.0979 | 2-丙烯基 | CH3 | CH3 | Cl | 6-C6H5 |
| A.0980 | (E)-3-氯-2-丙烯基 | CH3 | CH3 | Cl | H |
| A.0981 | 2-氯-2-丙烯基 | CH3 | CH3 | Cl | H |
| A.0982 | (E)-2-丁烯基 | CH3 | CH3 | Cl | H |
| A.0983 | 2-甲基-2-丙烯基 | CH3 | CH3 | Cl | H |
| A.0984 | (Z)-3-氯-2-丁烯基 | CH3 | CH3 | Cl | H |
| A.0985 | 3-甲基-2-丁烯基 | CH3 | CH3 | Cl | H |
| A.0986 | 2-丙炔基 | CH3 | CH3 | Cl | H |
| A.0987 | 2-丙炔基 | CH3 | CH3 | Cl | 3-Cl |
| A.0988 | 2-丙炔基 | CH3 | CH3 | Cl | 4-Cl |
| A.0989 | 2-丙炔基 | CH3 | CH3 | Cl | 6-Cl |
| A.0990 | 2-丙炔基 | CH3 | CH3 | Cl | 3-OCH3 |
| A.0991 | 2-丙炔基 | CH3 | CH3 | Cl | 4-OCH3 |
| A.0992 | 2-丙炔基 | CH3 | CH3 | Cl | 3-CF3 |
| A.0993 | 2-丙炔基 | CH3 | CH3 | Cl | 6-CH3 |
| A.0994 | 2-丙炔基 | CH3 | CH3 | Cl | 6-C6H5 |
| A.0995 | 2-丁炔基 | CH3 | CH3 | Cl | H |
| A.0996 | 3-丁炔-2-基 | CH3 | CH3 | Cl | H |
| A.0997 | 氰基甲基 | CH3 | CH3 | Cl | H |
| A.0998 | 甲氧基羰基甲基 | CH3 | CH3 | Cl | H |
| A.0999 | 叔丁氧基羰基甲基 | CH3 | CH3 | Cl | H |
| A.1000 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | Cl | H |
| A.1001 | 环丙基甲基 | CH3 | CH3 | Cl | H |
| A.1002 | 1-甲基环戊基 | CH3 | CH3 | Cl | H |
| A.1003 | 环己基 | CH3 | CH3 | Cl | H |
| A.1004 | 1-甲氧基丙-2-基 | CH3 | CH3 | Cl | H |
| A.1005 | 苄基 | CH3 | CH3 | Cl | H |
| A.1006 | 苄基 | CH3 | CH3 | Cl | 3-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1007 | 苄基 | CH3 | CH3 | Cl | 4-Cl |
| A.1008 | 苄基 | CH3 | CH3 | Cl | 6-Cl |
| A.1009 | 苄基 | CH3 | CH3 | Cl | 3-OCH3 |
| A.1010 | 苄基 | CH3 | CH3 | Cl | 4-OCH3 |
| A.1011 | 苄基 | CH3 | CH3 | Cl | 3-CF3 |
| A.1012 | 苄基 | CH3 | CH3 | Cl | 6-CH3 |
| A.1013 | 苄基 | CH3 | CH3 | Cl | 6-C6H5 |
| A.1014 | 3-甲基苄基 | CH3 | CH3 | Cl | H |
| A.1015 | 2-氟苄基 | CH3 | CH3 | Cl | H |
| A.1016 | 3-氟苄基 | CH3 | CH3 | Cl | H |
| A.1017 | 4-氯苄基 | CH3 | CH3 | Cl | H |
| A.1018 | 3,4-二氯苄基 | CH3 | CH3 | Cl | H |
| A.1019 | 2,6-二氟苄基 | CH3 | CH3 | Cl | H |
| A.1020 | 3-三氟甲基苄基 | CH3 | CH3 | Cl | H |
| A.1021 | 3-氰基苄基 | CH3 | CH3 | Cl | H |
| A.1022 | 4-甲氧基苄基 | CH3 | CH3 | Cl | H |
| A.1023 | 4-甲氧基羰基苄基 | CH3 | CH3 | Cl | H |
| A.1024 | 3-苯基苄基 | CH3 | CH3 | Cl | H |
| A.1025 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | Cl | H |
| A.1026 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | Cl | H |
| A.1027 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | Cl | H |
| A.1028 | 1-苯基乙基 | CH3 | CH3 | Cl | H |
| A.1029 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | Cl | H |
| A.1030 | 1-(4-氯苯基)乙基 | CH3 | CH3 | Cl | H |
| A.1031 | 1-(3-三氟甲基苯基)乙基 | CH3 | CH3 | Cl | H |
| A.1032 | 2-苯基乙基 | CH3 | CH3 | Cl | H |
| A.1033 | 3-苯基丙-1-基 | CH3 | CH3 | Cl | H |
| A.1034 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | Cl | H |
| A.1035 | 甲基 | CH3 | CH3 | Br | H |
| A.1036 | 甲基 | CH3 | CH3 | Br | 3-Cl |
| A.1037 | 甲基 | CH3 | CH3 | Br | 4-Cl |
| A.1038 | 甲基 | CH3 | CH3 | Br | 6-Cl |
| A.1039 | 甲基 | CH3 | CH3 | Br | 3-OCH3 |
| A.1040 | 甲基 | CH3 | CH3 | Br | 4-OCH3 |
| A.1041 | 甲基 | CH3 | CH3 | Br | 3-CF3 |
| A.1042 | 甲基 | CH3 | CH3 | Br | 6-CH3 |
| A.1043 | 甲基 | CH3 | CH3 | Br | 6-C6H5 |
| A.1044 | 乙基 | CH3 | CH3 | Br | H |
| A.1045 | 正丙基 | CH3 | CH3 | Br | H |
| A.1046 | 异丙基 | CH3 | CH3 | Br | H |
| A.1047 | 正丁基 | CH3 | CH3 | Br | H |
| A.1048 | 异丁基 | CH3 | CH3 | Br | H |
| A.1049 | 仲丁基 | CH3 | CH3 | Br | H |
| A.1050 | 叔丁基 | CH3 | CH3 | Br | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1051 | 正戊基 | CH3 | CH3 | Br | H |
| A.1052 | 正己基 | CH3 | CH3 | Br | H |
| A.1053 | 2-丙烯基 | CH3 | CH3 | Br | H |
| A.1054 | 2-丙烯基 | CH3 | CH3 | Br | 3-Cl |
| A.1055 | 2-丙烯基 | CH3 | CH3 | Br | 4-Cl |
| A.1056 | 2-丙烯基 | CH3 | CH3 | Br | 6-Cl |
| A.1057 | 2-丙烯基 | CH3 | CH3 | Br | 3-OCH3 |
| A.1058 | 2-丙烯基 | CH3 | CH3 | Br | 4-OCH3 |
| A.1059 | 2-丙烯基 | CH3 | CH3 | Br | 3-CF3 |
| A.1060 | 2-丙烯基 | CH3 | CH3 | Br | 6-CH3 |
| A.1061 | 2-丙烯基 | CH3 | CH3 | Br | 6-C6H5 |
| A.1062 | (E)-3-氯-2-丙烯基 | CH3 | CH3 | Br | H |
| A.1063 | 2-氯-2-丙烯基 | CH3 | CH3 | Br | H |
| A.1064 | (E)-2-丁烯基 | CH3 | CH3 | Br | H |
| A.1065 | 2-甲基-2-丙烯基 | CH3 | CH3 | Br | H |
| A.1066 | (Z)-3-氯-2-丁烯基 | CH3 | CH3 | Br | H |
| A.1067 | 3-甲基-2-丁烯基 | CH3 | CH3 | Br | H |
| A.1068 | 2-丙炔基 | CH3 | CH3 | Br | H |
| A.1069 | 2-丙炔基 | CH3 | CH3 | Br | 3-Cl |
| A.1070 | 2-丙炔基 | CH3 | CH3 | Br | 4-Cl |
| A.1071 | 2-丙炔基 | CH3 | CH3 | Br | 6-Cl |
| A.1072 | 2-丙炔基 | CH3 | CH3 | Br | 3-OCH3 |
| A.1073 | 2-丙炔基 | CH3 | CH3 | Br | 4-OCH3 |
| A.1074 | 2-丙炔基 | CH3 | CH3 | Br | 3-CF3 |
| A.1075 | 2-丙炔基 | CH3 | CH3 | Br | 6-CH3 |
| A.1076 | 2-丙炔基 | CH3 | CH3 | Br | 6-C6H5 |
| A.1077 | 2-丁炔基 | CH3 | CH3 | Br | H |
| A.1078 | 3-丁炔-2-基 | CH3 | CH3 | Br | H |
| A.1079 | 氰基甲基 | CH3 | CH3 | Br | H |
| A.1080 | 甲氧基羰基甲基 | CH3 | CH3 | Br | H |
| A.1081 | 叔下氧基羰基甲基 | CH3 | CH3 | Br | H |
| A.1082 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | Br | H |
| A.1083 | 环丙基甲基 | CH3 | CH3 | Br | H |
| A.1084 | 1-甲基环戊基 | CH3 | CH3 | Br | H |
| A.1085 | 环己基 | CH3 | CH3 | Br | H |
| A.1086 | 1-甲氧基丙-2-基 | CH3 | CH3 | Br | H |
| A.1087 | 苄基 | CH3 | CH3 | Br | H |
| A.1088 | 苄基 | CH3 | CH3 | Br | 3-Cl |
| A.1089 | 苄基 | CH3 | CH3 | Br | 4-Cl |
| A.1090 | 苄基 | CH3 | CH3 | Br | 6-Cl |
| A.1091 | 苄基 | CH3 | CH3 | Br | 3-OCH3 |
| A.1092 | 苄基 | CH3 | CH3 | Br | 4-OCH3 |
| A.1093 | 苄基 | CH3 | CH3 | Br | 3-CF3 |
| A.1094 | 苄基 | CH3 | CH3 | Br | 6-CH3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1095 | 苄基 | CH3 | CH3 | Br | 6-C6H5 |
| A.1096 | 3-甲基苄基 | CH3 | CH3 | Br | H |
| A.1097 | 2-氟苄基 | CH3 | CH3 | Br | H |
| A.1098 | 3-氟苄基 | CH3 | CH3 | Br | H |
| A.1099 | 4-氯苄基 | CH3 | CH3 | Br | H |
| A.1100 | 3,4-二氯苄基 | CH3 | CH3 | Br | H |
| A.1101 | 2,6-二氟苄基 | CH3 | CH3 | Br | H |
| A.1102 | 3-三氟甲基苄基 | CH3 | CH3 | Br | H |
| A.1103 | 3-氰基苄基 | CH3 | CH3 | Br | H |
| A.1104 | 4-甲氧基苄基 | CH3 | CH3 | Br | H |
| A.1105 | 4-甲氧基羰基苄基 | CH3 | CH3 | Br | H |
| A.1106 | 3-苯基苄基 | CH3 | CH3 | Br | H |
| A.1107 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | Br | H |
| A.1108 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | Br | H |
| A.1109 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | Br | H |
| A.1110 | 1-苯基乙基 | CH3 | CH3 | Br | H |
| A.1111 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | Br | H |
| A.1112 | 1-(4-氯苯基)乙基 | CH3 | CH3 | Br | H |
| A.1113 | 1-(3-三氟甲基苯基)乙基 | CH3 | CH3 | Br | H |
| A.1114 | 2-苯基乙基 | CH3 | CH3 | Br | H |
| A.1115 | 3-苯基丙-1-基 | CH3 | CH3 | Br | H |
| A.1116 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | Br | H |
| A.1117 | 甲基 | CH3 | CH3 | CN | H |
| A.1118 | 甲基 | CH3 | CH3 | CN | 3-Cl |
| A.1119 | 甲基 | CH3 | CH3 | CN | 4-Cl |
| A.1120 | 甲基 | CH3 | CH3 | CN | 6-Cl |
| A.1121 | 甲基 | CH3 | CH3 | CN | 3-OCH3 |
| A.1122 | 甲基 | CH3 | CH3 | CN | 4-OCH3 |
| A.1123 | 甲基 | CH3 | CH3 | CN | 3-CF3 |
| A.1124 | 甲基 | CH3 | CH3 | CN | 6-CH3 |
| A.1125 | 甲基 | CH3 | CH3 | CN | 6-C6H5 |
| A.1126 | 乙基 | CH3 | CH3 | CN | H |
| A.1127 | 正丙基 | CH3 | CH3 | CN | H |
| A.1128 | 异丙基 | CH3 | CH3 | CN | H |
| A.1129 | 正丁基 | CH3 | CH3 | CN | H |
| A.1130 | 异丁基 | CH3 | CH3 | CN | H |
| A.1131 | 仲丁基 | CH3 | CH3 | CN | H |
| A.1132 | 叔丁基 | CH3 | CH3 | CN | H |
| A.1133 | 正戊基 | CH3 | CH3 | CN | H |
| A.1134 | 正己基 | CH3 | CH3 | CN | H |
| A.1135 | 2-丙烯基 | CH3 | CH3 | CN | H |
| A.1136 | 2-丙烯基 | CH3 | CH3 | CN | 3-Cl |
| A.1137 | 2-丙烯基 | CH3 | CH3 | CN | 4-Cl |
| A.1138 | 2-丙烯基 | CH3 | CH3 | CN | 6-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1139 | 2-丙烯基 | CH3 | CH3 | CN | 3-OCH3 |
| A.1140 | 2-丙烯基 | CH3 | CH3 | CN | 4-OCH3 |
| A.1141 | 2-丙烯基 | CH3 | CH3 | CN | 3-CF3 |
| A.1142 | 2-丙烯基 | CH3 | CH3 | CN | 6-CH3 |
| A.1143 | 2-丙烯基 | CH3 | CH3 | CN | 6-C6H5 |
| A.1144 | (E)-3-氯-2-丙烯基 | CH3 | CH3 | CN | H |
| A.1145 | 2-氯-2-丙烯基 | CH3 | CH3 | CN | H |
| A.1146 | (E)-2-丁烯基 | CH3 | CH3 | CN | H |
| A.1147 | 2-甲基-2-丙烯基 | CH3 | CH3 | CN | H |
| A.1148 | (Z)-3-氯-2-丁烯基 | CH3 | CH3 | CN | H |
| A.1149 | 3-甲基-2-丁烯基 | CH3 | CH3 | CN | H |
| A.1150 | 2-丙炔基 | CH3 | CH3 | CN | H |
| A.1151 | 2-丙炔基 | CH3 | CH3 | CN | 3-Cl |
| A.1152 | 2-丙炔基 | CH3 | CH3 | CN | 4-Cl |
| A.1153 | 2-丙炔基 | CH3 | CH3 | CN | 6-Cl |
| A.1154 | 2-丙炔基 | CH3 | CH3 | CN | 3-OCH3 |
| A.1155 | 2-丙炔基 | CH3 | CH3 | CN | 4-OCH3 |
| A.1156 | 2-丙炔基 | CH3 | CH3 | CN | 3-CF3 |
| A.1157 | 2-丙炔基 | CH3 | CH3 | CN | 6-CH3 |
| A.1158 | 2-丙炔基 | CH3 | CH3 | CN | 6-C6H5 |
| A.1159 | 2-丁炔基 | CH3 | CH3 | CN | H |
| A.1160 | 3-丁炔-2-基 | CH3 | CH3 | CN | H |
| A.1161 | 氰基甲基 | CH3 | CH3 | CN | H |
| A.1162 | 甲氧基羰基甲基 | CH3 | CH3 | CN | H |
| A.1163 | 叔丁氧基羰基甲基 | CH3 | CH3 | CN | H |
| A.1164 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | CN | H |
| A.1165 | 环丙基甲基 | CH3 | CH3 | CN | H |
| A.1166 | 1-甲基环戊基 | CH3 | CH3 | CN | H |
| A.1167 | 环己基 | CH3 | CH3 | CN | H |
| A.1168 | 1-甲氧基丙-2-基 | CH3 | CH3 | CN | H |
| A.1169 | 苄基 | CH3 | CH3 | CN | H |
| A.1170 | 苄基 | CH3 | CH3 | CN | 3-Cl |
| A.1171 | 苄基 | CH3 | CH3 | CN | 4-Cl |
| A.1172 | 苄基 | CH3 | CH3 | CN | 6-Cl |
| A.1173 | 苄基 | CH3 | CH3 | CN | 3-OCH3 |
| A.1174 | 苄基 | CH3 | CH3 | CN | 4-OCH3 |
| A.1175 | 苄基 | CH3 | CH3 | CN | 3-CF3 |
| A.1176 | 苄基 | CH3 | CH3 | CN | 6-CH3 |
| A.1177 | 苄基 | CH3 | CH3 | CN | 6-C6H5 |
| A.1178 | 2-甲基苄基 | CH3 | CH3 | CN | H |
| A.1179 | 2-氟苄基 | CH3 | CH3 | CN | H |
| A.1180 | 3-氟苄基 | CH3 | CH3 | CN | H |
| A.1181 | 4-氯苄基 | CH3 | CH3 | CN | H |
| A.1182 | 3,4-二氯苄基 | CH3 | CH3 | CN | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1183 | 2,6-二氟苄基 | CH3 | CH3 | CN | H |
| A.1184 | 3-三氟甲基苄基 | CH3 | CH3 | CN | H |
| A.1185 | 3-氰基苄基 | CH3 | CH3 | CN | H |
| A.1186 | 4-甲氧基苄基 | CH3 | CH3 | CN | H |
| A.1187 | 4-甲氧基羰基苄基 | CH3 | CH3 | CN | H |
| A.1188 | 3-苯基苄基 | CH3 | CH3 | CN | H |
| A.1189 | (5-氯-3-噻吩基)甲基 | CH3 | CH3 | CN | H |
| A.1190 | (2,5-二氯-3-噻吩基)甲基 | CH3 | CH3 | CN | H |
| A.1191 | (1,3-二氧杂环戊-2-基)甲基 | CH3 | CH3 | CN | H |
| A.1192 | 1-苯基乙基 | CH3 | CH3 | CN | H |
| A.1193 | 1-(4-甲基苯基)乙基 | CH3 | CH3 | CN | H |
| A.1194 | 1-(4-氯苯基)乙基 | CH3 | CH3 | CN | H |
| A.1195 | 1-(3-三氟甲基苯基)乙基 | CH3 | CH3 | CN | H |
| A.1196 | 2-苯基乙基 | CH3 | CH3 | CN | H |
| A.1197 | 3-苯基丙-1-基 | CH3 | CH3 | CN | H |
| A.1198 | 4-(4-氯苯基)-2-丁烯基 | CH3 | CH3 | CN | H |
| A.1199 | 甲基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1200 | 乙基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1201 | 2-丙烯基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1202 | 2-丙炔基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1203 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1204 | 3-甲基苄基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1205 | 1-苯基乙基 | CH3 | CH3 | OCH2C≡CH | H |
| A.1206 | 甲基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1207 | 乙基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1208 | 2-丙烯基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1209 | 2-丙炔基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1210 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1211 | 3-甲基苄基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1212 | 1-苯基乙基 | CH3 | CH3 | OCH2CH2C6H5 | H |
| A.1213 | 甲基 | CH3 | CH3 | SCH2CH3 | H |
| A.1214 | 乙基 | CH3 | CH3 | SCH2CH3 | H |
| A.1215 | 2-丙烯基 | CH3 | CH3 | SCH2CH3 | H |
| A.1216 | 2-丙炔基 | CH3 | CH3 | SCH2CH3 | H |
| A.1217 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | SCH2CH3 | H |
| A.1218 | 3-甲基苄基 | CH3 | CH3 | SCH2CH3 | H |
| A.1219 | 1-苯基乙基 | CH3 | CH3 | SCH2CH3 | H |
| A.1220 | 甲基 | CH3 | CH3 | NH-CH3 | H |
| A.1221 | 乙基 | CH3 | CH3 | NH-CH3 | H |
| A.1222 | 2-丙烯基 | CH3 | CH3 | NH-CH3 | H |
| A.1223 | 2-丙炔基 | CH3 | CH3 | NH-CH3 | H |
| A.1224 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | NH-CH3 | H |
| A.1225 | 3-甲基苄基 | CH3 | CH3 | NH-CH3 | H |
| A.1226 | 1-苯基乙基 | CH3 | CH3 | NH-CH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1227 | 甲基 | CH3 | CH3 | N(CH3)2 | H |
| A.1228 | 乙基 | CH3 | CH3 | N(CH3)2 | H |
| A.1229 | 2-丙烯基 | CH3 | CH3 | N(CH3)2 | H |
| A.1230 | 2-丙炔基 | CH3 | CH3 | N(CH3)2 | H |
| A.1231 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | N(CH3)2 | H |
| A.1232 | 3-甲基苄基 | CH3 | CH3 | N(CH3)2 | H |
| A.1233 | 1-苯基乙基 | CH3 | CH3 | N(CH3)2 | H |
| A.1234 | 甲基 | CH3 | CH3 | OC6H5 | H |
| A.1235 | 乙基 | CH3 | CH3 | OC6H5 | H |
| A.1236 | 2-丙烯基 | CH3 | CH3 | OC6H5 | H |
| A.1237 | 2-丙炔基 | CH3 | CH3 | OC6H5 | H |
| A.1238 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | OC6H5 | H |
| A.1239 | 3-甲基丁基 | CH3 | CH3 | OC6H5 | H |
| A.1240 | 1-苯乙基 | CH3 | CH3 | OC6H5 | H |
| A.1241 | 甲基 | CH3 | CH3 | SC6H5 | H |
| A.1242 | 乙基 | CH3 | CH3 | SC6H5 | H |
| A.1243 | 2-丙烯基 | CH3 | CH3 | SC6H5 | H |
| A.1244 | 2-丙炔基 | CH3 | CH3 | SC6H5 | H |
| A.1245 | 1-(叔丁氧基羰基)乙基 | CH3 | CH3 | SC6H5 | H |
| A.1246 | 3-甲基苄基 | CH3 | CH3 | SC6H5 | H |
| A.1247 | 1-苯基乙基 | CH3 | CH3 | SC6H5 | H |
| A.1248 | 甲基 | 2-Cl | H | OCH3 | H |
| A.1249 | 甲基 | 2-Cl | H | OCH3 | 3-Cl |
| A.1250 | 甲基 | 2-Cl | H | OCH3 | 4-Cl |
| A.1251 | 甲基 | 2-Cl | H | OCH3 | 6-Cl |
| A.1252 | 甲基 | 2-Cl | H | OCH3 | 3-OCH3 |
| A.1253 | 甲基 | 2-Cl | H | OCH3 | 4-OCH3 |
| A.1254 | 甲基 | 2-Cl | H | OCH3 | 3-CF3 |
| A.1255 | 甲基 | 2-Cl | H | OCH3 | 6-CH3 |
| A.1256 | 甲基 | 2-Cl | H | OCH3 | 6-C6H5 |
| A.1257 | 乙基 | 2-Cl | H | OCH3 | H |
| A.1258 | 正丙基 | 2-Cl | H | OCH3 | H |
| A.1259 | 异丙基 | 2-Cl | H | OCH3 | H |
| A.1260 | 正丁基 | 2-Cl | H | OCH3 | H |
| A.1261 | 异丁基 | 2-Cl | H | OCH3 | H |
| A.1262 | 仲丁基 | 2-Cl | H | OCH3 | H |
| A.1263 | 叔丁基 | 2-Cl | H | OCH3 | H |
| A.1264 | 正戊基 | 2-Cl | H | OCH3 | H |
| A.1265 | 正己基 | 2-Cl | H | OCH3 | H |
| A.1266 | 2-丙烯基 | 2-Cl | H | OCH3 | H |
| A.1267 | 2-丙烯基 | 2-Cl | H | OCH3 | 3-Cl |
| A.1268 | 2-丙烯基 | 2-Cl | H | OCH3 | 4-Cl |
| A.1269 | 2-丙烯基 | 2-Cl | H | OCH3 | 6-Cl |
| A.1270 | 2-丙烯基 | 2-Cl | H | OCH3 | 3-OCH3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1271 | 2-丙烯基 | 2-Cl | H | OCH3 | 4-OCH3 |
| A.1272 | 2-丙烯基 | 2-Cl | H | OCH3 | 3-CF3 |
| A.1273 | 2-丙烯基 | 2-Cl | H | OCH3 | 6-CH3 |
| A.1274 | 2-丙烯基 | 2-Cl | H | OCH3 | 6-C6H5 |
| A.1275 | (E)-3-氯-2-丙烯基 | 2-Cl | H | OCH3 | H |
| A.1276 | 2-氯-2-丙烯基 | 2-Cl | H | OCH3 | H |
| A.1277 | (E)-2-丁烯基 | 2-Cl | H | OCH3 | H |
| A.1278 | 2-甲基-2-丙烯基 | 2-Cl | H | OCH3 | H |
| A.1279 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | OCH3 | H |
| A.1280 | 3-甲基-2-丁烯基 | 2-Cl | H | OCH3 | H |
| A.1281 | 2-丙炔基 | 2-Cl | H | OCH3 | H |
| A.1282 | 2-丙炔基 | 2-Cl | H | OCH3 | 3-Cl |
| A.1283 | 2-丙炔基 | 2-Cl | H | OCH3 | 4-Cl |
| A.1284 | 2-丙炔基 | 2-Cl | H | OCH3 | 6-Cl |
| A.1285 | 2-丙炔基 | 2-Cl | H | OCH3 | 3-OCH3 |
| A.1286 | 2-丙炔基 | 2-Cl | H | OCH3 | 4-OCH3 |
| A.1287 | 2-丙炔基 | 2-Cl | H | OCH3 | 3-CF3 |
| A.1288 | 2-丙炔基 | 2-Cl | H | OCH3 | 6-CH3 |
| A.1289 | 2-丙炔基 | 2-Cl | H | OCH3 | 6-C6H5 |
| A.1290 | 2-丁炔基 | 2-Cl | H | OCH3 | H |
| A.1291 | 3-丁炔-2-基 | 2-Cl | H | OCH3 | H |
| A.1292 | 氰基甲基 | 2-Cl | H | OCH3 | H |
| A.1293 | 甲氧基羰基甲基 | 2-Cl | H | OCH3 | H |
| A.1294 | 叔丁氧基羰基甲基 | 2-Cl | H | OCH3 | H |
| A.1295 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OCH3 | H |
| A.1296 | 环丙基甲基 | 2-Cl | H | OCH3 | H |
| A.1297 | 1-甲基环戊基 | 2-Cl | H | OCH3 | H |
| A.1298 | 环己基 | 2-Cl | H | OCH3 | H |
| A.1299 | 1-甲氧基丙-2-基 | 2-Cl | H | OCH3 | H |
| A.1300 | 苄基 | 2-Cl | H | OCH3 | H |
| A.1301 | 苄基 | 2-Cl | H | OCH3 | 3-Cl |
| A.1302 | 苄基 | 2-Cl | H | OCH3 | 4-Cl |
| A.1303 | 苄基 | 2-Cl | H | OCH3 | 6-Cl |
| A.1304 | 苄基 | 2-Cl | H | OCH3 | 3-OCH3 |
| A.1305 | 苄基 | 2-Cl | H | OCH3 | 4-OCH3 |
| A.1306 | 苄基 | 2-Cl | H | OCH3 | 3-CF3 |
| A.1307 | 苄基 | 2-Cl | H | OCH3 | 6-CH3 |
| A.1308 | 苄基 | 2-Cl | H | OCH3 | 6-C6H5 |
| A.1309 | 3-甲基苄基 | 2-Cl | H | OCH3 | H |
| A.1310 | 2-氟苄基 | 2-Cl | H | OCH3 | H |
| A.1311 | 3-氟苄基 | 2-Cl | H | OCH3 | H |
| A.1312 | 4-氯苄基 | 2-Cl | H | OCH3 | H |
| A.1313 | 3,4-二氯苄基 | 2-Cl | H | OCH3 | H |
| A.1314 | 2,6-二氟苄基 | 2-Cl | H | OCH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1315 | 3-三氟甲基苄基 | 2-Cl | H | OCH3 | H |
| A.1316 | 3-氰基苄基 | 2-Cl | H | OCH3 | H |
| A.1317 | 4-甲氧基苄基 | 2-Cl | H | OCH3 | H |
| A.1318 | 4-甲氧基羰基苄基 | 2-Cl | H | OCH3 | H |
| A.1319 | 3-苯基苄基 | 2-Cl | H | OCH3 | H |
| A.1320 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | OCH3 | H |
| A.1321 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | OCH3 | H |
| A.1322 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | OCH3 | H |
| A.1323 | 1-苯基乙基 | 2-Cl | H | OCH3 | H |
| A.1324 | 1-(4-甲基苯基)乙基 | 2-Cl | H | OCH3 | H |
| A.1325 | 1-(4-氯苯基)乙基 | 2-Cl | H | OCH3 | H |
| A.1326 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | OCH3 | H |
| A.1327 | 2-苯基乙基 | 2-Cl | H | OCH3 | H |
| A.1328 | 3-苯基丙-1-基 | 2-Cl | H | OCH3 | H |
| A.1329 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | OCH3 | H |
| A.1330 | 甲基 | 2-Cl | H | OC2H5 | H |
| A.1331 | 甲基 | 2-Cl | H | OC2H5 | 3-Cl |
| A.1332 | 甲基 | 2-Cl | H | OC2H5 | 4-Cl |
| A.1333 | 甲基 | 2-Cl | H | OC2H5 | 6-Cl |
| A.1334 | 甲基 | 2-Cl | H | OC2H5 | 3-OCH3 |
| A.1335 | 甲基 | 2-Cl | H | OC2H5 | 4-OCH3 |
| A.1336 | 甲基 | 2-Cl | H | OC2H5 | 3-CF3 |
| A.1337 | 甲基 | 2-Cl | H | OC2H5 | 6-CH3 |
| A.1338 | 甲基 | 2-Cl | H | OC2H5 | 6-C6H5 |
| A.1339 | 乙基 | 2-Cl | H | OC2H5 | H |
| A.1340 | 正丙基 | 2-Cl | H | OC2H5 | H |
| A.1341 | 异丙基 | 2-Cl | H | OC2H5 | H |
| A.1342 | 正丁基 | 2-Cl | H | OC2H5 | H |
| A.1343 | 异丁基 | 2-Cl | H | OC2H5 | H |
| A.1344 | 仲丁基 | 2-Cl | H | OC2H5 | H |
| A.1345 | 叔丁基 | 2-Cl | H | OC2H5 | H |
| A.1346 | 正戊基 | 2-Cl | H | OC2H5 | H |
| A.1347 | 正己基 | 2-Cl | H | OC2H5 | H |
| A.1348 | 2-丙烯基 | 2-Cl | H | OC2H5 | H |
| A.1349 | 2-丙烯基 | 2-Cl | H | OC2H5 | 3-Cl |
| A.1350 | 2-丙烯基 | 2-Cl | H | OC2H5 | 6-Cl |
| A.1351 | 2-丙烯基 | 2-Cl | H | OC2H5 | 6-Cl |
| A.1352 | 2-丙烯基 | 2-Cl | H | OC2H5 | 3-OCH3 |
| A.1353 | 2-丙烯基 | 2-Cl | H | OC2H5 | 4-OCH3 |
| A.1354 | 2-丙烯基 | 2-Cl | H | OC2H5 | 3-CF3 |
| A.1355 | 2-丙烯基 | 2-Cl | H | OC2H5 | 6-CH3 |
| A.1356 | 2-丙烯基 | 2-Cl | H | OC2H5 | 6-C6H5 |
| A.1357 | (E)-3-氯-2-丁烯基 | 2-Cl | H | OC2H5 | H |
| A.1358 | 2-氯-2-丙烯基 | 2-Cl | H | OC2H5 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1359 | (E)-2-丁烯基 | 2-Cl | H | OC2H5 | H |
| A.1360 | 2-甲基-2-丙烯基 | 2-Cl | H | OC2H5 | H |
| A.1361 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | OC2H5 | H |
| A.1362 | 3-甲基-2-丁烯基 | 2-Cl | H | OC2H5 | H |
| A.1363 | 2-丙炔基 | 2-Cl | H | OC2H5 | H |
| A.1364 | 2-丙炔基 | 2-C1 | H | OC2H5 | 3-Cl |
| A.1365 | 2-丙炔基 | 2-Cl | H | OC2H5 | 4-Cl |
| A.1366 | 2-丙炔基 | 2-Cl | H | OC2H5 | 6-Cl |
| A.1367 | 2-丙炔基 | 2-Cl | H | OC2H5 | 3-OCH3 |
| A.1368 | 2-丙炔基 | 2-Cl | H | OC2H5 | 4-OCH3 |
| A.1369 | 2-丙炔基 | 2-Cl | H | OC2H5 | 3-CF3 |
| A.1370 | 2-丙炔基 | 2-Cl | H | OC2H5 | 6-CH3 |
| A.1371 | 2-丙炔基 | 2-Cl | H | OC2H5 | 6-C6H5 |
| A.1372 | 2-丁炔基 | 2-Cl | H | OC2H5 | H |
| A.1373 | 3-丁炔-2-基 | 2-Cl | H | OC2H5 | H |
| A.1374 | 氰基甲基 | 2-Cl | H | OC2H5 | H |
| A.1375 | 甲氧基羰基甲基 | 2-Cl | H | OC2H5 | H |
| A.1376 | 叔丁氧基羰基甲基 | 2-Cl | H | OC2H5 | H |
| A.1377 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OC2H5 | H |
| A.1378 | 环丙基甲基 | 2-Cl | H | OC2H5 | H |
| A.1379 | 1-甲基环戊基 | 2-Cl | H | OC2H5 | H |
| A.1380 | 环己基 | 2-Cl | H | OC2H5 | H |
| A.1381 | 1-甲氧基丙-2-基 | 2-Cl | H | OC2H5 | H |
| A.1382 | 苄基 | 2-Cl | H | OC2H5 | H |
| A.1383 | 苄基 | 2-Cl | H | OC2H5 | 3-Cl |
| A.1384 | 苄基 | 2-Cl | H | OC2H5 | 4-Cl |
| A.1385 | 苄基 | 2-Cl | H | OC2H5 | 6-Cl |
| A.1386 | 苄基 | 2-Cl | H | OC2H5 | 3-OCH3 |
| A.1387 | 苄基 | 2-Cl | H | OC2H5 | 4-OCH3 |
| A.1388 | 苄基 | 2-Cl | H | OC2H5 | 3-CF3 |
| A.1389 | 苄基 | 2-Cl | H | OC2H5 | 6-CH3 |
| A.1390 | 苄基 | 2-Cl | H | OC2H5 | 6-C6H5 |
| A.1391 | 3-甲基苄基 | 2-Cl | H | OC2H5 | H |
| A.1392 | 2-氟苄基 | 2-Cl | H | OC2H5 | H |
| A.1393 | 3-氟苄基 | 2-Cl | H | OC2H5 | H |
| A.1394 | 4-氯苄基 | 2-Cl | H | OC2H5 | H |
| A.1395 | 3,4-二氯苄基 | 2-Cl | H | OC2H5 | H |
| A.1396 | 2,6-二氟苄基 | 2-Cl | H | OC2H5 | H |
| A.1397 | 3-三氟甲基苄基 | 2-Cl | H | OC2H5 | H |
| A.1398 | 3-氰基苄基 | 2-Cl | H | OC2H5 | H |
| A.1399 | 4-甲氧基苄基 | 2-Cl | H | OC2H5 | H |
| A.1400 | 4-甲氧基羰基苄基 | 2-Cl | H | OC2H5 | H |
| A.1401 | 3-苯基苄基 | 2-Cl | H | OC2H5 | H |
| A.1402 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | OC2H5 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1403 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | OC2H5 | H |
| A.1404 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | OC2H5 | H |
| A.1405 | 1-苯基乙基 | 2-Cl | H | OC2H5 | H |
| A.1406 | 1-(4-甲基苯基)乙基 | 2-Cl | H | OC2H5 | H |
| A.1407 | 1-(4-氯苯基)乙基 | 2-Cl | H | OC2H5 | H |
| A.1408 | 1-(3-三氯甲基苯基)乙基 | 2-Cl | H | OC2H5 | H |
| A.1409 | 2-苯基乙基 | 2-Cl | H | OC2H5 | H |
| A.1410 | 3-苯基丙-1-基 | 2-Cl | H | OC2H5 | H |
| A.1411 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | OC2H5 | H |
| A.1412 | 甲基 | 2-Cl | H | CH2CH=CH2 | H |
| A.1413 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 3-Cl |
| A.1414 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 4-Cl |
| A.1415 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 6-Cl |
| A.1416 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 3-OCH3 |
| A.1417 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 4-OCH3 |
| A.1418 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 3-CF3 |
| A.1419 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 6-CH3 |
| A.1420 | 甲基 | 2-Cl | H | OCH2CH=CH2 | 6-C6H5 |
| A.1421 | 乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1422 | 正丙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1423 | 异丙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1424 | 正丁基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1425 | 异丁基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1426 | 仲丁基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1427 | 叔丁基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1428 | 正戊基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1429 | 正己基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1430 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1431 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 3-Cl |
| A.1432 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 4-Cl |
| A.1433 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 6-Cl |
| A.1434 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 3-OCH3 |
| A.1435 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 4-OCH3 |
| A.1436 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 3-CF3 |
| A.1437 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 6-CH3 |
| A.1438 | 2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | 6-C6H5 |
| A.1439 | (E)-3-氯-2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1440 | 2-氯-2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1441 | (E)-2-丁烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1442 | 2-甲基-2-丙烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1443 | (Z)-3-氯-2-丁烯基 | 2-C l | H | OCH2CH=CH2 | H |
| A.1444 | 3-甲基-2-丁烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1445 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1446 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 3-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1447 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 4-Cl |
| A.1448 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 6-Cl |
| A.1449 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 3-OCH3 |
| A.1450 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 4-OCH3 |
| A.1451 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 3-CF3 |
| A.1452 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 6-CH3 |
| A.1453 | 2-丙炔基 | 2-Cl | H | OCH2CH=CH2 | 6-C6H5 |
| A.1454 | 2-丁炔基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1455 | 3-丁炔-2-基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1456 | 氰基甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1457 | 甲氧基羰基甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1458 | 叔丁氧基羰基甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1459 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1460 | 环丙基甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1461 | 1-甲基环戊基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1462 | 环己基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1463 | 1-甲氧基丙-2-基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1464 | 苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1465 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 3-Cl |
| A.1466 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 4-Cl |
| A.1467 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 6-Cl |
| A.1468 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 3-OCH3 |
| A.1469 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 4-OCH3 |
| A.1470 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 3-CF3 |
| A.1471 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 6-CH3 |
| A.1472 | 苄基 | 2-Cl | H | OCH2CH=CH2 | 6-C6H5 |
| A.1473 | 3-甲基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1474 | 2-氟苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1475 | 3-氟苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1476 | 4-氯苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1477 | 3,4-二氯苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1478 | 2,6-二氟苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1479 | 3-三氟甲基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1480 | 3-氰基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1481 | 4-甲氧基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1482 | 4-甲氧基羰基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1483 | 3-苯基苄基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1484 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1485 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1486 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1487 | 1-苯基乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1488 | 1-(4-甲基苯基)乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1489 | 1-(4-氯苯基)乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1490 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1491 | 2-苯基乙基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1492 | 3-苯基丙-1-基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1493 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | OCH2CH=CH2 | H |
| A.1494 | 甲基 | 2-Cl | H | SCH3 | H |
| A.1495 | 甲基 | 2-Cl | H | SCH3 | 3-Cl |
| A.1496 | 甲基 | 2-Cl | H | SCH3 | 4-Cl |
| A.1497 | 甲基 | 2-Cl | H | SCH3 | 6-Cl |
| A.1498 | 甲基 | 2-Cl | H | SCH3 | 3-OCH3 |
| A.1499 | 甲基 | 2-Cl | H | SCH3 | 4-OCH3 |
| A.1500 | 甲基 | 2-Cl | H | SCH3 | 3-CF3 |
| A.1501 | 甲基 | 2-Cl | H | SCH3 | 6-CH3 |
| A.1502 | 甲基 | 2-Cl | H | SCH3 | 6-C6H5 |
| A.1503 | 乙基 | 2-Cl | H | SCH3 | H |
| A.1504 | 正丙基 | 2-Cl | H | SCH3 | H |
| A.1505 | 异丙基 | 2-Cl | H | SCH3 | H |
| A.1506 | 正丁基 | 2-Cl | H | SCH3 | H |
| A.1507 | 异丁基 | 2-Cl | H | SCH3 | H |
| A.1508 | 仲丁基 | 2-Cl | H | SCH3 | H |
| A.1509 | 叔丁基 | 2-Cl | H | SCH3 | H |
| A.1510 | 正戊基 | 2-Cl | H | SCH3 | H |
| A.1511 | 正己基 | 2-Cl | H | SCH3 | H |
| A.1512 | 2-丙烯基 | 2-Cl | H | SCH3 | H |
| A.1513 | 2-丙烯基 | 2-Cl | H | SCH3 | 3-Cl |
| A.1514 | 2-丙烯基 | 2-Cl | H | SCH3 | 4-Cl |
| A.1515 | 2-丙烯基 | 2-Cl | H | SCH3 | 6-Cl |
| A.1516 | 2-丙烯基 | 2-Cl | H | SCH3 | 3-OCH3 |
| A.1517 | 2-丙烯基 | 2-Cl | H | SCH3 | 4-OCH3 |
| A.1518 | 2-丙烯基 | 2-Cl | H | SCH3 | 3-CF3 |
| A.1519 | 2-丙烯基 | 2-Cl | H | SCH3 | 6-CH3 |
| A.1520 | 2-丙烯基 | 2-Cl | H | SCH3 | 6-C6H5 |
| A.1521 | (E)-3-氯-2-丙烯基 | 2-Cl | H | SCH3 | H |
| A.1522 | 2-氯-2-丙烯基 | 2-Cl | H | SCH3 | H |
| A.1523 | (E)-2-丁烯基 | 2-Cl | H | SCH3 | H |
| A.1524 | 2-甲基-2-丙烯基 | 2-Cl | H | SCH3 | H |
| A.1525 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | SCH3 | H |
| A.1526 | 3-甲基-2-丁烯基 | 2-Cl | H | SCH3 | H |
| A.1527 | 2-丙炔基 | 2-Cl | H | SCH3 | H |
| A.1528 | 2-丙炔基 | 2-Cl | H | SCH3 | 3-Cl |
| A.1529 | 2-丙炔基 | 2-Cl | H | SCH3 | 4-Cl |
| A.1530 | 2-丙炔基 | 2-Cl | H | SCH3 | 6-Cl |
| A.1531 | 2-丙炔基 | 2-Cl | H | SCH3 | 3-OCH3 |
| A.1532 | 2-丙炔基 | 2-Cl | H | SCH3 | 4-OCH3 |
| A.1533 | 2-丙炔基 | 2-Cl | H | SCH3 | 3-CF3 |
| A.1534 | 2-丙炔基 | 2-Cl | H | SCH3 | 6-CH3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1535 | 2-丙炔基 | 2-Cl | H | SCH3 | 6-C6H5 |
| A.1536 | 2-丁炔基 | 2-Cl | H | SCH3 | H |
| A.1537 | 3-丁炔-2-基 | 2-Cl | H | SCH3 | H |
| A.1538 | 氰基甲基 | 2-Cl | H | SCH3 | H |
| A.1539 | 甲氧基羰基甲基 | 2-Cl | H | SCH3 | H |
| A.1540 | 叔丁氧基羰基甲基 | 2-Cl | H | SCH3 | H |
| A.1541 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | SCH3 | H |
| A.1542 | 环丙基甲基 | 2-Cl | H | SCH3 | H |
| A.1543 | 1-甲基环戊基 | 2-Cl | H | SCH3 | H |
| A.1544 | 环己基 | 2-Cl | H | SCH3 | H |
| A.1545 | 1-甲氧基丙-2-基 | 2-Cl | H | SCH3 | H |
| A.1546 | 苄基 | 2-Cl | H | SCH3 | H |
| A.1547 | 苄基 | 2-Cl | H | SCH3 | 3-Cl |
| A.1548 | 苄基 | 2-Cl | H | SCH3 | 4-Cl |
| A.1549 | 苄基 | 2-Cl | H | SCH3 | 6-Cl |
| A.1550 | 苄基 | 2-Cl | H | SCH3 | 3-OCH3 |
| A.1551 | 苄基 | 2-Cl | H | SCH3 | 4-OCH3 |
| A.1552 | 苄基 | 2-Cl | H | SCH3 | 3-CF3 |
| A.1553 | 苄基 | 2-Cl | H | SCH3 | 6-CH3 |
| A.1554 | 苄基 | 2-Cl | H | SCH3 | 6-C6H5 |
| A.1555 | 3-甲基苄基 | 2-Cl | H | SCH3 | H |
| A.1556 | 2-氟苄基 | 2-Cl | H | SCH3 | H |
| A.1557 | 3-氟苄基 | 2-Cl | H | SCH3 | H |
| A.1558 | 4-氯苄基 | 2-Cl | H | SCH3 | H |
| A.1559 | 3,4-二氯苄基 | 2-Cl | H | SCH3 | H |
| A.1560 | 2,6-二氟苄基 | 2-Cl | H | SCH3 | H |
| A.1561 | 3-三氟甲基苄基 | 2-Cl | H | SCH3 | H |
| A.1562 | 3-氰基苄基 | 2-Cl | H | SCH3 | H |
| A.1563 | 4-甲氧基苄基 | 2-Cl | H | SCH3 | H |
| A.1564 | 4-甲氧基羰基苄基 | 2-Cl | H | SCH3 | H |
| A.1565 | 3-苯基苄基 | 2-Cl | H | SCH3 | H |
| A.1566 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | SCH3 | H |
| A.1567 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | SCH3 | H |
| A.1568 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | SCH3 | H |
| A.1569 | 1-苯基乙基 | 2-Cl | H | SCH3 | H |
| A.1570 | 1-(4-甲基苯基)乙基 | 2-Cl | H | SCH3 | H |
| A.1571 | 1-(4-氯苯基)乙基 | 2-Cl | H | SCH3 | H |
| A.1572 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | SCH3 | H |
| A.1573 | 2-苯基乙基 | 2-Cl | H | SCH3 | H |
| A.1574 | 3-苯基丙-1-基 | 2-Cl | H | SCH3 | H |
| A.1575 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | SCH3 | H |
| A.1576 | 甲基 | 2-Cl | H | Cl | H |
| A.1577 | 甲基 | 2-Cl | H | Cl | 3-Cl |
| A.1578 | 甲基 | 2-Cl | H | Cl | 4-Cl |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1579 | 甲基 | 2-Cl | H | Cl | 6-Cl |
| A.1580 | 甲基 | 2-Cl | H | Cl | 3-OCH3 |
| A.1581 | 甲基 | 2-Cl | H | Cl | 4-OCH3 |
| A.1582 | 甲基 | 2-Cl | H | Cl | 3-CF3 |
| A.1583 | 甲基 | 2-Cl | H | Cl | 6-CH3 |
| A.1584 | 甲基 | 2-Cl | H | Cl | 6-C6H5 |
| A.1585 | 乙基 | 2-Cl | H | Cl | H |
| A.1586 | 正丙基 | 2-Cl | H | Cl | H |
| A.1587 | 异丙基 | 2-Cl | H | Cl | H |
| A.1588 | 正丁基 | 2-Cl | H | Cl | H |
| A.1589 | 异丁基 | 2-Cl | H | Cl | H |
| A.1590 | 仲丁基 | 2-Cl | H | Cl | H |
| A.1591 | 叔丁基 | 2-Cl | H | Cl | H |
| A.1592 | 正戊基 | 2-Cl | H | Cl | H |
| A.1593 | 正己基 | 2-Cl | H | Cl | H |
| A.1594 | 2-丙烯基 | 2-Cl | H | Cl | H |
| A.1595 | 2-丙烯基 | 2-Cl | H | Cl | 3-Cl |
| A.1596 | 2-丙烯基 | 2-Cl | H | Cl | 4-Cl |
| A.1597 | 2-丙烯基 | 2-Cl | H | Cl | 6-Cl |
| A.1598 | 2-丙烯基 | 2-Cl | H | Cl | 3-OCH3 |
| A.1599 | 2-丙烯基 | 2-Cl | H | Cl | 4-OCH3 |
| A.1600 | 2-丙烯基 | 2-Cl | H | Cl | 3-CF3 |
| A.1601 | 2-丙烯基 | 2-Cl | H | Cl | 6-CH3 |
| A.1602 | 2-丙烯基 | 2-Cl | H | Cl | 6-C6H5 |
| A.1603 | (E)-3-氯-2-丙烯基 | 2-Cl | H | Cl | H |
| A.1604 | 2-氯-2-丙烯基 | 2-Cl | H | Cl | H |
| A.1605 | (E)-2-丁烯基 | 2-Cl | H | Cl | H |
| A.1606 | 2-甲基-2-丙烯基 | 2-Cl | H | Cl | H |
| A.1607 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | Cl | H |
| A.1608 | 3-甲基-2-丁烯基 | 2-Cl | H | Cl | H |
| A.1609 | 2-丙炔基 | 2-Cl | H | Cl | H |
| A.1610 | 2-丙炔基 | 2-Cl | H | Cl | 3-Cl |
| A.1611 | 2-丙炔基 | 2-Cl | H | Cl | 4-Cl |
| A.1612 | 2-丙炔基 | 2-Cl | H | Cl | 6-Cl |
| A.1613 | 2-丙炔基 | 2-Cl | H | Cl | -OCH3 |
| A.1614 | 2-丙炔基 | 2-Cl | H | Cl | 4-OCH3 |
| A.1615 | 2-丙炔基 | 2-Cl | H | Cl | 3-CF3 |
| A.1616 | 2-丙炔基 | 2-Cl | H | Cl | 6-CH3 |
| A.1617 | 2-丙炔基 | 2-Cl | H | Cl | 6-C6H5 |
| A.1618 | 2-丁炔基 | 2-Cl | H | Cl | H |
| A.1619 | 3-丁炔-2-基 | 2-Cl | H | Cl | H |
| A.1620 | 氰基甲基 | 2-Cl | H | Cl | H |
| A.1621 | 甲氧基羰基甲基 | 2-Cl | H | Cl | H |
| A.1622 | 叔丁氧基羰基甲基 | 2-Cl | H | Cl | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1623 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | Cl | H |
| A.1624 | 环丙基甲基 | 2-Cl | H | Cl | H |
| A.1625 | 1-甲基环戊基 | 2-Cl | H | Cl | H |
| A.1626 | 环己基 | 2-Cl | H | Cl | H |
| A.1627 | 1-甲氧基丙-2-基 | 2-Cl | H | Cl | H |
| A.1628 | 苄基 | 2-Cl | H | Cl | H |
| A.1629 | 苄基 | 2-Cl | H | Cl | 3-Cl |
| A.1630 | 苄基 | 2-Cl | H | Cl | 4-Cl |
| A.1631 | 苄基 | 2-Cl | H | Cl | 6-Cl |
| A.1632 | 苄基 | 2-Cl | H | Cl | 3-OCH3 |
| A.1633 | 苄基 | 2-Cl | H | Cl | 4-OCH3 |
| A.1634 | 苄基 | 2-Cl | H | Cl | 3-CF3 |
| A.1635 | 苄基 | 2-Cl | H | Cl | 6-CH3 |
| A.1635 | 苄基 | 2-Cl | H | Cl | 6-C6H5 |
| A.1637 | 3-甲基苄基 | 2-Cl | H | Cl | H |
| A.1638 | 2-氟苄基 | 2-Cl | H | Cl | H |
| A.1639 | 3-氟苄基 | 2-Cl | H | Cl | H |
| A.1640 | 4-氯苄基 | 2-Cl | H | Cl | H |
| A.1641 | 3,4-二氯苄基 | 2-Cl | H | Cl | H |
| A.1642 | 2,6-二氟苄基 | 2-Cl | H | Cl | H |
| A.1643 | 3-三氟甲基苄基 | 2-Cl | H | Cl | H |
| A.1644 | 3-氰基苄基 | 2-Cl | H | Cl | H |
| A.1645 | 4-甲氧基苄基 | 2-Cl | H | Cl | H |
| A.1646 | 4-甲氧基羰基苄基 | 2-Cl | H | Cl | H |
| A.1647 | 3-苯基苄基 | 2-Cl | H | Cl | H |
| A.1648 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | Cl | H |
| A.1649 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | Cl | H |
| A.1650 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | Cl | H |
| A.1651 | 1-苯基乙基 | 2-Cl | H | Cl | H |
| A.1652 | 1-(4-甲基苯基)乙基 | 2-Cl | H | Cl | H |
| A.3653 | 1-(4-氯苯基)乙基 | 2-Cl | H | Cl | H |
| A.1654 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | Cl | H |
| A.1655 | 2-苯基乙基 | 2-Cl | H | Cl | H |
| A.1656 | 3-苯基丙-1-基 | 2-Cl | H | Cl | H |
| A.1657 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | Cl | H |
| A.1658 | 甲基 | 2-Cl | H | Br | H |
| A.1659 | 甲基 | 2-Cl | H | Br | 3-Cl |
| A.1660 | 甲基 | 2-Cl | H | Br | 4-Cl |
| A.1661 | 甲基 | 2-Cl | H | Br | 6-Cl |
| A.1662 | 甲基 | 2-Cl | H | Br | 3-OCH3 |
| A.1663 | 甲基 | 2-Cl | H | Br | 4-OCH3 |
| A.1664 | 甲基 | 2-Cl | H | Br | 3-CF3 |
| A.1665 | 甲基 | 2-Cl | H | Br | 6-CH3 |
| A.1666 | 甲基 | 2-Cl | H | Br | 6-C6H5 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1567 | 乙基 | 2-Cl | H | Br | H |
| A.1668 | 正丙基 | 2-Cl | H | Br | H |
| A.1669 | 异丙基 | 2-Cl | H | Br | H |
| A.1670 | 正丁基 | 2-Cl | H | Br | H |
| A.1671 | 异丁基 | 2-Cl | H | Br | H |
| A.1672 | 仲丁基 | 2-Cl | H | Br | H |
| A.1673 | 叔丁基 | 2-Cl | H | Br | H |
| A.1674 | 正戊基 | 2-Cl | H | Br | H |
| A.1675 | 正己基 | 2-Cl | H | Br | H |
| A.1676 | 2-丙烯基 | 2-Cl | H | Br | H |
| A.1677 | 2-丙烯基 | 2-Cl | H | Br | 3-Cl |
| A.1678 | 2-丙烯基 | 2-Cl | H | Br | 4-Cl |
| A.1679 | 2-丙烯基 | 2-Cl | H | Br | 6-Cl |
| A.1680 | 2-丙烯基 | 2-Cl | H | Br | 3-OCH3 |
| A.1681 | 2-丙烯基 | 2-Cl | H | Br | 4-OCH3 |
| A.1682 | 2-丙烯基 | 2-Cl | H | Br | 3-CF3 |
| A.1683 | 2-丙烯基 | 2-Cl | H | Br | 6-CH3 |
| A.1684 | 2-丙烯基 | 2-Cl | H | Br | 6-C6H5 |
| A.1685 | (E)-3-氯-2-丙烯基 | 2-Cl | H | Br | H |
| A.1686 | 2-氯-2-丙烯基 | 2-Cl | H | Br | H |
| A.1687 | (E)-2-丁烯基 | 2-Cl | H | Br | H |
| A.1688 | 2-甲基-2-丙烯基 | 2-Cl | H | Br | H |
| A.1689 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | Br | H |
| A.1690 | 3-甲基-2-丁烯基 | 2-Cl | H | Br | H |
| A.1691 | 2-丙炔基 | 2-Cl | H | Br | H |
| A.1592 | 2-丙炔基 | 2-Cl | H | Br | 3-Cl |
| A.1693 | 2-丙炔基 | 2-Cl | H | Br | 4-Cl |
| A.1694 | 2-丙炔基 | 2-Cl | H | Br | 6-Cl |
| A.1695 | 2-丙炔基 | 2-Cl | H | Br | 3-OCH3 |
| A.1696 | 2-丙炔基 | 2-Cl | H | Br | 4-OCH3 |
| A.1697 | 2-丙炔基 | 2-Cl | H | Br | 3-CF3 |
| A.1698 | 2-丙炔基 | 2-Cl | H | Br | 6-CH3 |
| A.1699 | 2-丙炔基 | 2-Cl | H | Br | 6-C6H5 |
| A.1700 | 2-丁炔基 | 2-Cl | H | Br | H |
| A.1701 | 3-丁炔-2-基 | 2-Cl | H | Br | H |
| A.1702 | 氰基甲基 | 2-Cl | H | Br | H |
| A.1703 | 甲氧羰基甲基 | 2-Cl | H | Br | H |
| A.1704 | 叔丁氧基羰基甲基 | 2-Cl | H | Br | H |
| A.1705 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | Br | H |
| A.1706 | 环丙基甲基 | 2-Cl | H | Br | H |
| A.1707 | 1-甲基环戊基 | 2-Cl | H | Br | H |
| A.1708 | 环己基 | 2-Cl | H | Br | H |
| A.1709 | 1-甲氧基丙-2-基 | 2-Cl | H | Br | H |
| A.1710 | 苄基 | 2-Cl | H | Br | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1711 | 苄基 | 2-Cl | H | Br | 3-Cl |
| A.1712 | 苄基 | 2-Cl | H | Br | 4-Cl |
| A.1713 | 苄基 | 2-Cl | H | Br | 6-Cl |
| A.1714 | 苄基 | 2-Cl | H | Br | 3-OCH3 |
| A.1715 | 苄基 | 2-Cl | H | Br | 4-OCH3 |
| A.1716 | 苄基 | 2-Cl | H | Br | 3-CF3 |
| A.1717 | 苄基 | 2-Cl | H | Br | 6-CH3 |
| A.1718 | 苄基 | 2-Cl | H | Br | 6-C6H5 |
| A.1719 | 3-甲基苄基 | 2-Cl | H | Br | H |
| A.1720 | 2-氟苄基 | 2-Cl | H | Br | H |
| A.1721 | 3-氟苄基 | 2-Cl | H | Br | H |
| A.1722 | 4-氯苄基 | 2-Cl | H | Br | H |
| A.1723 | 3,4-二氯苄基 | 2-Cl | H | Br | H |
| A.1724 | 2,6-二氟苄基 | 2-Cl | H | Br | H |
| A.1725 | 3-三氟甲基苄基 | 2-Cl | H | Br | H |
| A.1726 | 3-氰基苄基 | 2-Cl | H | Br | H |
| A.1727 | 4-甲氧基苄基 | 2-Cl | H | Br | H |
| A.1728 | 4-甲氧基羰基苄基 | 2-Cl | H | Br | H |
| A.1729 | 3-苯基苄基 | 2-Cl | H | Br | H |
| A.1730 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | Br | H |
| A.1731 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | Br | H |
| A.1732 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | Br | H |
| A.1733 | 1-苯基乙基 | 2-Cl | H | Br | H |
| A.1734 | 1-(4-甲基苯基)乙基 | 2-Cl | H | Br | H |
| A.1735 | 1-(4-氯苯基)乙基 | 2-Cl | H | Br | H |
| A.1736 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | Br | H |
| A.1737 | 2-苯基乙基 | 2-Cl | H | Br | H |
| A.1738 | 3-苯基丙-1-基 | 2-Cl | H | Br | H |
| A.1739 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | Br | H |
| A.1740 | 甲基 | 2-Cl | H | CN | H |
| A.1741 | 甲基 | 2-Cl | H | CN | 3-Cl |
| A.1742 | 甲基 | 2-Cl | H | CN | 4-Cl |
| A.1743 | 甲基 | 2-Cl | H | CN | 6-Cl |
| A.1744 | 甲基 | 2-Cl | H | CN | 3-OCH3 |
| A.1745 | 甲基 | 2-Cl | H | CN | 4-OCH3 |
| A.1746 | 甲基 | 2-Cl | H | CN | 3-CF3 |
| A.1747 | 甲基 | 2-Cl | H | CN | 6-CH3 |
| A.1748 | 甲基 | 2-Cl | H | CN | 6-C6H5 |
| A.1749 | 乙基 | 2-Cl | H | CN | H |
| A.1750 | 正丙基 | 2-Cl | H | CN | H |
| A.1751 | 异丙基 | 2-Cl | H | CN | H |
| A.1752 | 正丁基 | 2-Cl | H | CN | H |
| A.1753 | 异丁基 | 2-Cl | H | CN | H |
| A.1754 | 仲丁基 | 2-Cl | H | CN | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1755 | 叔丁基 | 2-Cl | H | CN | H |
| A.1756 | 正戊基 | 2-Cl | H | CN | H |
| A.1757 | 正己基 | 2-Cl | H | CN | H |
| A.1758 | 2-丙烯基 | 2-Cl | H | CN | H |
| A.1759 | 2-丙烯基 | 2-Cl | H | CN | 3-Cl |
| A.1760 | 2-丙烯基 | 2-Cl | H | CN | 4-Cl |
| A.1761 | 2-丙烯基 | 2-Cl | H | CN | 6-Cl |
| A.1762 | 2-丙烯基 | 2-Cl | H | CN | 3-OCH3 |
| A.1763 | 2-丙烯基 | 2-Cl | H | CN | 4-OCH3 |
| A.1764 | 2-丙烯基 | 2-Cl | H | CN | 3-CF3 |
| A.1765 | 2-丙烯基 | 2-Cl | H | CN | 6-CH3 |
| A.1766 | 2-丙烯基 | 2-Cl | H | CN | 6-C6H5 |
| A.1767 | (E)-3-氯-2-丙烯基 | 2-Cl | H | CN | H |
| A.1768 | 2-氯-2-丙烯基 | 2-Cl | H | CN | H |
| A.1769 | (E)-2-丁烯基 | 2-Cl | H | CN | H |
| A.1770 | 2-甲基-2-丙烯基 | 2-Cl | H | CN | H |
| A.1771 | (Z)-3-氯-2-丁烯基 | 2-Cl | H | CN | H |
| A.1772 | 3-甲基-2-丁烯基 | 2-Cl | H | CN | H |
| A.1773 | 2-丙炔基 | 2-Cl | H | CN | H |
| A.1774 | 2-丙炔基 | 2-Cl | H | CN | 3-Cl |
| A.1775 | 2-丙炔基 | 2-Cl | H | CN | 4-Cl |
| A.1776 | 2-丙炔基 | 2-Cl | H | CN | 6-Cl |
| A.1777 | 2-丙炔基 | 2-Cl | H | CN | 3-OCH3 |
| A.1778 | 2-丙炔基 | 2-Cl | H | CN | 4-OCH3 |
| A.1779 | 2-丙炔基 | 2-Cl | H | CN | 3-CF3 |
| A.1780 | 2-丙炔基 | 2-Cl | H | CN | 6-CH3 |
| A.1781 | 2-丙炔基 | 2-Cl | H | CN | 6-C6H5 |
| A.1782 | 2-丁炔基 | 2-Cl | H | CN | H |
| A.1783 | 3-丁炔-2-基 | 2-Cl | H | CN | H |
| A.1784 | 氰基甲基 | 2-Cl | H | CN | H |
| A.1785 | 甲氧基羰基甲基 | 2-Cl | H | CN | H |
| A.1786 | 叔丁氧基羰基甲基 | 2-Cl | H | CN | H |
| A.1787 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | CN | H |
| A.1788 | 环丙基甲基 | 2-Cl | H | CN | H |
| A.1789 | 1-甲基环戊基 | 2-Cl | H | CN | H |
| A.1790 | 环己基 | 2-Cl | H | CN | H |
| A.1791 | 1-甲氧基丙-2-基 | 2-Cl | H | CN | H |
| A.1792 | 苄基 | 2-Cl | H | CN | H |
| A.1793 | 苄基 | 2-Cl | H | CN | 3-Cl |
| A.1794 | 苄基 | 2-Cl | H | CN | 4-Cl |
| A.1795 | 苄基 | 2-Cl | H | CN | 6-Cl |
| A.1796 | 苄基 | 2-Cl | H | CN | 3-OCH3 |
| A.1797 | 苄基 | 2-Cl | H | CN | 4-OCH3 |
| A.1798 | 苄基 | 2-Cl | H | CN | 3-CF3 |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1799 | 苄基 | 2-Cl | H | CN | 6-CH3 |
| A.1800 | 苄基 | 2-Cl | H | CN | 6-C6H5 |
| A.1801 | 3-甲基苄基 | 2-Cl | H | CN | H |
| A.1802 | 2-氟苄基 | 2-Cl | H | CN | H |
| A.1803 | 3-氟苄基 | 2-Cl | H | CN | H |
| A.1804 | 4-氯苄基 | 2-Cl | H | CN | H |
| A.1805 | 3,4-二氯苄基 | 2-Cl | H | CN | H |
| A.1806 | 2,6-二氟苄基 | 2-Cl | H | CN | H |
| A.1807 | 3-三氟甲基苄基 | 2-Cl | H | CN | H |
| A.1808 | 3-氰基苄基 | 2-Cl | H | CN | H |
| A.1809 | 4-甲氧基苄基 | 2-Cl | H | CN | H |
| A.1810 | 4-甲氧基羰基苄基 | 2-Cl | H | CN | H |
| A.1811 | 3-苯基苄基 | 2-Cl | H | CN | H |
| A.1812 | (5-氯-3-噻吩基)甲基 | 2-Cl | H | CN | H |
| A.1813 | (2,5-二氯-3-噻吩基)甲基 | 2-Cl | H | CN | H |
| A.1814 | (1,3-二氧杂环戊-2-基)甲基 | 2-Cl | H | CN | H |
| A.1815 | 1-苯基乙基 | 2-Cl | H | CN | H |
| A.1816 | 1-(4-甲基苯基)乙基 | 2-Cl | H | CN | H |
| A.1817 | 1-(4-氯苯基)乙基 | 2-Cl | H | CN | H |
| A.1818 | 1-(3-三氟甲基苯基)乙基 | 2-Cl | H | CN | H |
| A.1819 | 2-苯基乙基 | 2-Cl | H | CN | H |
| A.1820 | 3-苯基丙-1-基 | 2-Cl | H | CN | H |
| A.1821 | 4-(4-氯苯基)-2-丁烯基 | 2-Cl | H | CN | H |
| A.1822 | 甲基 | 2-Cl | H | OCH2C≡CH | H |
| A.1823 | 乙基 | 2-Cl | H | OCH2C≡CH | H |
| A.1824 | 2-丙烯基 | 2-Cl | H | OCH2C≡CH | H |
| A.1825 | 2-丙炔基 | 2-Cl | H | OCH2C≡CH | H |
| A.1826 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OCH2C≡CH | H |
| A.1827 | 3-甲基苄基 | 2-Cl | H | OCH2C≡CH | H |
| A.1828 | 1-苯基乙基 | 2-Cl | H | OCH2C≡CH | H |
| A.1829 | 甲基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1830 | 乙基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1831 | 2-丙烯基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1832 | 2-丙炔基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1833 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1834 | 3-甲基苄基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1835 | 1-苯基乙基 | 2-Cl | H | OCH2CH2C6H5 | H |
| A.1836 | 甲基 | 2-Cl | H | SCH2CH3 | H |
| A.1837 | 乙基 | 2-Cl | H | SCH2CH3 | H |
| A.1838 | 2-丙烯基 | 2-Cl | H | SCH2CH3 | H |
| A.1839 | 2-丙炔基 | 2-Cl | H | SCH2CH3 | H |
| A.1840 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | SCH2CH3 | H |
| A.1841 | 3-甲基苄基 | 2-Cl | H | SCH2CH3 | H |
| A.1842 | 1-苯基乙基 | 2-Cl | H | SCH2CH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1843 | 甲基 | 2-Cl | H | NH-CH3 | H |
| A.1844 | 乙基 | 2-Cl | H | NH-CH3 | H |
| A.1845 | 2-丙烯基 | 2-Cl | H | NH-CH3 | H |
| A.1846 | 2-丙炔基 | 2-Cl | H | NH-CH3 | H |
| A.1847 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | NH-CH3 | H |
| A.1848 | 3-甲基苄基 | 2-Cl | H | NH-CH3 | H |
| A.1849 | 1-苯基乙基 | 2-Cl | H | NH-CH3 | H |
| A.1850 | 甲基 | 2-Cl | H | N(CH3)2 | H |
| A.1851 | 乙基 | 2-Cl | H | N(CH3)2 | H |
| A.1852 | 2-丙烯基 | 2-Cl | H | N(CH3)2 | H |
| A.1853 | 2-丙炔基 | 2-Cl | H | N(CH3)2 | H |
| A.1854 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | N(CH3)2 | H |
| A.1855 | 3-甲基苄基 | 2-Cl | H | N(CH3)2 | H |
| A.1856 | 1-苯基乙基 | 2-Cl | H | N(CH3)2 | H |
| A.1857 | 甲基 | 2-Cl | H | OC6H5 | H |
| A.1858 | 乙基 | 2-Cl | H | OC6H5 | H |
| A.1859 | 2-丙烯基 | 2-Cl | H | OC6H5 | H |
| A.1860 | 2-丙炔基 | 2-Cl | H | OC6H5 | H |
| A.1861 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | OC6H5 | H |
| A.1862 | 3-甲基丁基 | 2-Cl | H | OC6H5 | H |
| A.1863 | 1-苯基乙基 | 2-Cl | H | OC6H5 | H |
| A.1864 | 甲基 | 2-Cl | H | SC6H5 | H |
| A.1865 | 乙基 | 2-Cl | H | SC6H5 | H |
| A.1866 | 2-丙烯基 | 2-Cl | H | SC6H5 | H |
| A.1867 | 2-丙炔基 | 2-Cl | H | SC6H5 | H |
| A.1868 | 1-(叔丁氧基羰基)乙基 | 2-Cl | H | SC6H5 | H |
| A.1869 | 3-甲基苄基 | 2-Cl | H | SC6H5 | H |
| A.1870 | 1-苯基乙基 | 2-Cl | H | SC6H5 | H |
| A.1871 | 甲基 | 2-F | H | OCH3 | H |
| A.1872 | 甲基 | 2-F | H | SCH3 | H |
| A.1873 | 甲基 | 2-F | H | Cl | H |
| A.1874 | 甲基 | 2-F | H | Br | H |
| A.1875 | 甲基 | 2-F | H | OC6H5 | H |
| A.1876 | 甲基 | 2-F | H | SC6H5 | H |
| A.1877 | 乙基 | 2-F | H | OCH3 | H |
| A.1878 | 乙基 | 2-F | H | OCH3 | 3-Cl |
| A.1879 | 乙基 | 2-F | H | OCH3 | 3-OCH3 |
| A.1880 | 乙基 | 2-F | H | SCH3 | H |
| A.1881 | 乙基 | 2-F | H | Cl | H |
| A.1882 | 乙基 | 2-F | H | Br | H |
| A.1883 | 乙基 | 2-F | H | OC6H5 | H |
| A.1884 | 乙基 | 2-F | H | SC6H5 | H |
| A.1885 | 2-丙烯基 | 2-F | H | OCH3 | H |
| A.1886 | 2-丙烯基 | 2-F | H | SCH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1887 | 2-丙烯基 | 2-F | H | Cl | H |
| A.1888 | 2-丙烯基 | 2-F | H | Br | H |
| A.1889 | 苄基 | 2-F | H | OCH3 | H |
| A.1890 | 苄基 | 2-F | H | SCH3 | H |
| A.1891 | 苄基 | 2-F | H | Cl | H |
| A.1892 | 苄基 | 2-F | H | Br | H |
| A.1893 | 甲基 | 2-CN | H | OCH3 | H |
| A.1894 | 甲基 | 2-CN | H | SCH3 | H |
| A.1895 | 甲基 | 2-CN | H | Cl | H |
| A.1896 | 甲基 | 2-CN | H | Br | H |
| A.1897 | 甲基 | 2-CN | H | OC6H5 | H |
| A.1898 | 甲基 | 2-CN | H | SC6H5 | H |
| A.1899 | 乙基 | 2-CN | H | OCH3 | H |
| A.1900 | 乙基 | 2-CN | H | OCH3 | 3-Cl |
| A.1901 | 乙基 | 2-CN | H | OCH3 | 3-OCH3 |
| A.1902 | 乙基 | 2-CN | H | SCH3 | H |
| A.1903 | 乙基 | 2-CN | H | Cl | H |
| A.1904 | 乙基 | 2-CN | H | Br | H |
| A.1905 | 乙基 | 2-CN | H | OC6H5 | H |
| A.1906 | 乙基 | 2-CN | H | SC6H5 | H |
| A.1907 | 2-丙烯基 | 2-CN | H | OCH3 | H |
| A.1908 | 2-丙烯基 | 2-CN | H | SCH3 | H |
| A.1909 | 2-丙烯基 | 2-CN | H | Cl | H |
| A.1910 | 2-丙烯基 | 2-CN | H | Br | H |
| A.1911 | 苄基 | 2-CN | H | OCH3 | H |
| A.1912 | 苄基 | 2-CN | H | SCH3 | H |
| A.1913 | 苄基 | 2-CN | H | Cl | H |
| A.1914 | 苄基 | 2-CN | H | Br | H |
| A.1915 | 甲基 | 5-CH3 | H | OCH3 | H |
| A.1916 | 甲基 | 5-CH3 | H | SCH3 | H |
| A.1917 | 甲基 | 5-CH3 | H | Cl | H |
| A.1918 | 甲基 | 5-CH3 | H | Br | H |
| A.1919 | 甲基 | 5-CH3 | H | OC6H5 | H |
| A.1920 | 甲基 | 5-CH3 | H | SC6H5 | H |
| A.1921 | 乙基 | 5-CH3 | H | OCH3 | H |
| A.1922 | 乙基 | 5-CH3 | H | OCH3 | 3-Cl |
| A.1923 | 乙基 | 5-CH3 | H | OCH3 | 3-OCH3 |
| A.1924 | 乙基 | 5-CH3 | H | SCH3 | H |
| A.1925 | 乙基 | 5-CH3 | H | Cl | H |
| A.1926 | 乙基 | 5-CH3 | H | Br | H |
| A.1927 | 乙基 | 5-CH3 | H | OC6H5 | H |
| A.1928 | 乙基 | 5-CH3 | H | SC6H5 | H |
| A.1929 | 2-丙烯基 | 5-CH3 | H | OCH3 | H |
| A.1930 | 2-丙烯基 | 5-CH3 | H | SCH3 | H |
| No. | R1 | R2 | R3 | R4 | R5 n |
| A.1931 | 2-丙烯基 | 5-CH3 | H | Cl | H |
| A.1932 | 2-丙烯基 | 5-CH3 | H | Br | H |
| A.1933 | 苄基 | 5-CH3 | H | OCH3 | H |
| A.1934 | 苄基 | 5-CH3 | H | SCH3 | H |
| A.1935 | 苄基 | 5-CH3 | H | Cl | H |
| A.1936 | 苄基 | 5-CH3 | H | Br | H |
| A.1937 | 甲基 | 2-Cl | 5-Cl | OCH3 | H |
| A.1938 | 甲基 | 2-Cl | 5-Cl | SCH3 | H |
| A.1939 | 甲基 | 2-Cl | 5-Cl | Cl | H |
| A.1940 | 甲基 | 2-Cl | 5-Cl | Br | H |
| A.1941 | 甲基 | 2-Cl | 5-Cl | OC6H5 | H |
| A.1942 | 甲基 | 2-Cl | 5-Cl | SC6H5 | H |
| A.1943 | 甲基 | 2-Cl | 5-Cl | OCH3 | H |
| A.1944 | 甲基 | 2-Cl | 5-Cl | OCH3 | 3-Cl |
| A.1945 | 甲基 | 2-Cl | 5-Cl | OCH3 | 3-OCH3 |
| A.1946 | 甲基 | 2-Cl | 5-Cl | SCH3 | H |
| A.1947 | 甲基 | 2-Cl | 5-Cl | Cl | H |
| A.1948 | 甲基 | 2-Cl | 5-Cl | Br | H |
| A.1949 | 甲基 | 2-Cl | 5-Cl | OC6H5 | H |
| A.1950 | 甲基 | 2-Cl | 5-Cl | SC6H5 | H |
| A.1951 | 2-丙烯基 | 2-Cl | 5-Cl | OCH3 | H |
| A.1952 | 2-丙烯基 | 2-Cl | 5-Cl | SCH3 | H |
| A.1953 | 2-丙烯基 | 2-Cl | 5-Cl | Cl | H |
| A.1954 | 2-丙烯基 | 2-Cl | 5-Cl | Br | H |
| A.1955 | 苄基 | 2-Cl | 5-Cl | OCH3 | H |
| A.1956 | 苄基 | 2-Cl | 5-Cl | SCH3 | H |
| A.1957 | 苄基 | 2-Cl | 5-Cl | Cl | H |
| A.1958 | 苄基 | 2-Cl | 5-Cl | Br | H |
| No. | R1 | R2 | R3 | R4 | (R5)n |
| B.001 | 甲基 | 2-CH3 | H | OCH3 | H |
| B.002 | 甲基 | 2-CH3 | H | OCH3 | 3-Cl |
| B.003 | 甲基 | 2-CH3 | H | OCH3 | 4-Cl |
| B.004 | 甲基 | 2-CH3 | H | OCH3 | 6-Cl |
| B.005 | 甲基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| B.006 | 甲基 | 2-CH3 | H | OCH3 | 6-CH3 |
| B.007 | 乙基 | 2-CH3 | H | OCH3 | H |
| B.008 | 异丙基 | 2-CH3 | H | OCH3 | H |
| B.009 | 2-丙烯基 | 2-CH3 | H | OCH3 | H |
| B.010 | 2-丙烯基 | 2-CH3 | H | OCH3 | 3-Cl |
| B.011 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | OCH3 | H |
| B.012 | 2-丙炔基 | 2-CH3 | H | OCH3 | H |
| B.013 | 2-丙炔基 | 2-CH3 | H | OCH3 | 3-Cl |
| B.014 | 2-丙炔基 | 2-CH3 | H | OCH3 | 3-OCH3 |
| B.015 | 2-丙炔基 | 2-CH3 | H | OCH3 | 6-CH3 |
| B.016 | 氰基甲基 | 2-CH3 | H | OCH3 | H |
| B.017 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OCH3 | H |
| B.018 | 环丙基甲基 | 2-CH3 | H | OCH3 | H |
| B.019 | 苄基 | 2-CH3 | H | OCH3 | H |
| B.020 | 3-甲基苄基 | 2-CH3 | H | OCH3 | H |
| B.021 | 3-甲基苄基 | 2-CH3 | H | OCH3 | 3-Cl |
| B.022 | 1-(4-氯苯基)乙基 | 2-CH3 | H | OCH3 | H |
| B.023 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | OCH3 | H |
| B.024 | 甲基 | 2-CH3 | H | OC2H5 | H |
| B.025 | 甲基 | 2-CH3 | H | OC2H5 | 3-Cl |
| B.026 | 甲基 | 2-CH3 | H | OC2H5 | 4-Cl |
| B.027 | 甲基 | 2-CH3 | H | OC2H5 | 6-Cl |
| B.028 | 甲基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| B.029 | 甲基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| B.030 | 乙基 | 2-CH3 | H | OC2H5 | H |
| B.031 | 异丙基 | 2-CH3 | H | OC2H5 | H |
| B.032 | 2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| B.033 | 2-丙烯基 | 2-CH3 | H | OC2H5 | 3-Cl |
| B.034 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | OC2H5 | H |
| B.035 | 2-丙炔基 | 2-CH3 | H | OC2H5 | H |
| B.036 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 3-Cl |
| B.037 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 3-OCH3 |
| B.038 | 2-丙炔基 | 2-CH3 | H | OC2H5 | 6-CH3 |
| B.039 | 氰基甲基 | 2-CH3 | H | OC2H5 | H |
| B.040 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | OC2H5 | H |
| B.041 | 环丙基甲基 | 2-CH3 | H | OC2H5 | H |
| B.042 | 苄基 | 2-CH3 | H | OC2H5 | H |
| B.043 | 3-甲基苄基 | 2-CH3 | H | OC2H5 | H |
| B.044 | 3-甲基苄基 | 2-CH3 | H | OC2H5 | 3-Cl |
| B.045 | 1-(4-氯苯基)乙基 | 2-CH3 | H | OC2H5 | H |
| B.046 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | OC2H5 | H |
| B.047 | 甲基 | 2-CH3 | H | Cl | H |
| B.048 | 甲基 | 2-CH3 | H | Cl | 3-Cl |
| B.049 | 甲基 | 2-CH3 | H | Cl | 4-Cl |
| B.050 | 甲基 | 2-CH3 | H | Cl | 6-Cl |
| B.051 | 甲基 | 2-CH3 | H | Cl | 3-OCH3 |
| B.052 | 甲基 | 2-CH3 | H | Cl | 6-CH3 |
| B.O53 | 乙基 | 2-CH3 | H | Cl | H |
| B.054 | 异丙基 | 2-CH3 | H | Cl | H |
| B.055 | 2-丙烯基 | 2-CH3 | H | Cl | H |
| B.056 | 2-丙烯基 | 2-CH3 | H | Cl | 3-Cl |
| B.057 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | Cl | H |
| B.058 | 2-丙炔基 | 2-CH3 | H | Cl | H |
| B.059 | 2-丙炔基 | 2-CH3 | H | Cl | 3-Cl |
| B.060 | 2-丙炔基 | 2-CH3 | H | Cl | 3-OCH3 |
| B.061 | 2-丙炔基 | 2-CH3 | H | Cl | 6-CH3 |
| B.062 | 氰基甲基 | 2-CH3 | H | Cl | H |
| B.063 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | Cl | H |
| B.064 | 环丙基甲基methyl | 2-CH3 | H | Cl | H |
| B.065 | 苄基 | 2-CH3 | H | Cl | H |
| B.066 | 3-甲基苄基 | 2-CH3 | H | Cl | H |
| B.067 | 3-甲基苄基 | 2-CH3 | H | Cl | 3-Cl |
| B.068 | 1-(4-氯苯基)乙基 | 2-CH3 | H | Cl | H |
| B.069 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | Cl | H |
| B.070 | 甲基 | 2-CH3 | H | SCH3 | H |
| B.071 | 甲基 | 2-CH3 | H | SCH3 | 3-Cl |
| B.072 | 甲基 | 2-CH3 | H | SCH3 | 4-Cl |
| B.073 | 甲基 | 2-CH3 | H | SCH3 | 6-Cl |
| B.074 | 甲基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| B.075 | 甲基 | 2-CH3 | H | SCH3 | 6-CH3 |
| B.076 | 乙基 | 2-CH3 | H | SCH3 | H |
| B.077 | 异丙基 | 2-CH3 | H | SCH3 | H |
| B.078 | 2-丙烯基 | 2-CH3 | H | SCH3 | H |
| B.079 | 2-丙烯基 | 2-CH3 | H | SCH3 | 3-Cl |
| B.080 | (E)-3-氯-2-丙烯基 | 2-CH3 | H | SCH3 | H |
| B.081 | 2-丙炔基 | 2-CH3 | H | SCH3 | H |
| B.082 | 2-丙炔基 | 2-CH3 | H | SCH3 | 3-Cl |
| B.083 | 2-丙炔基 | 2-CH3 | H | SCH3 | 3-OCH3 |
| B.084 | 2-丙炔基 | 2-CH3 | H | SCH3 | 6-CH3 |
| B.085 | 氰基甲基 | 2-CH3 | H | SCH3 | H |
| B.086 | 1-(叔丁氧基羰基)乙基 | 2-CH3 | H | SCH3 | H |
| B.087 | 环丙基甲基 | 2-CH3 | H | SCH3 | H |
| B.088 | 苄基 | 2-CH3 | H | SCH3 | H |
| B.089 | 3-甲基苄基 | 2-CH3 | H | SCH3 | H |
| B.090 | 3-甲基苄基 | 2-CH3 | H | SCH3 | 3-Cl |
| B.091 | 1-(4-氯苯基)乙基 | 2-CH3 | H | SCH3 | H |
| B.092 | 4-(4-氯苯基)-2-丁烯基 | 2-CH3 | H | SCH3 | H |
| B.093 | 甲基 | 6-CH3 | H | SCH3 | H |
| B.094 | 甲基 | 6-CH3 | H | OCH3 | 3-Cl |
| B.095 | 甲基 | 6-CH3 | H | OCH3 | 4-Cl |
| B.096 | 甲基 | 6-CH3 | H | OCH3 | 6-Cl |
| B.097 | 甲基 | 6-CH3 | H | OCH3 | 3-OCH3 |
| B.098 | 甲基 | 6-CH3 | H | OCH3 | 6-CH3 |
| B.099 | 乙基 | 6-CH3 | H | OCH3 | H |
| B.100 | 异丙基 | 6-CH3 | H | OCH3 | H |
| B.101 | 2-丙烯基 | 6-CH3 | H | OCH3 | H |
| B.102 | 2-丙烯基 | 6-CH3 | H | OCH3 | 3-Cl |
| B.103 | (E)-3-氯-2-丙烯基 | 6-CH3 | H | OCH3 | H |
| B.104 | 2-丙炔基 | 6-CH3 | H | OCH3 | H |
| B.105 | 2-丙炔基 | 6-CH3 | H | OCH3 | 3-Cl |
| B.106 | 2-丙炔基 | 6-CH3 | H | OCH3 | 3-OCH3 |
| B.107 | 2-丙炔基 | 6-CH3 | H | OCH3 | 6-CH3 |
| B.108 | 氰基甲基 | 6-CH3 | H | OCH3 | H |
| B.109 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | H | OCH3 | H |
| B.110 | 环丙基甲基 | 6-CH3 | H | OCH3 | H |
| B.111 | 苄基 | 6-CH3 | H | OCH3 | H |
| B.112 | 3-甲基苄基 | 6-CH3 | H | OCH3 | H |
| 8.113 | 3-甲基苄基 | 6-CH3 | H | OCH3 | 3-C1 |
| B.114 | 1-(4-氯苯基)乙基 | 6-CH3 | H | OCH3 | H |
| B.115 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | H | OCH3 | H |
| B.116 | 甲基 | 6-CH3 | H | OC2H5 | H |
| B.117 | 甲基 | 6-CH3 | H | OC2H5 | 3-Cl |
| B.118 | 甲基 | 6-CH3 | H | OC2H5 | 4-Cl |
| B.119 | 甲基 | 6-CH3 | H | OC2H5 | 6-Cl |
| B.120 | 甲基 | 6-CH3 | H | OC2H5 | 3-OCH3 |
| B.121 | 甲基 | 6-CH3 | H | OC2H5 | 6-CH3 |
| B.122 | 乙基 | 6-CH3 | H | OC2H5 | H |
| B.123 | 异丙基 | 6-CH3 | H | OC2H5 | H |
| B.124 | 2-丙烯基 | 6-CH3 | H | OC2H5 | H |
| B.125 | 2-丙烯基 | 6-CH3 | H | OC2H5 | 3-Cl |
| B.126 | (E)-3-氯-2-丙烯基 | 6-CH3 | H | OC2H5 | H |
| B.127 | 2-丙炔基 | 6-CH3 | H | OC2H5 | H |
| B.128 | 2-丙炔基 | 6-CH3 | H | OC2H5 | 3-Cl |
| B.129 | 2-丙炔基 | 6-CH3 | H | OC2H5 | 3-OCH3 |
| B.130 | 2-丙炔基 | 6-CH3 | H | OC2H5 | 6-CH3 |
| B.131 | 氰基甲基 | 6-CH3 | H | OC2H5 | H |
| B.132 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | H | OC2H5 | H |
| B.133 | 环丙基甲基 | 6-CH3 | H | OC2H5 | H |
| B.134 | 苄基 | 6-CH3 | H | OC2H5 | H |
| B.135 | 3-甲基苄基 | 6-CH3 | H | OC2H5 | H |
| B.136 | 3-甲基苄基 | 6-CH3 | H | OC2H5 | 3-Cl |
| B.137 | 1-(4-氯苯基)乙基 | 6-CH3 | H | OC2H5 | H |
| B.138 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | H | OC2H5 | H |
| B.139 | 甲基 | 6-CH3 | H | SCH3 | H |
| B.140 | 甲基 | 6-CH3 | H | SCH3 | 3-Cl |
| B.141 | 甲基 | 6-CH3 | H | SCH3 | 4-Cl |
| B.142 | 甲基 | 6-CH3 | H | SCH3 | 6-Cl |
| B.143 | 甲基 | 6-CH3 | H | SCH3 | 3-OCH3 |
| B.144 | 甲基 | 6-CH3 | H | SCH3 | 6-CH3 |
| B.145 | 乙基 | 6-CH3 | H | SCH3 | H |
| B.146 | 异丙基 | 6-CH3 | H | SCH3 | H |
| B.147 | 2-丙烯基 | 6-CH3 | H | SCH3 | H |
| B.148 | 2-丙烯基 | 6-CH3 | H | SCH3 | 3-Cl |
| B.149 | (E)-3-氯-2-丙烯基 | 6-CH3 | H | SCH3 | H |
| B.150 | 2-丙炔基 | 6-CH3 | H | SCH3 | H |
| B.151 | 2-丙炔基 | 6-CH3 | H | SCH3 | 3-Cl |
| B.152 | 2-丙炔基 | 6-CH3 | H | SCH3 | 3-OCH3 |
| B.153 | 2-丙炔基 | 6-CH3 | H | SCH3 | 6-CH3 |
| B.154 | 氰基甲基 | 6-CH3 | H | SCH3 | H |
| B.155 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | H | SCH3 | H |
| B.156 | 环丙基甲基 | 6-CH3 | H | SCH3 | H |
| B.157 | 苄基 | 6-CH3 | H | SCH3 | H |
| B.158 | 3-甲基苄基 | 6-CH3 | H | SCH3 | H |
| B.159 | 3-甲基苄基 | 6-CH3 | H | SCH3 | 3-Cl |
| B.160 | 1-(4-氯苯基)乙基 | 6-CH3 | H | SCH3 | H |
| B.161 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | H | SCH3 | H |
| B.162 | 甲基 | 6-CH3 | H | Cl | H |
| B.163 | 甲基 | 6-CH3 | H | Cl | 3-Cl |
| B.164 | 甲基 | 6-CH3 | H | Cl | 4-Cl |
| B.165 | 甲基 | 6-CH3 | H | Cl | 6-Cl |
| B.166 | 甲基 | 6-CH3 | H | Cl | 3-OCH3 |
| B.167 | 甲基 | 6-CH3 | H | Cl | 6-CH3 |
| B.168 | 乙基 | 6-CH3 | H | Cl | H |
| B.169 | 异丙基 | 6-CH3 | H | Cl | H |
| B.170 | 2-丙烯基 | 6-CH3 | H | Cl | H |
| B.171 | 2-丙烯基 | 6-CH3 | H | Cl | 3-Cl |
| B.172 | (E)-3-氯-2-丙烯基- | 6-CH3 | H | Cl | H |
| B.173 | 2-丙炔基 | 6-CH3 | H | Cl | H |
| B.174 | 2-丙炔基 | 6-CH3 | H | Cl | 3-Cl |
| B.175 | 2-丙炔基 | 6-CH3 | H | Cl | 3-OCH3 |
| B.176 | 2-丙炔基 | 6-CH3 | H | Cl | 6-CH3 |
| B.177 | 氰基甲基 | 6-CH3 | H | Cl | H |
| B.178 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | H | Cl | H |
| B.179 | 环丙基甲基 | 6-CH3 | H | Cl | H |
| B.180 | 苄基 | 6-CH3 | H | Cl | H |
| B.181 | 3-甲基苄基 | 6-CH3 | H | Cl | H |
| B.182 | 3-甲基苄基 | 6-CH3 | H | Cl | 3-Cl |
| B.183 | 1-(4-氯苯基)乙基 | 6-CH3 | H | Cl | H |
| B.184 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | H | Cl | H |
| B.185 | 甲基 | 4-CH3 | H | OCH3 | H |
| B.186 | 甲基 | 4-CH3 | H | OCH3 | 3-Cl |
| B.187 | 甲基 | 4-CH3 | H | OCH3 | 4-Cl |
| B.188 | 甲基 | 4-CH3 | H | OCH3 | 6-Cl |
| B.189 | 甲基 | 4-CH3 | H | OCH3 | 3-OCH3 |
| B.190 | 甲基 | 4-CH3 | H | OCH3 | 6-CH3 |
| B.191 | 乙基 | 4-CH3 | H | OCH3 | H |
| B.192 | 异丙基 | 4-CH3 | H | OCH3 | H |
| B.193 | 2-丙烯基 | 4-CH3 | H | OCH3 | H |
| B.194 | 2-丙烯基 | 4-CH3 | H | OCH3 | 3-Cl |
| B.195 | (E)-3-氯-2-丙烯基 | 4-CH3 | H | OCH3 | H |
| B.196 | 2-丙炔基 | 4-CH3 | H | OCH3 | H |
| B.197 | 2-丙炔基 | 4-CH3 | H | OCH3 | 3-Cl |
| B.198 | 2-丙炔基 | 4-CH3 | H | OCH3 | 3-OCH3 |
| B.199 | 2-丙炔基 | 4-CH3 | H | OCH3 | 6-CH3 |
| B.200 | 氰基甲基 | 4-CH3 | H | OCH3 | H |
| B.201 | 1-(叔丁氧基羰基)乙基 | 4-CH3 | H | OCH3 | H |
| B.202 | 环丙基甲基 | 4-CH3 | H | OCH3 | H |
| B.203 | 苄基 | 4-CH3 | H | OCH3 | H |
| B.204 | 3-甲基苄基 | 4-CH3 | H | OCH3 | H |
| B.205 | 3-甲基苄基 | 4-CH3 | H | OCH3 | 3-Cl |
| B.206 | 1-(4-氯苯基)乙基 | 4-CH3 | H | OCH3 | H |
| B.207 | 4-(4-氯苯基)-2-丁烯基 | 4-CH3 | H | OCH3 | H |
| B.208 | 甲基 | 4-CH3 | H | Cl | H |
| B.209 | 甲基 | 4-CH3 | H | Cl | 3-Cl |
| B.210 | 甲基 | 4-CH3 | H | Cl | 4-Cl |
| B.211 | 甲基 | 4-CH3 | H | Cl | 6-Cl |
| B.212 | 甲基 | 4-CH3 | H | Cl | 3-OCH3 |
| B.213 | 甲基 | 4-CH3 | H | Cl | 6-CH3 |
| B.214 | 乙基 | 4-CH3 | H | Cl | H |
| B.215 | 异丙基 | 4-CH3 | H | Cl | H |
| B.216 | 2-丙烯基 | 4-CH3 | H | Cl | H |
| B.217 | 2-丙烯基 | 4-CH3 | H | Cl | 3-Cl |
| B.218 | (E)-3-氯-2-丙烯基- | 4-CH3 | H | Cl | H |
| B.219 | 2-丙炔基 | 4-CH3 | H | Cl | H |
| B.220 | 2-丙炔基 | 4-CH3 | H | Cl | 3-Cl |
| B.221 | 2-丙炔基 | 4-CH3 | H | Cl | 3-OCH3 |
| B.222 | 2-丙炔基 | 4-CH3 | H | Cl | 6-CH3 |
| B.223 | 氰基甲基 | 4-CH3 | H | Cl | H |
| B.224 | 1-(叔丁氧基羰基)乙基 | 4-CH3 | H | Cl | H |
| B.225 | 环丙基甲基 | 4-CH3 | H | Cl | H |
| B.226 | 苄基 | 4-CH3 | H | Cl | H |
| B.227 | 3-甲基苄基 | 4-CH3 | H | Cl | H |
| B.228 | 3-甲基苄基 | 4-CH3 | H | Cl | 3-Cl |
| B.229 | 1-(4-氯苯基)乙基 | 4-CH3 | H | Cl | H |
| B.230 | 4-(4-氯苯基)-2-丁烯基 | 4-CH3 | H | Cl | H |
| B.231 | 甲基 | 6-Cl | H | OCH3 | H |
| B.232 | 甲基 | 6-Cl | H | OCH3 | 3-Cl |
| B.233 | 甲基 | 6-Cl | H | OCH3 | 4-Cl |
| B.234 | 甲基 | 6-Cl | H | OCH3 | 6-Cl |
| B.235 | 甲基 | 6-Cl | H | OCH3 | 3-OCH3 |
| B.236 | 甲基 | 6-Cl | H | OCH3 | 6-CH3 |
| B.237 | 乙基 | 6-Cl | H | OCH3 | H |
| B.238 | 异丙基 | 6-Cl | H | OCH3 | H |
| B.239 | 2-丙烯基 | 6-Cl | H | OCH3 | H |
| B.240 | 2-丙烯基 | 6-Cl | H | OCH3 | 3-Cl |
| B.241 | (E)-3-氯-2-丙烯基 | 6-Cl | H | OCH3 | H |
| B.242 | 2-丙烯基 | 6-Cl | H | OCH3 | H |
| B.243 | 2-丙烯基 | 6-Cl | H | OCH3 | 3-Cl |
| B.244 | 2-丙烯基 | 6-Cl | H | OCH3 | 3-OCH3 |
| B.245 | 2-丙烯基 | 6-Cl | H | OCH3 | 6-CH3 |
| B.246 | 氰基甲基 | 6-Cl | H | OCH3 | H |
| B.247 | 1-(叔丁氧基羰基)乙基 | 6-Cl | H | OCH3 | H |
| B.248 | 环丙基甲基 | 6-Cl | H | OCH3 | H |
| B.249 | 苄基 | 6-Cl | H | OCH3 | H |
| B.250 | 3-甲基苄基 | 6-Cl | H | OCH3 | H |
| B.251 | 3-甲基苄基 | 6-Cl | H | OCH3 | 3-Cl |
| B.252 | 1-(4-氯苯基)乙基 | 6-Cl | H | OCH3 | H |
| B.253 | 4-(4-氯苯基)-2-丁烯基 | 6-Cl | H | OCH3 | H |
| B.254 | 甲基 | 6-Cl | H | OC2H5 | H |
| B.255 | 甲基 | 6-Cl | H | OC2H5 | 3-Cl |
| B.256 | 甲基 | 6-Cl | H | OC2H5 | 4-Cl |
| B.257 | 甲基 | 6-Cl | H | OC2H5 | 6-Cl |
| B.258 | 甲基 | 6-Cl | H | OC2H5 | 3-OCH3 |
| B.259 | 甲基 | 6-Cl | H | OC2H5 | 6-CH3 |
| B.260 | 乙基 | 6-Cl | H | OC2H5 | H |
| B.261 | 异丙基 | 6-Cl | H | OC2H5 | H |
| B.262 | 2-丙烯基 | 6-Cl | H | OC2H5 | H |
| B.263 | 2-丙烯基 | 6-Cl | H | OC2H5 | 3-Cl |
| B.264 | (E)-3-氯-2-丙烯基 | 6-Cl | H | OC2H5 | H |
| B.265 | 2-丙炔基 | 6-Cl | H | OC2H5 | H |
| B.266 | 2-丙炔基 | 6-Cl | H | OC2H5 | 3-Cl |
| B.267 | 2-丙炔基 | 6-Cl | H | OC2H5 | 3-OMe |
| B.268 | 2-丙炔基 | 6-Cl | H | OC2H5 | 6-CH3 |
| B.269 | 氰基甲基 | 6-Cl | H | OC2H5 | H |
| B.270 | 1-(叔丁氧基羰基)乙基 | 6-Cl | H | OC2H5 | H |
| B.271 | 环丙基甲基 | 6-Cl | H | OC2H5 | H |
| B.272 | 苄基 | 6-Cl | H | OC2H5 | H |
| B.273 | 3-甲基苄基 | 6-Cl | H | OC2H5 | H |
| B.274 | 3-甲基苄基 | 6-Cl | H | OC2H5 | 3-Cl |
| B.275 | 1-(4-氯苯基)乙基 | 6-Cl | H | OC2H5 | H |
| B.276 | 4-(4-氯苯基)-2-丁烯基 | 6-Cl | H | OC2H5 | H |
| B.277 | 甲基 | 6-Cl | H | SCH3 | H |
| B.278 | 甲基 | 6-Cl | H | SCH3 | 3-Cl |
| B.279 | 甲基 | 6-Cl | H | SCH3 | 4-Cl |
| B.280 | 甲基 | 6-Cl | H | SCH3 | 6-Cl |
| B.281 | 甲基 | 6-Cl | H | SCH3 | 3-OCH3 |
| B.282 | 甲基 | 6-Cl | H | SCH3 | 6-CH3 |
| B.283 | 乙基 | 6-Cl | H | SCH3 | H |
| B.284 | 异丙基 | 6-Cl | H | SCH3 | H |
| B.285 | 2-丙烯基 | 6-Cl | H | SCH3 | H |
| B.286 | 2-丙烯基 | 6-Cl | H | SCH3 | 3-Cl |
| B.287 | (E)-3-氯-2-丙烯基 | 6-Cl | H | SCH3 | H |
| B.288 | 2-丙炔基 | 6-Cl | H | SCH3 | H |
| B.289 | 2-丙炔基 | 6-Cl | H | SCH3 | 3-Cl |
| B.290 | 2-丙炔基 | 6-Cl | H | SCH3 | 3-OCH3 |
| B.291 | 2-丙炔基 | 6-Cl | H | SCH3 | 6-CH3 |
| B.292 | 氰基甲基 | 6-Cl | H | SCH3 | H |
| B.293 | 1-(叔丁氧基羰基)乙基 | 6-Cl | H | SCH3 | H |
| B.294 | 环丙基甲基 | 6-Cl | H | SCH3 | H |
| B.295 | 苄基 | 6-Cl | H | SCH3 | H |
| B.296 | 3-甲基苄基 | 6-Cl | H | SCH3 | H |
| B.297 | 3-甲基苄基 | 6-Cl | H | SCH3 | 3-Cl |
| B.298 | 1-(4-氯苯基)乙基 | 6-Cl | H | SCH3 | H |
| B.299 | 4-(4-氯苯基)-2-丁烯基 | 6-Cl | H | SCH3 | H |
| B.300 | 甲基 | 6-Cl | H | Cl | H |
| B.301 | 甲基 | 6-Cl | H | Cl | 3-Cl |
| B.302 | 甲基 | 6-Cl | H | Cl | 4-Cl |
| B.303 | 甲基 | 6-Cl | H | Cl | 6-Cl |
| B.304 | 甲基 | 6-Cl | H | Cl | 3-OCH3 |
| B.305 | 甲基 | 6-Cl | H | Cl | 6-CH3 |
| B.306 | 乙基 | 6-Cl | H | Cl | H |
| B.307 | 异丙基 | 6-Cl | H | Cl | H |
| B.308 | 2-丙烯基 | 6-Cl | H | Cl | H |
| B.309 | 2-丙烯基 | 6-Cl | H | Cl | 3-Cl |
| B.310 | (E)-3-氯-2-丙烯基 | 6-Cl | H | Cl | H |
| B.311 | 2-丙炔基 | 6-Cl | H | Cl | H |
| B.312 | 2-丙炔基 | 6-Cl | H | Cl | 3-Cl |
| B.313 | 2-丙炔基 | 6-Cl | H | Cl | 3-OCH3 |
| B.314 | 2-丙炔基 | 6-Cl | H | Cl | 6-CH3 |
| B.315 | 氰基甲基 | 6-Cl | H | Cl | H |
| B.316 | 1-(叔丁氧基羰基)乙基 | 6-Cl | H | Cl | H |
| B.317 | 环丙基甲基 | 6-Cl | H | Cl | H |
| B.318 | 苄基 | 6-Cl | H | Cl | H |
| B.319 | 2-甲基苄基 | 6-Cl | H | Cl | H |
| B.320 | 2-甲基苄基 | 6-Cl | H | Cl | 3-Cl |
| B.321 | 1-(4-氯苯基)乙基 | 6-Cl | H | Cl | H |
| B.322 | 4-(4-氯苯基)-2-丁烯基 | 6-Cl | H | Cl | H |
| B.323 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.324 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | 3-Cl |
| B.325 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | 4-Cl |
| B.326 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | 6-Cl |
| B.327 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | 3-OCH3 |
| B.328 | 甲基 | 6-CH3 | 4-CH3 | OCH3 | 6-CH3 |
| B.329 | 乙基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.330 | 异丙基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.331 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.332 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | 3-Cl |
| B.333 | (E)-3-氯-2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.334 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.335 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | 3-Cl |
| B.336 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | 3-OCH3 |
| B.337 | 2-丙烯基 | 6-CH3 | 4-CH3 | OCH3 | 6-CH3 |
| B.338 | 氰基甲基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.339 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.340 | 环丙基甲基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.341 | 苄基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.342 | 3-甲基苄基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.343 | 3-甲基苄基 | 6-CH3 | 4-CH3 | OCH3 | 3-Cl |
| B.344 | 1-(4-氯苯基)乙基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.345 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | 4-CH3 | OCH3 | H |
| B.346 | 甲基 | 6-CH3 | 4-CH3 | Cl | H |
| B.347 | 甲基 | 6-CH3 | 4-CH3 | Cl | 3-Cl |
| B.348 | 甲基 | 6-CH3 | 4-CH3 | Cl | 4-Cl |
| B.349 | 甲基 | 6-CH3 | 4-CH3 | Cl | 6-Cl |
| B.350 | 甲基 | 6-CH3 | 4-CH3 | Cl | 3-OCH3 |
| B.351 | 甲基 | 6-CH3 | 4-CH3 | Cl | 6-CH3 |
| B.352 | 乙基 | 6-CH3 | 4-CH3 | Cl | H |
| B.353 | 异丙基 | 6-CH3 | 4-CH3 | Cl | H |
| B.354 | 2-丙烯基 | 6-CH3 | 4-CH3 | Cl | H |
| B.355 | 2-丙烯基 | 6-CH3 | 4-CH3 | Cl | 3-Cl |
| B.356 | (E)-3-氯-2-丙烯基 | 6-CH3 | 4-CH3 | Cl | H |
| B.357 | 2-丙炔基 | 6-CH3 | 4-CH3 | Cl | H |
| B.358 | 2-丙炔基 | 6-CH3 | 4-CH3 | Cl | 3-Cl |
| B.359 | 2-丙炔基 | 6-CH3 | 4-CH3 | Cl | 3-OCH3 |
| B.360 | 2-丙炔基 | 6-CH3 | 4-CH3 | Cl | 6-CH3 |
| B.361 | 氰基甲基 | 6-CH3 | 4-CH3 | Cl | H |
| B.362 | 1-(叔丁氧基羰基)乙基 | 6-CH3 | 4-CH3 | Cl | H |
| B.363 | 环丙基甲基 | 6-CH3 | 4-CH3 | Cl | H |
| B.364 | 苄基 | 6-CH3 | 4-CH3 | Cl | H |
| B.365 | 3-甲基苄基 | 6-CH3 | 4-CH3 | Cl | H |
| B.366 | 3-甲基苄基 | 6-CH3 | 4-CH3 | Cl | 3-Cl |
| B.367 | 1-(4-氯苯基)乙基 | 6-CH3 | 4-CH3 | Cl | H |
| B.368 | 4-(4-氯苯基)-2-丁烯基 | 6-CH3 | 4-CH3 | Cl | H |
| B.369 | 甲基 | 2-F | H | OCH3 | H |
| B.370 | 甲基 | 2-F | H | OCH3 | 3-Cl |
| B.371 | 甲基 | 2-F | H | OCH3 | 4-Cl |
| B.372 | 甲基 | 2-F | H | OCH3 | 6-Cl |
| B.373 | 甲基 | 2-F | H | OCH3 | 3-OCH3 |
| B.374 | 甲基 | 2-F | H | OCH3 | 6-CH3 |
| B.375 | 乙基 | 2-F | H | OCH3 | H |
| B.376 | 异丙基 | 2-F | H | OCH3 | H |
| B.377 | 2-丙烯基 | 2-F | H | OCH3 | H |
| B.378 | 2-丙烯基 | 2-F | H | OCH3 | 3-Cl |
| B.379 | (E)-3-氯-2-丙烯基 | 2-F | H | OCH3 | H |
| B.380 | 2-丙炔基 | 2-F | H | OCH3 | H |
| B.381 | 2-丙炔基 | 2-F | H | OCH3 | 3-Cl |
| B.382 | 2-丙炔基 | 2-F | H | OCH3 | 3-OCH3 |
| B.383 | 2-丙炔基 | 2-F | H | OCH3 | 6-CH3 |
| B.384 | 氰基甲基 | 2-F | H | OCH3 | H |
| B.385 | 1-(叔丁氧基羰基)乙基 | 2-F | H | OCH3 | H |
| B.386 | 环丙基甲基 | 2-F | H | OCH3 | H |
| B.387 | 苄基 | 2-F | H | OCH3 | H |
| B.388 | 3-甲基苄基 | 2-F | H | OCH3 | H |
| B.389 | 3-甲基苄基 | 2-F | H | OCH3 | 3-Cl |
| B.390 | 1-(4-氯苯基)乙基 | 2-F | H | OCH3 | H |
| B.391 | 4-(4-氯苯基)-2-丁烯基 | 2-F | H | OCH3 | H |
| B.392 | 甲基 | 2-F | H | Cl | H |
| B.393 | 甲基 | 2-F | H | Cl | 3-Cl |
| B.394 | 甲基 | 2-F | H | Cl | 4-Cl |
| B.395 | 甲基 | 2-F | H | Cl | 6-Cl |
| B.396 | 甲基 | 2-F | H | Cl | 3-OCH3 |
| B.397 | 甲基 | 2-F | H | Cl | 6-CH3 |
| B.398 | 乙基 | 2-F | H | Cl | H |
| B.399 | 异丙基 | 2-F | H | Cl | H |
| B.400 | 2-丙烯基 | 2-F | H | Cl | H |
| B.401 | 2-丙烯基 | 2-F | H | Cl | 3-Cl |
| B.402 | (E)-3-氯-2-丙烯基 | 2-F | H | Cl | H |
| B.403 | 2-丙炔基 | 2-F | H | Cl | H |
| B.404 | 2-丙炔基 | 2-F | H | Cl | 3-Cl |
| B.405 | 2-丙炔基 | 2-F | H | Cl | 3-OCH3 |
| B.406 | 2-丙炔基 | 2-F | H | Cl | 6-CH3 |
| B.407 | 氰基甲基 | 2-F | H | Cl | H |
| B.408 | 1-(叔丁氧基羰基)乙基 | 2-F | H | Cl | H |
| B.409 | 环丙基甲基 | 2-F | H | Cl | H |
| B.410 | 苄基 | 2-F | H | Cl | H |
| B.411 | 3-甲基苄基 | 2-F | H | Cl | H |
| B.412 | 3-甲基苄基 | 2-F | H | Cl | 3-Cl |
| B.413 | 1-(4-氯苯基)乙基 | 2-F | H | Cl | H |
| B.414 | 4-(4-氯苯基)-2-丁烯基 | 2-F | H | Cl | H |
| B.415 | 甲基 | 6-CN | H | OCH3 | H |
| B.416 | 甲基 | 6-CN | H | OCH3 | 3-Cl |
| B.417 | 甲基 | 6-CN | H | OCH3 | 4-Cl |
| B.418 | 甲基 | 6-CN | H | OCH3 | 6-Cl |
| B.419 | 甲基 | 6-CN | H | OCH3 | 3-OCH3 |
| B.420 | 甲基 | 6-CN | H | OCH3 | 6-CH3 |
| B.421 | 乙基 | 6-CN | H | OCH3 | H |
| B.422 | 异丙基 | 6-CN | H | OCH3 | H |
| B.423 | 2-丙烯基 | 6-CN | H | OCH3 | H |
| B.424 | 2-丙烯基 | 6-CN | H | OCH3 | 3-Cl |
| B.425 | (E)-3-氯-2-丙烯基 | 6-CN | H | OCH3 | H |
| B.426 | 2-丙炔基 | 6-CN | H | OCH3 | H |
| B.427 | 2-丙炔基 | 6-CN | H | OCH3 | 3-Cl |
| B.428 | 2-丙炔基 | 6-CN | H | OCH3 | 3-OCH3 |
| B.429 | 2-丙炔基 | 6-CN | H | OCH3 | 6-CH3 |
| B.430 | 氰基甲基 | 6-CN | H | OCH3 | H |
| B.431 | 1-(叔丁氧基羰基)乙基 | 6-CN | H | OCH3 | H |
| B.432 | 环丙基甲基 | 6-CN | H | OCH3 | H |
| B.433 | 苄基 | 6-CN | H | OCH3 | H |
| B.434 | 3-甲基苄基 | 6-CN | H | OCH3 | H |
| B.435 | 3-甲基苄基 | 6-CN | H | OCH3 | 3-Cl |
| B.436 | 1-(4-氯苯基)乙基 | 6-CN | H | OCH3 | H |
| B.437 | 4-(4-氯苯基)-2-丁烯基 | 6-CN | H | OCH3 | H |
| B.438 | 甲基 | 6-CN | H | Cl | H |
| B.439 | 甲基 | 6-CN | H | Cl | 3-Cl |
| B.440 | 甲基 | 6-CN | H | Cl | 4-Cl |
| B.441 | 甲基 | 6-CN | H | Cl | 6-Cl |
| B.442 | 甲基 | 6-CN | H | Cl | 3-OCH3 |
| B.443 | 甲基 | 6-CH | H | Cl | 6-CH3 |
| B.444 | 乙基 | 6-CN | H | Cl | H |
| B.445 | 异丙基 | 6-CN | H | Cl | H |
| B.446 | 2-丙烯基 | 6-CN | H | Cl | H |
| B.447 | 2-丙烯基 | 6-CN | H | Cl | 3-Cl |
| B.448 | (E)-3-氯-2-丙烯基 | 6-CN | H | Cl | H |
| B.449 | 2-丙炔基 | 6-CN | H | Cl | H |
| B.450 | 2-丙炔基 | 6-CN | H | Cl | 3-Cl |
| B.451 | 2-丙炔基 | 6-CN | H | Cl | 3-OCH3 |
| B.452 | 2-丙炔基 | 6-CN | H | Cl | 6-CH3 |
| B.453 | 氰基甲基 | 6-CN | H | Cl | H |
| B.454 | 1-(叔丁氧基羰基)乙基 | 6-CN | H | Cl | H |
| B.455 | 环丙基甲基 | 6-CN | H | Cl | H |
| B.456 | 苄基 | 6-CN | H | Cl | H |
| B.457 | 3-甲基苄基 | 6-CN | H | Cl | H |
| B.458 | 3-甲基苄基 | 6-CN | H | Cl | 3-Cl |
| B.459 | 1-(4-氯苯基)乙基 | 6-CN | H | Cl | H |
| B.460 | 4-(4-氯苯基)-2-丁烯基 | 6-CN | H | Cl | H |
| B.461 | 甲基 | 2-CH3 | H | Br | H |
| B.462 | 甲基 | 2-CH3 | H | CN | H |
| B.463 | 甲基 | 2-CH3 | H | SC6H5 | H |
| B.464 | 甲基 | 2-CH3 | H | OC6H5 | H |
| B.465 | 甲基 | 6-CH3 | H | Br | H |
| B.466 | 甲基 | 6-CH3 | H | CN | H |
| B.467 | 甲基 | 6-CH3 | H | SC6H5 | H |
| B.468 | 甲基 | 6-CH3 | H | OC6H5 | H |
| B.469 | 甲基 | 4-CH3 | H | Br | H |
| B.470 | 甲基 | 4-CH3 | H | CN | H |
| B.471 | 甲基 | 4-CH3 | H | SC6H5 | H |
| B.472 | 甲基 | 4-CH3 | H | OC6H5 | H |
| B.473 | 甲基 | 6-Cl | H | Br | H |
| B.474 | 甲基 | 6-Cl | H | CN | H |
| B.475 | 甲基 | 6-Cl | H | SC6H5 | H |
| B.476 | 甲基 | 6-Cl | H | OC6H5 | H |
| B.477 | 甲基 | 6-CH3 | 4-CH3 | Br | H |
| B.478 | 甲基 | 6-CH3 | 4-CH3 | CN | H |
| B.479 | 甲基 | 6-CH3 | 4-CH3 | SC6H5 | H |
| B.480 | 甲基 | 6-CH3 | 4-CH3 | OC6H5 | H |
| B.481 | 甲基 | 2-F | H | Br | H |
| B.482 | 甲基 | 2-F | H | CN | H |
| B.483 | 甲基 | 2-F | H | SC6H5 | H |
| B.484 | 甲基 | 2-F | H | OC6H5 | H |
| B.485 | 甲基 | 6-CN | H | Br | H |
| B.486 | 甲基 | 6-CN | H | CN | H |
| B.487 | 甲基 | 6-CN | H | SC6H5 | H |
| B.488 | 甲基 | 6-CN | H | OC6H5 | H |
| B.489 | 乙基 | 2-CH3 | H | Br | H |
| B.490 | 乙基 | 2-CH3 | H | CN | H |
| B.491 | 乙基 | 2-CH3 | H | SC6H5 | H |
| B.492 | 乙基 | 2-CH3 | H | OC6H5 | H |
| B.493 | 乙基 | 6-CH3 | H | Br | H |
| B.494 | 乙基 | 6-CH3 | H | CN | H |
| B.495 | 乙基 | 6-CH3 | H | SC6H5 | H |
| B.496 | 乙基 | 6-CH3 | H | OC6H5 | H |
| B.497 | 乙基 | 4-CH3 | H | Br | H |
| B.498 | 乙基 | 4-CH3 | H | CN | H |
| B.499 | 乙基 | 4-CH3 | H | SC6H5 | H |
| B.500 | 乙基 | 4-CH3 | H | OC6H5 | H |
| B.501 | 乙基 | 6-Cl | H | Br | H |
| B.502 | 乙基 | 6-Cl | H | CN | H |
| B.503 | 乙基 | 6-Cl | H | SC6H5 | H |
| B.504 | 乙基 | 6-Cl | H | OC6H5 | H |
| B.505 | 乙基 | 6-CH3 | 4-CH3 | Br | H |
| B.506 | 乙基 | 6-CH3 | 4-CH3 | CN | H |
| B.507 | 乙基 | 6-CH3 | 4-CH3 | SC6H5 | H |
| B.508 | 乙基 | 6-CH3 | 4-CH3 | OC6H5 | H |
| B.509 | 乙基 | 2-F | H | Br | H |
| B.510 | 乙基 | 2-F | H | CN | H |
| B.511 | 乙基 | 2-F | H | SC6H5 | H |
| B.512 | 乙基 | 2-F | H | OC6H5 | H |
| B.513 | 乙基 | 6-CN | H | Br | H |
| B.514 | 乙基 | 6-CN | H | CN | H |
| B.515 | 乙基 | 6-CN | H | SC6H5 | H |
| B.516 | 乙基 | 6-CN | H | OC6H5 | H |
| B.517 | 2-丙烯基 | 2-CH3 | H | Br | H |
| B.518 | 2-丙烯基 | 2-CH3 | H | CN | H |
| B.519 | 2-丙烯基 | 2-CH3 | H | SC6H5 | H |
| B.520 | 2-丙烯基 | 2-CH3 | H | OC6H5 | H |
| B.521 | 2-丙烯基 | 6-CH3 | H | Br | H |
| B.522 | 2-丙烯基 | 6-CH3 | H | CN | H |
| B.523 | 2-丙烯基 | 6-CH3 | H | SC6H5 | H |
| B.524 | 2-丙烯基 | 6-CH3 | H | OC6H5 | H |
| B.525 | 2-丙烯基 | 4-CH3 | H | Br | H |
| B.526 | 2-丙烯基 | 4-CH3 | H | CN | H |
| B.527 | 2-丙烯基 | 4-CH3 | H | SC6H5 | H |
| B.528 | 2-丙烯基 | 4-CH3 | H | OC6H5 | H |
| B.529 | 2-丙烯基 | 6-Cl | H | Br | H |
| B.530 | 2-丙烯基 | 6-Cl | H | CN | H |
| B.531 | 2-丙烯基 | 6-Cl | H | SC6H5 | H |
| B.532 | 2-丙烯基 | 6-Cl | H | OC6H5 | H |
| B.533 | 2-丙烯基 | 6-CH3 | 4-CH3 | Br | H |
| B.534 | 2-丙烯基 | 6-CH3 | 4-CH3 | CN | H |
| B.535 | 2-丙烯基 | 6-CH3 | 4-CH3 | SC6H5 | H |
| B.536 | 2-丙烯基 | 6-CH3 | 4-CH3 | OC6H5 | H |
| B.537 | 2-丙烯基 | 2-F | H | Br | H |
| B.538 | 2-丙烯基 | 2-F | H | CN | H |
| B.539 | 2-丙烯基 | 2-F | H | SC6H5 | H |
| B.540 | 2-丙烯基 | 2-F | H | OC6H5 | H |
| B.541 | 2-丙烯基 | 6-CN | H | Br | H |
| B.542 | 2-丙烯基 | 6-CN | H | CN | H |
| B.543 | 2-丙烯基 | 6-CN | H | SC6H5 | H |
| B.544 | 2-丙烯基 | 6-CN | H | OC6H5 | H |
新的取代的苯甲氧基苯基衍生物I可以用各种方法来制备,特别优选的是通过下述方法中的一种来制备:
A)苯酚II或它的碱金属盐,碱土金属盐,银或铵盐与苯基化合物III反应得到取代的苯氧基甲基苯基衍生物I,Y是氧:
L是常见的离去基团如氯,溴,碘,甲磺酸根、三氟甲磺酸根或甲苯磺酸根。
上述反应通常是在惰性溶剂或稀释剂如丙酮,二甲基甲酰胺或甲苯中或在水和如二氯甲烷的二相体系中使用相转移催化剂来进行。
适用的相转移催化剂是铵盐,锍盐或鏻盐,这些盐的阴离子类型不是十分重要。业已证实有利的实例为苄基三甲基铵盐如氢氧化苄基三甲基铵和四丁基铵盐。
上述反应通常是在0至100℃,特别是20至60℃的反应温度下进行。
起始物质II和III通常是以近似等摩尔的量相互进行反应。但是对于收率而言,以起始物质II计算,使用过量约1至20摩尔%,优选1至10摩尔%的起始物质III是有利的。
通常,以起始物质II或III计,相转移催化剂的催化量为约1至10摩尔%。
X为=CH-OCH3或=N-OCH3的苯基化合物III公开在EP-A386561中,
X为=CH-CH3的苯基化合物III公开在EP-A513580中。该两份欧洲专利申请中还公开了Y为氧的苯甲氧基苯基衍生物I的制备方法。以Y是氧和R6是C1-C4烷基的苯甲氧基苯基衍生物I为起始物质用已知的酯裂解的方法可以制得R6是氢的相应化合物I(该方法公开在如Houben-Weyl,Methoden der Organischen Chemie(Methods of Organic Chemistry),Vol.E5,223-254页;Org.Reactions
24,(1976),187-224页中)。
B) 羟肟酸(硫)酯IVa或异羟肟酸酯IVb的烷基化R4′是烷氧基或烷硫基;R*是氢、酚保护基如甲氧甲基、烯丙基、苯甲酰甲基、乙酰基、叔丁基、苄基或如下基团:烷基化可以用公知的方法来进行。例如对于羟肟酸(硫)酯IVa的烷基化,可参照Houben-Weyl、Methoden der OrganischenChemie(有机化学方法)、10/1卷、1190页;J.Org.Chem.46(1981),3623-3629页。
合适的烷基化试剂为烷基卤、烷基磺酸盐、硫酸二烷基酯或Meerwein盐(参见如J.Org.Chem.36(1971)、284-294页),三氟甲磺酸烷基酯(参见如J.Org.Chem.54(1989),1736 ff页)和重氮甲烷(参见如Austr.J.Chem.27(1974),1341-1349页)。
反应通常在0到60℃下进行,优选在0到20℃下进行。
合适的溶剂是醚,例如乙醚、二噁烷;酮,例如丙酮、甲基乙基酮;醇,例如甲醇、乙醇;以及乙腈、二甲基亚砜、二甲基甲酰胺和N-甲基吡咯烷酮。特别优选丙酮、二甲基亚砜和二甲基甲酰胺。
R*为酚保护基的化合物Va可以通过去保护基转化成R*=H的化合物Va(参见如Th.W.Green″Protective Groups in OrganicSynthesis″Wiley+Sons 87-108页)。
R*=H的化合物Va可以用方法A)的相似方法与苯基化合物III反应得到Y是氧的取代的苯甲氧基苯基衍生物I。
c)异羟肟酸酯IVb经卤化生成羟肟酸酯氯化物或羟肟酸酯溴化物Vb,并且进而亲核取代卤素(参见如J.Org.Chem.50(1985),3348-3355页)得到化合物Vc:
Hal是氯或溴,R4″是除了氯和溴以外的R4。
合适的卤化剂如,元素氯或溴、次卤酸盐、亚硫酰(二)氯、磺酰氯、N-氯代丁二酰亚胺、三溴化磷、五氯化磷、溶于四氯甲烷中的三苯基膦或溶于四溴甲烷中的三苯基膦(参见如EP-A 158153;Houben-Weyl,Methoden der Organischen chemie(Methodsof Organic Chemistry),第VIII卷,691页; Synth.Commun.16(1986),763-765;Gazz.Chim.Ital.114(1984),131-132页)。
卤化反应是在惰性溶剂或稀释剂中进行,所说的溶剂和稀释剂可以为如四氯甲烷、苯、乙醚、二甲基甲酰胺、二噁烷或二噁烷/水。
优选反应温度取决于卤化剂。大多数情况下温度为大约10到30℃,特别是0到10℃已足以能满足要求。更高的温度,约20到80℃,特别是40到80℃被证明对于用溶于四氯甲烷或四溴甲烷中的三苯基膦来进行卤化是有利的。
卤化剂用量没有特别限制。通常每摩尔IVb需要0.8到2.0摩尔卤化剂,优选0.95至1.2摩尔的卤化剂。
合适的亲核试剂包括醇盐(参见如EP-A 158153)、烷基胺(参见如J.Org Chem 45(1980),4198 ff页和Heterocycles 26(1987)、188页)硫酚和烷基硫醇盐(参见如EP-A-426460)。
亲核取代的合适溶剂为烷基胺本身,以及醚,例如乙醚和四氢呋喃,醇,例如乙醇,二甲基甲酰胺,二甲基亚砜和乙腈。
对于每摩尔Vb,一般需要用0.8至2.0摩尔的亲核试剂,特别是1.0到1.2摩尔的亲核试剂。过量的亲核试剂,甚至相对于每摩尔Vb过量20倍的烷基胺,一般也不会产生更佳效果。
据目前所知,反应可在0至80℃,优选0至30℃下以足够的速率进行。
R*是酚保护基团的化合物Vb和Vc可以通过去保护基而转化成R*为氢的化合物Vb或Vc(参见如Th.W.Green″Protective Groupsin Organic Synthesis″,Wiley+Sons,87-108页。
通过方法A)的相似方法,R*为氢的化合物Vb和Vc可以与苯基化合物III反应得到Y=氧的取代苯甲氧基苯基衍生物I。
D)-亲核取代异羟肟酸氯化物或溴化物IVC中的氯或溴,并且将所得产物IVd烷基化或
合适的亲核试剂为醇盐(参见如EP-A 158153),烷基胺(参见如J.Org.Ghem.45(1980),4198 ff页和Heterocycles 26(1987),188页)和烷基硫醇盐(参见如EP-A 426460)。
B)中的解释也适用于这里的烷基化反应,关于L的定义可参照A)。
对于亲核取代,可参照C)中的解释。C)也叙述了关于Vb和Vc进一步反应生成结构式I的苯甲氧基苯基衍生物,其中Y是氧。
E)羟肟酸氰化物IVe的烷基化{参见如Liebigs Ann.Chem.10,1623-1629(1989)}:B)中给出的关于烷基化反应的解释也在这里适用。L如A)中的定义。
关于化合物Vd进一步与苯基化合物III反应生成Y为氧并且R4是氰基的取代的苯氧甲基苯基衍生物I,可参照C)中的详细说明。
F)式I取代的苯氧甲基苯基衍生物(其中Y是氧)或活性羧酸衍生物VI与伯(H2N-R6)或仲胺(HN(CH3)-R6)反应,可制备Y=-NH-或-N(CH3)-的相应化合物I:R7是羰基活化基团,例如氯、溴或1-咪唑基。
通常,上述反应可以用已知的方法进行。(参见如Houben Weyl,Methoden der Organischen Chemie(有机化学方法),Vol.E5,941-977页,983-991页;Methoden der OrganischenChemie,Vol.VIII,654 ff页)。
反应通常于-10至60℃在惰性熔剂或稀释中进行。
现已证明,如果Y=氧的化合物I作为反应起始物,在10至30℃温度下,其与约等摩尔量的胺或过量10倍的胺(以Y为氧的化合物I计)进行反应特别有利。其中特别适合的溶剂是醚,如四氢呋喃或二噁烷,醇如甲醇和乙醇。如需要,可在上述溶剂中另外加入水。
如起始物为活化羧酸衍生物VI,特别优选的反应温度为-10-5℃,对于每摩尔VI通常优选的胺量为0.9至5摩尔,特别是0.95至2摩尔。其中特别适合的溶剂为醚,如乙基醚和四氢呋喃,芳烃如甲苯,氯化烃如二氯甲烷或吡啶。
活化羧酸衍生物VI可以由-YR6=OH的苯氧甲基苯基衍生物I获得(参见如Houben Weyl,Methoden der OrganischenChemie(有机化学方法),Vol.VIII,463页)。
式IVa、IVb和IVc的起始产物通过以下步骤获得:
G)通过苯基氰VII与醇或硫醇的Pinner反应,接着生成的亚胺与羟胺反应制备羟肟酸酯1Va(参见如U.S.4,743,701 and EP-A 158153):该反应通常在惰性溶剂或稀释中进行。特别适合的溶剂为醚,如二噁烷和氯代烃如氯仿。VII与醇的反应也可以在过量醇和不另加其它溶剂的条件下进行。
醇量没有特别限制。通常在优选的VII反应中每摩尔VII需1至10摩尔醇。如果在所说醇中在没有溶剂的条件下进行反应,则反应中可存在有过量的醇。
对于每摩尔VII,羟胺的量优选为0.9至10摩尔,特别是1至2摩尔。
Pinner反应通常在20至150℃,优选40至80℃的温度下进行。接下来与羟胺反应中,反应温度为0至60℃,优选20到40℃。
合适的卤化剂为,例如,元素氯或溴或次卤酸盐(参见如EP-A158153;Houben-Weyl,Methoden der Organischen Chemie(有机化学方法),Vol.VIII,691页;Synth.Commun.16(1986),763-765;Gazz.Chim.Ital.114(1984),131-132页)。
合适的溶剂或稀释剂为醚,如乙醚和二噁烷,氯代烃如二氯甲烷,以及二甲基甲酰胺或乙酸。
为使反应达到最佳转化率,通常每摩尔IX,所用卤化剂为0.9至5摩尔,特别是1.0至1.5摩尔。
通过苯甲醛VIII与羟胺反应得到醛肟IX。(参见如Houben-Weyl,Methoden der Organischen Chemie(有机化学方法),Volume 10/4,4th edtion,1968,Georg-Thieme Verlag,Stuttgart,55-66页)。
合适的溶剂或稀释剂是水、醇如甲醇和乙醇,或水和醇的混合物。
羟胺优选以羟铵盐形式使用,特别是盐酸盐、乙酸盐或硫酸盐,实际用量为每摩尔VIII约0.8至2.0摩尔,特别是0.95至1.2摩尔。
为了中和生成的酸,反应在碱存在下进行是有利的。合适的碱如碱金属碳酸氢盐,例如碳酸氢钠,碱金属乙酸盐如乙酸钠、氨和有机碱如吡啶。
通常每摩尔羟铵盐需要1.0至1.7摩尔碱。
温度范围为0至80℃,特别是20至60℃。
J)通过苯甲酸衍生物XI与羟胺H2N-OR1的反应制备异羟肟酸酯IVb(参见Houben-Weyl,Methoden der OrganischenChemie(有机化学方法),Vol.E5,1144-1146页):
R*为下述基团的苯甲酸衍生物XI是新的(=α-甲氧基亚氨基苯乙酸甲酰胺XI′)。
而且化合物IVb也是新化合物,其中R*是下述基团(=2-(苯氧甲基)苯乙酸衍生物IVb′)
苯甲酸衍生物XI和α-甲氧基亚氨基苯乙酸甲酰胺XI′通过以下反应得到-乙酰苯X或X′进行卤仿反应,(参见如J.Am.Chem.Soc.68(1946),1648 ff页和J.Org.Chem.12(1947),603 ff页;Helv.Chim.Acta49(1966),561 ff页)。 现已证明,特别适合的试剂是碱金属次卤酸盐,如次氯酸钠、次氯酸钾和次溴酸钠。次卤酸盐的量没有特别的限制;每摩尔X或X′,其用量为0.8至20摩尔,特别是约1.0至10摩尔是有利的。
在反应温度约0至100℃,特别优选5至30℃,在水或水-二噁烷混合物中进行反应是有利的。-或者通过羰基化卤代芳香物XII,其中使用Pd催化剂是有利的(参见如J,Org.Met.Chem.358(1988),563-565页; J.Org.Chem.56(1991),4320-4322页和美国专利4,990,657):
羰基化反应优选在水与例如四甲基脲、甲苯或二甲基甲酰胺的混合物中进行。
现已证明,合适的催化剂为Pd(II)化合物,如PdCl2、Pd(O-COCH3)2和Pd[P(C6H5)3]2Cl2,如需要可添加P(C6H5)3,每摩尔XII,催化剂量为0.01至0.1摩尔,优选0.01至0.05摩尔,对反应是合适的。
该反应通常在碱存在下进行,例如,在碱金属碳酸盐如碳酸钾、或有机碱如三乙胺或吡啶存在下进行,对于每摩尔XII,碱量优选为约1至10摩尔,特别是2至4摩尔。
反应温度通常为30至200℃,优选100至150℃。羰基化反应在2至200巴,优选约50巴的一氧化碳过压的条件下进行特别有利。
除了卤代芳香物XII的羰基化反应之外,上述所有反应通常在大气压或相应的稀释剂自然压力下进行。制备实施例实施例1E-2-甲氧亚氨基-2-[2-(4-[乙氧亚氨基甲氧甲基]-2,5二甲基苯氧甲基)苯基]乙酸甲酰胺(表1,1.004号)
向3.1g E-2-甲氧亚氨基-2-[2-(4-乙氧亚氨基羰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例5制备)和1.74g精细研磨的碳酸钾悬浮在60ml无水丙酮的悬浮液中逐滴加入1.6g硫酸二甲基酯。搅拌16小时后,将反应混合物倒入100ml冰水中,并与20ml稀氨水混合。混合物用甲基叔丁基醚萃取三次,合并有机相并用饱和氯化钠溶液洗涤,然后用硫酸钠干燥并且浓缩至干。粗产物用中压硅胶色谱提纯(洗脱剂:正庚烷/乙酸乙酯1∶1 V/V)。产物:0.45g油状所需的O-烷基化的产物。1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=1.35(t,3H);2.2(s,3H);2.35(s,3H);2.9(d,3H);3.6(s,3H);3.95(s,3H);4.2(q,2H);5.0(s,2H);6.6(s,1H);6.7(broad,NH);7.1(s,1H);7.2-7.6(m,4H)实施例2E-2-甲氧亚氨基-2-[2-(4-(氯乙氧亚氨基甲基]-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(表1,1.008号)将3.3g E-2-甲氧亚氨基-2-[2-(4-乙氧亚氨基羰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例5制备)和3.1g三苯基膦在无水条件下溶解在30ml乙腈中。加入3.7g四氯甲烷后,反应混合物回流2小时。然后将其冷却到20℃,用硅胶柱色谱分离(10g硅胶)(洗脱剂:甲苯/乙酸乙酯9∶1)。洗脱液用常规方法处理得到产物。产物:1.9g;熔点:87-90℃;1H-NMR(溶于CDCl3,TMS作内标):δ[ppm]=1.35(t,3H);2.15(s,3H);2.35(s,3H);2.9(d,3H);3.9(s,3H);4.3(q,2H);5.0(s,2H);6.6(s,1H);6.75(broad,NH);7.2-7.6(m,5H).实施例3E-2-甲氧亚氨基-2-[2-(4-[溴乙氧亚氨基甲基]-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(表1,1.009号)
在无水条件下将6.6g E-2-甲氧亚氨基-2-[2-(4-乙氧氨基羰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例5制备)和6.2g三苯基膦溶解在60ml乙腈中,加入8.0g四溴甲烷后,将反应混合物回流4小时,然后再次用2g四溴甲烷处理。并且再回流1小时,然后用实施例6相似的方法处理得到产物。产物:4.8g结晶产物;熔点:74-77℃;1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=1.3(t,3H):2.15(s,3H);2.35(s,3H);2.9(d,3H);3.95(s,3H);4.3(q,2H);4.95(s,2H);6.6(s,1H);6.75(broad,NH);7.2-7.6(m,5H).实施例4E-2-甲氧亚氨基-2-[2-(4-[乙氧亚氨基甲基硫甲基]-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(表1,1.010号)
0.42g固体甲硫醇钠加到1.9g E-2-甲氧亚氨基-2-[2-(4-[溴乙氧亚氨基甲基]-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例3制备)在20ml无水二甲基酰胺中的溶液中。在约20℃下搅拌16小时后,将反应混合物倒入冰水和甲基叔丁基醚的混合物中。进行相分离,水相再用甲基叔丁基醚萃取三次。然后合并有机相,并用20ml 2N氢氧化钠洗涤,然后用100ml饱和氯化钠溶液洗涤,用硫酸钠干燥并浓缩。用正庚烷/异丙醚研制,得到1.4g结晶产物;熔点:146-148℃。1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=1.35(t,3H);1.85(s,3H);2.2(s,3H);2.3(s,3H);2.9(d,3H);3.95(s,3H);4.3(q,2H);5.0(s,2H);6.65(s,1H);6.75(broad,NH);7.0(s,1H);7.2-7.6(m,4H).
下述表1中包含了用或可以用相同的方法制备的进一步取代的苯甲氧基苯基衍生物I。
表1
实施例5E-2-甲氧亚氨基-2-[2-(4-乙氧氨基羰基-2,5-二甲苯氧甲基)苯基]乙酸甲酰胺(表2,2.003号)
| 号 | X | Y-R6 | (R5)n | R2 | R3 | Z | 物理数据熔点[℃]/IR[cm-1]1H-NMR[ppm] |
| 1.01 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(OCH3)=NOCH3 | 2.2(3H);2.4(3H);3.6(3H);4.9(2H);6.6(1H);6.8(NH);7.1(1H);7.2-7.6(4H) |
| 1.02 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOCH3 | 3432,1671,1660,1118,1031 |
| 1.03 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(OCH3)=NOC2H5 | NMR数据见实施例1 |
| 1.04 | E-NOCH3 | NH-CH3 | H | 2-Cl | H | 4-C(OCH3)=NOC2H5 | 80-82 |
| 号 | X | Y-R6 | (R5)n | R2 | R3 | Z | 物理数据熔点[℃]/IR[cm-1]1H-NMR[ppm] |
| 1.05 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(OC2H5)=NOCH3 | 1.2(3H);2.2(3H);2.4(3H);2.9(3H);3.8(2H);3.9(3H);4.0(3H);4.9(2H);6.6(1H);6.8(NH);7.0(1H);7.2-7.5(4H) |
| 1.06 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Br)=NOCH3 | 98-101 |
| 1.07 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SCH3)=NOCH3 | 53-55 |
| 1.08 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOC2H5 | 87-90 |
| 1.09 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Br)=NOC2H5 | 79-77 |
| 1.10 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SCH3)=NOC2H5 | 100-148 |
| 1.11 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOCH(CH3)2 | 3435,1661,1529,1123,981 |
| 1.12 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Br)=NOCH(CH3)2 | 65-67 |
| 1.13 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SCH3)=NOCH(CH3)2 | 123-126 |
| 1.14 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOCH2CH=CH2 | 92-95 |
| 1.15 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(Br)=NOCH2CH=CH2 | 72-75 |
| 1.16 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SCH3)=NOCH2CH=CH2 | 87-89 |
| 1.17 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SC2H5)=NOC2H5 | 150-152 |
| 1.18 | E-NOCH3 | NH-CH3 | H | 2-CH3 | H | 4-C(Cl)=NOC2H5 | 89-92 |
| 1.19 | E-NOCH3 | NH-CH3 | H | 2-CH3 | H | 4-C(Cl)=NOCH2CH=CH2 | 86-89 |
| 1.20 | E-NOCH3 | NH-CH3 | H | 2-CH3 | H | 4-C(SC6H5)=NOCH2CH=CH2 | 59-61 |
| 号 | X | Y-R6 | (R5)n | R2 | R3 | Z | 物理数据熔点[℃]/IR[cm-1]1H-NMR[ppm] |
| 1.21 | E-NOCH3 | NH-CH3 | H | 2-CH3 | H | 4-C[S(4-Cl-C6H4)]=NOCH2CH=CH2 | 2.15(3H);2.9(3H);4.8(2H);4.9(2H);5.25(1H);5.35(1H);6.0(1H);6.6(1H);6.8(NH);7.0-7.5(10H) |
| 1.22 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(OC2H5)=NOCH(CH3)2 | 100-102 |
| 1.23 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(OC2H5)=NOC2H5 | 3340,2960,1673,1509,1326,1037 |
| 1.24 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C(SC6H5)=NOC2H5 | 3360,2920,1673,1505,1035 |
| 1.25 | E-NOCH3 | NH-CH3 | H | 2-CH3 | 5-CH3 | 4-C[S(4-Cl-C6H4)]=NOC2H5 | 3410,2920,1674,1505,1036 |
| 1.26 | E-NOCH3 | NH-CH3 | H | 2-CH3 | H | 4-C(Cl)=NOCH3 | 3350,2945,1671,1500,1236,1133,1037 |
| 1.27 | E-CHCH3 | OCH3 | H | 2-CH3 | 5-CH3 | 4-C(OCH3)=NOC2H5 | 1.25(3H);1.5(3H);2.1(3H);2.2(3H);3.5(3H);3.65(3H);4.0(2H);4.8(2H);6.5(1H);7.0(2H);7.2(1H);7.3(2H);7.5(1H) |
| 1.28 | E-CHCH3 | OCH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOC2H5 | 1.27(3H);1.65(3H);2.2(3H);2.36(3H);3.7(3H);4.3(2H);4.9(2H);6.58(1H);7.0-7.6(6H) |
| 号 | X | Y-R6 | (R5)n | R2 | R3 | Z | 物理数据熔点[℃]/IR[cm-1]1H-NMR[ppm] |
| 1.29 | E-CHCH3 | OCH3 | H | 2-CH3 | 5-CH3 | 4-C(Cl)=NOCH3 | 1.65(3H);2.2(3H);2.36(3H);3.7(3H);4.9(2H);6.6(1H);7.1-7.6(6H) |
| 1.30 | E-CHCH3 | OCH3 | H | 2-CH3 | 5-CH3 | 4-C(1-三唑)=NOCH3 | 1.4(3H);2.0(3H);2.2(3H);2.9(3H);3.95(3H);4.35(2H);4.97(2H);6.65(1H);6.75(1H);7.15(1H);7.2-7.6(4H);7.95(1H);9.24(1H) |
在0℃下用10.0g N-甲基吗啉处理5.15g O-乙基羟胺氢氯化物和50ml无水二氯甲烷的悬浮液,在冰冷却下,将18.6g 2-甲氧亚氨基-2-[2-(4-氯羰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例3制备)在50ml二氯甲烷中的溶液,逐滴加入上述混合物中。加完后,让反应混合物加热至20-25℃,并且在此温度下搅拌12小时。分离出固体部分,将得到的溶液浓缩至干。所得的残留物与乙酸乙酯搅拌混合,分离出不溶部分并将其溶解在二氯甲烷中。溶液用稀盐酸和水萃取,然后用硫酸钠干燥并浓缩。产物:17.4g异羟肟酰胺(hydroxamide);熔点:177-180℃。1H-NMR(溶于CDCl3,TMS作内标):δ[ppm]=1.3(t,3H);2,15(s,3H);2.4(s,3H);2.9(d,3H);3.95(s,3H);4.05(q,2H);4.95(s,2H);6.6(s,1H);6.75(broad,NH);7.2(s,1H);7.2-7.6(m,4H);8.5(s,1H).实施例6E-2-甲氧亚氨基-2-[2-(4-乙氧氨基羰基-2-甲基苯氧基甲基)苯基]乙酸甲酰胺(表2,2.06号)
用实施例5的相似方法,使30g 2-甲氧亚氨基-2[2-(4-氯羰基-2-甲基苯氧甲基苯基]乙酰胺与8.6g O-乙基羟胺氢氯化物反应。在室温搅拌18小时后,混合物按上述方法处理。得到19.1g异羟肟酰胺hydroxamide,熔点:142-145℃。1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=1,2(t,3H);2.2(s,3H);2.8(d,3H);3.9(s,3H);3.95(q,2H);4.9(s,2H);6.7(d,1H);6.9(broad,NH);7.1-7.6(m,6H);9.6(broad,NH).实施例7E-2-甲氧亚氨基-2-(2-(4-[乙氧亚氨基-(4-氯苯基硫)甲基]-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(表1,1.21号)
将1.8g碳酸钾和1.44g 4-氯苯硫酚加入到2.4g E-2-甲氧亚氨基-2-[2-(4-(溴代乙氧亚氨基甲基)-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺(依照实施例3制备)在20ml无水二甲基甲酰胺中的溶液中。在60℃加热5小时后,再向其中加入1.4g 3-氯代苯硫酚并将所得混合物在60℃下保持1小时。为处理所述的混合物将其加入冰水中并且用甲基叔丁基醚萃取。合并的有机相用碳酸钠和水洗涤,硫酸钠干燥并用旋转蒸发器浓缩。残留物用硅胶柱色谱分离(洗脱剂:甲苯/乙酸乙酯 95∶5):得到1.7g黄色油状标题化合物。1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=1.35(t,3H);2.0(s,3H);2.1(s,3H);2.9(d,3H);3.9(s,3H);4.3(q,2H);4.8(s,2H);6.4(s,1H);6.7(broad,NH);6.8(s,1H);7.0-7.5(m,8H).前体α)E-2-甲氧亚氨基-2-[2-(4-乙酰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺
将8.5ml40%(重量)浓度的甲胺水溶液加到由18.45g 2-甲氧基亚氨基-2[2-(4-乙酰基-2,5-二甲基苯氧甲基)苯基)乙酸甲基酯和180ml四氢呋喃组成的混合物中。在20-25℃搅拌16小时后,将反应混合物倒入200ml冰水/100ml甲基叔丁基醚中。然后向混合物中加入稀盐酸,直到水相pH值为2至3。进行相分离,水相用甲基叔丁基醚萃取数次。合并的有机相用饱和氯化钠溶液洗至中性,干燥和浓缩。产物:17.6g产物;熔点:146-148℃;1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=2.2(s,3H);2.5(s,3H);2.55(s,3H);2.9(d,3H);3.95(s,3H);5.0(s,2H);6.65(s,1H);6.75(broad,NH);7.2-7.6(m,5H).前体β)E-2-甲氧亚氨基-2-[2-(4-羧基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺
将24g溴缓慢加入到20g氢氧化钠在120ml升冷却至10℃的水的溶液中不使其温度超过10℃,得到的溴仿溶液在冰冷却下用溶于150ml二噁烷的从前体α)得到的E-2-甲氧亚氨基-2-[2-(4-乙酰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺的溶液处理。在20-25℃搅拌一小时后,向其中加入50ml 20%(重量)浓度的亚硫酸氢钠溶液,以除去过量溴仿。用浓盐酸酸化反应混合物至PH为2得到固体产物。分离出固体产物,用石油醚搅拌二次并在60℃下干燥。产物:18.5g;熔点:195-197℃1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=2.2(s,3H);2.6(s,3H);2.9(d,3H);3.95(s,3H);5.0(s,2H);6.6(s,1H);6.75(broad,NH);7.2-7.6(m,4H);7.85(s,1H).前体γ)2-甲氧亚氨基-2-[2-(4-氯羰基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺
从前体β)得到的9.2g E-2-甲氧亚氨基-2-[2-(4-羧基-2,5-二甲基苯氧甲基)苯基]乙酸甲酰胺在100ml无水二氯甲烷中的溶液用几滴二甲基甲酰胺处理。在20-25℃向混合物中逐滴加入4.5g亚硫酰氯,然后反应混合物回流1.5小时。冷却后减压除去易挥发馏分。残留物用100ml二氯甲烷处理数次并再次浓缩。产物:9.3g浅黄色酰基氯固体。不用进一步纯化可直接用于下步反应。1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=2.2(s,3H);2.6(s,3H);2.95(s,3H);4.0(s,3H);4.95(s,2H);6.6(s,1H);7.2-7.6(m,4H);7.85(s,1H);8.1(broad,1H).前体δ)E-2-甲氧亚氨基-2-[2-(4-羧基-2-甲基苯氧甲基)苯基]乙酸甲酰胺
用相似于制备前体β)的方法,使溶于1400ml二噁烷中的145gE-2-甲氧亚氨基-2-[2-(4-乙酰基-2-甲基苯氧甲基)苯基)乙酸甲酰胺反应生成羧酸。用浓硫酸将反应混合物的pH值调至2,并用二氯甲烷萃取。将合并的有机相洗至中性,用硫酸钠干燥并用旋转蒸发器浓缩。残留固体用异丙基醚研制,抽吸过滤并干燥。产物:110g,熔点:185℃(分解)1H-NMR(溶于CDCl3,TMS 作内标):δ[ppm]=2.25(s,3H);2.9(d,3H);3.95(s,3H);5.0(s,2H);6.75(broad,NH);6.85(d,1H);7.1-7.5(m,4H);7.9(m,2H);11.0(broad,OH).前体ε)
2-[2-(4-羧基-2,5-二甲基苯氧甲基)苯基]-E-丁-2-烯酸甲酯
用相似于制备前体δ的方法,使溶于60ml二噁烷的9.6g 2-[2-(乙酰基-2,5-二甲基苯氧甲基)苯基]-E-丁-2-烯酸甲酯经反应得到羧酸。经旋转蒸发器浓缩后得到黄色油状物,其中70%是标题化合物,30%是丁酸甲酯(methyl butanoate)水解形成的二酸。
本发明的化合物(见表1,1.29至1.32号)是通过该粗产物经本文所描述的相似方法和相应的色谱分离二酸衍生物得到的。1H-NMR(溶于DMSO,TMS 作内标):δ[ppm]=1.6(d,3H);2.1(s,3H);2.5(s,3H);3.6(s,3H);5.0(s,2H);6.8(s,1H);7.1(q,1H);7.4-7.5(m,2H);7.6(m,1H);7.7(m,2H).前体χ)
E-2-甲氧亚氨基-2-[2-(4-羧基-2-甲基苯氧甲基)苯基]乙酸甲酯
在装有50ml水的300ml HC高压釜中加入2.2g-E-2-甲氧亚氨基-2-[2-(4-碘-2-甲基苯氧甲基)苯基]乙酸甲酯、0.35g双三苯基膦钯(II)氯化物和80ml四甲基脲。然后通入一氧化碳使压力为30巴,将混合物加热到100℃。加热后,将CO压力调至100巴。此压力按小时调节。24小时后,过滤混合物,在75℃下在油泵真空中(0.2毫巴)从滤液中蒸除四甲基脲。残留物在MTBE/NaHCO3水溶液中处理,沉淀出产产物,在抽滤并干燥后,得到0.9g标题化合物。熔点:192℃1H-NMR(溶于CDCl3,TMS作内标):δ[ppm]=2.1(s,3H);3.7(s,3H);3.9(s,3H);5.0(s,2H);7.0(d,1H);7.25(d,1H);7.45(m,2H);7.55(d,1H);7.25(m,2H).
下述表2进一步列出了2-(苯氧甲基)苯乙酸衍生物IVb′,它们通过或可以通过实施例5的相似方法来制备。
熔点.[℃]/IR[cm-1]
1H-NMR[ppm]2.01 E-NOCH3 NH-CH3 H 2-Cl H 4-{-CO-NH-OCH3} 3340,1662,1493,1270,10372.02 E-NOCH3 NH-CH3 H 2-CH3 5-CH3 4-{-CO-NH-OCH3} 141-1452.03 E-NOCH3 NH-CH3 H 2-CH3 5CH3 4-{-CO-NH-OC2H5} 177-1802.04 E-NOCH3 NH-CH3 H 2-CH3 5-CH3 4-{-CO-NHOCH2CH=CH2} 130-1342.05 E-NOCH3 NH-CH3 H 2-CH3 5-CH3 4-{-CO-NH-OCH(CH3)2} 171-1752.06 E-NOCH3 NH-CH3 H 2-CH3 H 4-{-CO-NH-OC2H5} 142-1452.07 E-NOCH3 NH-CH3 H 2-CH3 H 4-{-CO-NH-OCH2CH=CH2} 127-129
取代的苯甲氧苯基衍生物I适用于控制有害真茵和害虫、蜘蛛纲动物和线虫纲。可用作保护庄稼的杀真菌剂和杀虫剂以及应用于卫生学、材料贮藏保存和兽医学领域。
害虫包括:
-蝴蝶目中(:Lepidoptera)、如小地老虎、芜菁夜蛾、棉叶波纹夜蛾、黎豆夜蛾、苹果银蛾、汉马夜蛾、松天蛾、cacoeciamūrinana,capua reticulana,冬尺蛾、枞色卷蛾、choritoneura occidentalis、一点粘虫、苹蠹蛾、瓜野暝、巨座玉米螟、非洲蔗螟、欧洲松梢小卷蛾、粒肤地虎、Eupoeciliaambiguella、蜡螟、李小食心虫、梨小食心虫、棉铃虫、烟芽夜蛾、棉铃虫、菜心野螟、Hibernia defoliaria、西部铁杉尺蛾、甜菜夜蛾、咖啡一点潜蛾、旋纹潜蛾、Lithocolletis blancardella、lobesia botrana、网锥额野螟、舞毒蛾、模毒蛾、桃潜蛾、无幕毛虫、甘蓝夜蛾、花旗松毒蛾、玉米螟、小眼夜蛾、棉红铃虫、豆杂色夜蛾、园掌舟蛾(phalera bucephola)、马铃薯麦蛾、桂叶潜蛾、大菜粉蝶、苜蓿绿夜蛾、小菜蛾、大豆夜蛾、二三针松小卷蛾、Scrobipalpula absoluta,麦蛾、葡萄长须卷蛾、草地贪夜蛾、Spodoptera littoralis,Spodoptera litura,Thaumatopoeapityocampa栎绿卷蛾、粉纹夜蛾Zeiraphera canadensis;- 甲虫目中(Coleoptera)、例如,梨长吉丁、直条叩甲、晦暗叩甲、Amphimallus solstitialis、李梨木小蠹、野棉象、梨花象、甜菜隐食甲、Blastophagus Piniperda、Blitophaga undata、Bruchus rufimanus、豌豆象、Bruchus lentis、桦卷叶象、甜菜大龟甲、豆叶甲、甘蓝荚象甲、Ceuthorrhynchus napi、甜菜胫跳甲、烟金针虫、天门冬叶甲、长角叶甲、Diabrotica 12-punctata、玉米幼芽根叶
、黑西哥豆
、烟草跳甲、棉籽灰象甲、松树皮象、埃及苜蓿象甲、苜蓿叶象虫、云杉八齿小蠹、烟负泥虫、橙足负泥虫(lema melanopus)、马铃薯甲虫、Limoniuscalifornicus、玉米叩甲、美洲稻象甲、油菜花露尾甲、Melolontha hippocastani、Melolontha melolontha、稻负泥虫、Ortiorrhynchus sulcatus、Otiorrhynchus ovatus、辣根猿叶虫、Phyllophaga SP.、Phyllopertha horticola、Phyllotreta chrysocephala、芜菁淡足跳甲、曲条跳甲、Popillia japonica、豌豆叶象甲(sitona lineatus)、谷象(Sitophilus granaria);- 双翅目昆虫目(Diptera),例如:Aedes aegypti、Aedesvexans、黑西哥桔实蝇(Anastrepha ludens)、Anophelesmaculipennis、地中海实蝇、Chrysomya bezziana、Chrysomyahominivorax、Chrysomya macellaria、高梁瘿蚊、Cordylobiaanthropophaga、Culex pipiens、瓜实蝇、油榄实蝇(Dacusoleae)、Dasineura brassicae、Fannia canicularis、肠胃蝇、Glossia morsitans、Haematobia irritans、Haplodiplosisequestris、种绳、纹皮蝇(Hypoderma lineata)、Liriomyzasativae、Liriomyza trifolii、Lucilia cuprina、丝光绿绳、Lycoria pectoralis、小麦瘿蚊、家蝇、Muscina stabulans、羊鼻蝇、瑞典麦杆蝇、菠菜潜叶花蝇、Phorbia antiqua、Phorbia brassicae、Phorbia coarctata、Rhagoletis cerasi、苹实蝇、Tabanus bovinus、Tipula oleracea、沼泽大蚊;-蓟马目(Thysanoptera)、例如烟褐蓟马、苜蓿蓟马、桔实蓟马、Frankliniella tritici、稻蓟马、棕黄蓟马、棉蓟马;-膜翅目昆虫(Hymenoptera),例如菜叶蜂、热带切叶蚁、切叶蚁、得州切叶蚁、叶蜂、苹实叶蜂、法老蚁、义蚁、红外来火蚁;-臭虫目(Heteroptera)、例如喜绿蝽、多毛长蝽、Cyrtopeltisnotatus、Dysdercus cingulatus、Dysdercus intermedius、Eūrygaster integriceps、Euchistus impictiventris、叶喙缘蝽、牧草盲蝽、稻绿蝽、甜菜拟网蝽、Solubea insularis、Thyanta perditor;-植物虱目昆虫(同翅亚目)、例如Acyrthosiphon onobrychis、落叶松球蚜、Aphidula nasturtii、甜菜蚜、苹果蚜、Aphissambuci、Brachycaudus cardui、甘蓝蚜、Cerosiphagossypii、Dreyfusia nordmannianae、Dreyfusia piceae、Dyasphis radicola、Dysaulacorthum Pseudosolani、蛋豆微叶蝉、麦长管蚜、马铃薯长管蚜、蔷薇长管蚜、Megouraviciae、Metopolophium dirhodum、Myzodes persicae、樱桃瘤蚜、稻褐飞虱、柄瘿绵蚜、蔗飞虱、忽布疣额蚜、苹木虱、梨木虱(Psylla piri)、Rhopalomyzus ascalonicus、玉米蚜、Sappaphis mala、Sappaphis maii、草间裂蚜茧蜂、榆梨绵蚜(Schizoneura lanuginosa)、温室粉虱、Viteus Vitifolii;- 白蚁目(Isoptera)、例如Calotermes flavicollis、Leucotermes flavipes、Reticulitermes lucifugus、Termesnatalensis;- 直翅目昆虫(Orthoptera)、例如家蟋蟀、东方 蠊、德国小蠊、欧洲球螋、欧洲蝼蛄、飞蝗(Locusta migratoria)、Melanoplusbirittatus、赤腿蚱蜢、墨西哥蚱蜢、迁徙蚱蜢、落矶山蚱蜢、红翅蝗、美洲大蠊、美洲蝗、Schistocerca peregrina、Stauronotus maroccanus、温室蟋螽。
有害的蜘蛛纲动物(Acarina)包括,例如美国花蜱、AmblyommaVariegatum、波斯锐缘蜱、环形牛蜱、褪色牛蜱、微小牛蜱、紫红短须螨、苜蓿苔螨、森林革蜱、鹅耳枥始叶螨、桔瘿螨、Hyalomma truncatum、蓖子硬蜱、Ixodes rubicundus、非洲钝缘蜱、耳刺残喙蜱(Otobins megnini)、苹果全爪螨、Permanyssus gallinae、Phyllocaptrata oleivora、侧多食跗线螨、Psoroptes ovis、非洲扇头蜱、Rhipicephalus evertsi、Saccoptes scabiei、棉红蜘蛛、神泽叶螨、太平洋叶螨、棉叶螨、二点叶螨。
有害线虫的例子有根虫瘿线虫,例如Meloidogyne hapla、黄麻根瘤线虫、Meloidogyne javanica,胞囊形成的线虫,例如Globodera rostochiensis、Heterodera avenae、Heteroderaglycinae、Heterodera Schatii、Heterodera trifolii,茎叶eelworms,例如,Belonolaimus longicaudatus、Ditylenchusdestructor、Ditylenchus dipsaci、Heliocotylenchusmulticinctus、Longidorus elongatus、Radopholus similis、Rotylenchus robustus、Trichodorus primitivus、Tylenchorhynchus claytoni、Tylenchorhynchus dubius、Pratylenchus neglectus、Pratylenchus penetrans、Pratylenchus curvitatus、Pratylenchus goodeyi。
取代的苯甲氧基苯基衍生物I有时是有内吸活性的杀真菌剂。它们可以用作叶面或土壤杀真菌剂,对植物病菌中的真菌具有广谱作用,特别是对子囊菌纲、半知菌类、藻状菌类、和担子菌纲特别适用。
它们对控制各种庄稼植物的多种真菌特别有用,例如对小麦、黑麦、大麦、燕麦、稻子、玉米、牧草、棉花、大豆、咖啡、甘蔗、葡萄、水果以及观赏性植物,和蔬菜类植物如黄瓜、豆类和葫芦类,以及这些植物的种子特别有用。
化合物I特别对下列植物疾病适用:- 谷物白粉病,葫芦白粉病,
苹果白粉病,葡萄白粉病,谷类丙锈菌属病,棉花和牧草立桔病谷物和甘蔗黑穗病,苹果黑星病,谷物条纹病,小麦颖枯病,草莓葡萄灰霉病,花生褐斑病,Pseudocercosporella herpotrichoideson wheat,barley,稻瘟病,马铃薯如西红柿晚疾病,各种植物的立枯病和黄萎病、葡萄霜霉病、蔬菜和水果的黑斑病
这些新化合物还可用来保护材料(保存木料),例如抗多变拟青霉。
它们可以制成常用制剂,如溶液、乳剂、悬浮剂、粉剂、粉末、糊剂或颗粒剂。使用的剂型取决于使用对象;每种情形应尽可能地将活性化合物达到最佳的分散。
制剂通过已知的方法制备,如将活性化合物与溶剂和/或载体相混合,如需要还可使用乳化剂和分散剂,其中如果水用作稀释剂,则其它有机溶剂也可以用作辅助溶剂。
适合的辅助剂主要是:
-溶剂如芳香族化合物(例如二甲苯)、氯代芳香族化合物(如氯苯)、链烷烃(例如石油馏份)、醇(例如甲醇、丁醇)、酮(例如环己酮)、胺(例如乙醇胺、二甲基甲酰胺)和水;
-载体如磨碎的天然矿物质(例如高岭土、矾土、滑石、白垩)和磨碎的合成矿物质(例如高分散二氧化硅、硅酸盐);
-乳化剂如非离子或阴离子乳化剂(例如聚氧乙烯脂肪醇醚、烷基磺酸盐和芳基磺酸盐)和
-分散剂如木素-亚硫酸盐废液和甲基纤维素。
合适的表面活性物质为碱金属、碱土金属和铵的芳香磺酸盐,例如木素磺酸、苯磺酸、萘磺酸和二丁基萘磺酸,以及脂肪酸、烷基和烷基芳基磺酸盐、烷基、月桂基醚和脂肪醇硫酸盐、以及硫酸化的己、庚和十八烷醇的盐,以及脂肪醇乙二醇醚、磺化的萘及其衍生物与甲醛的缩合产物、萘或萘磺酸与苯酚和甲醛的缩合产物、聚氧乙烯辛基苯酚醚、乙氧基化的异辛基、辛基或壬基酚、烷基苯酚或三丁基苯基聚乙二醇醚、烷基芳基聚醚醇、异十三烷基醇、脂肪醇环氧乙烷缩合物、乙氧基化的蓖麻油、聚氧乙烯或聚氧丙烯烷基醚、月桂醇聚乙二醇醚乙酸酯、山梨醇酯、木素-亚硫酸盐废液或甲基纤维素。
使用的水溶液可以由乳化浓缩物、分散液、糊剂、可湿性粉末或可水分散颗粒加水制成。为制备乳剂、糊剂或油分散剂,通过润湿剂、粘合剂、分散剂或乳化剂的作用,使基质均匀分散在水中,或溶解在油或溶剂中。然而,适于用水稀释的由活性物质、润湿剂、粘合剂、分散剂或乳化剂以也可以制备及可能的溶剂或油组成的浓缩物。
粉末、分散的和粉尘化的组合物可以通过将活性物质与固体载体混合或一同研磨来制备。
颗粒,如包衣的、浸制的和均匀的颗粒,可通过将活性化合物与固体载体结合来制备。
固体载体是无机土,如硅胶、硅酸、硅酸盐、滑石、高岭土、石灰石、石灰、白垩、bole、黄土、粘土、白云石、硅藻土、硫酸钙和硫酸镁、氧化镁、研细的合成材料、肥料如硫酸铵、磷酸铵、硝酸铵、尿素和植物产品如谷物、树皮粉、木粉和坚果壳粉、纤维粉或其它固体载体。在预备使用的制剂中的活性化合物的浓度可以在相当宽的范围内变化。
通常,组合物中活性化合物的含量为0.0001至95%(以重量计)的活性化合物。
活性化合物含量超过95%(以重量计)的制剂可以非常成功地应用于超低量方法(ULV)中,甚至可以在不加添加剂条件下使用活性化合物。
用作杀真菌剂时,活性化合物浓度为0.01至95%(以重量计),优选0.5至90%。用作杀虫剂时,制剂中活性化合物的合适含量为0.0001至10%(以重量计),优选0.01至1%(以重量计)。
一般使用的活性化合物的纯度为90%至100%,优选95%至100%(参照NMR谱)。
制剂的实例是:I.含90重量份的化合物I.01号和10重量份的N-甲基-α-吡咯烷酮的溶液,该制剂适用于以非常小的液滴形式使用。II.在由80重量份烷基化苯、10重量份由8至10摩尔的环氧乙烷与1摩尔油酰N-单乙醇酰胺形成的加成产物、5重量份十二烷基苯磺酸钙、5重量份由40摩尔环氧乙烷与1摩尔蓖麻油的加成产物组成的混合物中的20重量份的化合物I.02号的溶液;通过将上述组合物很好地分散在水中得到一种分散剂。III.20重量份化合物I.03号在由40重量份环己酮、30重量份异丁醇、20重量份7摩尔环氧乙烷与1摩尔异辛基苯酚的加成产物和10重量份40摩尔环氧乙烷与1摩尔蓖麻油的加成产物组成的混合物中的溶液;将上述组合物很好地分散在水中得到一种分散剂。IV.20重量份化合物I.04在由25重量份环己酮、65重量份沸点为210到280℃的石油馏份和10重量份40摩尔环氧乙烷与1摩尔蓖麻油的加成产物组成的混合物中的含水分散液;将上述组合物很好地分散在水中得到分散剂。V.在锤磨机中磨碎的20重量份化合物I.01号、3重量份二异丁基萘-α-磺酸钠、17重量份由亚硫酸盐废液得到的木素磺酸钠和60重量份磨细的硅胶组成的混合物,将上述组合物在水中很好的分散得到喷雾混合物;VI.3重量份化合物I.02号与97 重量份细粉碎的高岭土组成的紧密混合物;该粉状组合物含3%(以重量计)活性化合物;VII、30重量份化合物I.03号、92重量份粉状硅胶和8重量份已喷到上述硅胶表面上的液体石蜡组成的紧缩密混合物;该制剂使活性化合物有良好的粘性;VIII.40重量份化合物I.04号、10重量份苯磺酸钠/尿素/甲醛缩合物、2重量份硅胶和48重量份水组成的稳定的水分散液,该水分散液可以进一步稀释;IX.20重量份化合物I.01号、2重量份十二烷基苯磺酸钙、8重量份脂肪醇聚乙二醇醚、2重量份苯磺酸钠/尿素/甲醛缩合物和68重量份石蜡矿物油组成的稳定的油分散剂;X.在锤磨机中研碎的10重量份化合物2.1号、4重量份二异丁基萘-α-磺酸钠、20重量份由亚硫酸盐废液中得到的木素磺酸钠、38重量份硅胶和38重量份高岭土组成的混合物。将此混合物均匀分散到10,000重量份水中,得到含0.1%(以重量计)活性化合物的喷雾混合物。
这些化合物可通过下述方法来应用,即用杀菌有效量的活性化合物处理真菌或种子、植物、材料或土壤以防止其被真菌侵害。
它们可用于材料、植物或种子被真菌感染前或后。
依据想要达到的效果,使用量为每(ha)0.02至3kg活性化合物,优选0.1到1kg/ha。
在种子处理中,通常每千克种子需要0.001至50g活性化合物,优选0.01至10g。
在户外条件下用于控制害虫的活性化合物的用量为0.02至10kg/ha,优选0.1至2.0kg/ha。
化合物I,在以其自身与除草剂或杀真菌剂混合使用时,还可以与其它作物保护剂混和使用,例如与生长调节剂或与控制害虫或细菌的试剂混合使用。有价值的还有其与用来克服营养和微量元素缺乏的肥料或无机盐溶液的可混性。
作物保护剂和肥料可以以重量比为1∶10至10∶1的比例加到本发明组合物中,如可行甚至可在使用前即时混合(罐混合)。与杀真菌剂或杀昆虫剂混合时,多数情况会提高其杀真菌作用谱。
以下列出与本发明化合物共同使用的杀真菌剂,在此仅为了说明混合使用的可能性,而不是对它们进行限定:
硫,
二硫代氨基甲酸盐类及其衍生物,例如
二甲基二硫代氨基甲酸铁,
二甲基二硫代氨基甲酸锌,
亚乙基双二硫代氨基甲酸锌,
亚乙基双二硫代氨基甲酸锰,
乙二胺双二硫代氨基甲酸锰锌,
二硫化四甲基秋兰姆,
N,N-亚乙基双二硫代氨基甲酸锌的氨配合物,
N,N′-亚丙基双二硫代氨基甲酸锌的氨配合物,
N,N′-亚丙基双二硫代氨基甲酸锌,
二硫化N,N′-聚丙烯双(硫代氨基甲酰基),
硝基衍生物,例如巴豆酸二硝基(1-甲基庚基)苯酯,
3,3-二甲基丙烯酸2-仲丁基-4,6-二硝基苯酯、
碳酸2-仲丁基-4,6-二硝基苯基异丙酯
5-硝基间苯二甲酸二异丙酯;
杂环物质,例如2-十七烷基-2-咪唑啉乙酸酯,
2,4-二氯-6-(邻-氯苯胺基)-s-三嗪,
苯二酰亚氨基硫代磷酸O,O-二乙酯,
5-氨基-1-β-[双-(二甲基氨基)-氧膦基]-3-苯基-1,2,4-三嗪,
2,3-二氰基-1,4-二硫代蒽醌,
2-硫代-1,3-二硫杂环戊并-β-[4,5-b]喹喔啉,
1-(丁基氨基甲酰基)-2-苯并咪唑氨基甲酸甲酯,
2-甲氧羰基氨基苯并咪唑,
2-(呋喃-2-基)苯并咪唑,
2-(噻唑-4-基)苯并咪唑,
N-(1,1,2,2-四氯乙硫基)四氢苯邻二甲酰亚胺,
N-三氯甲硫基四氢苯邻二甲酰亚胺,
N-三氯甲硫基苯邻二甲酰亚胺,
N-二氯氟甲硫基-N′,N′-二甲基-N-苯硫酰胺,
5-乙氧基-3-三氯甲基-1,2,3-噻二唑,
2-氰硫基甲硫基苯并噻唑,
1,4-二氯-2,5-二甲氧基苯,
4-(2-氯苯基亚肼基)-3-甲基-5-异噁唑酮,
2-硫代吡啶-1-氧化物,
8-羟基喹啉或其铜盐,
2,3-二氢-5-羰基N,N′-草酰二苯氨基-6-甲基-1,4-氧硫杂环已二烯(2,3-dihydro-5-Carboxanilido-6-methyl-1,4-Oxathiin),
2,3-二氢-5-羰基N,N′草酰二苯氨基-6-甲基-1,4-氧硫杂环己二烯-4,4-二氧化物(2,3-dihydro-5-Carbo xanilido-6-mthyl-1,4.Oxathiin-4,4-dioxidy)
2-甲基-5,6-二氢-4H-吡喃-3-甲酰苯胺,
2-甲基呋喃-3-甲酰苯胺,
2,5-二甲基呋喃-3-甲酰苯胺,
2,4,5-三甲基呋喃-3-甲酰苯胺,
N-环己基-2,5-二甲基呋喃-3-甲酰胺,
N-环己基-N-甲氧基-2,5-二甲基呋喃-3-甲酰胺,
2-甲基-N-苯甲酰苯胺,
2-碘-N-苯甲酰苯胺,
N-甲酰-N-吗啉-2,2,2-三氯乙基缩醛
哌嗪-1,4-二基双(1-(2,2,2-三氯乙基)甲酰胺
1-(3,4-二氯苯胺基)-1-甲酰氨基-2,2,3-三氯乙烷,
2,6-二甲基-N-十三烷基吗啉或其盐,
2,6-二甲基-N-环十二烷基吗啉或其盐,
N-[3-(对叔丁苯基)-2-甲丙基]-顺-2,6-二甲基吗啉,
N-[3-(对叔丁苯基)-2-甲丙基]哌啶,
1-[2-(2,4-二氯苯基)-4-乙基-1,3-二氧戊环-2-基乙基]-1H-1,2,4-三唑,
1-[2-(2,4-二氯苯基)-4-正丙基-1,3-二氧戊环-2-基乙基]-1H-1,2,4-三唑,
N-[正丙基)-N-(2,4,6-三氯苯氧乙基)-N′-咪唑基脲,
1-(4-氯苯氧基)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)-2-丁酮,
1-(4-氯苯氧基)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)-2-丁醇,
α(2-氯苯基)-α-(4-氯苯基)-5-嘧啶甲醇,
5-丁基-2-二甲基氨基-4-羟基-6-甲基嘧啶,
双(对-氯苯基)-3-嘧啶甲醇,
1,2-双(3-乙氧羰基-2-硫脲基)苯,
1,2-双(3-甲氧羰基-2-硫脲基)苯,
还有其它的各种杀真菌剂,例如十二烷基胍乙酸盐,
3-[3-(3,5-二甲基-2-氧环已基)-2-羟乙基]戊二酰亚胺,
六氯苯,
DL-甲基-N-(2,6-二甲基苯基)-N-2-糠酰基氨基丙酸盐,
DL-N-(2,6-二甲基苯基)-N-(2′-甲氧乙酰基)氨基丙酸甲酯,
N-(2,6-二甲苯基)-N-氯乙酰-D,L-2-氨基丁内酯,
DL-N-(2,6-二甲基苯基)-N-(苯乙酰基)氨基丙酸甲酯,
5-甲基-5-乙烯基-3-(3,5-二氯苯基)-2,4-二氧-1,3-氧氮杂环戊烷,
3-(3,5-二氯苯基)-5-甲基-5-甲氧甲基-1,3-氧氮杂环戊烷-2,4-二酮,
3-(3,5-二氯苯基)-1-异丙基氨基甲酰基乙内酰脲,
N-(3,5-二氯苯基)-1,2-二甲基环丙烷-1,2-甲二酰亚胺(dicarboximide),
2-氰基-[N-乙基氨基羰基-2-甲氧亚氨基]乙酰胺,
1-[2-(2,4-二氯苯基)戊基]-1H-1,2,4-三唑,
2,4-二氟-α-(1H-1,2,4-三唑-1-甲基)二苯甲醇,
N-(3-氯-2,6-二硝基-4-三氟甲基苯基)-5-三氟甲基-3-氯-2-氨基吡啶,
1-((双(4-氟苯基)甲基甲硅烷基)甲基)-1H-1,2,4-三唑。
应用实施例(杀真菌剂活性)
应用实施例1
抗小麦褐锈活性
用褐锈胞子(Puccinia recondita)撒在生长在盆中的Kanzler麦苗叶上。将这些盆在20到22℃、具有高的空气湿度(从90至95%)的室中放置24小时。在此期间胞子生长并且菌管刺入叶组织。这些受感染组织用含水喷淋混合物喷淋直至其呈欲滴状湿润,喷淋混合物以干物质计含有80%(以重量计)活性化合物和20%(以重量计)乳化剂。喷淋层干结后,将试验植物放置在20至22℃、65至70%相对空气湿度的温室中。8天后,测定在叶上的锈菌程度。
通过用含63ppm的化合物1.01,1.02,1.03,1.04,1.05,1.07,1.08,1.09,1.10,1.11,1.14,1.15或1.16的含水活性化合物制剂处理,很可能可以防止真菌的侵害(0-15%)。
用对比化合物的含水制剂(浓度:63ppm)处理的植物,如同未处理的对照植物一样,65%叶面受到真菌侵害。
应用实施例2
抗稻瘟活性(Protective)
用以干物质计含80%(重量)活性化合物和20%(重量)乳化剂的含水乳剂喷淋生长在盆中的Tai-Nong类稻苗叶直至其呈欲滴状湿润并且24小时后用稻瘟胞子含水悬浮液接种。将试验植物放置在22-24℃和95-99%相对湿度的气候控制室。6天后测定病害程度。
未经处理的对照植物叶子被真菌侵害达70%,用化合物1.01,1.03,1.04,1.05,1.07,1.08,1.10,1.11,1.13,1.14,1.15和1.16的含水制剂(浓度:63PPM)处理的植物叶子上仅有0-25%受真菌侵害。
使用对比化合物的含水制剂(浓度:63ppm),真菌侵害没有明显减少(60%叶子受侵害)。应用实施例(杀虫剂活性)
将活性化合物制成浓度为10%(重量)的在下述混合物中的乳剂,并根据所需的浓度用水稀释,所说的混合物由70%(重量)环己醇,20%(重量)NekanilLN*)和10%(重量)EmulphorEL**)所组成。试验结束后,最低浓度是这样确定的,即在该浓度下相比于未经处理的对照试验,化合物I仍能导致80-100%的死亡率(活性阈值或最低浓度)
*)LutensolAP6为含有以乙氧基化烷基酚为基的乳化剂且具有分散作用的润湿剂
**)EmulanEL为以乙氧基化脂肪醇为基的乳化剂。应用实施例3(杀虫活性)
抗Nephotettix cincticeps活性(绿稻叶蚱蜢);接触作用
将5只成龄叶蚱蜢放入用含水活性化合物制剂处理过的圆筒(9cm)中。24小时后,死亡率评估如下:
100%=无叶蚱蜢存活;
80%=有1只叶蚱蜢存活;
60%=有2只叶蚱蜢存活;
<60%-至少有3只叶蚱蜢存活(=无效果)。
化合物1.01,1.02,1.03,1.04,1.08,1.09.1.10,1.11,1.14,1.15和1.16的活性阈值为每圆筒最多使用0.4mg。
应用实施例4(杀虫接触活性)
抗Prodenia litura活性(Egyptian lotton leafworm)
将5条毛虫放入用含水活性化合物制剂处理过的圆筒(约9cm)中。4小时后进行第一次评估。如仍至少有一毛虫活着,则加入下述组合物。
20L水;
800g琼脂;
13L水;
1370g酵母粉(Engevita酵母);
5150g玉米粉;
1300g小麦胚;
200g韦宋(Wesson)盐;
100g纤维粉;
50g山梨酸;
50g尼泊金A;
10g维生素混合物,含
30gVB1,
60gVB2,
30gVB6,
120g烟酸/烟酸,
120g D-泛酸钙,
30g叶酸和
1.2g维生素H;
50ml抗生素(1%醇溶液);
180g抗坏血酸;
1.5L水用来冲洗维生素并冲出容器。
24小时后测定死亡率。
化合物1.02,1.04和1.05活性阈值(=4条毛虫死亡)是每圆筒最多使用0.4mg。
应用实施例5(杀壁虫接触作用)
抗Tetranychus telarius活性(棉红蜘蛛)
被蜘蛛严重侵害的已长成第二对成龄叶的盆栽开花矮株豆,用含水活性化合物制剂进行喷淋直至其呈欲滴状湿润。其中用约30ml喷淋混合物喷淋置于转台上的植物的所有侧面。在温室中5天之后,用显微镜(双目显微镜)以死亡百分率%来确定其控制虫害的成功。
该试验中化合物1.01至1.16的活性阈值的最大值为400ppm。
Claims (14)
1.式I的取代的苯氧基甲基苯基衍生物:其中:
X为=CH-OCH3,=CH-CH3或=N-OCH3;
R1为C1-C6烷基,C2-C6链烯基,C3-C6链炔基,C1-C6卤代烷基,C3-C6卤代链烯基,C1-C4烷氧基-C1-C6烷基,氰基-C1-C6烷基,C1-C6-烷氧基羰基-C1-C6烷基,C3-C6环烷基或C3-C6环烷基-C1-C4烷基,芳基-C1-C6烷基或芳基-C3-C6链烯基或芳氧基-C1-C6烷基,饱和或未饱和的4至6元杂环基或杂环-C1-C4烷基或杂芳基-C1-C6烷基,所说的杂环除了含有碳原子以外,还含有一个或二个选自如下的杂原子的环原子:氧原子或硫原子,一个或二个氮原子和一个或二个-N(CH3)-基团,
对于上述碳环和杂环来说,其还可能含有一个或多个选自下述的基团:卤素,C1-C4烷基,C1-C2卤代烷基,C3-C6环烷基,C1-C4烷氧基,C1-C2卤代烷氧基,芳基和芳氧基;
R2和R3为氢,卤素,氰基,硝基,C1-C4烷基,C1-C2-卤代烷基,C1-C4烷氧基,C1-C2卤代烷氧基,如果R2和R3彼此相邻,则R2和R3可以构成氧亚甲基氧桥或氧亚乙基氧桥,对于这些桥中的每个碳原子来说,还可以含有一个或二个卤原子和/或甲基;
R4为氰基,氯,溴,C1-C6烷氧基,C1-C6烷硫基,C1-C4卤代烷氧基,C1-C4烷氧基-C1-C4烷氧基,C3-C6环烷基-C1-C2烷氧基,C1-C6烷基氨基,二-(C1-C6烷基)氨基,C3-C6链烯氧基,C3-C6链炔氧基,芳氧基,芳硫基,对于芳族环还可能含有一至三个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中进一步还可包含足够的卤原子以使取代基的总数达到4或5个;
R5为硝基,氰基,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷硫基,苯基或苯氧基,其中芳环可能含有1至3个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中可能还进一步含有足够的卤原子以使取代基的总数达到4或5个;
或如果n是2,3或4,则R5是与母体物质的二个相邻碳原子稠合的1,3-丁二烯-1,4-二基或一或二卤代的1,3-丁二烯-1,4-二基,这些稠合环还可能含有一个或二个选自下述的基团:硝基,氰基,卤素,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基;
n是0.1,2,3或4,如果n为2,3或4时,R5基团可以相同或不同;
Y是氧,-NH-或-N(CH3)-;
R6是氢或C1-C4烷基。
3.权利要求1所述的Y是-NH-或-N(CH3)-的式I的取代的苯氧基甲基苯基衍生物的制备的方法,包括Y是氧的式I苯氧基甲基苯基衍生物,或式VI的苯基苄基醚与式为H2N-R6或HN(CH3)-R6的胺进行反应,其中R7是羰基活性基团。
4.通式XI′的苯基乙醛酸衍生物的制备方法,包括使通式X′的乙酰苯进行卤仿反应: 其中Y′是-NH-或-N(CH3)-。
Y′是-NH-或-N(CH3)-;
R2和R3分别为氢,卤素,氰基,硝基,C1-C4烷基,C1-C2卤代烷基,C1-C4烷氧基,C1-C2卤代烷氧基:
R5为硝基,氰基,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷硫基,苯基或苯氧基,其中芳环可能含有1至3个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中可能还进一步含有足够的卤原子以使取代基的总数达到4或5个;
或如果n是2,3或4,则R5是与母体物质的二个相邻碳原子稠合的1,3-丁二烯-1,4-二基或一或二卤代的1,3-丁二烯-1,4-二基,这些稠合环还可能含有一或二个选自下述的基团:硝基,氰基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基;
n是0,1,2,3或4,如果n为1,2,3或4时,R5基团可以相同或不同;
R6是氢或C1-C4烷基。
其中X是=CH-OCH3,=CH-CH3或=N-OCH3;
Y是氧,-NH-或-N(CH3)-;
R1是C1-C6烷基,C2-C6链烯基,C3-C6链炔基,C1-C6卤代烷基,C3-C6卤代烯基,C1-C4烷氧基-C1-C6烷基,氰基-C1-C6烷基,C1-C6烷氧基羰基-C1-C6烷基,C3-C6环烷基或C3-C6环烷基-C1-C4烷基,芳基C1-C6烷基或芳基C3-C6链烯基或芳氧基-C1-C6烷基,饱和或不饱和的4元至6元杂环基或杂环基-C1-C4烷基或杂芳基-C1-C6烷基,杂环上除了碳原子以外还含有1个或2个选自下述的基团作为环原子,氧或硫原子,1个或2个氮原子和1个或2个-N(CH3)-基团。
碳环和杂环上可能还含有一个或多个选自下述的基团:卤素,C1-C4烷基,C1-C2卤代烷基,C3-C6环烷基,C1-C4烷氧基,C1-C2卤代烷氧基,芳基和芳氧基;
R2和R3为氢,卤素,氰基,硝基,C1-C4烷基,C1-C2-卤代烷基,C1-C4烷氧基,C1-C2卤代烷氧基,如果R2和R3彼此相邻,则R2和R3可以构成氧亚甲基氧桥或氧亚乙基氧桥,对于这些桥中的每个碳原子来说,还可以含有一个或二个卤原子和/或甲基;
R5为硝基,氰基,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷硫基,苯基或苯氧基,其中芳环可能含有1至3个选自下述的基团:C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基,芳环中可能还进一步含有足够的卤原子以使取代基的总数达到4或5个;
或如果n是2,3或4,则R5是与母体物质的二个相邻碳原子稠合的1,3-丁二烯-1,4-二基或一或二卤代的1,3-丁二烯-1,4-二基,这些稠合环还可能含有一或二个选自下述的基团:硝基,氰基,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基和C1-C4烷硫基;
n是0,1,2,3或4,如果n为1,2,3或4时,R5基团可以相同或不同;
R6是氢或C1-C4烷基。
7.按照权利要求1所述的式I的苯氧基甲基苯基衍生物,其中:
n为0或1;
X为=CH-OCH3,=CH-CH3或=N-OCH3;
Y为氧或-NH;
R1是C1-C6烷基,C2-C6链烯基,C3-C6链炔基,C1-C6卤代烷基或C3-C6卤代烯基;
R2是氰基,氯,氟,甲基,三氟甲基或甲氧基;
R3是氢,氰基,氯,氟,甲基或甲氧基;
R4是氰基,氯,溴,C1-C6烷氧基,C1-C6烷硫基,C3-C6链烯氧基,芳氧基或芳硫基,
R5是氰基,卤素,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基或苯基。
8.按照权利要求1所述的式I的苯氧基甲基苯基衍生物,其中:
n是0或1;
X是=NO-CH3;
Y是-NH-;
R1是C1-C6烷基,C2-C6链烯基,C3-C6链炔基,C1-C6卤代烷基或C3-C6卤代链烯基;
R2是氰基,氯,氟,甲基,三氟甲基或甲氧基;
R3是氢,氰基,氯,氟,甲基或甲氧基;
R4是氰基,氯,溴,C1-C6烷氧基,C1-C6烷硫基,C3-C6链烯氧基,苯氧基或苯硫基;
R5是氰基,氯,氟,甲基,三氟甲基,甲氧基或苯基。
9.权利要求1所述的式I的苯氧基甲基苯基衍生物作为杀真菌剂的应用。
10.权利要求1所述的式I的苯氧基甲基苯基衍生物用于抑制害虫的应用。
11.一种杀真菌组合物,它含有固体和/或液体载体和杀真菌有效量的至少一种如权利要求1所述的式I取代的苯氧基甲基苯基衍生物。
12.一种抑制真菌的方法,它包括用杀真菌有效量的至少一种如权利要求1所述的式I取代的苯氧基甲基苯基衍生物处理真菌或可能受真菌侵害的物料,植物,种子或土壤。
13.一种抑制害虫的组合物,它含有惰性添加剂和杀虫有效量的至少一种如权利要求1所述的式I的取代苯氧基甲基苯基衍生物。
14.一种抑制害虫的方法,它包括用杀虫有效量的至少一种如权利要求1所述的式I的取代苯氧基甲苯基衍生物处理害虫和/或它们的栖息地。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4410424 | 1994-03-25 | ||
| DEP4410424.3 | 1994-03-25 |
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| Publication Number | Publication Date |
|---|---|
| CN1121510A true CN1121510A (zh) | 1996-05-01 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN95105106A Pending CN1121510A (zh) | 1994-03-25 | 1995-03-25 | 取代的苯氧基甲基苯基衍生物和其制备方法及其作为抑制害虫和真菌的应用 |
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| Country | Link |
|---|---|
| US (2) | US5545664A (zh) |
| EP (1) | EP0673923B1 (zh) |
| JP (1) | JPH07278084A (zh) |
| KR (1) | KR950032091A (zh) |
| CN (1) | CN1121510A (zh) |
| AT (1) | ATE166341T1 (zh) |
| AU (1) | AU680718B2 (zh) |
| CA (1) | CA2145234A1 (zh) |
| DE (1) | DE59502205D1 (zh) |
| NZ (1) | NZ270787A (zh) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1092181C (zh) * | 1996-06-06 | 2002-10-09 | 陶氏益农有限责任公司 | 苄氧基取代的芳基化合物及其作为杀真菌剂和杀虫剂的用途 |
| CN115215761A (zh) * | 2021-04-15 | 2022-10-21 | 湖南大学 | 二苯肟醚衍生物及其作为杀菌剂和杀虫剂的用途 |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3591743B2 (ja) * | 1996-02-02 | 2004-11-24 | 東京応化工業株式会社 | 化学増幅型レジスト組成物 |
| JP2000506848A (ja) * | 1996-03-08 | 2000-06-06 | ビーエーエスエフ アクチェンゲゼルシャフト | ジフェニルエーテル、その製造法、製造に用いられる中間体、および前記化合物の使用法 |
| CN1126742C (zh) * | 1997-02-03 | 2003-11-05 | 道农业科学公司 | 杀真菌化合物 |
| TW577866B (en) * | 1999-05-05 | 2004-03-01 | Dow Agrosciences Llc | Fungicidal and insecticidal benzyloxy cyclopropyl substituted aromatic compounds |
| ITMI20020814A1 (it) * | 2002-04-17 | 2003-10-17 | Isagro Ricerca Srl | Nuovi analoghi delle strobilurine e loro uso quali acaricidi e insetticidi |
| TW201429401A (zh) * | 2013-01-25 | 2014-08-01 | Univ Nat Taiwan | 斜紋夜盜蛾幼蟲誘引取食劑與其使用方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK47590A3 (en) * | 1989-03-09 | 1997-08-06 | Basf Ag | Fungicidal agent and a method of producing its active substance |
| ATE145891T1 (de) * | 1989-05-17 | 1996-12-15 | Shionogi & Co | Verfahren zur herstellung von alkoxyiminoacetamid-derivaten und ein zwischenproduckt dafür |
| DE4116090A1 (de) * | 1991-05-17 | 1992-11-19 | Basf Ag | (alpha)-phenylacrylsaeurederivate, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung von schaedlingen und schadpilzen |
| DE4117371A1 (de) * | 1991-05-28 | 1992-12-03 | Basf Ag | Antimykotische mittel, die phenylessigsaeurederivate enthalten |
| ES2093327T3 (es) * | 1992-07-15 | 1996-12-16 | Basf Ag | Oximeteres substituidos, procedimiento para su obtencion y su empleo para la lucha contra las pestes y los hongos. |
-
1995
- 1995-03-17 EP EP95103942A patent/EP0673923B1/de not_active Expired - Lifetime
- 1995-03-17 AT AT95103942T patent/ATE166341T1/de not_active IP Right Cessation
- 1995-03-17 DE DE59502205T patent/DE59502205D1/de not_active Expired - Lifetime
- 1995-03-22 CA CA002145234A patent/CA2145234A1/en not_active Abandoned
- 1995-03-23 NZ NZ270787A patent/NZ270787A/en unknown
- 1995-03-23 AU AU15040/95A patent/AU680718B2/en not_active Ceased
- 1995-03-23 US US08/409,039 patent/US5545664A/en not_active Expired - Fee Related
- 1995-03-25 CN CN95105106A patent/CN1121510A/zh active Pending
- 1995-03-25 KR KR1019950006464A patent/KR950032091A/ko not_active Withdrawn
- 1995-03-27 JP JP7068424A patent/JPH07278084A/ja not_active Withdrawn
-
1996
- 1996-05-13 US US08/645,428 patent/US5696161A/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1092181C (zh) * | 1996-06-06 | 2002-10-09 | 陶氏益农有限责任公司 | 苄氧基取代的芳基化合物及其作为杀真菌剂和杀虫剂的用途 |
| CN115215761A (zh) * | 2021-04-15 | 2022-10-21 | 湖南大学 | 二苯肟醚衍生物及其作为杀菌剂和杀虫剂的用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP0673923B1 (de) | 1998-05-20 |
| EP0673923A1 (de) | 1995-09-27 |
| AU680718B2 (en) | 1997-08-07 |
| KR950032091A (ko) | 1995-12-20 |
| JPH07278084A (ja) | 1995-10-24 |
| NZ270787A (en) | 1996-05-28 |
| DE59502205D1 (de) | 1998-06-25 |
| US5696161A (en) | 1997-12-09 |
| ATE166341T1 (de) | 1998-06-15 |
| US5545664A (en) | 1996-08-13 |
| AU1504095A (en) | 1995-10-05 |
| CA2145234A1 (en) | 1995-09-26 |
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