TW308595B - - Google Patents
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- TW308595B TW308595B TW085105422A TW85105422A TW308595B TW 308595 B TW308595 B TW 308595B TW 085105422 A TW085105422 A TW 085105422A TW 85105422 A TW85105422 A TW 85105422A TW 308595 B TW308595 B TW 308595B
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- TW
- Taiwan
- Prior art keywords
- ch2f
- ocf3
- ch2cn
- scf2h
- cho
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- 150000001875 compounds Chemical class 0.000 claims description 151
- -1 2,6-difluorophenyl Chemical group 0.000 claims description 77
- 238000011049 filling Methods 0.000 claims description 58
- 125000000217 alkyl group Chemical group 0.000 claims description 48
- 239000000203 mixture Substances 0.000 claims description 48
- 229910052799 carbon Inorganic materials 0.000 claims description 38
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 38
- 229910052731 fluorine Inorganic materials 0.000 claims description 37
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 31
- 241000238421 Arthropoda Species 0.000 claims description 22
- 125000003545 alkoxy group Chemical group 0.000 claims description 22
- 125000001188 haloalkyl group Chemical group 0.000 claims description 19
- 239000007787 solid Substances 0.000 claims description 19
- 239000000460 chlorine Substances 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 239000003085 diluting agent Substances 0.000 claims description 13
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- 239000007788 liquid Substances 0.000 claims description 7
- 239000004094 surface-active agent Substances 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000001204 N-oxides Chemical class 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims description 3
- 229910052801 chlorine Inorganic materials 0.000 claims description 3
- 230000005180 public health Effects 0.000 claims description 3
- 239000013589 supplement Substances 0.000 claims description 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 238000001467 acupuncture Methods 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 125000000664 diazo group Chemical group [N-]=[N+]=[*] 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 249
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 240
- 125000001246 bromo group Chemical group Br* 0.000 description 224
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 description 176
- 125000004093 cyano group Chemical group *C#N 0.000 description 172
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 164
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 description 148
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 132
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 92
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 73
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 description 54
- 238000006243 chemical reaction Methods 0.000 description 47
- 229910052698 phosphorus Inorganic materials 0.000 description 36
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 35
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 25
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 25
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 24
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 24
- 125000001309 chloro group Chemical group Cl* 0.000 description 23
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 23
- 239000000243 solution Substances 0.000 description 22
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 21
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 21
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 20
- 239000002904 solvent Substances 0.000 description 20
- 241000607479 Yersinia pestis Species 0.000 description 19
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 18
- 239000003921 oil Substances 0.000 description 18
- 235000019198 oils Nutrition 0.000 description 18
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 description 17
- 125000005843 halogen group Chemical group 0.000 description 17
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 15
- 238000002360 preparation method Methods 0.000 description 15
- 238000012360 testing method Methods 0.000 description 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 14
- 125000000304 alkynyl group Chemical group 0.000 description 14
- 229910014585 C2-Ce Inorganic materials 0.000 description 13
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 13
- 241000196324 Embryophyta Species 0.000 description 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 13
- 125000003342 alkenyl group Chemical group 0.000 description 13
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 description 13
- 238000005481 NMR spectroscopy Methods 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 12
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 12
- 125000000753 cycloalkyl group Chemical group 0.000 description 12
- 238000007639 printing Methods 0.000 description 12
- 239000002253 acid Substances 0.000 description 11
- 125000004414 alkyl thio group Chemical group 0.000 description 11
- 229940125904 compound 1 Drugs 0.000 description 11
- 230000002079 cooperative effect Effects 0.000 description 11
- BGNGWHSBYQYVRX-UHFFFAOYSA-N 4-(dimethylamino)benzaldehyde Chemical compound CN(C)C1=CC=C(C=O)C=C1 BGNGWHSBYQYVRX-UHFFFAOYSA-N 0.000 description 10
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 10
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 238000009472 formulation Methods 0.000 description 10
- 238000002844 melting Methods 0.000 description 10
- 230000008018 melting Effects 0.000 description 10
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 10
- 238000003786 synthesis reaction Methods 0.000 description 10
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 description 9
- IWZSHWBGHQBIML-ZGGLMWTQSA-N (3S,8S,10R,13S,14S,17S)-17-isoquinolin-7-yl-N,N,10,13-tetramethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-amine Chemical compound CN(C)[C@H]1CC[C@]2(C)C3CC[C@@]4(C)[C@@H](CC[C@@H]4c4ccc5ccncc5c4)[C@@H]3CC=C2C1 IWZSHWBGHQBIML-ZGGLMWTQSA-N 0.000 description 9
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 9
- 241000238631 Hexapoda Species 0.000 description 9
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 9
- KGNDCEVUMONOKF-UGPLYTSKSA-N benzyl n-[(2r)-1-[(2s,4r)-2-[[(2s)-6-amino-1-(1,3-benzoxazol-2-yl)-1,1-dihydroxyhexan-2-yl]carbamoyl]-4-[(4-methylphenyl)methoxy]pyrrolidin-1-yl]-1-oxo-4-phenylbutan-2-yl]carbamate Chemical compound C1=CC(C)=CC=C1CO[C@H]1CN(C(=O)[C@@H](CCC=2C=CC=CC=2)NC(=O)OCC=2C=CC=CC=2)[C@H](C(=O)N[C@@H](CCCCN)C(O)(O)C=2OC3=CC=CC=C3N=2)C1 KGNDCEVUMONOKF-UGPLYTSKSA-N 0.000 description 9
- 229940125758 compound 15 Drugs 0.000 description 9
- 229940125833 compound 23 Drugs 0.000 description 9
- 235000013601 eggs Nutrition 0.000 description 9
- 235000019439 ethyl acetate Nutrition 0.000 description 9
- 239000000284 extract Substances 0.000 description 9
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 9
- 125000002971 oxazolyl group Chemical group 0.000 description 9
- 239000000843 powder Substances 0.000 description 9
- 125000004076 pyridyl group Chemical group 0.000 description 9
- 239000007921 spray Substances 0.000 description 9
- IQAJMALOOLNRLN-GORDUTHDSA-N (6-oxocyclohexen-1-yl)methyl (e)-but-2-enoate Chemical compound C\C=C\C(=O)OCC1=CCCCC1=O IQAJMALOOLNRLN-GORDUTHDSA-N 0.000 description 8
- 239000000126 substance Substances 0.000 description 8
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 7
- 125000000262 haloalkenyl group Chemical group 0.000 description 7
- 125000000232 haloalkynyl group Chemical group 0.000 description 7
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 7
- 239000000741 silica gel Substances 0.000 description 7
- 229910002027 silica gel Inorganic materials 0.000 description 7
- 238000005507 spraying Methods 0.000 description 7
- 229910052717 sulfur Inorganic materials 0.000 description 7
- 238000005160 1H NMR spectroscopy Methods 0.000 description 6
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 description 6
- IBSREHMXUMOFBB-JFUDTMANSA-N 5u8924t11h Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O3)C=C[C@H](C)[C@@H](C(C)C)O4)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 IBSREHMXUMOFBB-JFUDTMANSA-N 0.000 description 6
- 239000005660 Abamectin Substances 0.000 description 6
- 241000239290 Araneae Species 0.000 description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 6
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 6
- 229950008167 abamectin Drugs 0.000 description 6
- 230000015572 biosynthetic process Effects 0.000 description 6
- 238000007796 conventional method Methods 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- HJOVHMDZYOCNQW-UHFFFAOYSA-N isophorone Chemical compound CC1=CC(=O)CC(C)(C)C1 HJOVHMDZYOCNQW-UHFFFAOYSA-N 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 6
- 238000002156 mixing Methods 0.000 description 6
- 239000000725 suspension Substances 0.000 description 6
- 241000488562 Eotetranychus Species 0.000 description 5
- 241001674048 Phthiraptera Species 0.000 description 5
- 239000005663 Pyridaben Substances 0.000 description 5
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 5
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 5
- 125000002947 alkylene group Chemical group 0.000 description 5
- 150000001412 amines Chemical class 0.000 description 5
- 125000004432 carbon atom Chemical group C* 0.000 description 5
- 229940125782 compound 2 Drugs 0.000 description 5
- 238000001816 cooling Methods 0.000 description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 125000005347 halocycloalkyl group Chemical group 0.000 description 5
- 239000002917 insecticide Substances 0.000 description 5
- 238000009434 installation Methods 0.000 description 5
- 229910052757 nitrogen Inorganic materials 0.000 description 5
- 125000004433 nitrogen atom Chemical group N* 0.000 description 5
- 125000001715 oxadiazolyl group Chemical group 0.000 description 5
- 150000002918 oxazolines Chemical class 0.000 description 5
- 239000006187 pill Substances 0.000 description 5
- DWFZBUWUXWZWKD-UHFFFAOYSA-N pyridaben Chemical compound C1=CC(C(C)(C)C)=CC=C1CSC1=C(Cl)C(=O)N(C(C)(C)C)N=C1 DWFZBUWUXWZWKD-UHFFFAOYSA-N 0.000 description 5
- 239000012312 sodium hydride Substances 0.000 description 5
- 229910000104 sodium hydride Inorganic materials 0.000 description 5
- 229910052727 yttrium Inorganic materials 0.000 description 5
- QSLPNSWXUQHVLP-UHFFFAOYSA-N $l^{1}-sulfanylmethane Chemical compound [S]C QSLPNSWXUQHVLP-UHFFFAOYSA-N 0.000 description 4
- 241000254032 Acrididae Species 0.000 description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- WQDUMFSSJAZKTM-UHFFFAOYSA-N Sodium methoxide Chemical compound [Na+].[O-]C WQDUMFSSJAZKTM-UHFFFAOYSA-N 0.000 description 4
- 150000001299 aldehydes Chemical class 0.000 description 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 4
- 239000012267 brine Substances 0.000 description 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 4
- 150000001721 carbon Chemical group 0.000 description 4
- 239000000969 carrier Substances 0.000 description 4
- 230000001276 controlling effect Effects 0.000 description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 description 4
- 239000007789 gas Substances 0.000 description 4
- 125000004438 haloalkoxy group Chemical group 0.000 description 4
- 239000001257 hydrogen Substances 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 4
- 239000002689 soil Substances 0.000 description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 4
- 125000003258 trimethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])[*:1] 0.000 description 4
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 description 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 3
- 241000255925 Diptera Species 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 3
- 244000068988 Glycine max Species 0.000 description 3
- 241000258937 Hemiptera Species 0.000 description 3
- 229920001732 Lignosulfonate Polymers 0.000 description 3
- 241000244206 Nematoda Species 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 3
- 239000013543 active substance Substances 0.000 description 3
- 238000005054 agglomeration Methods 0.000 description 3
- 230000002776 aggregation Effects 0.000 description 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 3
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 description 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 3
- 150000001408 amides Chemical class 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 125000005605 benzo group Chemical group 0.000 description 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 3
- 229910052794 bromium Inorganic materials 0.000 description 3
- 239000011575 calcium Substances 0.000 description 3
- 239000003153 chemical reaction reagent Substances 0.000 description 3
- 238000006482 condensation reaction Methods 0.000 description 3
- 125000004966 cyanoalkyl group Chemical group 0.000 description 3
- 125000004119 disulfanediyl group Chemical group *SS* 0.000 description 3
- 239000004495 emulsifiable concentrate Substances 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- XQUXKZZNEFRCAW-UHFFFAOYSA-N fenpropathrin Chemical compound CC1(C)C(C)(C)C1C(=O)OC(C#N)C1=CC=CC(OC=2C=CC=CC=2)=C1 XQUXKZZNEFRCAW-UHFFFAOYSA-N 0.000 description 3
- 235000013305 food Nutrition 0.000 description 3
- 230000037406 food intake Effects 0.000 description 3
- 239000000417 fungicide Substances 0.000 description 3
- 230000036541 health Effects 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- 239000012442 inert solvent Substances 0.000 description 3
- 239000013067 intermediate product Substances 0.000 description 3
- 230000002147 killing effect Effects 0.000 description 3
- 244000144972 livestock Species 0.000 description 3
- 239000007937 lozenge Substances 0.000 description 3
- VNWKTOKETHGBQD-UHFFFAOYSA-N methane Natural products C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 description 3
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 description 3
- 150000003254 radicals Chemical class 0.000 description 3
- 238000010992 reflux Methods 0.000 description 3
- 239000004576 sand Substances 0.000 description 3
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 125000003396 thiol group Chemical class [H]S* 0.000 description 3
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
- QYYZXEPEVBXNNA-QGZVFWFLSA-N (1R)-2-acetyl-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-5-methylsulfonyl-1,3-dihydroisoindole-1-carboxamide Chemical compound C(C)(=O)N1[C@H](C2=CC=C(C=C2C1)S(=O)(=O)C)C(=O)NC1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)O QYYZXEPEVBXNNA-QGZVFWFLSA-N 0.000 description 2
- XERJKGMBORTKEO-VZUCSPMQSA-N (1e)-2-(ethylcarbamoylamino)-n-methoxy-2-oxoethanimidoyl cyanide Chemical compound CCNC(=O)NC(=O)C(\C#N)=N\OC XERJKGMBORTKEO-VZUCSPMQSA-N 0.000 description 2
- NHOWDZOIZKMVAI-UHFFFAOYSA-N (2-chlorophenyl)(4-chlorophenyl)pyrimidin-5-ylmethanol Chemical compound C=1N=CN=CC=1C(C=1C(=CC=CC=1)Cl)(O)C1=CC=C(Cl)C=C1 NHOWDZOIZKMVAI-UHFFFAOYSA-N 0.000 description 2
- ZMYFCFLJBGAQRS-IAGOWNOFSA-N (2S,3R)-epoxiconazole Chemical compound C1=CC(F)=CC=C1[C@]1(CN2N=CN=C2)[C@@H](C=2C(=CC=CC=2)Cl)O1 ZMYFCFLJBGAQRS-IAGOWNOFSA-N 0.000 description 2
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- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 235000008160 pyridoxine Nutrition 0.000 description 1
- 239000011677 pyridoxine Substances 0.000 description 1
- WQGWDDDVZFFDIG-UHFFFAOYSA-N pyrogallol Chemical compound OC1=CC=CC(O)=C1O WQGWDDDVZFFDIG-UHFFFAOYSA-N 0.000 description 1
- FBQQHUGEACOBDN-UHFFFAOYSA-N quinomethionate Chemical compound N1=C2SC(=O)SC2=NC2=CC(C)=CC=C21 FBQQHUGEACOBDN-UHFFFAOYSA-N 0.000 description 1
- 239000002516 radical scavenger Substances 0.000 description 1
- 238000006462 rearrangement reaction Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000007670 refining Methods 0.000 description 1
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 229940080817 rotenone Drugs 0.000 description 1
- JUVIOZPCNVVQFO-UHFFFAOYSA-N rotenone Natural products O1C2=C3CC(C(C)=C)OC3=CC=C2C(=O)C2C1COC1=C2C=C(OC)C(OC)=C1 JUVIOZPCNVVQFO-UHFFFAOYSA-N 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 230000002000 scavenging effect Effects 0.000 description 1
- 206010039766 scrub typhus Diseases 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 150000003354 serine derivatives Chemical class 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 238000009958 sewing Methods 0.000 description 1
- 229910021332 silicide Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229910001388 sodium aluminate Inorganic materials 0.000 description 1
- ODZPKZBBUMBTMG-UHFFFAOYSA-N sodium amide Chemical compound [NH2-].[Na+] ODZPKZBBUMBTMG-UHFFFAOYSA-N 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- XUXNAKZDHHEHPC-UHFFFAOYSA-M sodium bromate Chemical compound [Na+].[O-]Br(=O)=O XUXNAKZDHHEHPC-UHFFFAOYSA-M 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- CRWJEUDFKNYSBX-UHFFFAOYSA-N sodium;hypobromite Chemical compound [Na+].Br[O-] CRWJEUDFKNYSBX-UHFFFAOYSA-N 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 239000000021 stimulant Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 239000005936 tau-Fluvalinate Substances 0.000 description 1
- ZZYSLNWGKKDOML-UHFFFAOYSA-N tebufenpyrad Chemical compound CCC1=NN(C)C(C(=O)NCC=2C=CC(=CC=2)C(C)(C)C)=C1Cl ZZYSLNWGKKDOML-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- UBCKGWBNUIFUST-YHYXMXQVSA-N tetrachlorvinphos Chemical compound COP(=O)(OC)O\C(=C/Cl)C1=CC(Cl)=C(Cl)C=C1Cl UBCKGWBNUIFUST-YHYXMXQVSA-N 0.000 description 1
- BSYVTEYKTMYBMK-UHFFFAOYSA-N tetrahydrofurfuryl alcohol Chemical compound OCC1CCCO1 BSYVTEYKTMYBMK-UHFFFAOYSA-N 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 239000004308 thiabendazole Substances 0.000 description 1
- 235000010296 thiabendazole Nutrition 0.000 description 1
- WJCNZQLZVWNLKY-UHFFFAOYSA-N thiabendazole Chemical compound S1C=NC(C=2NC3=CC=CC=C3N=2)=C1 WJCNZQLZVWNLKY-UHFFFAOYSA-N 0.000 description 1
- 229960004546 thiabendazole Drugs 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- BAKXBZPQTXCKRR-UHFFFAOYSA-N thiodicarb Chemical compound CSC(C)=NOC(=O)NSNC(=O)ON=C(C)SC BAKXBZPQTXCKRR-UHFFFAOYSA-N 0.000 description 1
- YFNCATAIYKQPOO-UHFFFAOYSA-N thiophanate Chemical compound CCOC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OCC YFNCATAIYKQPOO-UHFFFAOYSA-N 0.000 description 1
- RMVRSNDYEFQCLF-UHFFFAOYSA-N thiophenol Chemical compound SC1=CC=CC=C1 RMVRSNDYEFQCLF-UHFFFAOYSA-N 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- YWSCPYYRJXKUDB-KAKFPZCNSA-N tralomethrin Chemical compound CC1(C)[C@@H](C(Br)C(Br)(Br)Br)[C@H]1C(=O)O[C@H](C#N)C1=CC=CC(OC=2C=CC=CC=2)=C1 YWSCPYYRJXKUDB-KAKFPZCNSA-N 0.000 description 1
- NFACJZMKEDPNKN-UHFFFAOYSA-N trichlorfon Chemical compound COP(=O)(OC)C(O)C(Cl)(Cl)Cl NFACJZMKEDPNKN-UHFFFAOYSA-N 0.000 description 1
- DQJCHOQLCLEDLL-UHFFFAOYSA-N tricyclazole Chemical compound CC1=CC=CC2=C1N1C=NN=C1S2 DQJCHOQLCLEDLL-UHFFFAOYSA-N 0.000 description 1
- XAIPTRIXGHTTNT-UHFFFAOYSA-N triflumuron Chemical compound C1=CC(OC(F)(F)F)=CC=C1NC(=O)NC(=O)C1=CC=CC=C1Cl XAIPTRIXGHTTNT-UHFFFAOYSA-N 0.000 description 1
- CWMFRHBXRUITQE-UHFFFAOYSA-N trimethylsilylacetylene Chemical group C[Si](C)(C)C#C CWMFRHBXRUITQE-UHFFFAOYSA-N 0.000 description 1
- 239000002383 tung oil Substances 0.000 description 1
- 241000701447 unidentified baculovirus Species 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- JARYYMUOCXVXNK-IMTORBKUSA-N validamycin Chemical compound N([C@H]1C[C@@H]([C@H]([C@H](O)[C@H]1O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)CO)[C@H]1C=C(CO)[C@H](O)[C@H](O)[C@H]1O JARYYMUOCXVXNK-IMTORBKUSA-N 0.000 description 1
- 229910052720 vanadium Inorganic materials 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 238000001238 wet grinding Methods 0.000 description 1
- 239000004563 wettable powder Substances 0.000 description 1
- 239000002023 wood Substances 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/74—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/36—One oxygen atom
- C07D263/40—One oxygen atom attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- General Health & Medical Sciences (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Description
經濟部中央樣準局貝工消費合作社印製 A7 ___B7 _ 五、發明説明(i ) 本發明係關於一些噚唑啉及睡唑啉化合物,其N -氧 化物,農業上適用之鹽類與組成物,及其用於農業與非農 業環境中作爲節肢動物殺除劑的方法。 控制節肢動物害蟲類在達成高收成率上極爲重要。節 肢動物破壞生長中與保存中的農作物會造成生產力明顯降 低,導致消费者花费增加。控制節肢動物害蟲類對於林業 ,溫室農作物,景觀植物,苗圃農作物,保存食品及纖維 性產物,家畜,家務,公共衛生與動物健康亦爲重要。針 對此目的,有許多產品可商業上購得,但仍然一些較有效 ,费用較低,毒性較低,對環境較安全或具有不同之作用 模式的化合物。 美國專利案第5 ,141 ,948號揭示式i之節肢 動物殺除性噚唑啉及_唑啉:
其中: 尺1與3各自獨自爲Η,鹵基,低碳數烷基,低碳數烷 氧基,硝基,低碳數鹵烷基或低碳數鹵烷氧基,但是Ri 與R 2不同時爲Η ; R3是Η,鹵基,低碳數烷基或低碳數烷氧基; R4是具7個或7個以上碳原子之烷基,具7個或7 個以上碳原子之烷氧基,烷硫基,低碳數烷氧基-低碳數 本紙張尺度適用中國國家標準(CNS ) A4規格(210'乂 297公釐) f 丨裝 訂 I 線 (請先閲讀背面之注意^項再4-寫本頁) A7 B7 308595 五、發明説明(2 ) (請先閱讀背面之注意事項再填肖本頁) 烷基,低碳數烷氧基-低碳數烷氧基,具3個或3個以上 碳原子之烯氧基,低碳數块氧基,三(低碳數烷基)甲矽 烷基,可被低碳數烷基取代之環烷基,或
B是鍵,0,低碳數伸烷基,低碳數伸烷氧基,低碳 數伸烷基二氧基或二(低碳數烷基)甲矽烷基; Q是C Η或N ; η 是 0 — 5 ; 每一個Rs各自獨自爲氫,烷基,烷氧基,低碳數鹵 烷基,低碳數鹵烷氧基或三(低碳數烷基)甲矽烷基; A是鍵或低碳數伸烷基:及 Z是0或S。 美國專利案第4,977,171號揭示式i i之節 肢動物殺除性與殺恙蟲性噚唑啉或瞎唑啉: Y1
經濟部中央標準局員工消費合作社印袈 其中: X1與X2各自獨自爲Η,低碳數烷基,低碳數烷氧基 |鹵基,三氟甲基或三氟甲氧基: Υ1與Υ2各自獨自爲Η,低碳數烷基,低碳數烷氧基 ,低碳數烷硫基,氰基,硝基,鹵基或三氟甲基; 本紙張尺度適用中國阁家橾準(CNS ) Α4说格(210Χ297公瘦) -5 - 經濟部中央標準局員工消費合作社印衮 A7 _B7_ 五、發明説明(3 ) Z是0或S ;且 η是〇或1。 W 0 95/04726揭示式i i i之節肢動物殺 除性與殺恙蟲性鸣唑啉及_唑啉: R3
iii 其中,如上所陳, A係選自鍵或Cx- (:3不分支或分支伸烷基; R3係選自C3— 鹵環烷基;C2_Ci〇鹵烯基,其 被至少一個獨立選自氰基或C2 - Ce烷氧羰基之基任意取 代;Ci— Ci。烷基,其被至少一個獨立選自Si (R6) (R7) R8,氰基,C2— Ce烷羰基,C2— Ce鹵烷羰基 ,C2— Ce鹵烷氧羰基,或C2_ Ce烷氧羰基之基任意取 代:c2-ce烷羰基:C2— Ct。烯基,其被至少一個獨 立選自R9之基任意取代;C2— Ci。炔基,其被至少一個 獨立選自R9之基任意取代;C2 — Ce鹵烷羰基;C2-Ce烷氧羰基:C2— Ce鹵烷氧羰基:C (0) R0; C ( 0) OR9: C (Ο) N (R10) R11; OR12;四氫吡 喃基;其被至少一個獨立選自W1之基,取代的苯基:或 者8至1 2員融合雙環系統,其含有獨立選自0 — 4個氮 原子,0 — 2個氧原子,或0 — 2個硫原子的0_4個雜 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再填寫本頁) 裝.
*-IT -6 - 經濟部中央標準局員工消f合作社印裝 A7 _____B7 五、發明説明(4 ) 原子,此環系統被至少一個獨立選自W之基任意取代: R9係選自苯基或吡啶基,其任一者被至少一個_自 W之基任意取代;且 W係選自鹵基,氰基,甲醯基,硝基,SFs, — C3院基’ Ci—C3_院基’ Ci — C3院硫基, 烷氧基,Ci-Cs鹵烷氧基,C2-C4烷羰基或(:2 — C 4烷氧羰基。 本發明之暍唑啉與睡唑啉化合物並未揭示於這些文獻 任一者中。 發明簡沭 本發明係針對式I化合物,包括其全部及立髖異構物 ,N -氧化物類及農業上適用之鹽類,含有該化合物之農 業用組成物及其作爲節肢動物殺除劑之用途:
其中: 每一個E各自獨自選自C i — c4烷基或C 1一(:4鹵烷 基; X係選自Ci— C4伸烷基,一(CH2) η - A -或一 (CH2) p-A — CH2—,上述任一者被1至4個R4任 本紙張尺度適用中國國家梯準(〇奶>八4规格(2丨0/297公釐) --------^ —裝------訂------<-:银 * - (請先閱讀背面之注意事項再填寫本頁) 308595 經濟部中央橾準局員工消費合作社印裝 五 發明説明 ( 5 ) }· 1 意 取 代 1 Y 與Ζ 各 白 獨 白 選 白 〇 或 S 1 A 係選 白 〇 t S 或 Ν R 1 α • 1 I 請 1 I Q 係選 白 Η 或 J 1 或 者 Q 係 選 白 C 1 " -C 1 β烷基 > 先 閱 1 I 讀 1 C 1 ~ -C 1 β _院基 C 2 — C 4烯基 C 2 C 4決基 ,C 3 — 背 1 I 之 1 C 7環烷基 ,C 3 — C 7鹵代環烷基或 :4 C 7環院基院基 素 1 事 1 > 上 述 任一 者 被 W 任 意 取 代 , 項 再 "1 填 1 J 係選 白 苯 基 » 某 基 » Μ 基 菲 基 > 1 Η 一 吡 咯 基 > 本 裝 I 呋 喃 基 ,PS 嗯 基 1 Η — 吡 唑 基 » 1 Η — 咪 唑 基 » 異 0咢 唑 頁 1 1 基 » D咢 唑基 > 異 唑 基 * m 唑 基 j 1 Η — 1 2 > 3 — 二 1 1 唑 基 » 2 Η — 1 2 » 3 — 三 唑 基 , 1 Η — 1 2 > 4 — 1 1 二 唑 基 ,4 Η — 1 > 2 4 — 三 唑 基 — 1 t 2 3 — D咢 一 訂 I 唑 基 1, 2 4 — D咢 二 唑 基 1 > 2 5 — D咢 一 唑 基 ) 1 I 1 3 ,4 — D咢 二 唑 基 1 2 3 — m 二 唑 基 1 2 \ 1 I » 4 — _ 二 唑 基 1 2 5 — m 二 唑 基 1 3 4 — 1 吡 嗪 妹 睡 二 唑 基, 1 Η — 四 唑 基 2 Η — 四 唑 基 陡 基 » 噠 1 基 嘧 啶基 吡 嗪 基 1 3 5 — 二 嗪 基 1 2 4 1 1 — 二 嗪 基, 1 2 4 5 — 四 嗪 基 1 Η — 口引 跺 基 苯 1 1 並 呋 喃 基, 苯 並 C b ] ui 吩 基 1 Η — 吲 唑 基 1 Η — 苯 1 I 並 咪 唑 基, 苯 並 0咢 唑 基 » 苯 並 m 唑 基 喹啉 基 異 喹啉 基 1 I » 噌 啉 基, 酞 嗪 基 晻 唑 啉 基 ♦ 晻 D咢 唑 基 1 ♦ 8 — Β定 1 1 I 基 y 蝶 啶基 » 2 1 3 — 一 氫 — 1 Η — ΕΡ 基 1 2 3 » 1 1 4 一 四 氫某 基 » 6 » 7 8 ϊ 9 — 四 氫 — 5 Η — 苯 並 環 戊 J 1 基 1 2 ,3 — 二 氫 苯 並 呋 喃 基 ’ 3 4 — 二 氫 — 2 Η — 1 1 丨 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 一 8 - 經濟部中央橾华局員工消费合作社印袈 A7 B7 五、發明説明(6 ) —苯並吡喃基,2 ,3 ,4 ,5 —四氫—1-苯並哩呼基 (benzoxepiny) ,1,3 —苯並二嗜茂基,1 ,3 —二 氫一 1—氧基異苯並呋喃基,2 ,3 -二·氫~2—氧基苯 並呋喃基,3,4 —二氫—4 —酮—2H— 1—苯並紕喃 --------一-丨裝------訂-----丄線 (請先閱讀背面之注意事項再填寫本1) 基 或 9 Η —芴基1 1其中J被1 - -4個 R 3任意取代; R 1係選自1 一 2個_基, C 1 - C β烷基,C i - C β 鹵 院 基 * C ! - C β烷氧基,C 1 一 C β 鹵 院氧 基, S ( 0 ),R 11 ' 氰基或硝基; R 2是選自Η ,1 — 2個鹵 基,c i -C β焼基,C 1 — C β齒院基,C 1 - * C β院氧基, C 1 — C β鹵烷氧基, S ( 〇 ).R 11 ♦ 氰基或硝基; 每 一個R 3各 自獨自選自鹵 基,c 1 -C 1 β院基,C 1 — C 1 Θ 鹵烷基,C2— Cle烯基 ,C 2 — C 1 β 鹵烯基,C 2 — C 1 β 块基.C 2 - -C 16鹵炔基, C 2 - -c 1β烷氧烷基,c 2 ~ -Ci β烷硫烷基 ,c2-cle氧院基 C 3 ' -C β環烷基, C 3 _ -ce鹵環烷基,氰基,硝基,s ( 0 ) 尤R 11 · 〇 R 9, C 1 — C 5 焼基聯硫基, C 1 - C 5鹵烷基聯硫基, 甲 醯 基 ,c ( 0 ) R 2 1 , C ( C ))〇 R 2 1 , C ( 〇 )NR12R13,S (〇) 2N 1 4R 15, N R 1 β R 1 7 ♦ S (R ” ( R 7 ) ( R 8 ) ,S F ,5 或Μ -J 1 ; 每 一個R 4各 自獨自選自C 1 ~ C 烷基, C 1 — C 4 鹵 院 基 9 c2— C4氰烷基,C2- C 4烷 氧 烷基 ,或被1 _ 3 個 W 1任意取代之 苯基;或者兩 m r 4 鍵 結至 相同的碳原子 並 與 將 其連接在- -起的碳原子- -起形 成 C ( =0 )或 C ( 本紙張尺度適用中國國家標準(CNS ) A4规格(210x297公釐) -9 - 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(7 ) =S ); R5係選自Η,鹵基,Cx-Ce烷基,Ci—Ce鹵烷 基,Ci—Ce烷氧基,Ci—Ce鹵烷氧基,Ci—Ce烷硫 基,Ci— (:6烷基亞磺醯基,Ci—Ca烷基磺醯基,Cl -Ce鹵烷硫基,C^ — Ce鹵烷基亞磺醯基或Ci_Ce鹵 垸基磺酸基; 每一個118與1?7各爲Ci-C12烷基; 每一個R8各自獨自選自Ci — C 12烷基或被1 - 3個 W1任意取代之苯基; 每一個R9各自獨自選自Η,Ci— Ce烷基,Ci — Ce鹵烷基,C2— Ce烯基,C2— Ce鹵烯基,C2— Ce 炔基,C2—Ce鹵炔基,C3— Ce環烷基,C3— Ce鹵環 烷基,c4—c7氰環烷基,c4— c7烷基環烷基,c4 — 環烷基烷基,C4— C7鹵環烷基烷基,C2_Ce烷氧
院 基 C 2 — C β 院硫院基 C 2 - C 4氟 烷基 * C ( 〇 ) R 1 8 , C ( 0 ) 0 R 18 'C ( 〇 ) N R 1 2 R 1 3 S ( 〇 ) 2ν R 1 4R 15 或 S (〇 ) 2R 11 1 R 1 0 係選自 Η,C 1 - C 4烷基,C 1 ~ C 4鹵烷基, 醯 基 » C 2 — C 4 烷羰基, C 2 — C 4院氧 羰基 , N Η 2 c (〇 ), (Cl~ C 4院基 )N H C ( 0 )或(C -C 4烷基)2 N C Ο ); 每一個R11各自獨自選自Ci— Ce烷基,Ci-Ce鹵 烷基,c2— Ce烯基,c2— ce鹵烯基,c2—ce炔基, C2— Ce_炔基,C3— Ce環烷基,C3— Ce鹵環烷基, 本紙張尺度通用t國國家標準(CNS ) Λ4規格(210X 297公釐) --------_-丨裝------訂------線 (請先閱讀背面之注意事項再填寫本頁) 10 - 經濟部中央標率局員工消費合作杜印裝 A7 B7 五、發明説明(8 ) c4-c7氰環烷基,C4-C7烷基環烷基’ c4 — c7環院 基烷基,C4— Ct鹵環烷基烷基,C2 - ce烷氧烷基, c2 — Ce烷硫烷基,C2 — C4氰烷基’被1 一 3個W1任 意取代之苯基,或被1 - 3個W1任意取代之笮基; 每一個R12,R14及Rie各自獨自選自Η ’ Ci —
Ce院基,Cjt—Ce齒垸基,C2 — Ce嫌基,c2 — ce圍 烯基,c2— ce炔基,c2— ce鹵炔基,c2_ce烷氧烷 基,ce烷硫烷基,c3— ce環烷基,c3— ce鹵環 烷基,c4—c7環烷基烷基,被1 一 3種W1任意取代之 苯基,或被1 — 3個W1任意取代之笮基; 每一個R13,R15及R17各自獨自選自Η,Cl — C4烷基或Ci — C4烷氧基;或 R12與R13,R14與R15,或尺18與1^17,當連接在 相同原子時,可一起形成(ch2)4,(ch2)5或 c H2C H2〇 c H2C h2,上述任一基被 1 — 3個c H3 任意取代; 每一個R18各自獨自選自(::_ Ce烷基,Cl — Ce鹵 烷基,c2~ce烯基,c2— (:6鹵烯基,c2-ce炔基, C2 — (:8鹵炔基,c2 — ce烷氧烷基,c2-ce烷硫烷基 ’ c3— Ce環烷基,c3_ce鹵環烷基,c4-c7環烷基 院基’被1 一 3個W1任意取代之苯基,或被1 一 3個 W1任意取代之笮基; 每一個R19各自獨自選自鹵基,氰基,硝基,Cl — Ce院基’ Cl— ce鹵烷基,c2-ce烯基,C2— Ce鹵 本紙浪尺度適用中國國轉準(CNS} A4現格(2ιϋχ297公慶) --------^丨裝------訂-----4 線 (請先閲讀背面之注意事項再填寫本頁) -11 - A7 B7 308595 五、發明説明(9 ) 烯 基 y C 2 一 -C β炔基 C 2 " -C 4 氰 烷基 ,S (〇 ) tR 1 1 1 0 R 2 0 t c α —C 5 院 基 聯 硫基 t C 1 - -C 5 齒院基 聯硫 基 > S F 5 1 •甲醯 基,C (丨 0 ) R 1 8 , ,C < :〇) 0R1 8或 S i ( R 9 ) ( R 7) ( R 8 ) ; 每 一 個 R 2 0各自 獨 白 選 自Η » Cl- -C β 烷基, C 1 - C β鹵烷基, C 2 — C β烯基, 'C 2 一 C β鹵烯基,C 2 -C β 炔 基 * C 2 ~ -C β齒块 基 C (0 ) R 18 9 C ( 0 ) 0 R 1 8,C ( 〇 ) NR 1 2 R 13 t S ( 0 ) [R 14R 1 5 ,S (0 ) 2 R 1 1 ,被 1-3 個W 1 任 意 取 代 之 苯基或被 1 — 3 個w 1任意取代之笮基; 每 — 個 R 2 1各自 獨 白 選 自c 1 - -c β 烷基 ’Ci - -C β 鹵 垸 基 > C 2 一 -C β烯基 t C 2 - -C β 鹵 烯基 -C 2 — C β 炔基 9 C 2 - -C β 鹵 炔基,C 2 ~ -I C β 烷氧 垸 基, C 2 - _ c β院 硫院 基 ,C3 — Ce環烷基,C3-Ce鹵環烷基或C4 — C7環烷基 烷基: 每一個Μ各自獨自選自鍵,S,0,C (0) ,Cx —C 4伸烷基,C 2 — C 4伸烯基或C 2 - C 4伸块基; 每一個J1各自獨自選自Si^R22) (R2” ( R 24) ; Ge ( R 22) ( R 23) ( R 24) ; 2 , 8 , 9— 三聘—5 -氮雜—1 一政雙環〔3. 3. 3〕十~院—1 —基,其被1-6個〇:1— C3烷基任意取代:Ci—Ce烷 基,其被1 一 3個(:1一 C4烷氧基任意取代;或苯基,棻 基或吡啶基,其中任一者被1 — 4個R19任意取代; 每一個R22及R23各自獨自選自C C 12烷基或 本紙伕尺度適用中國國家標準(CNS ) A4規格(210Χ2<Π公釐1 ~~ -12 - ^ 裝 訂 ,^ (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標隼局員工消費合作社印製 A7 B7 經濟部中央標準局員工消費合作社印聚 五、 發明説明 ( 10 ) - 1 C X - C 1 2院氧基 1 每一 個 R 24各 自獨自選 自C i - - C 1 2院基; C 1 — ,1 1 C i 2烷氧 基 : 或被 1 - 3個 W1任意取代之苯基 t 1 Ί W係 選 白 J , C 1 — C β 焼氧基 或C 1 一 C β豳 烷氧 基 f 請 先 閱 1 I 每一 個 W 1各自獨自選自鹵基 ,氰基,硝基 » C ! 一 讀 背 ίί 1 I C 2院基 C ! -C 2鹵烷基 * C x- C 2烷氧基, -» 1 — C 2 之 注 意 I 1 I 鹵 院氧基 > C 1 一 C 2院硫基 1 C ,- -C 2鹵烷硫基 y C 1 — 事 項 再 1 C 2烷基亞磺醯基 C 1 - C 2鹵烷基亞磺醯基, 1 — C 2 填 寫 本 1 裝 烷 基磺醯 基 » 或C 1 — C 2 鹵 烷基磺 醯基; I 1 1 m是 1 或 2 ; 1 1 η是 1 » 2或 3 ; 1 | Ρ是 1 或 2 ; 訂 1 q是 0 1或 2 :且 1 1 | 每一 個 t 各自 獨立爲0 ,1或 2 。 1 1 1 上述 列 舉 說明 中’ '像 基”乙 詞(單獨使用 或 :用 於 諸 I 如 烷硫 基 fr 或' 鹵烷基1 等化合 物用語中)包 括 .不 分 十 辣 1 或 分支院 基 例如 甲基,乙 基,正 丙基,異丙基 » 或 不 同 1 1 之 丁基, 戊 基 或己 基異構物 • '1 —6烷基"乙 詞 表 示 1 1 | 至 6個提 供 取 代基 使用之位 置可爲 烷基,其爲獨 •選 擇 者 1 I 〇 '烯基 雖 包 括不 分支或分 支烯類 ,例如乙烯基 ♦ 1 一 丙 1 1 | 烯 基,2 — 丙 烯基 ,及不同 之丁烯 基,戊烯基及 己 烯 基 異 1 1 稱 物》' 烯 基 ,亦 包括多烯 類,例 如1 ,2 —丙 二 烯 基 及 1 1 2 * 4 - 己 二 烯基 » 、炔基 〃包括 不分支或分支 炔 類 » 例 1 如 乙炔基 > 1 —丙 块基,2 -丙炔 基及不同之丁 炔 基 > 戊 1. 本紙張尺度適用中國國湖叫Μ规格™㈣)_i3_ 經濟部中央標準局員工消費合作社印袈 A7 B7 五、發明説明(ll ) 炔基及己炔基異構物。·'炔基"亦包括含有多個三鍵之部 份,例如2,5 —己二決基。伸院基’表示不分支或分 支烷二基》申烷基,之範例包括CH2,ch2ch2, C Η ( C Η a ) ,C H2CH2C Hz· C H 2 C Η ( C Η 3 ) 及不同之伸丁基異構物。''伸烯基’表示不分支或分支烯 二基,其含有一個烯鍵。伸烯基^之範例包括CH = CH,CH2CH = CH,CH=C (CH3)及不同之伸 丁烯基異構物。 ''伸炔基〃表示不分支或分支炔二基,其 含有一個三鍵。Μ申炔基〃之範例包括CeC,CH2C 三C,c三cch2及不同之伸丁炔基異構物》 *烷氧基 I包括甲氧基,乙氧基,正丙氧基,異丙氧基及不同之丁 氧基,戊氧基與己氧基異構物等等。'1- 3烷氧基^乙 詞表示1至3個提供取代基使用之位置可爲烷氧基,其爲 獨立選擇者。''烷氧烷基^乙詞表示烷基上有烷氧基之取 代。*烷氧烷基^之範例包括CH3OCH2, ch3och2ch2, ch3ch2och2* ch3ch2ch2och2 及 ch3ch2och2ch2。' 烷硫基1包括支鏈或直鏈烷硫基部份,例如甲硫基,乙硫 基,及不同之丙硫基,丁硫基,戊硫基與己硫基異構物。 ^烷硫烷基'表示烷基上有烷硫基取代。'烷硫烷基"之 範例包括 ch3sch2,ch3sch2ch2, C Η 3 c H 2 S C Η 2 - CH3CH2CH2CH2SCHd CH3CH2SCH2CH2。、烷基亞磺醯基^•包括烷基亞 磺醯基之兩種鏡相異構物。烷基亞磺醯基I之範例包括 本紙張尺度適用中國國家橾孪(CNS ) Λ4規格(210X297公釐) (請先閱讀背面之注意事項再填寫本頁) .裝 訂 經濟部中央橾準扃員工消費合作杜印製 A7 B7 五、發明説明(12) C Η 3 S ( 0 ) > C H a C Η 2 S ( Ο ), CH3CH2CH2S (0) ,(CH3)2CHS(0)及 不同之丁基亞磺醯基,戊基亞磺醯基與己基亞磺醯基異構 物。 ''烷基磺醯基^之範例包括CH3S(0)2, C Η 3 c H 2 S (0) 2> CH3CH2CH2S ( 0 ) 2 -( C H a ) 2 C Η S (〇)2,及不同之丁基磺醯基,戊基磺 醯基與己基磺醯基異構物。^烷基聯硫基^表示支鏈或直 鏈烷基聯硫基部份。t烷基聯硫基f之範例包括 C Η 3 s S,ch3ch2ss,CH3CH2CH2SS,( C H3) 2C H S S及不同之丁基聯硫基與戊基聯硫基異構 物。^氰烷基^表示被一個氰基取代之烷基。' 氰烷基〃 之範例包括NCCH2,NCCH2CH2及 c Η 3 c H (CN) CH2。、環烷基〃包括環丙基,環丁 基,環戊基及環己基等等。 ' 環烷基烷基〃之範例包括環 丙基甲基,環戊基乙基,及其它鍵結在直鏈或支鏈烷基上 的環烷基。''烷基環烷基〃表示環烷基上有烷基取代。ιί 例包括4 -甲基環己基與3 -乙基環戊基。氰環烷基^" 表示被一個氟基取代之環烷基。'氰環烷基I之範例包括 4 -氰環己基及3 _氰環戊基。熟悉該技藝之士會了解, 並非所有的含氮雜類可形成N-氧化物,因爲氮原子需要 可用之未配對電子對,才可氧化爲氧化物;熟悉該技藝之 士會辨別這些可形成N _氧化物之含氮雜環類。 '鹵基〃乙詞(單獨使用或用於諸如 ''鹵烷基"等化 學用語中)包括氟基,氯基,溴基或碘基。— 2鹵基 本紙張尺度適历中國國家標準(CNS ) Α4規格(210Χ297公釐) --------^丨裝------訂------線 (請先閲讀背面之注意事項再填寫本頁) 15 308595 A7 B7 五、發明説明(13 ) 乙 詞表示1 或2個提供取 代基使用之位置 可爲鹵基,其 係 獨 立選擇者 。再者,當用 於諸如 ' 鹵烷基 ^等化學用語 時 9 該烷基可 部份或全部被 相同或不同的鹵 原子取代。' 鹵 烷 基#之範 例包括F 3 C, C 又 C Η 2,C F 3 C Η 2及 C F 3 C C 5 2 。、鹵烯基, ,、鹵炔基,, ^鹵烷氧基| 等 詞 之定義與 a鹵烷基〃乙 詞類似。%鹵烯 基^之範例包 括 ( C β ) 2C :=C H C Η 2 及 c f3c h2c Η = C Η C Η 2。, k鹵炔基〃之範例包括HCsCCHC^ , C F 3 C = C, C C j? a C ξ C 及 F C H 2 C Ξ ξ C C Η 2。' 菌 院 氧基#之 範例包括C F : 3 〇 f C C 又 3 C Η 2 0, Η C F 2 C Η 2 C Η 2 〇 及 C F 3CH20 ^ 、齒院硫基〃之 範 例 包括c c Si 3 s,C F 3 S , CC53CH2S 及 C % C H 2 C H [2 C H 2 S ·, ‘鹵烷基磺醯基π 之範例包括 C F 3 S ( 0 ) 2 ' C C ^ 3 S (0 ) 2, C F 3 c H 2 S (〇 ) 2及 C F 3 c F 2 S ( 0 ) 2 ° 取代基碳 原子之總數以 ' C i - C j ' 表示在前,其 中 i 與j爲1 至1 6之數字 。舉例而言,C i 一 C 3烷基磺 jr I裝------訂-----k 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標隼局員工消費合作社印製 醯基表示甲基磺醯基至丙基磺醯基;C2烷氧烷基表示 (:Η30(:Η2; c3烷氧烷基表示,舉例而言, c η 3 c Η ( 0 C Η 3 ) ,CH30CH2CH2 或 C H3C H2〇 C H2;及C4烷氧烷基表示被含有總共4個 碳原子之烷氧基取代之烷基的多種異構物,其範例包括 CH3CH2CH2〇CHdCH3CH2OCH2CH2。' 烷羰基f之範例包括C (〇) CH3. 本紙張尺度適用巾國國家標準(CNS ) ( 210X 297公釐) " -16 - 經濟部中央標準局員工消费合作社印製 A7 B7 五、發明説明(14) C (0) CH2CH2CH3 及 C (0) CH (ch3) 2。 '"烷氧羰基^之範例包括CH30C ( = 0), C Η 3 c Η 2 0 ( = Ο ) . CH3CH2CH20C ( = 0) ’ (ch3) 2CH〇 ( = 0)及不同之丁氧羰基異構物β 上述列舉說明中’當式I化合物含有1個或i個以上的雜 環時,取代基皆利用任何可使用的碳原子或氮原子,藉置 換該碳原子或氮原子上的氫而連接至這些環上。 2 ’ 8 ’ 9 一三D等一 5 -氮雜一 1 一砂雙環〔3. 3. 3〕十—烷一1—基〃表示甲矽烷基團:
當一化合物被具有下標之取代基(表示該取代基之數 目可超過1個)取代時,該取代基(當其數目超過1時) 及獨立選自具有所界定之取代基的基團。 當一基團含有一個可爲氫之取代基時,例如R2或 R1Q’則當此取代基係爲氫,可理解此相當於該基團未被 取代。 本發明之化合物可呈現一種或一種以上立體異構物。 此多種立體異構物包括鏡相異構物,非鏡相異構物,阿托 異構物(atropisomes)與幾何異構物。熟悉此技藝之士 將了解,當—種立體異構物比其它立體異構物含量更大或 與其它立體異構物分離時,其可更具活性及/或呈現有利 效果。再者,熟悉該技藝之士知道如何分離,增加含量, 本紙張尺度適用中國國家梯準(CNS ) A4規格(2丨OX 297公釐) -------γ丨裝------訂-----~ 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作祆印褽 A7 B7 五、發明説明(15 ) 及/或選擇地製備該立體異構物。因此,本發明包括式I 化合物,其N -氧化物及其農業上適合之鹽類等等。本發 明之化合物可以立體異構物之混合物,單獨立體異構物或 光學活性形式存在。 本發明化合物之鹽類包括與無機酸類或有機酸類形成 之酸加成鹽,這些酸類包括氫溴酸,氫氯酸,硝酸,磷酸 ’硫酸,醋酸,丁酸,反式丁烯二酸,乳酸,順式丁烯二 酸,丙二酸,乙二酸,丙酸,水楊酸,酒石酸,4 -甲苯 磺酸或戊酸。當化合物含有酸性基團例如苯酚時,本發明 化合物之鹽類亦包括與有機碱(例如吡啶,氨,或三乙胺 )或無機碱(例如鈉,鉀,鋰,鈣,鎂或鋇之氫化物,氫 氧化物,或碳酸鹽)》 所形成的鹽類》 具較佳活性及/或合成方便性之較佳化合物爲: 較佳第1類:上述式I化合物及其農業上適合之鹽類 ’其中: X是被1至4個R4任意取代之一(CH2) n— A- 1 Y是ο ; Α是Ο : Q係選自】或(:1— Cie烷基; J係選自苯基,pg嗯基或吡啶基,其任一者被1 — 3 個R 3任意取代; m是1 ; 且 本紙張尺度適用中圉國家標準(CNS ) Λ4規格'(2丨Ο X 297公釐) ~ '' -18 - ^ 訂 I 1 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標隼局員工消費合作社印製 A7 B7五、發明説明(16 ) η是1。 較佳第2類:較佳第1類化合物,其中: Ζ是0 ; Q是J ; J係選自苯基或吡啶基,其任一者被1 一 3個R3任 意取代;且 q是0。 較佳第3類:較佳第2類化合物,其中: R1係選自F或C5 ,在第2位置; R2係選自Η,F,或C5,在第6位置; 每一個R3各自獨自選自鹵基,Ct — Ce烷基,Ci — C6 鹵烷基,S (0) tR11,OR9 或 M — J1; 每一個R9各自獨自選自Ci_ C4烷基或Ci — 04鹵 烷基; 每一個R11各自獨自選自Ci — Ce烷基或Ci - Ce_ 烷基;且 每一個J 1各自獨自選自苯基,PS嗯啉,吡啶基或呋 喃基。 最佳化合物乃選自下列之較佳第3類化合物: (Z) — 5 —〔 (4-氯苯基)伸甲基〕一3 —〔2 —(2,6 —二氟苯基)一4,5-二氫一4 —噚唑基〕 ^ 裝 訂 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用t國國家操準(CNS〉A4規格(210X 297公釐) 19 - 經濟部中央標隼局員工消費合作社印裝 A7 __ B7五、發明説明(17 ) —4 —暍唑啶酮; (Z) -3-〔2 — (2,6-二氟苯基)-4,5 一二氫—4 —曙唑基〕—5 —〔 〔4 —(三氟甲基)苯基 〕伸甲基〕一 4 -鸣唑啶酮; (Z) — 5 —〔 (4> 一氮〔1,1>_ 雙苯基〕4 —基)伸甲基〕一3 —〔2 —(2 ’ 6 —二氟苯基)一4 ,5 —二氫—4 一啃唑基〕-4-皞唑啶酮; (Z) — 3 —〔2— (2,6—二氟苯基)—4 ’ 5 一二氫 一4一 噚唑基〕—5-〔(4"一 氟〔1,1 一― 雙苯基〕4 —基)伸甲基〕一4 一噚唑啶酮;或 (Z) -5 -〔(2 一,4 -二氯〔1,1 一 -二苯 基〕一 4 —基)伸甲基〕—3 —〔2 —(2,6_二箱I苯 基)—4,5 —二氫—4 — 0等唑基〕-4 一噚唑啶酮。 本發明亦關於殺除節肢動物之組成物,其包括殺除節 肢動物有效量之本發明化合物與至少一種界面活性劑,固 體稀釋劑或液體稀釋劑》本發明之較佳組成物爲含有上述 較佳化合物者。 本發明亦關於控制節肢動物之方法,包括令節肢動物 或其所處環境與殺除節肢動物有效置之本發明化合物(例 如上文所述之組成物)。所使用之較佳方法涉及上述較佳 發明之詳細說明 ^紙張尺度遴用中國國家標準(CNS > A4说格(210X 297公釐) ^ —裝 訂 \ 夕 (請先閲讀背面之注意事項再填寫本頁) -20 _ A7 B7 經濟部中央榡芈局員工消費合作社印裝 五、發明説明(18 ) 製備式I化合物可根據下列計劃i — 1 4所述之一種 或一種以上的方法與變化。 下列式I-IXI化合物中,E,X,Y,Z,A, Q ' J •R1-R24*M> J^W-W^m - η > ρ -Q與t之定義係如上述發明簡述中界定者。 製備式 I 化合物(R5=H,X = - c (R4a) 2A -)可據式π化合物與式m化合物之反應,此反應係在諸如 氫化鈉或二異丙基醯胺鋰等碱類存在下進行(計劃1) ^ 此反應可在有或無諸如四氫呋喃(TH F ),二甲基甲醯 胺(DMF),乙醚,苯或甲苯等溶劑存在下進行。反應 溫度可在0°C至所用溶劑之沸點之間變化,反應通常在 2 4小時之內完成。 計割1 式I R5 = H X=-C(R4a)2A-, 其中A原子係連接 在烯碳上且每一 個R4e各爲Η或R4) 式Π化合物(Y=S)之製備係使用2,4 -雙(4 一甲氧苯基)_1 ,3—二瞎―2 ’ 4_diphosphetane —2,4 —二硫化物(Lawesson’s試劑)’將式Π化合物
本紙張尺度遥用中國國家標隼(CNS ) A4規格(210 X 297公釐) --Γ · (請先閲讀背面之注意事項再填寫本頁) T丨裝· 訂
-A 經濟部中央橾準局員工消費合作社印製 A7 ______B7_五、發明説明(19 ) (Y = 〇 )硫化。硫化反應在M. Cava與M. Levinson發表 於 Tetrahedron ( 1 987 ), 4 1,5 0 6 1 -5 0 8 7 的文獻中有充分 說明。此轉化反應示於計劃2 » 計割2 Lawesson’ s 式H -^式I (Y = 0) 試劑 (Y = S) 式Π化合物之製備係根據式I V丙酸(V = OH)與 式V胺之間的縮合反應,反應中有諸如雙環己基碳化二亞 胺(D C C )之類的偶合劑存在。傅統上,此反應涉及將 式I V化合物(V = OH)與一當置之式V化合物於適合 溶劑中,例如二氣甲烷,乙酸乙酯或DMF,混合並添加 稍稍過置之DCC。反應溫度可介於〇 — 1 50°C之間( DC C偶合反應之評析可參見Tetrahedron (1981),.3 7, 233)。或者,可令式IV之氣酸(V=Ci?)與式V化 合物在酸清除劑(通常是三級胺碱,例如三乙胺存在下, 進行縮合反應,反.應溫度爲室溫或更低。反應可在惰性溶 劑中進行,此溶劑例如二氯甲烷,氯仿,苯,四氫呋喃, 甲苯或不與氯酸或碱類反應之其它溶劑。反應通常在2 4 小時之內完成(參見設計3 )。用於形成醯胺類之其它實 用方法在 Larock,Comprohems i ve Organic Transformations, VCH Publishers, Inc.,紐約,有所 討論。 本紙張尺度適用中國國家標準(CNS )__ A4規格(210X 297公釐) """ -22 - J I I |「4裴 訂 (請先閲讀背面之注意事唷再填寫本頁) 五、發明説明(20 ) 計割 A7 B7 IV (V = OH, C1) 0
式II 偶合劑 I 或酸清除ί , (Υ=0) 經濟部中央標準局員工消費合作杜印敦 計應14說明了製備式I V化合物之方法。在惰性溶劑 中,例如二氯甲烷,四氯化碳,氯仿或乙醚,以溴將式 V I之醯酸溴化,然後以諸如氫氧化鈉或氫氧化鉀等碱類 將此二溴中間產物去氫溴化》此反應可在諸如甲酵*乙醇 ,水或DMF等溶劑中進行•轉化反應之範例可參見 Organic Synthesis,Col 1. Vol. Π , p2 7 0。另一種製造 式I V化合物(V = 〇H)的方法記載於Chenault and D n p i η, S y n t h e s i s ( 1 9 8 7 ),4 9 8,Y a m a n a k a 氏等人, Synthesis (1992), 746,與 Hendrickson及Hussoin, Synthesis (1989),217。式 I V 化合物(V = 〇 H )可 再進一步轉化爲式IV化合物(V=C5),其係使用將 羧酸轉換爲氯酸之習知方法(參見Larock, Comprehensine Organic Transformations, VCH Pnblishers, Inc., New York)。 計割4 Brj
.COOL
VI 2. Base
式VI (L * Me. Et) (V = OH) (V = C1) 式乂丨化台物(L=Me ,E t )之製備係根據式 本紙張尺度遑用中HU家標準(CNS)从胁(210χ297公羞) --------裝------訂-----I 線 (請先閣讀背面之注意事項再填寫本頁) 306595 A7 _____B7_ 五、發明説明(21 )
Vn醛類與式VIE鱗鹽(L=Me,E t )之反應,於強 碱存在下進行。式乂 Π醛類與式VIE鱗鹽可在商業上購得 或可用習知方法製備。典型反應涉及式vm化合物與強喊 混合,該強碱例如有烷基鋰(例如丁基鋰),金靥烷氧化 物(例如甲氧化鈉),醯胺鈉或氫化鈉,反應進行於適合 溶劑中,例如四氫呋喃,乙醚,苯,甲醇,甲苯,乙腈, 二甲氧乙烷及二甲亞碉,然後添加式v π醛。反應溫度可 介於—70 — 200°C ’較好溫度介於0 - 1 〇(KC之間 。此witting反應已記載於Maercker氏發表之Organic Reactions ( 1 9 6 5 ),1 4, 2 7 0 -4 9 0。轉化反應係說明"於計 劃5 » 計割5 ^ + PhsP^’^COOL ^ r vn vm 式 (L=Me,B (L=Me,Et) X = aBr,I) 經濟部中央標準局員工消費合作社印裝 (請先閲讀背面之注意事項再填寫本頁) 或者,式I化合物之製備可令式I X化合物與式V Π醛 進行醛醇型縮合反應。計劃6說明此轉化反應。此反應可 在碱存在下進行’該碱例如金靥烷氧化物(例如甲氧化鈉 ),或胺碱(例如哌啶),或1,4 —重氮雜雙環〔2. 2. 2〕辛烷(DABC0)。此轉化反應所用之適合溶 劑可選自’但不受限於,甲醇,乙醇,水,二甲苯, DMF ’二喝烷或THF。此反應溫度可介於〇-2 0 0°C之間且此反應在4 8小時之內完成。此反應的範 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 24 A7 B7 五、發明説明(22 ) 例可參見 Organic Synthesis, Coll. Vo. 5, (1973), p6 2 7。 計割fi
R1 Q—CHO VD
計割7顯示式I X化合物(其中X = — A (CH2) „ —)之製造方法。此反應涉及式X化合物與式X I在碱 存在下進行環化反應。式X I化合物乃商業上可購得者或 可以習知方法製備者。可使用的碱,其範例包括氫化鈉或 特丁氧化鉀。此反應可在諸如苯,THF,乙醚,甲苯, DMF,二甲亞碘(DMSO)或二噚烷等溶劑中進行。 反應溫度可介於0 — 2 0 0°C之間且反應通常在2 4小時 內完成。 計割7 裝 訂 I ^ —線 - - (請先閲讀背面之注意事項再填寫本頁)
經濟部中央標準局員工消費合作社印R
R1 X
I(CH2)„I Base XI
式IX (X = -A(CH2)n-) 式X化合物(Y = 〇)之製備可令式χπ之羧酸與式 V之胺反應。式X Π化合物可自商業上購得或可由習知方 法製得。反應條件如計劃3所示。 本紙浪尺度遑用中國國家樣準·( CNS ) Α4规格(210X297公釐〉 -25 - 25 五、發明说明(23 ) 0 ^〇„ AH (A = 0. S) + χπ A7 B7 計割8
式V 式X (Y = 〇) 式I X化合物(其中X是一CH2(CH2) η—)之 製備可令式X瓜之溴化物在碱存在下進行環化反應’如計 劃9所示。反應條件與計劃7所示者類似· 計割9
Base
K X = *CH2(CH2)n· 計割1 0說明式X瓜化合物之合成法。此反應涉及式 X I V之酸與式V之胺進行偶合反應,如計舾3所示。 計割1 0 --------p—^------ΐτ------ ^ (請先閱讀背面之注意事項再填寫本頁) 經濟部中央橾準局員工消費合作社印製
+式V
式 XIII 式V化合物之製備,可令式XV化合物與次溴酸鈉( 或氫氧化鈉及溴化鈉)反應。此轉化反應如計割1 0所示 本紙張尺度適用中國®家橾準(CNS ) A4現格(2丨0><297公缓> -26 - A7 A7 經濟部中央標準局員工消費合作.杜印製 ____B7__ 五、發明説明(24 ) 。霍夫曼(Hofmann)再排列反應之介紹可參見Organic Reactions (1946),3, 267-306。典型反應涉及將式X瓜 化合物添加至次溴酸鈉水溶液中。此反應之溫度可介於〇 —200 °C之間,較佳溫度介於30 — 1 00 °c之間。反 應通常在2 4小時之內完成。或者,此轉化反應可藉使用 含有〔羥(甲苯磺醯基)碘代〕苯之回流乙腈與式X.V化 合物反應而達成(參見J. Org. Chem. ( 1 986 ), 5 1, 2669 -267 1 )。
式XV化合物之製備,可令式XV I化合物與銨反應 。此轉化反應示於計劃1 2。此反應可在諸如甲醇,乙醇 ’乙醚,苯及甲苯之類的溶劑中進行。典型反應係在常溫 下進行,且此反應通常在2 4小時之內完成。參考資料可 參見 W. Jones, J. Chem. Soc. ( 1 969 ),1 72 9。 計割1 2
本紙張尺度遙用中國囷家標準(CNS > A4%格(210X 297公釐) -------γ—裝------訂-----f 線 (請先閲讀背面之注意事項再填寫本頁) -27 - 經濟部中央標準局員工消费合作社印裝 A7 ____B7_五、發明説明(25 ) 式XV I化合物之製備,可令絲胺酸衍生物(式 χνπ )與式χνπι之亞胺酸鹽反應,如計劃1 3所示。 式X v m之絲胺酸衍生物可自商業上購得或可由習知方法 製備。此反應可在甲醇,二氯甲烷,氯仿,苯,二噚烷與 四氫呋喃之類的溶劑中進行。可添加水以作爲共溶劑。此 反應可在o°c至所用特定溶劑之回流溫度之間進行,且此 反應通常在2 4小時內完成。參考資料可參見Agric. Biol· Chem. (1986), 50, 615-623 。計割1 3
如計劃1 4所示,式XV I之亞胺酸鹽可由式XVII 之醯胺類製備,其係與四氟硼酸三烴基氧錨鹽於諸如二氯 甲烷,苯或甲苯之類的惰性溶劑中反應。式XVE之醯胺 類可在商業上購得或可由已知方法製備。亞胺酸鹽類的合 成已在 D.A. Neilson 於 The Chemistry of Amidines and Imidates, Patai and Pappoport, Eds., Vol. 2,(1991) ,pp 425-483中有廣泛介紹。 -------一--^------,玎------- (请先閱讀背面之注意事項再填寫本頁) 本紙張尺度遑用中國國家標率(CNS ) A4現格(210X 297公釐) -28 - A7 A7 經濟部中央標準局員工消費合作社印製 __B7 五、發明説明(26 ) 計割1 4
可理解的是,上述製備式I化合物之一些試劑與反應 條件可不與中間產物所呈的官能性相容。在這類情況下, 將保護/去保護順序或官能基分子內轉換作用納入合成法 中,有助於獲得所欲產物。使用與選擇保護基乃熟悉化學 合成之士可輕易思及者(例如,參見Greene, T.W.,
Wuts, P.G.M. Protective Groups in Organic Synthesis, 2nd ed·, Wiley: New York, 1991) * 熟悉 此藝之士將了解,將任何單獨計劃中所述的特定試劑加入 之後,有些情況下必須進行未予詳述之其它途徑合成步驟 ,始能完成式I化合物的合成。熟悉此藝之士亦能了解, 可能必須進行計劃1 -?所述步驟的組合,其順序不同於 製備式I化合物所示之特定順序。 熟悉此藝之士亦將了解,本文所述之式I化合物與中 間產物可進行多種親電子性,親核性,基團性,有機金屬 性氧化反應與還原反應,藉以增加取代基或改變存在中的 取代基。 不用其它營思,咸信熟悉此技藝之士利用前述說明將 可使用本發明至其最大範圍β因此·下列將予以說明之實 施例僅爲說明性質,絕不以任何方式限定本發明。百分比 本紙張尺度適用中國國家標率(CNS ) Α4規格(210X 297公釐) ~ -29 - ^1裝 訂 ί 涨 (請先閲讀背面之注意事項再填寫本頁) 308595 A7 B7 經濟部中央標隼局員工消費合作社印製 五、發明説明(27 ) 係按重量計,除了用於層析溶劑混合液,或者另有指明, 層析溶劑混合液所用之部份與百分比係按體稹計,除#另 有指定e 1H NMR光譜係以p pm表示,自四甲基砂 院向下算起,s=單峰’ d=雙峰,tE三峰,C[=四峰 ’ ABq = ,AB 〃四重峰,m =多峰,dd=成對雙峰 ,b r s =廣單峰a 窗例1 步驟A : 2 ,6 —二氟苯甲醯亞胺甲酯 將10. 62克(0 068莫耳)之2,6 —二氟 苯醯胺加入含有10. 0克(0. 068莫耳)之四氟硼 酸三甲基錨鹽之7 0毫升二氣甲烷懸浮液。此反應在氮氣 下,攪拌一夜。將飽和之重碳酸鈉水溶液慢慢加入並以二 氮甲烷萃取此混合物。以鹽水清洗匯合後的萃取物,置 Mg S 04上脫水,並蒸發之。令殘留物通過矽膠管柱, 以EtOAc:己烷(1:6)溶離,生成9. 13克之 步驟A標的化合物,呈淡黃色油。 1 Η N M R ( C D C 1 a ) : δ 7 . 7 0 ( b r s,lH),7.73(m,lH) ,6. 94(t,2H) ,3. 94(s,3H)。 步驟B : 2 — ( 2 ,6 —二氟苯基)-4,5 —二氫一 4 —曙 唑羧酸甲酯 本紙张尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) ^--- I - ————1111^0^1—lllllt———— T I I I n I L t ( 0¾. i t 〆 (請先閱讀背面之注意事項再填寫本頁)
經濟部中央標準局員工消费合作杜印製 五、發明説明(28 ) 將9. 09克(〇. 058莫耳)之絲胺酸甲酯鹽酸 鹽逐份加入10· 〇克(〇. 058莫耳)之步驟A之標 的化合物溶液中(於15毫升EOH及5毫升水)。回流 下攪拌此混合液歷1. 5小時》減壓下將揮發物蒸發掉, 令殘留物於乙酸乙酯(E t 〇A c )與水之間分佈分離》 以鹽水清洗E t OA c層:置於Mg S 04上脫水並蒸發 之。令殘留物通過矽膠管柱,其係以EtOAc:己烷( 1 : 4)溶離,生成6. 0克之步驟B標的化合物,其爲 無色油。 1 Η N M R ( C D C 1 a ) : δ 7. 4 3 ( m - 1 H ) ,6. 9 8 ( t * 2 H ), 5 . 0 0 ( t - 1 H ), 4 . 63 — 4. 72 (2t,2H), 3. 84(s,3H)。 步驟C : 2_ (2,6 —二氟苯基)—4,5 -二氫—4 —噚 唑羧醯胺 室溫下,令含有10. 0克(0. 041莫耳)之步 驟B標的化合物(其於1 0 0毫升含2M銨之甲醇溶液中 )的溶液攪拌一夜。蒸發溶劑後’製得9. 〇4克之步驟 C標的化合物,其爲白色粉末,熔點爲148〜149t 〇 1 H NMR (Me2S0-de) : δ 本紙張尺度適用中國國家標準(CNS〉A4規格(210 X 297公釐) ^ I裝--------訂------線 (請先閱讀背面之注意事項再填寫本頁)
經濟部中央橾準局貝工消費合作社印製 A7 -____B7__ 五、發明説明(29 ) 7.67(m,lH),7.49(br s,lH) ,7.39(br s,lH), 7. 2 7 ( t * 2 H ) ,4. 8 5 ( t - 1 H ), 4 . 56(2t,2H)。 步驟D : 2— (2,6 —二氟苯基)一4,5 —二氫一 4 —吗 唑胺 將0. 386克(0. 0044莫耳)溴逐滴加入含 有0. 440克(0. 011莫耳,於3. 7毫升H20 中)NaOH之冷卻溶液。將〇. 5〇〇克(〇· 002 莫耳)之步驟C標的化合物逐份加入。令反應於8 0°C攪 拌0. 5小時。添加Et2〇與H20並以EtOAc萃取 此混合液。以鹽水清洗匯合後的萃取液,置Mg S 〇4上 脫水,蒸發而生成0. 350克步驟D之標的化合物,其 爲白色固體,熔點爲8 1 — 85 °C。 1 H NMR(Me2S0-de) : δ 7. 6 2 ( m > 1 Η ) > 7 . 24(t,2H), 5. 1 5 ( t * 1 Η ) 4 . 7 0 ( t * 1 Η ), 3 · 8 3 ( t,1 Η )。 步驟E : 3 — (4 -氯苯基)一 N_〔2 —(2,6 - 二氟苯 基)—4,5 -二氫—4 —噚唑基〕一 2 —丙炔醢胺 本紙張尺度適用中國國家標準(cns)a4規格(210X297公釐) I I I J —裝— I „ 訂 II I —線 (請先閱讀背面之注意事項再填寫本頁) -32 - 308595 A7 B7 五、發明説明(3〇 ) 經濟部中央標隼局員工消費合作社印製 將 1 t 3 —_. 雙 環 己 基 碳 化 二 亞 胺 ( 1 * 0 3 克 > 0 0 0 5 莫 耳 ) 逐 份 加 入 冷 卻 ( 冰 浴 ) 混 合 物 中 * 該 混 合 物 由 下 列 組 成 步 驟 D 之 栖 懷 的 化 合 物 ( 0 9 9 1 克 0 0 0 5 莫 耳 ) 4 — 一 甲 基 胺 基 吡 淀 ( 0 0 6 1 克 » 0 0 0 0 5 莫 耳 ) 及 3 — ( 4 — 氣 苯 基 ) 丙 炔 酸 ( 0 9 6 3 克 0 0 0 5 莫 耳 ) » 及 1 8 毫 升 二 氯 甲 院 組 成 〇 令 此 混 合 液 於 室 溫 攪 拌 0 5 小 時 < 然 後 濾 除 固 體 〇 蒸 發 濾 液 並 令 殘 留 物 通 週 矽 膠 管 柱 1 溶 離 使 用 E t 〇 A C : 己 院 ( 1 ; 3 ) 生 成 1 6 6 克 步 驟 E 標 的 化 合 物 * 其 爲 黃 色 固 體 » 熔 點 爲 1 3 4 — 1 3 5 °C 0 1 Η N M R (C D C ] ί 3) δ 4 3 5 ( d d » 1 Η ) , 4 7 0 ( t > 1 Η ) 6 2 0 ( m 1 Η ) > 6 5 1 ( d > 1 Η ) 7 0 0 ( t > 2 Η ) 7 3 5 ( m > 2 Η ) > 7 4 5 ( m > 3 Η ) 0 步 驟 F ; ( Ζ ) — 5 — C ( 4 — 氣 苯 基 ) 伸 甲 基 ) — 3 — C 2 — ( 2 I 6 — 二 氟 苯 基 ) — 4 t 5 — 二 氫 — 4 — 噚 唑 基 ] — 4 — D咢 唑 啶 酮 將 氫 化 鈉 ( 6 0 % 9 分 散 於 油 中 » 0 0 8 8 克 9 0 0 0 2 2 莫 耳 ) 加 入 冷 卻 ( 冰 浴 ) 混 合 液 中 > 該 混 合 液 由 步 驟 E 之 標 的 化 合 物 ( 0 7 3 1 克 * 0 0 0 2 莫 耳 ) 與 仲 甲 醛 ( 0 3 0 0 克 1 0 0 1 莫 耳 ) 9 2 毫 升 本紙伕尺度適用中國國家橾準(CNS ) A4規格(210 X 297公釐) ---------j I 裝--------訂---^----線 (請先閲讀背面之注意事項再填寫本頁) -33 - A7 B7 經濟部中央標準局貝工消費合作社印裝 五、發明説明(31 ) 撕 水 D Μ F 組 成 0 冷 房 中攪 拌 此 混 合 液 0 5 小 時 ,再小 心 地 以 水 驟 止 反 rrtff 應 並 同 時冷 卻 〇 所 生 成 的 混 合 液 係 以 Ε t 〇 A C 萃 取 » 經 匯 合的 萃 取 物 以 水 清 洗 0 令 有 機層脫 水 ( Μ g S 0 4) •蒸發而得黃色固體 ,經乙醇/己烷對 此 固 體 碾 製 後 > 生 成 0 .4 3 2 克 步 驟 F 之 標 的 化 合物, 即 本 發 明 之 化 合 物 J 其 爲白 色 固 體 » 熔 點 爲 1 3 1 ~ 1 3 4 V 0 1 Η N M R (C :D C 1 3) δ 4 * 2 5 ( d d » 1 Η ) 9 4 7 0 ( t » 1 Η ), 5 4 8 ( A B q 贅 2 Η ) 9 6 2 8 ( s ) 1 Η ), 6 5 0 ( d d ί 1 Η ), 7 0 0 ( t y 2 Η ), 7 3 5 ( d > 2 Η ) 7 5 0 ( m * 1 Η ), 7 6 0 ( d 2 Η ) 〇 實例2 步驟A : 3— (4 —碘苯基)—2 -丙烯酸甲酯 將5. 0克(0. 0215莫耳)4 一碘苯甲醛溶於 2 2毫升乙腈。添加乙酸三苯基phosphoranylidene)甲 酯(14. 41克,0. 043莫耳),令此混合液回流 —夜。以IN HCj?驟止反應,以EtOAc萃取三次 。以水清洗匯合後之萃取物,脫水(Mg S 04)及蒸發 。令殘留物通過矽膠管柱,以EtOAc :己烷(1 : 10)溶離,生成5. 60克之步驟A標的化合物,其爲 本紙張尺度適用中國國家揉準(CNS ) A4規格(210 X 297公釐) " ' ' -34 - I I I 丄' I I J 訂. 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(32 ) 油。 1 Η N M R ( C D C 1 3 ) : δ 3. 805(s,3H), 6. 4 3 9 ( d > 1 H ), 7 . 2 2 8 ( d > 2 H ), 7. 6 2 9 ( d > 1 H ), 7 . 712(d,2H)。 步驟B : 3 -(4 —碘苯基)—2 —丙炔酸 將5· 60克(0. 019莫耳)之步驟Α標的化合 物溶於1 9毫升二氯甲烷中。將此混合液冷卻至〇°C並逐 滴添加溴(0. 97毫升)。反應於室溫攪拌1小時,蒸 發溶劑。將殘留物加入5 0 °C之溶液,此溶液由4. 7 8 克KOH (於2 3毫升E t OH中)組成。令此混合液回 流1 8小時》蒸發溶劑並將固體溶於水。濾掉不溶物質, 以H C j?將溶液p Η校正至2。濾出所生成之沈澱物,生 成4. 7克步驟Β之標的化合物,其爲不純白色固體,熔 點爲 1 80 — 1 84°Ce 1 H NMR (DMSO-de) ·· δ 7 . 3 9 0 ( d - 2 Η ) * 7 . 5 0 ( d - 2 Η )。 步驟C : N —〔2 (2,6 -二氟苯基)—4,5 —二氫—4 本紙張尺度適用中國國家標隼(CNS ) A4規格(210X297公釐)~ ~ '—" -35 - ------------------III---r--ΙΦ (請先閲讀背面之注意事項再填寫本頁) A7五、發明説明(33 ) 經濟部中央樣準局員工消費合作社印製 ___B7 — D咢 唑 基 ) — 3 — (4 — «ft wk 苯 基 ) — 2 — 丙 炔 醯 :胺 對 0 6 8 0克( 0 0 0 2 5 莫 耳 ) 步 OS 驟 B 標 的 化 合 物 之 7 毫 升 C Η 2 C l 2 冷 卻 ( 0 °C ) 溶 液 » 添 加 0 5 3 3 克 ( 0 . 0 0 2 5 莫 耳 ) 1 t 3 — 雙 環 己 基 碳 化 二 亞 胺 » 0 0 3 2 克 4 — 二 甲 基 胺 基 吡 淀 > 及 0 5 0 0 克 實 例] L中 步 驟 D 之 標 的 化 合 物 0 令 此 反 應 混 合 物 於 室 溫 攪 拌 3 0分 鍾 並 濾 除 固 相 0 將 溶 劑 白 濾 液 蒸 發 出 來 » 產 生 一 殘 留物, 令 其 通 •ija 過 矽 膠 管 柱 > 溶 離 係 用 E t 〇 A C : 己 焼丨 (1 1 ) 1 生 成 0 9 6 0 克 之 步 驟 C 標 的 化 合 物 其爲固 體 熔 點 爲 1 5 0 — 1 5 2 °c 〇 1 Η N M R (CD C 1 3 ) δ 4 3 4 0 ( m , 1 Η ) 4 6 9 1 ( t » 1 Η ) t 6 2 0 4 ( m , 1 Η ) 7 2 0 0 ( m » 3 Η ) 9 7 2 0 5 ( d - 2 Η ) 7 4 4 9 ( m ♦ 1 Η ) 9 7 6 8 4 ( d , 2 Η ) 〇 步 驟 D ( Z ) — 3 -I :2 — ( 2 I 6 一 二 氟 苯 基 ) — 4 » 5 — 一 氫 — 4 — ϋ咢 唑基〕 — 5 — ( ( 4 — W 苯 基 ) 伸 甲 基 ) 一 4 — 噚 唑 啉 酮 將 氫 化 鈉 ( 6 C )% 1 分 散 於 油 中 > 0 0 4 4 克 1 0 0 0 1 1 莫 耳) 加 入 冷 卻 ( 冰 浴 ) 混 合 液 中 > 此 混 合 液 由 步 驟 C 之 標 的化合 物 ( 0 4 5 2 克 1 0 0 0 1 莫 耳 ) 及 仲 甲 醛 ( 0 . 1 4 8 克 » 0 0 0 5 莫 耳 ) 及 1 毫 本紙张尺度適用中國國家標準(cm ) Α4規格(210X 297公釐) --------ί _ 裝-----^-I 訂----^----線 (請先閱讀背面之注意事項再填寫本頁) 308595 經濟部中央橾準局員工消費合作社印製 A7 B7五、發明説明(34 ) 升無水DMF組成。令此混合物於冷房中攪拌1小時,然 後小心地在冷房中以水驟止反應*所生成的混合物係以 E t OA c萃取,並且以水清洗匯合後的萃取物。令有機 層脫水(Mg S 〇4)並蒸發之。令殘留物通過矽膠管柱 ,溶離用EtOAc:己烷(1:2) ’生成〇. 170 克步驟D之標的化合物’即本發明之化合物,其爲油,靜 置時固化爲固體’熔點爲1 6 5 — 1 6 7 °C。 1 Η N M R ( C D C 1 a ) : δ 4. 4 7 1 ( q ' 1 H ), 4. 6 7 9 ( t > 1 H ) ,5. 4 3 9 ( d > 1 H ), 5. 5 1 6 ( d - 1 H ) ,6. 2 3 7 ( s - 1 H ), 6 . 5 0 7 ( m - 1 H ) ,7. 026(t,2H) ’ 7. 3 8 1 ( m > 2 H ) ’7. 505 (m,lH), 7 . 683 (m,2H)。 窗例3 (Z) — 5 —〔 (2 一,4 一 -二氯〔1 ,1二苯 基〕—4 —基)伸甲基〕一3 —〔2— (2,6_二氟苯 基)—4,5 —二氫—4-噚唑基〕-4 一噚唑啉酮 將實例2步驟D之標的化合物(0 . 4 8 2克, 0. 001莫耳)溶於2毫升二甲氧基乙烷。對此溶液添 加 1. 04 毫升之 2M N a 2 C 0 3 1 0 . 036 克( 0. 00003莫耳)四個(三苯基膦)鈀(〇),及 0 . 191克(0. 001莫耳)之2,4 —二氯苯硼酸 (請先閱讀背面之注意事項再填寫本頁) 裝- 訂 本紙張尺度適用中國國家標準(CNS ) A4規格(2I〇X297公釐) A7 B7 五、發明説明(35 ) (於0. 53毫升甲醇中)。反應係於80 °C攪拌一夜’ 然後以9. 75毫升之2M Na2C03溶液(含有 0. 78毫升之30%NH4OH)驟止反應。以二氯甲 烷萃取此混合物並以N a H C 03飽和水溶液清洗有機萃 取物》令此有機萃取物脫水,過濾及蒸發,生成一殘留物 ,令其通過矽膠管柱並以EtOAc :己醇(1 : 2)溶 離,生成0. 300克之實例3標的化合物,即本發明之 化合物,其爲固體,熔點爲1 5 1 — 1 5 3°C。 Η N M R ( C D C 1 7 7 4 8 8 ( m 5 3 2 ( m 3 7 0 ( s 0 2 6 ( m 4 2 4 ( m 7 1 9 ( m 1 H ) 1 H ) 1 H ) 2 H ) 2 H ) 2 H ) 5 4 . 6 8 8 ( m > 1 H ) 5 . 4 6 3 ( d > 1 H ) 6 . 5 2 2 ( m,1 h ) 7 . 2 8 5 ( m,2 H ) 7 . 4 8 6 ( m ,2 H ) --------ί 裝-----.—訂------線 (請先閱讀背面之注意事項再填寫本頁) 窗例4 經濟部中央樣準局員工消費合作社印製 Z) — 3 —〔2 — (2,6—二氟苯基)—4 —二氫—4 —腭唑基〕—5-〔 〔4 —〔(三甲基甲矽烷 基)乙炔基〕苯基〕伸甲基-4-噚唑啉酮 將實例2步驟D之標的化合物(0. 482克, 0. 001莫耳)加入2. 3毫升CH3CN與2. 3毫 升E t 3N »對此混合物添加(三甲基甲矽烷基)乙炔( 0. 28毫升,0. 002莫耳),氣化雙(三苯基膦) 本紙張尺度適用中國國家橾準(CNS ) A4規格(210X297公釐) 五、發明説明(36 ) A7 B7 經濟部中央標準局貝工消費合作社印製 鈀 ( Π ) ( 0 0 : 3 5 克 » 0 0 0 0 0 5 莫 耳 ) 及 •nfft Wk 化 銅 ( I ) ( 0 0 ( D 9 5 克 0 0 0 0 0 5 莫 耳 ) ο 令 此 反 應混 合 物 於 室Ϊ 昆攪 拌 一 夜 〇 蒸 發 溶 劑 9 加 水 至 殘 留 物 上 並 以Ε t 0 A c萃取 所 生 成 之 混 合 物 〇 以 鹽 水 清 洗 Ε t 0 A c 萃 取 物 ,脫 水 ( Μ g S 0 4) >過濾並蒸發< » 令 殘 留物 通 過 矽 膠管柱 » 溶 離 用 E t 0 A C ; 己 院 ( 1 ; 2 ) ,生 成 0 3 8 0 克 的 固 體 » 熔 點 爲 1 2 3 一 1 2 4 °C 0 1 Η N M R ( :C D C ] [3) ; 0 .2 5 3 ( S ,9 Η ) » 4 4 4 9 ( m 9 1 Η ) 4 .6 7 4 ( m ,1 Η ) 5 4 4 5 ( d J 1 Η ) 9 5 .5 2 5 ( d ,1 Η ) 6 2 8 8 ( s 9 1 Η ) > 6 .5 1 2 ( m ,1 Η ) j 7 0 2 3 ( m » 2 Η ) 7 .7 4 5 ( m ,3 Η ) > 7 * 5 8 1 ( d 1 2 Η ) 〇 藉由 上 述 製 程與該 技 藝 已 知 的 方 法 * 可 製 備 表 1 至 7 所 示 之下 列 化 合 物’ >下 列 縮 寫 用 於 表 中 > 其 爲 : t = 第 二 > S =第 二 > η =正, i = 異 » C 環 9 Μ e = 甲 基 1 Ε t :乙 基 > Ρ r =丙 基 » η 一 P r = 正 丙 基 9 i — P r = 異 丙基 > B U =丁基 » η — B U = 正 丁 基 > i — Β U == 異 丁 基, S — Β U = =第 二 丁 基 t B U = 第 二 丁 基 y C — C 5 H g =: rag 壊 戊 基 ,C — C βΗ ϊ 1 = =環己基, P h = =苯基 I 0 Me = 甲 氧 基 -0 Ε t — 乙 氧 基 1 0 Ρ h = 苯 氧 基 , S Μ e = 甲 硫 基 'S E t = 乙 硫 基 > S P h = 苯 硫 基 N C Μ e ) 2 ~ =二甲基 胺基, C N = =氰基, N 0 2 = 硝 基 » 本紙張尺度逋用中國國家標準(CNS ) A4規格(210 X 29*7公釐) ---------^ I 裝---------- 訂---r---L 線 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(37 ) COOMe =甲氧激基,CHO =甲酸基’ C〇Me==甲 羰基,COPh =苯基羰基,S iMe3 =三甲基甲矽烷 基,及S02Me =甲基磺醯基。
R1 =F, R2 =F,P 二 H, A = 0, Y = 0, m = 1, n = i 且R19= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-fi-Pr 2-i-Pr 2-n-Bu 2-z-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMe 3-F 3-CI 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 3-/-Ργ 3-n-Bu 3-i-Bu 3-j-Bu 3-f-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4-CX3i2CF3 4-CH2CF3 4-nBu 4-/-Bu 4-j-Bu 4-/i-Pr 4-r-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4*CH:CHCI 4-CH2CN 4-CN 4-N〇2 ‘S02Me 4-〇Me 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCFnH 2-OMe 2w-Bu 本紙張尺度適用中國國家橾準(CNS ) Α4規格(210Χ297公釐) 訂 (請先閱讀背面之注意事項再填寫本頁) -40 - 五、發明説明(38) A7 B7
I 3-λ-Ργ 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CH0 2-SMe 3-SCF2H R1 =F, R2 = F, P = H, A = 0, Y = 0. m = 1,n = 2 且R19= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-/-Pr 2-rt-Bu 2-i-Bu 2-5-Bu 2-CH2CN 2-CH2F 2-CH0 2-COMc 2-COOMc 3-F 3-Ci 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 3-i-Pr 3-rt-Bu 3-i-Bu 3-ι-Βυ 3-nBu 3^CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 tOCF3 4-OCH2CF3 4-CH2CF3 4-f-Bu 4-/-Bu 4-s-Bu 4-n-Pr 4-(-Pr 4-Et ‘Me 4-CH2F 4-CsCH 4-CH=CHCI 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-0Me 4-COMe 4-COOMe 4-C0NHMe 4-S02NHMc 4-SiMe3 4-SF5 2-0Et 2-SEt 2-OCF2H 2.SCF2H 3-0Et 3-SMc 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-0Me 2-/-Bu 3-λ-Ργ 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CH0 2-SMe 3-SCF2H · Rl =F. R2 = F, P = H.. A = S, Y = 0, m= 1. n = 1 且Rie: 2-F 2-a 2-Br 2-CF3 2-OCF3 2-CN 2·Ν〇2 2-Me 2-Et 2-rt-Pr .2·/·Ργ 2*/i-Bu 2-i-Bu 2-5-Bu 2-CH2CN 2-CH2F 2-CH0 2-C0Mc 2-C00Me 3-F 3-Cl 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 3w-Pr 3-rt-Bu 3-i-Bu 3-j-Bu 3-i-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-CaCH 3.SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-r-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-ChCH 4-CH=CHCl 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-0Me 4-COMe 4-CO〇Me 4-C0NHMe 4-S02NHMe 4-SiMe3 4-SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-0Et 3-SMc 3-SEt 3-OCF2H 4-OEi 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-0Mc 2-i-Bu 3*n-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CH0 2-SMe 3-SCF2H 請 先 閱 讀 背 面 注 意 事 項 再 填 本 頁 本紙張尺度適用中國國家標準(CNS ) A4現格(210X 297公釐) 41 A7 B7 發明説明(39 ) i 五 _ 經濟部中央標隼局員工消费合作杜印製 R1 =F. R,= F. P = H. A = 0, Y = O, m = 2, n = 1 且 Rie= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-j.Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMe 3-F 3·α 3-CF3 3-OCF3 3-CN 3-N〇2 3-〇Mc 3-Me 3-Et 3-/-Pr 3-n-Bu 3-i-Bu 3-5-Bu 3-/-Bu 3-CH2CN 3-CH2F 3-COMc 3-COOMe 3-SiMe3 30CH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4.CF3 4-OCF3 4-och2cf3 4-CH2CF3 4-r-Bu 4-f-Bu 4-i-Bu 4-n-Pr 4-i.Pr 4-Et 4-Me 4-CH2F 4-OCH 4-CH=CHCI 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-OMe 4-COMc 4-COOMc 4-CONHMc 4-S02NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3,SMc 3-SEt 3-OCF2H 4-〇Et 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMc 2-i-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4^CH=CH2 4-CHO 2-SMe 3-SCF2H R1 =F, R2 = F, P = H, a = nch3· y =0,m = 1,n =1 且Rie= 2-F 2·α 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Ec 2-/i-Pr 2-(-Pr 2-n-Bu 2-/-BU 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMe 3-F 3-C1 3-CF3 3-OCF3 3-CN 3_N〇2 3-OMe 3-Me 3-Et 3-/-Pr 3-n-Bu 3-/-Bu 3-5-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-CaCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 4.OCF3 4.〇CH2CF3 4-CH2CF3 4-/-Bu 4-i-Bu 4-s-Bu 4-n-Pr 4-j.Pr 知Et 4-Me 4-CH2F 4-CsCH 4*CH=CHC1 4-CH2CN 4-CN 4-NO〇 _ 4-S〇2Me ‘OMe 4-COMe ‘COOMe 4-CONHMe 4-S02NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-CX:F2H 4-SCF2H 2-OMe 2-r-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CHO 2-SMe 3-SCF2H R1 = F, R2 = f, p - h, A = 0, Y = S, 1,n = 1 且Rle= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-λ-Ργ 2-i-Pr 2-n-Bu 2-/-Bu 2-j-Bu 2-CH2CN 2,CH2F 2-CHO 2-COMe 2-COOMe 3-F 3-Ci 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et (請先閲讀背面之注意事項再填寫本頁) -裝. -9 線 本纸張尺度適用中國國家標準(CNS ) A4現格(210X 297公釐) 五、發明説明(40 ) A7 B7 經濟部中央標準局員工消費合作社印製 3-r-Pr 3-/i-Bu 3-/-Bu 3-i-Bu 3-i-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-C^:H 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CF3 4-i-Bu 4-i-Bu 4-j-Bu 4-/i-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4-CH=CHCl 4»CH2CN 4-CN 4-N〇2 4-S02Me 4-OMe 4-COMe 4-COOMc 4-CONHMe 4-S02NHM< =4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMc 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-〇CF2H 4-SCF2H 2-OMe 2-r-Bu 3-λ-Ργ 3CHO 4-F 4-n-Bu 4^H=CH2 4-OEiO 2-SMe 3-SCF2H R1 = F, R2 = F, P = 2-OMe, A = 0, Y = 0, m = 1,r 丨=l且R19= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-N02 2-Me 2-Et 2-λ-Ργ 2-/-Pr 2-n-Bu 2小Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMc 3_F 3-C1 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMc 3-Me 3-Et 3-/-Pr 3-n-Bu 3-f.Bu 3-5-Bu 3-/-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMc 3-SiMe3 3-CsCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4CH2CF3 4-/-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH2F 4-OCH 4-CH=CHCI 4-CH2CN 4-CN 4-NO2 4-S02Me 4-OMe 4-COMc 4-COOMe 4-CONHMc 4-S02NHMe 4-SiMe3 4-SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMc 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-i-Bu 3-«-Pr 3-CHO 4-F 4-n-Bu 4*CH=CH2 4-CHO 2-SMe 3-SCF2H R1 =F. R 2 = F, P = 2-CH3, A = 0.' Ϊ = 0, m = 1, n =1 且Rie= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-N02 2-Me 2-Et 2-n-Pr 2w-Pr 2-n-Bu 2-i-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMc 3-F 3-Cl 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMc 3-Me 3-Et 3-/-Pr 3-/i-Bu 3-i-Bu 3-j-Bu 3-i-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-CsCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-i-Bu 4w-Bu 4-5-Bu 4-n-Pr 4w*-Pr 4-Et 4-Me 4-CH2F 4-ChCH 4.CH=CHC! 4-CH2CN 4-CN 4-N〇2 4-S〇2Mc 4-QMe ----------裝--------訂------一線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4現格(210X 297公釐) A7 B7 s 五、發明説叨(41) 4-COMe 4-COOMc 4-CONHMe 4-S〇2NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2*OCF2H 2-SCF2H 3*0Et 3-SMe 3-SEt 3-OCF2H 4·〇Ε! 4-SMe 4-SEt 4-〇CF2H ‘scf2h 2-OMe 2-r-Bu 3-λ-Ργ 3-SCF2H 3-CHO 4-F 4-CH=CH2 4-CHO 2-SMt
R1 =F, r2 = F, P = 2-F, A = 0,Y = 0t m = 1, π = 1 且 R19= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CH0 2-C0Mc 2-C00Me 3-F 3-CI 3.CF3 3-OCF3 3-CN 3-N〇2 3-0Me 3-Me 3-Et 3-Z-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-f-Bu 3-CH2CN 3-CH2F 3-COMe 3-C00Me 3-SiMe3 3-CsCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4OCF3 4>OCH2CF3 4-CH2CF3 4-r-Bu 4-i-Bu 4-j-Bu 4-λ-Ργ 4-i-Pr 4-Et 4-Mc 4-CH2F 4-OCH 4-CH=CHCl 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-0Me 4-COMe 4-C00Me 4-CONHMe 4-S02NHMe 4-SiMe3 4*SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-0Et 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-〇CF2H 4-SCF2H 2-OMe 2-/-Bu 3-/i-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CHO 2-SMe 3-SCF2H (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製
R1 =F, R2 = F, P = 2-C1, A = 0, Y =0· m = 1, n = 1 且 R19= 2-F 2-CI 2·Βγ 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-λ-Ργ 2-/-Pr 2-n-Bu 2-/-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CH0 2-COMe 2-C00Me 3-F 3-CI 3-CF3 3-OCF3 3-CN 3-N〇2 3-0Mc 3-Me 3-Et 3-/-Pr 3-«-Bu 3-/-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMe 3-C00Me 3-SiMe3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-i-Bu 4-i-Bu 4-i'Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4-CH=CHCI 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-0Me 4-C0Me 4*C00Me 4-C0NHMe 4-S〇2NHMe 4-SiMej 4-SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMc 3-SEt 3-OCF2H 4-0Et 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-/-Bu 3-n-Pr 3-CHO 4-F 4-/i-Bu 4-CH=CH2 4-CHO 2-SMe 3-SCF7H .丨。丨装------訂-------線_---II--------- 本紙悵尺度適用中國國家標率(CNS ) Λ4規格(210 X297公釐) 五、發明説明(42 ) A7 B7
R1 =F. R2 s F, P = 2-OEt, A = 0, Y = O, m = lt n l 且 R19= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-/-Pr 2-n-Bu 2-/-Bu 2-5-Bu 2-CH2CN 2-CH2F 2-CH0 2-COMe 2-COOMe 3-F 3-C1 3_CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMc3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4CF3 4-OCF3 ‘och2cf3 4-CH2CF3 4-f-Bu 4-i-Bu 4-j-3u 4-n-Pr 4-t-Pr >Et 4-Me 4-CH2F 4-OCH 4-CH=CHC\ 4-CH2CN 4-CN 4-N〇2 4-S02Mc 4-〇Me 4-C〇Mc 4-C00Me 4-CONHMc 4-S〇2NHMc 4-SiMej 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMc 3-SEt 3-OCF2H 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-r-Bu 3-n-Pr 3-CH0 4-F 4-n-Bu ‘ch=ch2 4-CHO 2-SMe (請先閲讀背面之注意事項再填寫本f) 3-SCF2H -裝· 經濟部中夬標隼局員工消費合作社印製 R1 = F, R2 = F, P = 3-F, A = 0, Y = 0,m = 1, n = l 且 R19= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2*CN 2-N02 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMe 3-F 3-C1 3CF3 3-OCF3 3-CN 3-N02 3-OMe 3-Me 3-Et 3-/-Pr 3-rt-Bu 3w'-Bu 3-i-Bu 3-f-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH 4-CI 4-Br 4-CF3 4-OCF3 4.〇CH2CF3 4-CH2CF3 4-r-Bu 4-i-Bu 4-j-Bu 4-λ-Ργ 4./-Pr 4-Et 4-Me 4-CH2F 4-CaCH 4-CH=CHCl 4-CH2cn 4-CN 4-N〇2 4-S02Mc 4-OMe 4-COMe 4-COOMe 4-CONHMe 4.S02NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMc 4-SEt ‘ocf2h 4-SCF2H 2-OMe 2-r-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4*CH=CH2 4-CHO 2-SMe 3-SCF2H rUf. r2 = f. P = 3-CH3. A = 0. Y =0, m= 1, n =1 且R19= 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-^-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMe 3-F 3-C1 3-CF3 3-OCF3 3-CN 3-N02 3-OMe 3-Mc 3-El 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公犛)_ 45 _ 訂 308595 五、發明説明G 43 ) A7 B7 經濟部中央標隼局員工消費合作社印製 3-i-Pr 3-n-Bu 3-<-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-r-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-ChCH 4-CH=CHCl 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-0Mc 4-COMe 4-COOMc 4CONHMe 4-S02NHMc 4-SiMc3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 本 ocf2h 4-SCF2H 2-OMc 2-i-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CHO 2-SMe 3-SCF2H r! = f, R2 = F, P = 3-C1. a = o, y 2-F 2-C1 2-Br -0, m= 1, n = 2-CF3 l 且Rle= 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-i-Bu 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMc 3-F 3-C1 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 3-i-Pr 3-n-Bu 3-ι-Βυ 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMe3 3-OsCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4.CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-r-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-a 4-Me 4-CH2F 4-CsCH 4CHCHQ 4-CH2CN 4-CN 4-N〇2 本 S02Me 4-OMe 4-COMe 4-COOMe 4-CONHMc 4-S〇2NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-r-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4-CH=rCH2 4-CH0 2-SMe 3-SCF2H R1 = F, R2 = F, P = 3-OMe, A = 0, ’ 2-F 2-C1 2-Br ^ = 0, m = 1, n 2-CF3 =】且R19= 2.OCF3 2-CN 2-N〇2 2-Me 2-Et 2-n-Pr 2-ϊ-Ργ 2-n-Bu 2-/-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CHO 2COMc 2-COOMe 3-F 3·α 3-CF3 3-OCF3 3-CN 3·Ν02 3-OMe 3-Me 3-Et 3-i-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-f-Bu 3<CH2CN 3-CH2F 3-COMe 3-COOMe 3-SiMej 3-GbCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4-CH2CF3 4-f-Bu 4-i-Bu 4-i-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4-CHCHC1 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-〇Me (請先閲讀背面之注意事項再填寫本頁) .裝— —訂 線! 本紙張又度適用中國國家標準(CNS ) /\4坭格(210 X 297公t ) A7 B7
五、發明説明(44) I 4-COMe 4-C00Me 4-C0NHMe 4-S〇2NHMe 4-SiMc3 4-SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-0Et 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 2-0Me 2-r-Bu 3-n-Pr 3-CHO 4-F 3-SCF2H R1 = F, R2 = F, P = 3-OEt, A = 0, Y 4-n-Bu =0, m = 1, n 4-CH=CH2 =1 且R10= 4-CH0 2-SMe 2-F 2·α 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Mc 2·ΕΙ 2-n-Pr 2-i-Pr 2-n-Bu 2-ι-Βα 2-x-Bu 2-CH2CN 2-CH2F 2-CH0 2-C0Me 2-COOMe 3-F 3-C! 3-CF3 3-OCF3 3-CN 3-N〇2 3-0Me 3-Mc 3-Et 3-/-Pr 3,n-Bu 3-/-Bu 3-j-Bu 3-/-Bu 3-CH2CN 3-CH2F 3-C0Me 3-COOMe 3-SiMe3 3-C=CH 3-SF5 3-OCH2CF3 3-CH=CH2 4-C! 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-r-Bu 4-/-Bu 4-x-Bu 4-rt-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4-CH=CHCl -k:h2cn 4-CN 4-N02 4-S02Me 4-0Me 4-C0Me 4-COOMc 4-CONHMc 4-S〇2NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H ' 3-0Et 3-SMe 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-/-Bu 3-λ-Ργ 3-SCF2H 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CH0 2-SMc (請先閱讀背面之注意事項再填寫本頁) .裝· 訂 經濟部中夬標準局員工消贽合作社印製
R1 = F,] R2 = Η, P = H, A = 0. Y = 0. m = 1, n = 1 且 R19= 2-F 2·α 2-Br 2-CF3 2-OCF3 2-CN 2·Ν〇2 2-Me 2-Et 2-n-Pr 2-i-Pr 2-/i-Bu 2-/-Bu 2-j-Bu 2-CH2CN 2-CH2F 2-CH0 2-C0Me 2-COOMe 3-F 3-C1 3-CF3 3-OCF3 3-CN 3-N〇2 3-0Mc 3-Me 3-Et 3-/-Pr 3-n-Bu 3-t-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-C0Me 3-COOMe 3-SiMc3 3-CsCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4.OCH2CF3 4-CH2CF3 4-/-Bu 4-/-Bu 4-x-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH2F 4-CsCH 4-CH=CHCl 4.CH2CN 4-CN 4-NO2 4-S02Me 4-0Me 4-COMe 4-COOMc 4-C0NHMe 4-S02NHMe 4-S1MC3 4-SF5 2-0Et 2-SEt 2-OCF2H 2-SCF2H 3-0Et 3-SMe 3-SEt 3-OCF2H 4-0Et 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-0Me 2-f-Bu 3-λ-Ργ 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CH0 2-SMe 3-SCF2H 本紙張尺度適用中國國家標準(CNS )w\4規格(210XW7公釐) -47 - A7
五、發明説明/ 45 ) 經濟部中央搮準局員工消費合作社印製 R1 =C1, R2 = H, P = H, A = 0. Y : =0, m = 1, n = 1 且 Rle= 1· 1 1 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 2-Me 2-Et 2-/i-Pr 2-Z-Pr 2-n-Bu 2-/-Bu 2-5-Bu 1 | 2-CH2CN 2-CH2F 2-CH0 2-COMc 2-C00Me 3-F 3-Ci 請 先 閱 1 1 3-CF3 3.OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 1 3-i-Pr 3-n-Bu 3h-Bu 3-j-Bu 3-i-Bu 3-CH2CN 3-CH2F 讀 背 1 3-COMc 3-COOMc 3-SiMe3 3-CaCH 3.SF5 3-OCH2CF3 3-CH=CH2 1 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CF3 4-f-Bu * 1 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4»CH2F 事 項 1 Λ . 4-CsCH 4-CH=CHCl 4-CH2CN 4-CN 4-N02 4-S02Me 4-OMe 再 填 寫 本 頁 | 4-COMc 4-COOMe 4-CONHMe 4-S02NHMe 4-SiMe3 4-SF5 2-OEt 裝 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3.〇CF2H 1 4-OEt 4-SMe 4-SEt 4-OCF2H ' 4-SCF2H 2-OMe 2-i-Bu N._«· 1 3-n-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CHO 2-SMe 1 I 3-SCF2H 1 1 Rl =F, R2 = C1, Ρ» Hr A = Ο, Y = Ot m - 1, n = 】且1?10= I 訂 I 2-F 2-Cl 2-Br 2-CF3 2-OCF3 2-CN 2-NOo 2-Me 2-Et 2-rtrPr 2-/-Pr 2-n-Bu 2-i-Bu 2-j-Bu 1 I 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-C00Me 3-F 3-CI 1 | 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Et 1 3-/-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 1 3-COMe 3-COOMc 3-SiMc3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 1 線 I 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-i-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-Et 4-Me 4-CH2F 1 I 4-CsCH 4-CH=CHCI 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-〇Me 1 I 4-COMe 4-COOMc 4-CONHMe 4-S02NHMe 4-SiMe3 4.SF5 2-OEt 1 1 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMe 3-SEt 3-OCF2H 1 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMe 2-/-Bu 1 3-n-Pr 3-CHO 4-F 4-n-Bu 4<H=CH2 4-CHO 2-SMc 1 3-SCF2H 1 | R1 =C1, R2 = CI. P = H, A = 0, Y = 〇, m = I, π =] 且 R19= 1 1 2-F 2-a 2-Br 2-CF3 2-OCF3 2-CN 2-N〇2 1 I 2-Mc 2-Et 2-/i-Pr 2-/-Pr 2-n-Bu 2-z-Bu 2-j-Bu 1 | 2-CH2CN 2-CH2F 2-CHO 2-COMe 2-COOMc 3-F 3-Ci I 3-CF3 3.OCF3 3-CN 3-N〇2 3-OMe 3-Me 3-Ei 1 1 本紙悵尺度適用中國國家標隼(CNS ) Λ4规格(21〇X297公釐) 五、發明説明/ 46 A7 B7 3-i-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-r-Bu 3-CH2CN 3-CH2F 3-COMc 3-COOMe 3-SiMc3 3-OCH 3-SF5 3-OCH2CF3 3-CH=CH2 4-CI 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4.CH2CF3 4-f-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-Et 4-Me 4-CH2F 4*〇bCH 4-CHCHC1 4-CH2CN 4CN 4-N〇2 4-S〇2Me 4-OMe 4-COMe 4-COOMe 4-CONHMc 4-S02NHMe 4-SiMe3 4-SF5 2-OEt 2-SEt 2-OCF2H 2-SCF2H 3-OEt 3-SMc 3-SEt 3-OCF2H 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 2-OMc 2-f-Bu 3-n-Pr 3-CHO 4-F 4-n-Bu 4-CH=CH2 4-CHO 2-SMe 3-SCF2H .表2 »
C
(請先閲讀背面之注意事項再填寫本頁) 裝. 訂 經濟部中央標嗥局員工消费合作社印製 RLf, R2 = F, P = F,且Rie= 3-F 3-C1 3-Mc 3-Et 3-CH2CN 3-CH2F 3- OCH2CF3 3-CH=CH 4- CH2CF3 4-r-Bu 4-CH2F 4- 〇Me 3-OEt 屯 〇cf2h 5- 〇Me 6- OCF3 3-〇Me 4*SMe 4-Mc 4-S〇2Me 4-SF5 4- SEt 5- N〇2 6- CF3 6-CH2F 4-SiMe-i 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-5-Bu 3-CHO 3-COMe 3-COOMe 3-SiMe3 3-CsCH 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-CH=CH2 4-CsCH 4-CH=CHCl 4^CH2CN 4-CN 4-CHO 4-COMe 4-COOMc 4-CONHMc 4-S02NHMe 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SCF2H 5-C1 5-Br 5-CF3 5-OCF3 5-Me 5-r-Bu 5-SF5 5-CH2F 6-CI 6-CN 6-N02 6-OMe 6-Mc 6-r-Bu 3-/-Bu 3-SF5 4-OCH2CF3 4-Et 4-N〇2 5-CN 6-Br 6-SF5 本紙張尺度適财賴家縣(CNS) A4C格(21()x297公资) -49 B7 五、發明説明(47) ίR1 =F,R2 = F, P = C1 且 R19= 經濟部中央樣準局員工消費合作社印製
3-F 3-CI 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Me 3-Et 3-/j-Pr 3-i-Pr 3-n-Bu 3-Z-Bu 3-j-Bu 3-CH2CN 3-CH2F 3«CH〇 3-COMc 3-C00Me 3-SiMe3 3-CsCH 3-OCH2CF3 3-CH=CH2 4-F 4C1 4-Br 4-CF3 4-OCF3 4-CH2CF3 4-i-Bu 4-π-Βα 4-/-Bu 4-«r-Bu 4-n-Pr 4-f-Pr 4-Mc 4.CH2F 4-CH=CH2 4-OCH 4^H=CHa 4«CH2CN 4-CN 4-S〇2Mc 4-OMe 4-CHO 4-COMc 4-COOMe 4-CONHMc 4-S02NHMe 4-SF5 3-OEt 3-SMe 3-S^t s-ocf2h 3-SCF2H 4-OEi 4-SEt 4-OCF2H 4-SCF2H 5-c\ 5-Br 5-CF3 5.OCF3 5-N02 5-OMe 5-Mc 5-f-Bu 5-SF5 5-CH2F 6-C1 6-CF3 6-OCF3 6-CN 6-NO2 6-OMc 6-Me 6-r-Bu 6-CH2F 3-OMe 3-/-Bu 3-SF5 4-OCH2CF3 4-Et 4-N〇2 4-SiMe3 4-SMe 5-CN 6-Br 6-SF5 R1 =F,R2 :F,P = 〇Me 且 3-F 3-Cl 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Me 3-Et 3-rt-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMc 3-SiMe3 3-CsCH 3-OCH2CF3 3-CH=CH2 4-F 4-CJ 4-Br 4*CF3 4.OCF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-Me 4-CH2F 4-CH=CH2 4-feCH 4-CH=CHCl 4^H2CN 4-CN 4-S02Me 4-〇Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SF5 3-〇Et 3-SMc 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4*OCF2H 4-SCF2H 5-Ci 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Me 5-r-Bu 5-SF5 5-CH2F 6-C1 6-CF3 6-OCF3 6-CN 6-NO2 6-OMe 6-Me 6-i-Bu 6-CH2F 3-〇Me 3-r-Bu 3-SF5 4.〇CH2CF3 4-Et 4-N〇2 4-SiMe3 4-SMc 5-CN 6-Br 6-SF5 R1 = F. R2 = F· p = 〇Et 且Ri9= 3-F 3-Cl 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Mc 3-Et 3-λ-Ργ 3-/-Pr 3-«-Bu 3-i-Bu 3-j-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMe 3-SiMc3 3-OCH 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4.OCF3 . 4-CH2CF3 4-nBu 4-n-Bu 4-i-Bu 4-j-Bu 4-/i-Pr 4-/-Pr 4-Me 4-CH2F 4-CH=CH2 4-CaCH 4-CH=CHCl 4-CH2CN 4-CN (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國园家標準(CNS ) Λ4规格(2Γ0Χ297公釐) -50 - A7 B7 五、發明说明·( 48 ) 經濟部中央梯隼扃員工消費合作社印裝 4-S〇2Me 4-OMc 4-CHO 4-COMc 4-COOMe 4-C〇NHMe 4-S〇2NHMe 4-SF5 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-〇Et 4-SEt 4-OCF2H 4-SCF2H 5-Cl 5·Βγ 5-CF3 5-OCF3 5-N〇2 5-OMc 5-Me 5-f-Bu 5-SF5 5-CH2F 6-C1 6-CF3 6^0CF3 6-CN 6-N〇2 6-OMc 6-Me 6-r-Bu 6-CH2F 3-OMe 3-/-Bu 3-SF5 4-OCH2CF3 4-Et 4-NO2 4-SiMe3 4-SMc 5-CN 6-Br 6-SF5 R1 =F, R2 = F, P = CH3 且Rle= 3-F 3-a 3-Br 3-CF3 3-OCF3 3CN 3-N〇2 3-Me 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-CH2CN 3-CH2F 3CH0 3-COMc 3-COOMe 3-SiMc3 3-CsCH 3-OCH2CF3 3-CH=CH2 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-CH2CF3 4-/,Bu 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-t-Pr 4-Me 4-CH2F 4-CH=CH2 4-OCH 4-CH=CHCl 4-CH2CN 4-CN 4-S02Me 4-OMe 4-CHO 4-COMc 4-COOMe 4-CONHMc 4-S02NHMe 4-SF5 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4-OCF2H 4-SCF2H 5-Cl 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Me 5-r-Bu 5-SF5 5-CH2F 6-Cl 6-CF3 6-OCF3 6-CN 6-NO2 6-OMe 6-Me 6-/-Bu 6-CH2F 3-OMe 3-/-Bu 3-SF5 4-OCH2CF3 4-El 4-N02 4-SiMe3 4-SMe 5-CN 6-Br 6-SF5 R1 =F, R2 =F. P = CH3 且 R19= 3-F 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Me 3-Et 3-λ-Ργ 3-/-Pr 3-n-Bu 3-i-Bu 3-s-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMe 3-SiMc3 3-OCH 3-OCH2CF3 3-CH^CH2 4-F 4-C1 4-Br 4.CF3 4-OCF3 4-CH2CF3 4*r-Bu 4-/i-Bu 4-i-Bu 4-n-Pr 4-i-Pr 4-Me 4-CH2F 4-CH=CH2 4-ChCH 4-CH=CHCl 4-CH2cn 4-CN 4-S〇2Me 4-〇Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SFj 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4-〇CF2H 4-SCF2H 5-Cl 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Me 5-i-Bu 5-SF5 5-CH2F 6-Cl o-Cr3 6-OCF3 6-CN 6-NO2 6-OMc 6-Me 6-ί-Βυ 6-CH2F 4-SiMe3 3-〇Me 4~SMe 3-i-Bu 5-CN 3-SF5 6-Br 4-OCH2CF3 6-SF5 4-Et 4-N〇2 --------1¾---^----1ί--l·----0 (請先閱誚背面之注意事項再填寫本頁) 本紙浪尺度賴巾賴家轉(CNS ) M規格(2齡297公缓) -51 A7 B7 五、發明説明(49 ) 經濟部中央標準局負工消費合作社印製 R1 = F. R2 = C1, P = F &r19= 3-F 3-CI 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-Me 3-Et 3-λ-Ργ 3-/-Pr 3-n-Bu 3-/-Bu 3-i-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMe 3-SiMe3 3-CsCH 3.〇CH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4*OCF3 4-CH2CF3 4-f-Bu 4-n-Bu 4-/-Bu 4-^-Bu 4-n-Pr 4-/-Pr 4-Me 4-CH2F 4-CH=CH2 4-CsCH 4-CH=CHCl 4-CH2CN 4-CN 4-S02Me 4-OMe 4-CHO 4-COMe 4-COOMe 4C0NHMe 4-S02NHMe 4-SF5 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-〇Et 4-SEt 4-OCF2H 4-SCF2H 5-C1 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Me 5-r-Bu 5-SF5 5-CH2F 6-C1 6-CF3 6-OCF3 6-CN 6-NO2 6-OMe 6-Me 6-r-Bu 6-CH2F 3-OMe 3-f-Bu 3-SF5 4-OCH2CF3 4-Et 4-N〇2 4-SiMe3 4-SMe 5-CN 6-Br 6*SF5 R1 = F, R2 = C1, P = C1 且 R19= 3-F 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Me 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-5-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMe 3-SiMe3 3-C^CH 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-CH2CF3 4-nBu 4-n-Bu 4-z-Bu 4-j-Bu 4-λ-Ργ 4-i-Pr 4-Me 4-CH2F 4-CH=CH2 4-CsCH 4-CH=CHCl 4-CH2CN 4-CN 4-S02Mc 4-OMe 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S02NHMe 4-SF5 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4-OCF2H 4-SCF2H 5-C1 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Mc 5-/-Bu 5-SF5 5-CH2F 6-C1 6-CF3 6-OCF3 6-CN 6-NO2 6-OMe 6-Me 6-r-Bu 6-CH2F 3-OMe 3-r-Bu 3-SF5 4-OCH2CF3 4-Et 4-N〇2 4-SiMe3 4-SMe 5-CN 6-Br 6-SF5 --------丨裝----——訂—一—^丨線 (請先閱讀背面之注意事項再填寫本頁) 本紙浪尺度適用中國國家標隼(CNS ) Λ4現格(210X297公釐) A7 B7 五、發明説明(50 ) * 表3
經濟部中央標準局員工消費合作社印製 R1 =F, R2 = F. P = F 且Rle= 4-F 4-a 4-Br 4-CFj 4-OCF3 4-〇CH2CF3 4>CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-λ-Ργ 4^i-Pr 4-Et 4-Mc 4-CH=CH2 4-OCH 4-CH=CHCl 4*CH2CN 4-CN 4-N〇2 4-S〇2Me 4-CHO 4-COMe 4-COOMe 4-CONHMc ‘S02NHMe 4-SiMc3 4-SFj 5-F 5-C1 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5-CH2CF3 5-n-Bu 5-/-Bu 5-i-Bu 5-n-Pr 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-OCH 5-CH=CHCI 5^CH2CN 5-CN 5-N02 5-S〇2Me 5CHO 5-COMe 5-COOMe 5-CONHMe 5-S02NHMe 5-SiMe3 5-SF5 4-f-Bu 4-CH2F 4-〇Me 5-/-Bu 4-CH2F 5-OMe RUf, R2 = F. P = C1 且Rle= 4-F 4-C) 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4-CsCH 4-CH=CHCl 4>CH2CN 4-CN 4-N〇2 4-S〇2Me 4-CHO 4-COMe 4-C〇〇Me 4-CONHMe 4-S〇2NHMc 4-SiMe3 4-SF5 5-F 5-a 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5-CH2CF3 5-n-Bu 5-i-Bu 5-j-Bu 5-n-Pr 5-z-Pr 5-Et 5-Me 5-CH=CH2 5-CsCH 5-CH=CHCl 5-CH2CN 5-CN 5-N〇2 5-S02Me 5-CHO 5-COMe 5-COOMc 5-CONHMc 5-S02NHMe 5-SiMc3 5-SF5 4-r-Bu 4-CH2F 4-OMe 5-i-Bu 4-CH2F 5-OMe R1 = Cl. R2 = Cl, P = F 且 fiI9= 4-F 4-CI 4-Br 4<P3 4-OCF3 4.〇CH2CF3 4.CH2CF3 4-n-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4-CaCH 4-CH=CHCl 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SiMe3 4-SF5 5-F 5-CI 5-Br 5-CFy 5-OCF3 5-OCH2CF3 5-CH2CF3 ---------¾衣-------IT--1--1 0 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家橾準(CNS ) Λ4規格(210X 297公釐) 五、發明説明(51 ) A7 B7 經濟部中央標準局員工消费合作社印製 5-Λ-Βυ 5-/-Bu 5-j-Bu 5-n-Pr 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-CsCH 5-CH=CHCl 5-CH2CN 5CN 5-N02 5-S02Mc 5-CHO 5-COMe 5-COOMc 5-CONHMe 5-S02NHMe 5-SiMe3 5-SF5 4-f-Bu 4-CH2F 4-OMe 5-r-Bu 4-CH2F 5-OMe rUci, r2 = ci. ρ = α 且R10= 3-F 3·α 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-Me 3-Et 3-n-Pr 3w-Pr 3-/i-Bu 3-i-Bu 3-j-Bu 3-CH2CN 3-CH2F 3-CHO 3-COMe 3-COOMe 3-SiMe3 3-ChCH 3-OCH2CF3 3-CH=CH2 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-CH2CF3 4-r-Bu 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Me 4-CH2F 4-CH=CH2 4-CsCH 4-CH=CHCl 4»CH2CN 4CN 4-S〇2Mc 4-OMc 4-CHO 4-COMc 4-COOMc 4C0NHMe 4-S〇2NHMe 4-SF5 3-OEt 3-SMc 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4-OCF2H 4-SCF2H 5-C1 5-Br 5«CF3 5-OCF3 5-N〇2 5-OMc 5-Me 5-r-Bu 5-SF5 5*CH2F 6-Ci 6-CF3 6-OCF3 6-CN 6-N〇2 6-OMc 6-Me 6-r-Bu 6-CH2F 3-OMc 3-r-Bu 3.SF5 4-OCH2CF3 4-Et 4-N〇2 4-SiMe3 4-SMe 5-CN 6-Br 6-SF5 R1 = Cl, R2 = C1, P = F 且Rie= 3-F 3-CI 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Me 3-Ei 3-n-Pr 3-i-Pr 3-/i-Bu 3-i-Bu 3-j-Bu 3-CH2CN 3*CH2F 3-CHO 3-COMe 3-COOMe 3-SiMe3 3-CsCH 3-OCH2CF3 3-CH=CH2 4-F 4CI 4-Br 4.CF3 4.OCF3 4-CH2CF3 4-f-Bu 4-t-Bu 4~s-Bu 4-n.Pr 4-/-Pr 4-Me 4-CH2F ‘ch=ch2 4-CaCH 4-CH=CHCl 4-CH2CN 4-CN 4-S〇2Me 4-〇Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SF5 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 4-OEt 4-SEt 4.〇CF2H 4-SCF2H 5-C1 5-Br 5-CF3 5-OCF3 5-N〇2 5-OMe 5-Me 5-r-Bu 5-SF5 5-CH2F 6-CI 6-CF3 6-OCF3 6-CN 6-N02 6-OMc 6-Mc 6-r-Bu 6-CH2F 3-OMc 3-/-Bu 3-SF5 4-OCH2CF3 4-Et 4-N02 4-SiMej 4-SMe 5-CN 6-Br 6-SF5 ----I:--- I裝------訂丨丨—丨丨丨線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標隼(CNS ) Λ4坭格(210 X 297公潑) A7 B7 五、發明説明(52) I = F, R: = F,P = OMe 且 R1 β= 經濟部中央標準局黃工消費合作杜印衆 4-F 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4.CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-/1-Pr 4-/-ΡΓ 4*Et 4-Mc 4-CH=CH2 4-CaCH 4-CH=CHCl 4-CH2CN 4-CN 4-N02 4-S〇2Me 4-CHO 4-COMe 4-COOMc 4-CONHMe 4-S02NHMe 4-SiMe3 4-SF5 5-F 5-CI 5-Br 5-CF3 5-OCF3 5*OCH2CF3 5-CH2CF3 5-n-Bu 5-/-Bu 5-j-Bu 5-u-Pr 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-OCH 5-CH=CHQ 5-CH2CN 5-CN S-N02 5-S02Me 5-CHO 5-COMe 5-COOMc 5-CONHMc 5-S〇2NHMc S-SiMe3 5-SF5 4-i-Bu 4-CH2f 4-OMe 5-i-Bu 4-CH2f 5-OMc rUf, R2 = F, P = OEt 且Rie= 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-GbCH 4-CH=CHa 4-CH2CN 4^N 4-N〇2 4-S〇2Mc 4-CHO 4-COMc 4-COOMe 4-CONHMc 4-S〇2NHMc 4-SiMe3 4-SF5 5-F 5-CI 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5.CH2CF3 5-n-Bu 5-/-Bu 5-j-Bu 5-n-Pr 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-CsCH 5-CH=CHCl 5-CH2CN 5-CN 5-N〇2 5-S02Mc 5-CHO 5-COMe 5-COOMe 5-CONHMc 5-S02NHMe 5-SiMe3 5-SF5 4-f-Bu 4-CH2F 4-OMe 5-r-Bu 4-CH2F SOMc R1 = F. R2 = F, P = CH3 且Rie= 4-F 4-C1 4-Br 4-CF3 4«〇CF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-/-Bu 4-j-Bu 4-/t-Pr 4-/-Pr 4-Et 4-Me 4-CH=CH2 4-CaCH 4-CH=CHCl 4^:H2CN 4-CN 4-N〇2 4-S〇2Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4-SiMe3 4-SF5 5-F 5-CI 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5-CH2CF3 5-n-Bu 5-t-Bu 5-5-Bu 5-n-Pr 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-CeCH 5-CH=CHG 5-CH2CN 5-CN 5-N〇2 5-S02Me 5-CHO 5-COMe 5-COOMe 5-CONHMe 5-S02NHMc 5-SiMe3 5-SF5 4-r-Ba 4-CH2F 4-OMe 5-f-Bu 4-CH2F 5-OMe rUf, R2 = Ci, P = ClandR^ = 4-F 4·α 4-Br 4-CF3 4-OCF3 ‘OCH2CF3 4.CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-/i-Pr 4-/-Pr 4-Et 4-Mc . 本 CH=CH2 4-OCH 4^CH=CHa 4*CH2CN 4-CN 4-N02 4.S〇2Me (請先閱讀背面之注意事項再填寫本頁) I 11^-----------一—裝-------訂.— 本紙张尺度適用中國國家標隼(CNS ) Λ4現格(210X 297公釐) -55 - 308595 at B7 五、發明説明(53 ) 4-CHO 4-COMc 4-COOMc 4-CONHMe 4-S〇2NHMe 4-SiMe3 4-SF5 5-F 5-C1 5-Br 5-CF3 5-〇CF3 5-OCH2CF3 5-CH2CF3 5-«-Βυ 5-/-Bu 5-j-Bu 5-λ-Ργ 5-i-Pr 5-Et 5-Me 5-CH=CH2 5-OCH 5-CH=CHCl 5-CH2CN 5-CN 5-N〇2 5-S〇2Me 5-CHO 5-COMe 5-COOMe 5-CONHMe 5-S〇2NHMe 5-SiMe3 5.SF5 4-r-Bu 4-CH2F 4-OMe 5-nBu 4»CH2F 5-OMe
Rl=F, R2 = C1, P = F 且Ri0= 4-F 4-C1 4-Br 4-CF3 4-OCF3 ‘och2cf3 4-CH2CF3 4-n-Bu 4-<-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4.〇CH 4-CH=CHa 4-CH2CN 4-CN ‘N〇2 4-S〇2Me 4-CHO 4-COMe 4-COOMc 4-CONHMe 4-S〇2NHMc 4-SiMe3 4.SF5 5-F 5-C1 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5-CH2CF3 5-n-Bu 5-i-Bu 5-s-Bu 5-n-Pr 5-i-Pr 5-Et 5-Mc 5-CH=CH2 5-CsCH 5-CH=CHCi 5-CH2CN 5-CN 5-N〇2 5-S02Mc 5-CHO 5-COMe 5-COOMe 5-CONHMe 5-S〇2NHMe 5-SiMe3 5-SF5 4-;-Bu 4-CH2F 4-OMc 5-f-Bu 4-CH2F 5-OMe R】=α· R2 = C1,P = C1 且R19= 經濟部中央標隼局員工消費合作社印製 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4^H2CF3 4-n-Bu 4-i-Bu 4十Bu 4-/i-Pr 4-i-Pr 4-Et 4-Me 4.CH=CH2 4-CaCH 4-CH=CHCI 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-CHO 4-COMe 4-COOMe 4-CONHMe 4-S〇2NHMe 4*SiMe3 4-SF5 5-F 5·α 5-Br 5-CF3 5-OCF3 5-OCH2CF3 5-CH2CF3 5-n-Bu 5-i-Bu 5-j-Bu 5-n-Pr 5-/-Pr 5-Et 5-Me 5-CH=CH2 5-CaCH 5-CH=CHCl 5-CH2CN 5-CN 5-N〇2 5-S〇2Me 5-CHO 5-COMe 5-COOMe 5-CONHMe 5-S02NHMe 5-SiMe3 5-SF5 4-r-Bu 4-CH2F 4-OMe 5-f-Bu 4-CH2F 5-OMe -------—批衣-------ΐτ!·----# (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) B7 五、發明説明(54)
經濟部中央標準局員工消費合作社印製 R1 =F. R2 = F, P = H, A =0, Y^Ot z =O· n = 1 且R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-OMe 2-Me 2-Et 2-λ-Ργ 2-i-Pr 2-/i-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CH0 2-COMe 3-Cl 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-λ-Ργ 3-/-Pr 3-/i-Bu 3-i-Bu 3-j-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-Cl-Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4-n-Bu 4-i-Bu 4-5-Bu 4-n-Pr 4-i-Pr 4-Et 4-CH=CH2 4-CsCH 4-CH=CHCl 4-CsC-CH2C1 4-CH2〇Me 4-CH2SMe 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-C0Me 4-S02NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 3-OEt 3-SMc 3-SEi 3-OCF2H 3-SCF2H 3-OPh 4-〇Ee 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-0Ph 2-N〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 4-r-Bu 4-CH2F 4-C-C5H9 4-CsC-SiMe3 4.CsC-CH(OEt)2 2-COPh 4-COPh 2-CN 2-/-Bu 2-COOMe 3-0Mc 3*r-Bu 3-(4-F-Ph) 3-CH2SMe 4-CH2CF3 4-Me 4-CH2CN 4-COOMe 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Mc)2 3-COPh Rl = F, r2 = Cl,P = H, A =0, Y = 0. z =0, n = 1 且R3= H 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-OMe 2-Me 2-Et 2-/i-Pr 2-Z-Pr 2-n-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-C0Me 3-Cl 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-n-Pr 3-(-Pr 3-n-Bu 3-i-Bu 3'i-Bu 3-CH2F 3-CHO 3-C0Me 3-COOMe 3-Ph 3-C4-Ci-Ph) (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Λ4規洛(210X 297公釐) 57 - 五、發明説明(55 ) { Μ Β7 經 濟 部 中 夬 標 準 Μ 員 X 消 f 合 作 社 印製 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 1 I 4-F 4-C! 4-Br 4-CF3 4.OCF3 4-OCH2CF3 1 I 4-n-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et ^—V 1 I 4.〇H=CH2 4-OCH 4-CH=CHCl 4.〇C-CH2CI 4-CH〇OMe — 4-CH2SMe 請 先 1 I 4-N02 4-S〇2Mc 4-OMe 4-CHO 4-COMc 閱 讀 背 1 4-S〇2NHMc 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 1 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 面 1 f 3-OEt 3-SWe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 意_ I 1 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 事 項 1 2-N〇2 2-j-Bu 3-F 3-Mc 3«CH2CN 3-SiMc3 再 填 寫 本 頁 1 4-r-Bu 4-CH2f 4-C-C5H9 4-〇sC-SiMc3 4-〇sC-CH(OEt)2 2-COPh 裝 4-COPh 2-CN 2-/-Bu 2-COOMc 3-OMc 3-f-Bu 1 3_(4-F-Ph) 3-CH2SMe 4»CH2CF3 4-Mc 4*CH2CN 4-COOMc v_^ 1 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Mc)2 3-COPh 1 | R1 =C1, R2 = C1, P = H. A=0. Y = 〇f Z = 0. n = l 且R3= 1 1 H 2-F 2-a 2-Br 2-CF3 2-OCF3 1 2-OMe 2-Mc 2-Et 2'Π-Ργ 2-i-Pr 2-/i*Bu 訂 2-/-Bu 2-CH2CN .2-CH2F 2-Ph 2-CHO 2-COMe 1 I 3-CI 3-Br 3^F3 3-OCF3 3-CN 3-N〇2 1 ί 3-E【 3-n-Pr 3-i-Pr 3-/j-Bu 3-i-Bu 3-i-Ba 3-CH2F 3-CHO 3-COMc 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4.OCF3 4-OCH2CF3 線 4-n-Bu 4-/-Bu 4-5-Bu 4-n-Pr 4-/-Pr 4-Et 4-CH=CH2 4-CsCH 4-CH=CHCI 4-OC-CH2CI 4-CH2〇Me 4-CH2SMc 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-S〇2NHMe 4-N(Me>2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 4-r-Bu 4-CH2F 4-c-C5H9 4-OC-SiMc3 4.C3C-CH(0Et)2 2-COPh 4-COPh 2-CN 2*i-Bu 2-COOMe 3-OMc 3-r-Bu 3-(4-F-Ph) 3-CH2SMe 4-CH2CF3 4-Me ‘ch2cn 4-COOMe 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Mc)2 3-COPh 本紙张尺度適用中國國家標率(CNS ) Α4規格(210X297公瘦) A7 B7 五、發明説明(56 ) « 經濟部中央標隼局員工消費合作社印製 R1 = Cl, R2 = Η, P = Η. A = 0. Y = 〇, Ζ = Ο, η = 1 且R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-0Me 2-Mc 2-Ee 2-n-Pr 2-i-Pr 2-卜 Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-Et 3-λ-Ργ 3-/-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-CH2F 3-CHO 3-COMe 3-C00Me 3-Ph 3-(4-Cl-Ph) 3-CsCH 3-C.C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-n-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-CH=CH2 4-CsCH 4-CH=CHQ 4-C=C-CH2CI 4-CH2〇Me 4-CH2SMe 4-CN 4-N〇2 4.S〇2Me 4-OMc umo 4-COMe 4-S〇2NHMc 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 4-OEt 4-SMe 4-SEt 冬 ocf2h 4-SCF2H 4-OPh 2-N〇2 2-5-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 4-r-Bu 4-CH2F 4-C-C5H9 4-CaC-SiMc3 4-OC-CH(OEt)2 2-C0Ph 4-C0Ph 2-CN 2-Z-Bu 2-COOMc 3-OMe 3-f-Bu 3-(4-F-Ph) 3-CH2SMc 4-CH2CF3 4-Mc 4-CH2CN 4-COOMe 4-CONHMc 2-SPh 3-SPh 4-SPh 3-N(Me)2 3-C0Ph R1 =F. R2 = F, P = H. A =0, Y = 0, z =S, n = I 且R3= H 2-F 2-C1 2-Br 2«CF3 2-OCF3 2-OMe 2-Me 2-Et 2-/j-Pr 2-Z-Pr 2-n-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2«CH0 2-COMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-λ-Ργ 3-i-Pr 3-Λ-Βυ 3-i-Bu 3-j-Bu 3-CH2F 3-CHO 3-C0Me 3-COOMc 3-Ph 3-(4-Cl-Ph) 3-CsCH 3-c-C^H^ 3.SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-CH=CH2 4-CsCH 4-CH=CHCl 4.C3sCCH^C1 4-CH2〇Mc 4-CH2SMe 4-CN 4-N〇2 4-S〇2Mc 4-OMe 4-CHO 4-COMe 4-S〇2NHMe 4-N(Mc>2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 2-0Et 2-SMe 2-SEt 2-OCF2H 2-SCF-^H *0 2-0Ph --------I 裝------訂---^------線 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) A7 B7 •3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 1 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh ! 1 2-N〇2 2-i-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 1 4-r-Bu 4-CH2F 4-c-C^H^ 4-CsC-S iMe ^ 4-CaC-CH(OEt)2 2-COPh 請 先 1 4-COPh 2-CN 2-i-Bu 2‘C00Me 3-0Me 3-/-Bu 閲 1 3-(4-F-Ph) 3-CH2SMe 4-CH2CF3 4-Me ‘ch2cn 4-C00Me 背 I 1 4-CONHMe 2-SPh *3-SPh 4-SPh 3-N(Me)2 3-COPh 之 注 1 1 rUf. r2 = =F. P = H, A =0, Y = S· z s 〇. π = 1 且R3= 意 事 I 1 H 2-F 2-a 2-Br 2-CF3 2-OCF3 項 再 1 2-OMe 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 填 寫 本 I I 2-/-Bu 2"CH2CN 2-CH2P 2-Ph 2-CH0 2^C0Me 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 1 I 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 1 | 3-CH2F 3CH0 3-C0Me 3-C00Me 3-Ph 3^4-Cl-Ph) 1 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-C1 4-Br 4-CF3 4*OCF3 4-〇CH2CF3 1 4-Λ-Βυ 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 1 4-CH=CH2 4-CsCH 4-CH=CHCl 4.CsC-CH2C1 4-CH2〇Me 4-CH2SMc 1 1 4-CN 4-N〇2 4-S02Me 4-0Me 4*CH〇 4-COMc 1 1 4-S〇2NHMc 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph I 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 1 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 1 4-〇Et 4-SMc 4-SEt 4<OCF2H 4-SCF2H 4-0Ph 線 2-N〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 4-f-Bu 4-CH2F 4^:-C5H9 4-CsC-SiMe3 4-〇C-CH(OEt)2 2-C0Ph 4-COPh 2-CN 2-/-Bu 2-COOMc 3-〇Mc 3-i-Bu 3-(4-F-Ph) 3-CH2SMe 4^H2CF3 4-Me 4-CH2CN 4-COOMc 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Me)2 3-C0Ph R1 =F. R2 = F,p = H, a =S, Y *0, Z :〇· 且R3 = H 2-OMe 2-F 2-Mc 2-a 2-Et 2-Br 2-n-Pr 2*CF3 2-i-Pr 2-OCF3 2-zi-Bu 2-bBu 2.CH2CN 2-CH2F 2-Ph 2-CH0 2-C0Me 3*CI λ r?* 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-CH2F 3-CHO 3-C0Me 3-C00Me 3-Ph 3-(4-CI-Ph) 五、發明説明(57 ) 經 濟 部 中 k 樣 隼 局 員 工 消 費 合 作 社 印 % 本紙張尺度適用中國國家標隼(CNS ) A4現格(210 x297公缝) 經濟部中央標準局員工消費合作社印策 308595 at B7 五、發明説明(58) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4^:I 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4~n-Pr 4-/-Pr 4-Et 4-CH=CH2 4-CsCH *4-CH=CHCI 4-C*C-CH2Cl 4-CH2〇Me 4-CH2SMC 4-CN 4-N〇2 4-S02Me ^OMe 4-CHO 4-COMe 4-S〇2N^^c 4~N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 20Ph 3-OEt 3-SMe 3-SEi 3-〇CF2H 3-SCF2H 3-OPh 4-OEt 4-SMe 4-SEt 4-OCF2h 4-SCF2H 4-OPh 2-N〇2 2-j-Bu 3-F 3-Me 3«CH2CN 3-SiMe3 4-/-Bu 4-CH2p 4-c-C5H9 4-CaC-SiMe3 4«CaC"CH(OEt)2 2-COPh 4-COPh 2-CN 2-i-Bu 2-C〇〇Me 3«0Me 3-nBu 3;(4-F-Ph) 3-CH2SMc 4-CH2CF3 4-Me 4»CH2CN 4.COOMe 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Me)2 3-COPh R1 =F. R2 = F, P = H, A =NH, Y = 0, Z = 〇,n s= 1 且 R3= H 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-OMe 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-w-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 3-CI 3-Br - 3-CF3 3.OCF3 3-CN 3-N〇2 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-<-Bu 3-j-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-C=CH 3-c-CjHp 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4·Βγ 4*CF3 4-OCF3 4-OCH2CF3 4-/i-Bu 4-i-Bu 4-j-Bu 4./i-Pr 4-i-Pr 4-El 4*CH:CH2 4-CH=CHCl 4.C=C-CH2C1 4-CH2°Me 4-CH2SMe 4-CN 4-N〇2 4-S〇2Me 4-OMc 4-CHO ‘COMe 4-S〇2NHMe 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2 - OPh 3-OEt 3-SMc 3-SEt 3-OCF2H 3-SCF2H 3-OPh 4-〇Et 4-SMc 4-SEt 4-OCF2H 4-scf2h 4-OPh 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2cn 3-SiMe3 4-;-Bu 4-CH2F 4-C-C5H9 4-C3C-SiMe3 4-CaC-CH(OEt)2 2-COPh 4-COPh 2-CN 2-/-Bu 2-COOMc 3-OMe 3-f-Bu 3-(4-F-Ph) 3-CH2SMe 4-CH2CF3 4-Me 4-CH2CN 4-COOMe 4-CONHMe 2-SPh 3-SPh 4-SPh 3-N(Me)2 3-COPb -------* -¾.---1---訂.--1----線、 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標率(CNS ) A4規格(21〇κ297公釐) 五、發明説明(59 A7 B7 R1 =F, R2 = F, P = H. A =0, Y = 0, z =0' n = 2 且R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-OMe 2-Me 2-£t 2-n-Pr 2-/-Pr 2-n-Bu 2-;-Bu 2-CH2CN 2-CH2F 2-Ph 2-CH0 2-C0Me 3-α 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-/i-Pr 3-(-Pr 3-/t-Bu 3-/-Bu 3*j-Bu 3-CH2F 3-CHO 3-C0Me 3-COOMc 3-Ph 3.(4-Cl-Ph) 3-CsCH 3-C-C5H9 3.SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 釦 〇cf3 4-OCH2CF3 4-n-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-CH=CH2 4-CaCH 4-CH=CHCI 4-OC-CH2Cl 4^H2〇Me 4-CH2SMe 4-CN 4-N〇2 4-S02Mc 4-0Mc 4-CH0 4-C0Me 4-S〇2NHMc 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 3-OEt 3-SMc 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-0Ph 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 4-r-Bu 4-CH2F 4-C^-SiMe3 4-ChC-CH(OE:)2 2-C0Ph 4-COPh 2-CN 2-i-Bu 2-C00Me 3-0Me 3-r-Bu 3-(4-F-Ph) 3-CH2SMc 4-CH2CF3 4-Me 4-CH2CN 4-COOMc 4-CONHMc 2-SPh 3-SPh 4-SPh 3-N(Mc)2 3-C0Ph R1 =F, R2 = F. P = Ht A =0, Y : 0, Z =0, n = 3 且 R3= H 2-F 2-C1 2-Br 2-CF3 2-0CF3 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CH0 2-C0Me 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-Et 3-n-Pr 3-/-Pr 3-π-Βα 3-(-Bu 3-j-Bu 3-CH2F 3-CHO 3-C0Mc 3-C00Me 3-Ph 3-(4-CI-Ph) 3-OsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-/i-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4W-Pr 4-Et 4-CH=CH2 4-C3CH 4-CH=CHCl 4-OC-CH2CI 4-CH2〇Me 4-CH2SMe 4-CN 4*N〇2 4-S〇2Mc 4-0Me 4-CH0 4-C0Me 4-S〇2NHMe 4-N(Me>2 4-SiMe3 4-SF< 4-CH2Ph 4-Ph 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 請 先 閱 讀 背 之 注 意 事 項 再 填 % 本 頁 本紙張尺度適用巾國國家料(CNS)M規格(210x 297公瘦 經濟部中央標隼局員工消費合作社印裝 A7 B7 五、發明説明(60 )
I 4-OEt 4-SMc 4-SEt 4-〇CF2H 4-SCF2H 4-〇Ph 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 4-r-Bu 4-CH2F 4.C-C5H9 4-〇BC-SiMe3 4-〇C-CH(OEt)2 2-C0Ph 4-COPh 2-CN 2-i-Bu 2-C00Me 3-OMe 3-r-Bu 3-(4-F-Ph) 3-CH2SMe 4-CH2CF3 4-Me 4-CH2CN ‘COOMe 4-CONHMc 2-SPh 3-SPh 4-SPh 3-N(Me)2 3-C0Ph R1 = F. R2 =F, P = 2-F, A = 0. Y = 〇, Z = 0, n = 1 且R3= 3-F 3-C1 3·Βγ 3-CF3 3-OCF3 3-OCH2CF3 3-j-Bu 3-i-Bu 3-/-Bu 3-/i-Pr 3-<-Pr 3-Me 3.CH=CH2 3-OCH 3-CH=CHCl 3«C»C*CH2C1 3-CH2°Me 3-CH2SMe 3-CN 3·Ν〇2 3-S〇2Me 3-OMc 3-CHO 3-COMc 3-N(Me)2 3-SiMe3 3-SF5 3-CH2Ph 3-Ph 3-(4-Cl.Ph) 4-F 4-CI 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-j-Bu 4-i-Bu 4-i-Bu 4-λ-Ργ 4-i-Pr 4-Mc 4-CH=CH2 4-OCH 4-CH=CHQ 4-OC-CH2c1 4^H2°Mc 4-CH2SMe 4-CN 4-N〇2 4-S02Me 4-CH2Ph 4-CHO 4-COMc 4-N(Me)2 4-SiMe3 4-SF5 4-OMe 4-Ph 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 3-/i-Bu 3-CH2F X5H9 3-CONHMe 3-S02NHMc 4«C0NHMc 4-S02NHMc 4«〇C-SiMe3 4-CsC-CH(OEt)2 3-CH2CF3 3-Et 3-CH2CN 3-COOMc 3-(4-F-Ph) 4«CH2〇F3 4-Et 4.CH2CN 4-COOMe 3-C0Ph 4-C0Ph R1 = F,R2 : =F,P = 2·α, A = 〇, Yx〇, Z = 0, n = l 且 R3= 3-F 3-α 3七r 3-CF3 3-OCF3 3-OCH2CF3 3-j-Bu 3-/-Bu 3-r-Bu 3-n-Pr 3-i-Pr 3-Mc 3-CH=CH2 3-C»CH 3-CH=CHCl 3-C*C-CH2cl 3-CH2〇Me 3-CH2SMe 3-CN 3-N〇2 3-S02Me 3-OMc 3-CH0 3-COMe 3-N(Me)2 3-SiMe3 3-SF5 3-CH2Ph 3-Ph 3-(4-Cl-Ph) 4-F 4-CI 4-Br 4*CF3 4-OCF3 4.〇CH2CF3 4-/-Bu 4-i-Bu 4-n-Pr 4-i-Pr 4-Me 4-CH=CH2 4-CaCH 4-CH=CHCl 4-C^Z.CH2a 4-CH2OMc 4-CH2SMe 4-CN 4·Ν〇2 4-S02Me 4-CH2Ph 4-CHO 4-C0Me 4.N(Me)2 4-SiMe3 4-SF5 4-OMe 4-Ph 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh (請先閱讀背面之注意事項再填寫本頁) • an— * --I 裝----·---訂— 本紙張尺度通用中國國家標準(CNS ) A4规格(210x 297公董) -63 - A7 B7
五、發明説明(61 ) I 經濟部中央樣準扃員工消費合作社印繁 4-SMe 4-SEt 4-〇CF2H 4~SCF2H 4-0Ph 4-SPh 3-n-Bu 3-CH2F 3-c-C5H9 3-CONHMc 3-S02NHMc 4-n-Bu 4.c-C5H9 4-C〇NHMe 4-S〇2NHMc 4-C£C-SiMe3 4-OC-CH(OE〇2 3-CH2CF3 3-Et 3-CH2CN 3-COOMc 3-(4-F-Ph) 4.CH2CF3 4-Et 4-CH2CN 4-COOMe 3-C0Ph 4-C0Ph 4-CH2F R1 =F, R2 =F, P = 2-OMe, A = 0, Y =( λ Z = 0. n = 1 MR3= 3-F 3-CI ' 3-Br 3-CF3 3-OCF3 3-OCH2CF3 3-j-Bu 3-f-Bu 3-i-Bu 3-λ-Ργ 3-i-Pr 3-Me 3-CH=CH2 3-OCH 3-CH=CHa 3-OC-CH2CI 3«CH2〇Mc 3-CH2SMc 3-CN 3-N〇2 3-S02Me 3-OMc 3^H0 3-C0Mc 3-N(Mc)2 3-SiMe3 3-SF5 3-CH2Ph 3-Ph 3-(4-Cl-Ph) 4-F 4-C1 4-Br 4-CF3 4-OCF3 4^CH2CF3 4-j-Bu 4-/-Bu 4-r-Bu 4-n-Pr 4-/-Pr 4-Mc 4-CH=CH2 4-C*CH 4-CH=CHCl 4-〇C-CH2a iM:H2〇Mc 4-CH2SMc 4-CN 4-N〇2 4*S02Mc 4CH2Ph 4-CHO 4-C0Mc 4-N(Me)2 4-SiMe3 4-SF5 4-〇Me 4-Ph 3-SMe 3-SEt 3-CX:F2H 3-SCF2H 3-0Ph 3-SPh 4-SMe 4-SEt 4^0CF2H 4-SCF2H 4-〇Ph 4-SPh 3-n-Bu 3-CH2F 3-C-C5H9 3-CONHMc 3-S02NHMc 4-/f-Bu 4-C-C5H9 4-C0NHMe 4.S02NHMc 4<^r-SiMe3 4-OC-CH(OEt)2 3-CH2CF3 3-Ec 3~CH2CN 3-COOMc 3-(4-F.Ph) 4-CH2CF3 4·Β 4-CH2CN 4-COOMe 3-C0Ph 4-C0Ph 4-CH2F rUf. r2: =F, P = 2-OEt, A = 0, Y = 0. Z = 〇, n = 1 且R3= 3-F 3-a 3-Br 3-CF3 3-OCF3 3-OCH2CF3 3-/-Bu 3-t-Bu 3-i-Bu 3-n-Pr 3-i-Pr 3-Mc 3-CH=CH2 3-CsCH 3-CH=CHCl 3-CaC-CH2Cl 3-CH2〇Me 3-CH2SMe 3-CN 3-N〇2 3-S〇2Me 3-OMe 3-CH0 3-COMe 3-N(Me)2 3-SiMe3 3-SF5 3-CH2Ph 3-Ph 3-(4-CI.Ph) 4-F 4-CI 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-j-Bu 4-/-Bu 4-i-Bu 4-n-Pr 4-i-Pr 4-Me 4-CH=CH2 4-OCH 4-CH^CHCi 4-CaC^H2CI 4-CH2〇Me 4-CH2SMe 4-CN 4-N〇2 4-S02Me 4-CH2Ph Φ€Η0 4-C0Me 4-N(Me)2 4-SiMe3 4-SF5 4*〇Me 4-Ph 3-SMc 3-SEt 3.〇CF2H 3-SCF2H 3-0Ph 3-SPh 4-SMc 4-SEt 4-〇CF2H 4-SCF2H 4-0Ph 4-SPh -------—裝----Γ— 訂,.--I----線 (請先閱讀背面之注意事項再填寫本頁) 本紙张尺度適用中國國家標隼(CNS ) Λ4規格(210X297公瘦> -64 - Λ7 B7 五、發明説明(62 )
I 經濟部中央標準局貝工消资合作社印策 3-n-Bu 3-CH2F S-C-CjHg 3-CONHMe 3-S02NHMc 4-/i-Bu 4-C-C5H9 4-CONHMc 4-S02NHMe 4-〇C-SiMe3 4-CsC-CH(OEt)2 3-CH2CF3 3-Et 3-CH2CN 3-COOMe 3-(4-F-Ph) 4-CH2CF3 4-Et 4-CH2CN 4-COOMc 3-COPh 4-C〇Ph 4-CH2F rUf, R2 = F, P = 3-F. A = 0. Y = 0, Z = 〇, n=l £r3= 2-Br 2-CF3 2-OCF3 2-OCH2CF3 2^CH2CF3 2-j-Bu 2-i-Bu 2-r-Bu 2-n-Pr 2-i-Pr 2-Mc 2-Et 2-CHCH2 2-OCH 2-CH=CHQ 2-〇C-CH2CI 2-CH2〇Mc 2>CH2SMe 2-CH2CN 2-CN 2-N〇2 2-S〇2Me 2-CHO 2-COMe 2-COOMe 2-N(Mc)2 2-SiMe3 2-SF5 2-CH2Ph 2-Ph 2-(4-Cl-Ph) 2-(4-F-Ph) 4-F 4-a 4-Br 4-CF3 4-OCF3 4-CX:H2CF3 4-CH2CF3 4-5-Bu 4-/-Bu 4-/-Bu 4-n-Pr 4-i-Pr 4-Me 4-Et 4-CH=CH2 4-C3CH 4-CH=CHQ 4-CC-CH2Cl 4-CH2〇Mc 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Mc 4-CH2Ph 4CH0 4-COMc 4-COOMc 4-N(Me)2 4-SiMe3 4-SF5 4-〇Me 4-Ph 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 3-SPh 3-COPh 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 4-COPh 2-/i-Bu 2-CH2F 2-C-C5H9 2-C〇NHMe 2-S〇2NHMc 4-n-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-S〇2NHMc 4-CaC-SiMe3 4-CaC-CH(OEt)2 R1 = F, R2 =F. P = 3-Cl. A = 0. Y = 0, Z = 0, n = 1 且R3= 2-Br 2CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-j-Bu 2-i-Bu 2-r-Bu 2-n-Pr 2-i-Pr 2-Me 2-Et 2-CH=CH2 2-CsCH 2-CH=CHCl 2-CsC-CH2a 2-CH2°Me 2-CH2SMe 2-CH2CN 2-CN 2-N02 2-S〇2Mc 2«CH〇 2-COMe 2-COOMe 2-N(Me)2 2-SiMc3 2-SF5 2-CH2Ph 2-Ph 2-(4-CI-Ph) 2-(4-F-Ph) 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-j-Bu 4-/-Bu 4-r-Bu 4-n-Pr 4-i-Pr 4-Mc 4-Et 4-CH=CH2 4-CsCH 4-CH=CHCI 4-CsC-CH2CI 4-CH2〇Me 4.CH2SMe 4-CH2CN 4-CN 4^N〇2 4-S02Me 4-CH2Ph 4-CHO 4-COMc 4-COOMe 4-N(Me)2 4-SiMe3 4-SF5 4-OMe 4-Ph 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 3-SPh 3-COPh 4*SMe 4-SEt 4-〇CF2H 4-SCF2H 4-OPh 4-SPh 4-COPh 2-n-Bu 2-CH2F 2-C-C5H9 2-CONHMc 2-S〇2NHMe 4-"-Bu 4-CH2F 4-C-C5H9 4-CONHMc 4-S〇2NHMc 4-OC-SiMe3 4-CsC.CH(OE〇2 (請先閲讀背面之注意事項再填寫本頁) .1 —裝——----.丨訂---I----線J--·! .I I Hi * 本紙裱尺度適用中國國家標準(CNS ) Λ4規格(210X297公釐) * 65 -
五、發明説明(63 )
Rl = F, R2 = F. P = 3-0Met A = 0, Y =0, Z = 0, n : :1 且R3= 2-Br 2-CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-j-Bu 2-Z-Bu 2-r-Bu 2-n-Pr 2-t-Pr 2-Me 2-Et 2-CH=CH2 2-CeCH 2-CH=CHCI 2-C=C-CH2Cl 2-CH2OMe 2.CH2SMc 2-CH2CN 2-CN 2·Ν〇2 2-S02Mc 2-CH0 2-C0Me 2-COOMe 2-N(Me)2 2-SiMc3 2-SF5 2-CH2Ph 2-Ph 2-(4-a-Ph) 2-(4-F-Ph) 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-j-Bu 4-i-Bu 4-r-3u 4-n-Pr 4-i-Pr 4-Me 4-Et 4-CH=CH2 4-OCH 4»CH=CHa 4-C»C-CH2a 4-CH2OMe 4-CH2SMc 4"CH2CN 4-CN 4-N〇2 4-S02Me 4-CH2Ph 4-CH0 4-C0Mc 4-C00Me 4.N(Mc)2 4-SiMe3 4-SF5 4-0Me 4-Ph 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 3-SPh 3-C0Ph 4-SMe 4-SEt 4.〇CF2H 4-SCF2H 4-OPh 4-SPh 4-C0Ph 2-/i-Bu 2-CH2F 2-CC5H9 2-C0NHMc 2-S〇2NHMc 4-n-Ba 4-CH2F 4-C-C5H9 4-CONHMc 4-S02NHMe 4-CsC-SiMc3 ^CsC-CH(pEt)2 經濟部中央標準局貝工消費合作社印製
R1 =F,R2 =F, P = 3-OEt, A = 0, Y = 0· Z = 0, n = 1 且 R3= 2-F 2-C3 2-Br 2.CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-j-Bu 2-/-Bu 2-f-Bu 2-n-Pr 2w*-Pr 2-Me 2-Et 2-CH=CH2 2-OCH 2-CH=CHCl 2-C®C-CH2Cl 2-CH2OMc 2-CH2SMe 2-CH2CN 2-CN 2-N02 2-S〇2Me 2-0Me 2-CH0 2-C0Me 2-COOMe 2-N(Me)2 2-SiMc3 2-SF5 2-CH2Ph 2-Ph 2-(4-Cl-Ph) 2-(4-F-Ph) 4-F 4-C1 4*Br 4-CF3 ‘ocf3 4-OCH2CF3 4-CH2CF3 4-s-Bu 4-i-Bu 4-r-Bu 4-n-Pr 4-i-Pr 4-Me 4-Et 4-CH=CH2 4-C*CH 4-CH=CHQ 4-CaC-CH2Cl 4-CH2OMe 4-CH2SMc 4-CH2CN 4<CN 4>N〇2 4-S〇2Mc 4-CH2Ph 4-CH0 4-C0Me 4-C00Me 4-N(Mc)2 4-SiMe3 4-SF5 4-0Me 4-Ph 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-01¾ 3-SPh 3-C0Ph 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-〇Ph 4-SPh 4-C0Ph 2-n-Bu 2-CH2F 2-c-C5H9 2-CONHMc 2-S〇2NHMc 4-n-Bu 4-CH2F 4-C-C5H9 4-C0NHMe 4-S〇2NHMe 4-OC-SiMe3 4-CsC-CH(OEt)2 R! =F. R2: =F, P = 4-F. A = 0· Y =: 〇· Z = 0, n = l 且 R3= 2-Br 2-CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-i-Bu 2-i-Bu 2-i-Bu 2-rt-Pr 2-i-Pr 2-Me 2·Εί 2-CH=CH2 2'CaCH 2-CH=CHCl 2-CsC -CH 2CI 2-CH2〇Me 2*CH2SMe 2-CH2CN ________ _^------訂 4^. (請先閱讀背面之注意事項再填寫本頁) ____ 本紙浪尺度適用中國國家橾隼(CNS ) Λ4現格(210X29?公t ) A7
五、發明説明(64 ) I 經濟部中央標準局員工消费合作社印製 2-CN 2-N〇2 2-S02Me 2-CHO 2-C0Mc 2-COOMc 2-N(Mc)2 2-SiMc3 2-SF5 2-CH2Ph 2-Ph 2-(4.a-Ph) 2-(4-F-Ph) 3-F 3-a 3-Br 3-CF3 3-OCF3 3-OCH2CF3 3-CH2CF3 3-j-Bu 3-/-Bu 3-r-Bu 3-rt-Pr 3-i-Pr 3-Mc 3-Et 3-CH=CH2 3-OCH 3-CH=CHCl 3.C*C-CH2C1 3-CH2〇Me 3-CH2SMe 3-CH2CN 3-CN 3-N〇2 3-S02Me 3-CH2Ph 3-CH0 3-C0Mc 3-COOMc 3-N(Mc)2 3-SiMe3 3-SF5 3-〇Me 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 2-COPh 3-SMe 3 - SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 3-COPh 2-/i-Bu 2-CH2F 2^>C5H9 2-CONHMe 2-S〇2NHMc 3-n-Bu 3^CH2F 3-C-C5H9 3-CONHMe 3-S02NHMe rUf, R2»F,: P = 4-C1, A = 0, Y = 0, z = 0, n = I.且 r3= 2-Br 2-CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-j-Bu 2-i-Bu 2-f-Bu 2-n-Pr 2-Z-Pr 2-Mc 2-Et 2-CH=CH2 2-OCH 2-CH=CHCl 2-CaC-CH2C] 2-CH2〇Me 2-CH2SMe 2«CH2cn 2-CN 2-N〇2 2-S02Me 2-CHO 2-COMc 2-COOMe 2-N(Me)2 2-SiMe3 2-SF5 2-CH2Ph 2-Ph 2-(4*Cl-Ph) 2-(4-F-Ph) 3-F 3-C1 3-Br 3-CF3 3-OCF3 3-OCH2CF3 3-CH2CF3 3-5-Bu 3-/-Bu 3+Bu 3-λ-Ργ 3-/-Pr 3-Me 3-Et 3-CH=CH2 3-CsCH 3-CH=CHCI 3-OC-CH2a 3-CH2〇Me 3-CH2SMc 3-CH2CN 3-CN 3·Ν02 3-S〇2Me 3.CH2Ph 3-CHO 3-COMe 3-COOMe 3-N(Mc)2 3-SiMe3 3-SF5 3-OMe 3-Ph 3-(4.CI-Ph) 3-(4-F-Ph) 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 2-C0Ph 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 3-SPh 3-C0Ph 2- n-Bu 3- c-CjH^ 2- CH2p 3- CONHMc 2- c-C^Hg 3- S〇2NHMe 2-C0NHMc 2-S02NHMe 3-n-Bu 3-CH2F R!=F. R2 = F, P = 4_〇Me A = 〇 γ=〇 z = 〇 n =】且r3= 2-j-Ba 2-CH=CH2 2-CN 2-i-Bu 2-OsCH 2-N〇2 2-Br 2-j-Bu 2-CH=CHa 2-S〇2Mc 2-CF3 2-rt-Pr 2-〇C.CH2Cl 2-OCF3 2-i-Pr 2-CH2〇Mc 2-CHO 2-OCH2CF3 2-Me 2-CH2SMc 2-C0Mc 2-CH2CF3 2-Et 2-CH2CN 2-COOMe 2- N(Me>2 3- F 3-j-Bu 3-CH=CH2 2- SiMe^ 3- C1 3-i-Bu 3-QeCH 2- SF5 3- Br 3-i-Bu 3-CH=CHC 2CH2Ph 3-CF3 3-n*Pr 3-C*C-CH2Cl 2- Ph 3- OCF3 3-/-Pr 3-CH2〇Mc 2- (4-Ct-Ph) 3- OCH2CF3 3-Me 3-CH2SMe 2- (4-F-Ph) 3- CH2CF3 3-Et 3-CH2CN (請先閲讀背面之注意事項再填寫本頁) -I.——^---------—襄------ 訂 -----線 1 丨 J--I, 本紙伕尺度適用中困'國家榡準(CNS ) A4規格(210X 297公绛) 五、發明説明(65 A7 B7 3-CN 3-N〇2 3-S02Me 3-CH2Ph 3-CH0 3-C0Me 3-C00Me 3-N(Me)2 3-SiMe3 3-SF5 3-OMe 3-Ph 3.(4-C]-Ph) 3-(4-F-Ph) 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-0Ph 2-SPh 2-C0Ph 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 3-SPh 3-C0Ph 2-n-Bu 2-CH2F 2-C-C5H9 2-CONHMe 2-S02NHM< s 3-n-Bu 3-CH2F 3-CONHMe 3-S02NHMc R1 = F,R2 =F, P = 4-0Et, A = 0, Y = 0,Z = 0, n = 1 :且 R3= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-OCH2CF3 2-CH2CF3 2-j-Bu 2-i-Bu 2-/-Bu 2-/i-Pr 2-i-Pr 2-Me 2-Et 2-CH=CH2 2-OCH 2-CH=CHCl 2^C*C«CH2C] 2-CH2〇Me 2-CH2SMc 2-CH2CN 2-CN 2-N〇2 2-S〇2Me 2-0Me 2-CH0 2-C0Me 2-C00Me 2-N(Me)2 2-SiMe3 2-SF5 2-CH2Ph 2-Ph 2-(4-(:1州 2-(4-F-Ph) 3-F 3-C1 3-Br 3-CF3 3.OCF3 3-OCH2CF3 3-CH2CF3 3-j-Bu 3-/-Bu 3-r-Bu 3-n-Pr 3-i-Pr 3-Mc 3-Et 3-CH=CH2 3-CsCH 3-CH=CHCl 3-OC-CH2Cl 3-CH2〇Me 3-CH2SMe 3-CH2CN 3-CN 3-N〇2 3-S〇2Me 3-CH〇Ph 3-CH0 3-C0Me 3-C00Me 3-N(Me)2 3-SiMe3 3-SF5 3-OMe 3-Ph 3-(4-CI-Ph) 3-(4-F-Ph) 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 2-C0Ph 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-0Ph 3-SPh 3-C0Ph 2-n-Bu 2-CH2F 2-c-C5H9 2-CONHMc 2-S02NHMc 3-n-Bu 3-CH2F 3-C-C5H9 3-CONHMe 3-S02NHMc 表5 抑衣 訂Ί . ! "線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標隼局貝工消費合作社印製
A i=F,R2=F, Α=0,Υ=0,Ζ=0且Q=
Η λ-Bu(CH2>4CH3 fcH2)8CH3 c_C6h1 I
Et /-Bu (CH2)5CH3 (CH2)9CH3 C-C5H9
λ-Ργ j-Bu (CH2)6CH3 cf3 CH2Ph-4-F /-Pr r-Bu (ch2)7ch3 ch2cf3 CH,Ph-4-Cl 本紙張尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) -68 - A7 B7 五、發明説明(66) ί 經濟部中央標準局員工消t合作杜印製 2-睡嗯基 3-睡嗯基 5-F-(2-Hi 嗯基) 5-tn-(2-ni 嗯基) 卜棻基 2-棻基 1H-吡咯-2-基 IH-吡咯-3-基 2-呋喃基 3-呋喃基 5-F-(2-呋喃基) 5-Cl-(2-呋喃基) 2-暍唑基 2-吡啶基 3-吡啶基 4-吡啶基 :5-F-(2-吡啶基)5-Cl-(2-吡啶基)5-CF3-(2-吡啶基) R1 = F, R2 = :Cl, A = 0, Y = 〇, z = 〇且Q= Η Et n-Pr i-Pr n-Bu i-Bu s~Bu t~Bu (CH2)4CH3 (ch2)5ch3 (CH2)6CH3 (CH2)7CH3 (CH2>gCH3 (CH2)9CH3 cf3 ch2cf3 c*c6h1 1 C-C5H9 CH2Ph-4-F CH2Ph-4-Cl ,2-Pf嗯基 3-睡嗯基 5-F-(2-〇S 嗯基) 5-C卜(2-_嗯基) 1 1-棻基 2-棻基 1H-吡咯-2-基 1H-吡咯-3-基 ;2-呋喃基 3-呋喃基 5-F-(2-呋喃基) 5-Cl-(2-呋喃基) ! 2-_唑基 2-吡啶基 3-吡啶基 4-妣啶基 5-F-(2-吡啶基)5-Cl-(2-吡啶基)5-CF3-(2-0比啶基) R1 = Cl, R2 = CI, A = 0, Y = 〇, ζ = 〇;且 Q= H Et n-Pr /-Pr λ-Bu /-Bu j-Bu f-Bu (CH2)4CH3 (CH2)5CH3 (CH2)6CH3 (CH2)7CH3 (ch2)8ch3 (CH2)9CH3 cf3 ch2cf3 c.C6HII C-C5H9 CH2Ph-4-F CH2Ph-4-Cl 丨2-_嗯基 3-噻嗯基 5-F-(2-OS 嗯基) 5-n-( 2-OS 嗯基) ;1-棻基 2-矣基 1H-吡咯-2-基 1H-吡咯-3-基 :2-呋喃基 3-呋喃基 5-F-(2-呋喃基) 5-α-(2-呋喃基) i 2-噚唑基 2_社淀基 3-吡啶基 4-fl比啶基 丨5-F-(2-吡啶基)5-α-(2-吡啶基)5-CF3-(2-吡啶基) R1 = ci, r2 = Η,Α = 0, Υ = 〇· z = 0 且Q= Η Et n-Pr /-Pr n-Bu "Bu j-Bu r-Bu (CH2)4CH3 (CH2)5CH3 (ch2)6ch3 (CH2)7CH3 (CH2)8CH3 (CH2)9CH3 cf3 ch2cf3 c*C6h1 ! C-C5H9 CH2Ph-4-F CH2Ph-4-CI 2-thicnyl 3-ihienyl 5-F-(2-thienyI) 5-CI-(2-thienyl) 本紙悵尺度適用中國國家標準(CNS ) Λ4規格(210X 297公f ) _ (請先閱讀背面之注意事項再填寫本頁) -¾衣------ 訂 ---線 308595 A7 B7 五、發明説明( 67 ) 2-唾嗯基 3-瞜嗯基 5-F-(2-Bl 嗯基) 5-Cl-(2-QS 嗯基) 1-条基 2-棻基 1H-吡咯-2-基 1H-吡咯-3-基 2-呋喃基 3-呋喃基 5-F-(2-呋喃基) 5-Cl-(2-呋喃基) 2-吡啶基 3-吡啶基 5-F-(2-U比淀基)5-Cl-(2-H比陡基)5-CF3-(2-tI比陡基) R1 = F, R2 = F, A = ο, γ = 〇, z = s 且Q= 4-吡啶基 Η Et π-Pr /-Pr n-Bu /-Bu 5-Bu r-Bu (ch2)4ch3 (ch2)5ch3 (CH2)6CH3 (CH2)7CH3 (ch2)8ch3 (^^2)9 ⑶3 cf3 CH2CF3 c'C6h1 1 CH2Ph-4-F CH2Ph-4-Cl 2-_嗯基 3-1«嗯基 5-F-(2-« 嗯基) 5-CI-(2-〇i 嗯基) 1-棻基 2-棻基 1H-吡咯-2-基 吡咯-3-基 2-呋喃基 3-呋喃基 5-F-(2-呋喃基) 5-Cl-(2-呋喃基) 号唑基 2-吡啶基 5-F-(2-吡啶基)5-CI-(2-ffi;啶基) R1 = F, R2 = F, A = 0, Y = s, Z = 0 .-H.y= 3-D比啶基 5-CF3-(2-吡啶基) 4-吡啶基 H Et η-Ρτ i-Pr λ-Bu i-Bu s-Bu ί-Bu (CH2)4CH3 (CH2)8CH3 c-c6Hh 2-Hi嗯基 1- 棻基 2- 呋喃基 (CH2)5CH3 (Cii2)9CH3 c-C5H9 3-睡嗯基 2- 棻基 3- 咲喃基 2-吡啶基 5_(]1__(2-社陡基) 經濟部中央橾準局員工消費合作社印製 2-Π咢唑基 5-F-(2-吡啶基) R1 = F, R2 = F, A = S, Y = 0· Z = 0 且Q= H Et n-Bu (CH2)4CH3 (ch2)8ch3 c-c6nn 2-(¾嗯基 1-棻基 *-Bu (CH2)5CH3 (CH2)9CH3 c-C^H^ 3-Hf嗯基 2-棻基 (CH2)6CH3 cf3 CH2Ph 冰 F 5-F-(2-« 嗯基) 1H-吡咯-2-基 5-F-(2-咲喃基) 3-吡啶基 5-CF3-(2-吡啶基) λ-Ργ j-Bu (CH2)6CH3 cf3 CH2Ph-4-F 5-F-(2-0i 嗯基) 1H-吡咯-2-基 (CH2)7CH3 CH2CF3 CH2Ph-4-Cl 5-Cl-(2-Pi 嗯基) 1H-吡咯-3-基 5-Cl-(2-呋喃基) 4-吡啶基 /-Pr r-Bu (CH2)7CH3 ch2cf3 CH2Ph-4-Cl 5-C卜(2-iS嗯基) 1H-吡咯-3-基 -------"丨裝------訂-------線 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) Λ4規格(210 X 297公釐) -70 A 7 B7 五、發明説明(68 ) Ϊ 2-呋喃基 2-ί萼唑基 5-F-(2-吡啶基) R1 =F, R2 = F, A Η n-Bu(CH2>4CH3 (CH2)8CH3 c*c6h1 1 2-¾嗯基 1- 棻基 2- 呋喃基 2-B萼唑基 5-F-(2-妣啶基) 3-呋喃基 5-F-(2-呋喃基) 2-吡啶基 3-吡啶基 5-α-(2-吡啶基)5-CF3-(2-吡啶基) = NH, Y = o, Z = 〇EQ= 5-Cl-(2-呋喃基) 4-吡啶基
Et i-Bu (CH2)5CH3(CH2>9CH3 C-C5H9 3-睡嗯基 2- 棻基 3- 呋喃基 2-吡啶基 η«Ρτ x-Bu (CH2)6CH3 cf3 CH2Ph-4-F 54-(2-¾ 嗯基) 1H-吡咯-2-基 5-F-(2-呋喃基) 3-虹啶基 i-Pr /-Bu (CH2)tCH3 ch2cf3 CH2Ph-4-a 5-a-(2-tii 嗯基) 1Η-Π比咯-3-基 5-a-(2-呋喃基) 4-吡啶基 5-Cl-(2-吡啶基)5-CF3-(2-吡啶基) 表6
--------—裝------訂-----> 線— (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局.只工消费合作杜印製 R1 =F,] R2 = F, X = CH2. Y = 0. Z = 0 且 R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-i-Bu 2-CH2CN 2-CH2F 2-Ph 2-CH0 2-C0Me 2-C00Me 3-Cl 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-0Me 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-f-Bu 3-CH2F 3-CH0 3-C0Me 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CsCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4-CH2CF3 本紙張尺度適用中國國家橾準(CNS) Λ4規格(210X2W公ft ) 308595 »7 五、發明説明(f 69) 4-n-Bu 4-/-Bu 4-j-Bu 4-zi-Pr 4-r-Pr 4-Et 4-Me 4-CH=CH2 4-C$CH 4-CH=CHCI 4-〇C-CH2Cl 4-CH2OMc 4-CH2SMe 4-CH2CN 4-CN 4-N02 4-S02Mc 4-*〇Me 4,CHO 4-COMe 4-COOMe 4-S〇2NHMe 4-N(Mc)2 4-S1MC3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2.〇CF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-OPh ‘SPh 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2CNt 3-SiMe3 3-N(Mc)2 4-f-Bu 4.CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh
經濟部中央標準局Mt.消资合作社印$L rUf· R2 = F, X = CH2, Υ = 0· z = s 且R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMc 3-α 3-Br 3-CF3 3-OCF3 3-CN 3·Ν〇2 3-OMe 3-Et 3-λ-Ργ 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-CI.Ph) 3.(4-F-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4./-BU 4-i-Bu 4-n-Pr 4-/-Pr 4-Et 4-Me 4-CHCH2 4-CsCH 4-CHCHCl 4.〇C-CH2CI 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Mc 4-OMc 4-CHO 4-COMc 4-COOMe 4-S〇2NHMc 4-N(Me)2 4-SiMe3 4-SF5 4CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N02 2-5-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Mc)2 4-r-Bu 4-CH2F 4-C-C5H5 4-CONHMc 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R! =F, r2 = F, X = CH2. Y = S, Z = 〇 且 R3= H 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMc 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-/i-Bu 2々-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-n-Pr 3-/-Pr 3-/i-Bu 3-i-Bu 3-5-Bu 3-/-Bu (讀先閲讀背面之注意事項再填寫本瓦) -装--- ΪΤ------ ^------ 11 I H1 · 本紙張尺度遑用中國國家標隼(CNS ) M規格(210x m公t ) -72 五
、發明説明(70 ) I A7 B7 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-ChCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-C1 4-Br 4-CF3 4.OCF3 4-〇CH2CF3 4-CH2CF3 4·/ι·Βιι 4-i-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-Et ‘Me 4-CH=CH2 4-OCH 4.CH=CHQ 4-C3C-CH2Cl 4-CH2OMe 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-〇Me 4-CHO 4-COMe 4-COOMe 4-S02NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2^SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMc 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4·〇Ε【 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-i-Bu 3_F 3-Me 3-SiMe3 3-N(Me)2 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh 請 先 閱 讀 背 面 % 事 3 r!*f, r2 = ci, x = ch2, y = o, Z = 0 ER3= H 2·Ρ 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Mc 2-Et 2-n-Pr 2-/-Pr 2-n-Bu 2-i-Bu 2-i-Bu 2-CH2CN 2-CH2F 2,Ph 2-CHO 2-COMc 2-COOMe 3-CI 3-Br 3-CF3 3.OCF3 3-CN 3-N〇2 3-OMc 3-Et 3-zi-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-5-Bu 3+Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3^4-Cl-Ph) 3-(4-F-Ph) 3-GeCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-Ci 4-Br 4-CF3 4-CXP3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-OCH 4.CH=CHC1 4-CsC-CH2CI 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 4-S〇2NHMe 4*N(Me)2 4-SiMe3 ‘sf5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMc 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMe 4-SEt 4.〇CF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-i-Bu 3-F 3-Me 3-CH2cn 3-SiMe3 3-N(Me)2 4-£-Bu 4-CH2F 4-c-C^H^ 4-CONHMe 4.(4-f-Ph) 2-COPh 3-COPh 4-COPh R1 = Cl, R2 = F, X = CH2, Y = 0. Z = 〇 且 R3= H 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Mc 2-Et 2-λ-Ργ 2-i-Pr 2-n-Bu 2-(-Bu 本紙張尺度適用中國闺家標隼(CNS ) Λ4规格(21<)x 297公旒)-73 - A7 B7 五、發明説明(71 ) 經濟部中夫標隼扃Μ工消f合作社4^ 2-r-Bu 2-CH2CN 2-CH〇F 2-Ph 2-CHO 2-COMe 2-COOMe 3-0 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-OMe 3-Et 3-λ-Ργ 3-i-Pr 3-«-Bu 3-/-Bu 3-j-Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-C00Me 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CaCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F ‘Cl 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-t-Bu 4-s-Bu 4-rt-Pr 4-Z-Pr 4-Et 4-Mc 4-CH=CH2 4-CaCH 4-CHaCHCl 4.〇C-CH2Cl 4-CH2°Mc 4^H2SMc 4-CH2cn 4-CN 4-N〇2 4-S〇2Me 4-OMc 4-CHO 4-COMe 4-C00Me 4-S〇2NHMc 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 4K4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 本 scf2h 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Mc 3-CH2CN 3-SiMej 3-N(Mc)2 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh rUf, r2 = :F· X = CH2CH2, Y:0· Z = 0 且R3= H 2-F 2-a 2-Br 2CFj 2.OCF3 2-CN 2-OMc 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-f-Bu 2<3I2CN 2-CH2f 2-Ph 2-CHO 2-COMe 2-COOMc 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-λ-Ργ 3-Z-Pr 3-n-Bu 3-i-Bu 3-5-Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4·α 4-Br 4-CF3 4-OCF3 4.〇CH2CF3 ‘ch2cf3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4-CsCH 4»CH=CHC】 4.CsC-CH2CJ 4-CH2OMc 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-C00Me 4-S〇2NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-G-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEr 4-OCF2H 4-SCF2H 4-〇Pb 4-SPh 2-N02 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh (請先閲讀背面之注意事項再填寫本頁) -裝. 訂 .…L^ — .1 --- - -1- I- - 7Γ氏张尺度邮中_家料(CNS ) Λ4規格(2U) X297公窠〉 Λ 7 Β7 五、發明説明(/2) 濟 部 央 橾 準
X 消 /v it 印 %
Rl = F, R2 = F, X = CH2CH2, Y = ο. z = S -S-R3= Η 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-α 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-C=CH 3-C-C5H9 3-SF5 3^H2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4.C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4^H2CF3 4-/i-Bu 4-/*Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-C*CH ‘CH=CHC1 4-C*C-CH2Cl 4-CH2〇Me 4^H2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 4-S02NHMc 4-N(Me)2 4-SiMe3 4-SF5 4-CHoPh 4m 4-Ph 4-(4-CI-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-S£t 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMc 4-SEt 4-OCF2H ‘scf2h 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-(4.F-Ph) 2-COPh 3-COPh 4-COPh Rl = F. R2 = F. X = CH2CH2, Y = S. z = o 且R3= H 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Mc 2-Et 2-λ-Ργ 2-i-Pr 2-n-Bu 2-/-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-/-Bu 3-j-Bu 3-i-Bu 3.CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CsCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CP3 4-n-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CHCH2 4-C»CH 4-CH=CHCl 4«OC-CH2a 4-CH2〇Mc 4-CH2SMc 4-CH2CN 4-CN 4-N〇2 ‘S〇2Me 4-OMe 4-CHO 4-COMc 4-COOMe 4-S〇2NHMe 4-N(Me)2 4-SiMe3 4.SF5 4-CH2Ph 4-Ph 4.(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEl 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 請 先 閱 讀 背 之 注 意 事 項 再 本 頁 裝 訂 線 本紙悵尺度通闲中同國家標準(CNS ) Λ4規格Ul〇X2‘)7公楚) 75 五、發明説明(73 ) A7 B7 2·齡 Λ. 2-j-Bu 3-F 3>Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-r-Bu 4-COPh R1 =F, R2 = 4.CH2F 4-c-C5H9 =Cl, X = CH2CH2. Y = 0 4-C〇NHMc ,z = o 且R3= 4-(4-F-Ph) 2-COPh 3-COPh H 2-F 2-C1 2-Br 2^F3 2-00=3 2-CN 2-OMe 2-Me 2-Et 2-λ-Ργ 2-i-Pr 2·η-Βιι 2-/-Bu 2-r-Bu 2-CH2CN 2^TH2F 2-Ph 2-CHO 2-COMe 2-COOMc 3-C1 3-Br 3-CF3 3-CX:F3 3-CN 3-N〇2 3-OMc 3-Et 3-λ-Ργ 3-<-Pr 3-a-Bu 3-i-Bu 3-j-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-CI-Ph) 3-(4-F-Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-Q 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-/i-Bu 4-/-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4*CH=CH2 4〇sCH 4-CH=CHQ 4-〇bC-CH2C1 4«CH2〇Mc ^CH2SMt 4-CH2CN 4-CN 4-N〇2 4-S02Me 4-OMe 4CHO 4-COMc 4-CCX)Me 4-S〇2NHMe 4-N(Me)2 4-SiMe3 4-SF5 4«CH2Ph 4-Ph 4-(4^:i-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3.〇Ph 3-SPh 4-OEt 4-SMe 4-SEr 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-/-Bu 4-COPh 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh RLci. r2 = ci,x = ch2ch2, Y = 0, z = o 且R3= (請先閱讀背面之注意事項其填寫本頁) 裝· 訂 蛵濟部中央標隼局Η工消1t·合作社印¾ H 2-F 2-C1 2-Br 2«CF3 2.OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-^-Bu 2-i-Bu 2-nBu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3.CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-λ-Ργ 3-(-Pr 3-/i-Bu 3-i-Bu 3-i--Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CaCH 3-C-C5H9 3-SF5 3*CH2Ph 3-OCH2CF3 3.CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4-CF3 4-OCF3 4.〇CH2CF3 4-CH2CF3 4-i-Bu 4-s-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-CsCH 4-CH=CHCI 4-CsC*CH2CI 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMc 4-COOMe 4's〇2NHMe 4-N(Me)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 4-(4-CI-Ph) I ' — __ , 本紙張尺度適枬中國國家標率(CNS )六4現格(2297公釐)— Λ 7 Β7 經濟部中央標隼局員工消费合作社印製 五、發明説明( i 74) - 1 1 I 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh - 1 1 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 1 I 4-〇Εί 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh I 2-Ν〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3.SiMe3 3-N(Me)2 請 先 I 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMc 4-(4-F-Ph) 2-COPh 3-COPh 閱 if 背 1 4-COPh i R1 = F. R2 = F· X = CH2CH2CH2· Y =〇· z = 0 且 R3= 之 注 1 1 H 2-F 2·α 2-Br 2-CF3 2-OCF3 2-CN 意 事 1 2-OMe 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-w-Bu 2-i-Bu 項 再 ! 2-i-Bu 2-CH2CN 2-CH2f 2-Ph 2-CHO 2-COMe 2«C00Me 填 寫 本 頁 1 裝 I 3-C1 3-Br 3^CF3 3.OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-f-Ba 1 I 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-CI-Ph) 3^4-F-Ph) 1 1 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 1 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4CH2CF3 1 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 1 47 1 4-CH=CH2 4-CsCH 4-CH=CHQ 4-〇C-CH2Cl 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 1 | 4-S〇2NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-CI-Ph) 1 I 2-OEt 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 1 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh • 2-N02 2-5-Bu 3-F 3-Me 3-CH2cn 3-SiMe3 3-N(Me)2 線 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh | 4-COPh 1 | r! = f, R2 = F, X = CH2CH2CH2, Y =0, z = s 且r3= 1 | H 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 1 I 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu I I 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 1 | 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe I 3-Et 3-n-Pr 3-(-Pr 3-/i-Bu 3-/-Bu 3-j-Bu 3-r-Bu 1 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-CI-Ph) 3-(4-F-Ph) 1 3-ChCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 1 4-F 4-CI 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CF3 1 | 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 1 1 1 本紙張尺度適用中國®家標隼((:NS ) ΛΒί丨各(210X2W公t ) C 3Q8595 五、發明説明(了5) 經濟部中央標準扃㈢工消费合作呔印裴 4-CH=CH2 4.〇CH 4.CH=CHC1 4-CsC-CH2C1 4-CH2°Me 4-CH2SMc u:r2cn 4-CN 4-N〇2 4-S〇2Mc 4-OMc 4-CHO 4-COMc 4-COOMc 4-S〇2NHMc 4-N(Mc)2 4-SiMe2 4*SF5 4-CH2Ph 4-Ph 4-(4.Ct-Ph) 2-OEt 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Mc ^ch2cn 3-SiMe3 3-N(Me)2 4-f-Bu 4-CH2f 4-C-C5H9 4-C〇NHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R1 =F,R2: H :F, X = CH2CH2CH2. Y 2-F 2-C1 =S, Z = 0 且 R: 2-Br 3= 2-CF3 2-OCF3 2CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-r-Bu 2"CH2CN 2-CH2f 2-Ph 2-CHO 2-COMe 2-COOMc 3-CI 3-Br 3-CF3 3-OCF3 3«CN 3-N〇2 3-OMc 3-Et 3-/j-Pr 3-i-Pr 3-n-Bu 3-i-Bu 3-s-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-CI-Ph) 3-(4-F-Ph) 3-OCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4CF3 4-0CF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-λ-Ργ 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4~CmCH 4-CH=CHCl 4-C=C-CH2CI 4CH2OMe 4CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 4-S〇2NHMe 4-N(Me)2 4-SiMc3 4-SF5 4*CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N02 2小Bu 3-F 3·Μ<5 3-CH2CN 3-SiMe3 3-N(Mc)2 4-f-Bu ‘ch2f 4-c-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh Rl = F· R〕= H Cl, x = ch2ch2ch2, y 2-F 2-CI =0, Z:0 且R3= 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Mc 2-Et 2-/i-Pr 2-/-Pr 2-n-Bu 2-/-Bu 2-i-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-C0Me 2-COOMc 3-Ci 3-Br 3-CF3 3-OCF3 3-CN 3·Ν02 3-OMe 3-Et 3-λ-Ργ 3-/-Fr 3-n-Bu 3-i-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-CI-Phj 3_(4-F-Ph) 本紙涞尺度適用中國國家標隼(CNS ) ,M現格(210x 297公f ) -78 - (請先閲讀背面之注意事項再填寫本頁) 裝i 訂 經濟部中央標隼局員工消費合作杜印裝 Λ7 ___^ A '發明説明(76 ) 3-ChCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4-CH2CF3 4-rt-Bu 4-i-Bu 4-j-Bu 4-λ-Ργ 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-CaCH 4-CHCHC1 4-CsC-CH2C1 4-CH2〇Me 4CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S02Mc 4-OMe 4-CHO 4-COMc 4-COOMc ‘S〇2NHMe 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEi 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMe 4-SEt ‘ocf2h 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-x-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 3-N(Mc)2 4-i-Bu 4-CH2F 4-C-C5H9 4-CONHMe 4^4-F-Ph) 2-COPh 3-COPh 4-COPh R^CU R2 H = C1. X = CH2CH2CH2, Y = 0, z = 0 且 R3= 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMc 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-r-Bu 2-ai2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-OMe 3-Et 3-n-Pr 3-/-Pr 3-n.Bu 3-i-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-CI 4-Br 4-CF3 4-OCF3 4<OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-i-Bu 4-n-Pr 4-i.Pr 4-Et 4-Me 4-CH=CH2 4-qaCH 4-CH=CHCl 4-OC-CH2Cl 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 4-S02NHMe 4»N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-C]-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-x-Bu 3-F 3-Mc 3-CH2CN 3-SiMe3 3-N(Me)2 4-i-Bu ‘ch2f 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R1 =F, R2 = F. X = CH2CH20 (其中0連接在氮原子上),Y=〇,Z=0且R3= H 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMc 2-Mc 2-Et 2-/i-Pr 2-i-Pr 2-n-Bu 2*(-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMc ---------装------訂------^ -線 (請先閱讀背面之注意事項再填寫本頁) _ 家標芈(CNS ) Λ4规格(210X297公釐〉 Α7 Β7 經濟部中央標準局負工消费合作权印11 五、發明説明(Ή )
I 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N02 3-OMc 3-Et 3-n-Pr 3-i-Pr 3-/i-Bu 3-i-Bu 3-j-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4.Cl-Ph) 3.(4-F-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH^Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4.CH2CF3 4-Λ-Βϋ 4-i-Bu 4-x-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-OCH 4-CH=CHC! 4^>C-CH2a 4-CH2〇Me 4CH2SMc 4-CH2CN 4^:N 4-NO2 4-S〇2Mc 4-OMe 4-CHO 4-COMe 4-COOMe 4-S02NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2ph 4-Ph 4-(4-Cl-Ph) 2-OEl 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N02 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-r-Bu 4-COPh 4-CH2F 4-C-C5H9 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh Rl =F. R2 = :F, X = 〇CH2CH2 (其中〇連接在烯碳上),Y=〇, Z=0且R3= H 2^F 2-C1 2-Br 2-CF3 2.OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-nBu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMc 2-COOMe 3-CI 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-λ-Ργ 3-i-Pr 3斗Bu 3-i-Bu 3-j-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-CI-Ph) 3-(4-F-Ph) 3-CsCH 3-C-C5H9 3.SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C! 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-/-Bu 4-x-Ba 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-CsCH 4-CH=CHCl 4-OC-CH2Cl 4-CH2〇Me 4-CH2SMc 4-CH2CN 4-CN 4-NO2 4-S〇2Me 4-OMe 4-CHO 4-COMe 4-COOMe 4-S02NHMe 4-N(Mc)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2.〇Et 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2·Ν〇2 2-j-Bu 3-F 3-Mc 3-CH2CN 3-SiMc3 3-N(Mc)2 4-r-Bu 4-COPh 4-CH2F 4-C-C5H9 4-CONHMc 4-(4-F-Ph) 2-COPh 3-COPh (請先閱讀背面之注意事項再填寫本I) 裝· 訂 丨線 本紙浪尺度適财酬家( CNS ) Λ4Β ( 21()><297公慶)-80 - 308595 五、發明説明(78 ) 表7
F
其中R4*與R4b各自獨立爲Η或R4 R4a = H. R4b = Mc 且 R3= 經濟部中央標準局貝工消費合作社印製 Η 2-F 2-C1 2·Βγ 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-ii-Pr 2-i-Pr 2-rt-Bu 2-i-Bu 2-r-Bu 2-CH2CN 2-CH2f 2-Ph 2-CHO 2-COMe 2-COOMc 3-ΟΪ 3-Br 3-CF3 3-OCF3 3-CN 3·Ν02 3-OMe 3-Et 3-n-Pr 3-Z-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CaCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-σ 4-Br 4-CFj 4.CXT3 4-OCH2CF3 4CH2CF3 4-n-Bu 4-i-Bu 4-5-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-OCH 4.CH=CHC1 4-C^Z-CH2Cl 4-CH2〇Mc 4-CH2SMe 4»CH2CN 4-CN 4-N〇2 4-S〇2Mc 4-OMe 4-CHO 4-COMc 4-CCX)Me 4.S02NHMc 4-N(Me)2 4-SiMc3 4-SF5 4*CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEe 3-SMc 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMe 4-SEt 4.〇CF2H 4-SCF2H 4-〇Ph 4-SPh 2-N02 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-f-Bu 4-CH2F 4-C-C5H9 4«CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R4a = H, R4b = Et 且R3 H 2-F 2-Ci 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-(-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-n-Pr 3-i-Pr 3-n-Bu 3*i-Bu 3-5-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-CCX)Me 3-Ph 3-(4-Cl-Ph) 3,(4-F-Ph) 3-C3CH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc (請先閱讀背面之注意事項再填寫本頁) -裝- 訂 L丨線 '本紙張尺度適财賴家料(CNS ) Λ4規格(21<)/2y7公廣 _ 81 Λ7 B7
五、發明説明(79) I 經濟部中央標準局Μ工消费合作杜印袈 4-F 4-C1 4-Br 4«CF3 4-OCF3 4-〇CH2CF3 4.CH2CF3 4-n-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i.Pr 4-Et 4-Mc 4-CH=CH2 4-OCH 4-CH=CHCl 夂 CsC-CH2C1 4-CH2OMe 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMc 4-COOMc 4-S〇2NHMe 4-N(Me)2 ‘SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(^-a-Ph) 2-OEt 2-SMe 2-SEt 2-〇CF2H 2-SCF2H 2-OPh 2_SPh 3-OEt 3-SMc S-SEt 3-〇CF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Mc 3~CH2CN 3-SiMc3 3-N(Mc)2 4-/-Bu 4-CH2F 4^:-C5H9 -K»NHMe 4-(4*F-Ph) 2-COPh 3-COPh 4-COPh R4a = H, R4t ,=λ·Ργ 且 R3 H 2-F 2-a 2·Βγ 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2W-Pr 2-n-Bu 2-i-Bu 2-r-Bu 2-CH2CN 2-CH2f 2-Ph 2-CHO 2*C0Me 2-COOMe 3-C] 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMc 3-Et 3-n-Pr 3h-Pt 3*n-Bu 3-i-Bu 3-5-Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-COOMe 3-Ph 3-(4-Cl-Ph> 3-(4-F-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-C1 4-Br 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-/-Bu 4-i-Bu 4-n-Pr 4-i-Pr 4-Et 4-Mc 4-CH=CH2 4-CaCH 4^CH=CHCI 4*CaC-CH2CI 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMc 4-COOMe 4-S〇2NHMe 4*N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEc 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEr 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-sa 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3*CH2CN 3-SiMe3 3-NCMc)2 4-r-Bu 4-CH2F 4-c-C5H9 4«C0NHMe 4-(4-F.Ph) 2-COPh 3-COPh 4-COPh R4a = H, R^b =r-Bu 且 R3 H 2*F 2«C 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-E: 2-n-Pr 2-i-Pr 2-n-Bu 2-/-Bu 2-r-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3-N〇2 3-OMc -------^----疼------II---^---1 .,^ (請先閱讀背面之注意事項再填寫本頁) _ 本紙浪尺度通用中國國家標準(CNS ) Λ4現格(21()Χ 297公缝) 經濟部中央標华局Μ工消費合作杜印¾ A7 B7 五、發明説明(80 ) 3-Ει 3-n-Pr 3-i-Pr 3-«-Bu 3-i-Bu 3-j-Bu 3-/-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3_(4«C1-Ph) 3,(4-F-Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-F 4-C1 4-Br 4«CF3 4-OCF3 4-OCH2CF3 ‘ch2cf3 4-n-Bu 4-i-Bu 4-j-Bu 4-η-Ρτ 4-/-Pr 4-Et 4-Me 4-CH=CH2 4-OCH 4-CH=CHa 40C*CH2C1 4-CH2〇Mc 4^H2SMe 4-CH2CN 4-CN 4-NO2 4.S〇2Mc 4-OMe 4^HO 4-COMe 4-COOMc 4-S02NHMc 4-N(Mc)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 4-(4^:l-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-〇Ph 4-SPh 2-N〇2 2-i-Bu 3-F 3-Me 3·€Η2〇Ν 3-SiMe3 3-N(Me)2 4-f-Bu 4^H2F 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R4a = H, R4b = CF3 且 R3 H 2-F 2-CI 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-/i-Bu 2-i-Bu 2-f-Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3-CN 3·Ν〇2 3-OMe 3-Et 3-λ-Ργ 3-i-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-f-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CsCH 3-0C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-CI 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-/i-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4.CH=CH2 4-CaCH 4-CH=CHCI 4-OC-CH2Cl 4-CH2〇Me 4^H2SMe 4-CH2CN 4-CN 4-NO2 4-S02Me 4-OMe 4»CHO 4»COMe 4-COOMc 4-S〇2NHMe 4-N(Me)2 4-SiMe3 4-SF5 4«CH2Ph 4-Ph 4-(4-Ci-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2十Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Mc)2 4-/-Bu 4-CH2F 4-c-CjH^ 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh ----------^------1T--:---^ ▲ (請先閱讀背面之注意事項再,填寫本頁) ___ 4-COPh 本紙張尺度逋用中國國家標隼(CNS ) Λ4規格(210X 297公煃) 五、發明説明(8,i) R4a = H. R4b = Ph 且 R"3 A7 B7 經濟部中央標準局員工消費合作社印製 Η 2-F 2·α 2-OMc 2-Mc 2-Et 2-/-Bu 2-CH2CN 2-CH2F 3-α 3-Br 3»CF3 3-Et 3-n-Pr 3-i-Pr 3-CH2F 3-CHO 3-COMe 3-OCH 3-C-C5H9 3-SF5 4-F 4-C1 4-Br 4-n-Bu 4-i-Bu 4-i-Bu 4-CHsCH2 4-OCH 4*CH=CHa 4-CN 4-N〇2 4-S〇2Mc 4-S〇2NHMc 4-N(Mc>2 ‘SiMe3 2-OEl 2-SMc 2-SEt 3^>Ex 3-SMe 3-SEt 4-OEt 4-SMe 4-SEt 2-N〇2 2-j-Bu 3-F 4-r-Bu ‘CH2F 4-C-C5H9 4-COPh R4a = H, R4t 丨= CH2CN 且 R3 H 2-F 2-a 2-OMe 2-Mc 2-Et 2-/-Bu 2-CH2CN 2*CH2F 3-C1 3-Br 3-CF3 3-Ei 3-/i-Pr 3-i-Pr 3-CH2F 3-CHO 3-COMe 3-OCH 3-C-C5H9 3-SF5 4-F 4-CI 4-Br 4-n-Bu 4-/-Bu 4-j-Bu 4-CH=CH2 4-CaCH 4-CH=CHa 4-CN 4-N〇2 4-S〇2Mc 4-S〇2NHMe 4-N(Mc>2 4-SiMe3 2-OEt 2-SMe 2-SEt 3-OEi 3-SMc 3-SEi 4-OEt 4-SMe 4-SEt 2-Br 2-CF3 2-OCF3 2-CN 2-λ-Ργ 2-i-Pr 2-n-Bu 2-i-Bu 2-Ph 2-CHO 2-COMe 2-COOMe 3-OCF3 3-CN 3-N〇2 3-OMe 3-n-Bu 3-i-Bu 3-i-Bu 3-i-Bu 3-COOMe 3-Ph 3-(4-Cl-Ph) 3-(4-F-Ph) 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMc 4-CF3 4*OCF3 4-〇CH2CF3 4*CH2CF3 4-n-Pr 4-i-Pr 4-Et 4-CH2SMc 4-Me 4-C^C-CH2a 4^CH2°Me 4«CH2CN 4-OMe 4-CHO 4-COMe 4-COOMe 4.SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OCF2H 4-SCF2H 4-〇Ph 4*SPh 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-CONHMc 4-(4-F-Ph) 2-COPh 3-COPh 2-Br 2-CF3 2-OCF3 2-CN 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-Ph 2-CHO 2-COMe 2-COOMe 3-OCF3 3-CN 3·Ν02 3-OMe 3-<-Bu 3-j-Bu 3-r-Bu 3-COOMc 3-Ph 3-(4Cl-Ph) 3-(4-F-Ph) 3-CH2Ph 3.〇CH2CF3 3*CH=CH2 3-CH2SMe 4-CF3 4-OCF3 4*OCH2CF3 4>CH2CF3 4-n-Pr 4-i-Pr 4^Et 4-Me 4*〇3C*CH2a 4*CH2OMe 4<M2SMe 4-CH2CN 4-〇Mc 4-CHO 4-COMe A-COOMc isf5 4-CH2Ph 4-Ph 4-(4-CI-Ph) 2-OCF2H 2-SCF^H 2-OPh 2-SPh 3-〇CF2H 3-SCF2H 3-OPh 3-SPh 4-OCF2H 4*SCF2H 4-〇Ph 4-SPh -------、——^------ΪΤ-----^ ▲ (請先閱讀背面之注I事項再處寫本頁) 本紙張尺度適用中國國家標準(CNS ) Λ4規格(2Ι()Χ 公釐) -84 ΚΊ 經濟部中失標隼局員工消费>作沁印裝 五、發明説明(82 ) 2-N〇2 2-i-Ba 3-F 3-Mc 3-CH2CN 3-SiMe3 3-N(Me)2 4-i-Bu 4-CH2F 4-C-C5H9 4-COPh R4a = H. R4b = CH2〇Me 且 R3 4C0NHMc 4-(4-F-Ph) 2-COPh 3-COPn 請 先 閱 · H 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 讀- 背 ιέ 2-OMe 2-Me 2-Et 2-n-Pr 2-/-ΡΓ 2*n-Bu 2-t-Bu 2-i-Bu 2CH2CN 2-CH2f 2-Ph 2-CHO 2-COMe 2-COOMe 3-C1 3·Βγ 3-CF3 3.OCF3 3-CN 3-N〇2 3-OMe 意· 事 3-Et 3-n-Pr 3-Z-Pr 3-n-Bu 3-i-Bu 3-j-Bu 3-f-Bu 項 再 填· 寫 本 3-CH2F 3<Ή0 3-COMc 3-COOMe 3-Ph 3.(4-CI-Ph) 3-(4-F-Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3^DCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4«CH2CF3 頁 4-«-Bu 4-x-Bu 4-j-Bu 4-n-Pr 4-/-Pr 4-Et 4-Me 4»CH=CH2 4-CaCH 4-CH=CHCl 4-C*C-CH2a 4-CH2OMe 4-CH2SMe 4-012°^ 4-CN 4-N〇2 4-S02Mc 4-OMc 4-CHO 4-COMe 4-COOMc 4-S02NHMe 4-N(Me)2 4-SiMc3 4-SF5 4-CH2Ph 4-Ph 4-(4-CI-Ph) 2-OEt 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEi 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMe 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2·Ν〇2 2-i-Bu 3-F 3_Me 3-CH2CN 3-SiMe3 3-N(Mc)2 4-i-Bu 4-CH2F 4-C-C5H9 4-COPh R4a = Me, R4b*Me 且 R3 4*C0NHMe 4^4-F-Ph) 2-COPh 3-COPh H 2-F 2-C1 2-Br 2-CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-z-Pr 2-n-Bu 2-/-Bu 2-i-Bu 2^Η2〇Ν 2*CH2F 2-Ph 2-CHO 2-COMe 2-COOMe 3-CI 3·Βγ 3-CF3 3.OCF3 3-CN 3-N〇2 3-OMe 3-Et 3-rt-Pr 3-/-Pr 3-n-Bu 3-i_-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMc 3-COOMe 3-Ph 3-(4«a-Ph) 3-(4-F*Ph) 3-OCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C1 4-Br 4-CF3 4-OCF3 4-〇CH2CF3 4-CH2CF3 4-/i-Bu 4-i-Bu 4-j-Bu 4-n-Pr 4-<-Pr 4-Et 4-Me 4-CH=CH2 4-CaCH 4-CH=CHCl 4-OC-CH2Cl 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-S〇2Me 4-OMe 4-CHO 4-COMc 4-COOMe 4-S02NHMe 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-CI-Ph) )A«(^ox 297^vt) - 85 - A7 B7 五、發明説明(83) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SE【 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-〇Et 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-〇Ph 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Me)2 4-r-Bu 4-CH2F 4-C-C5H9 4-CONHMc 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh 經濟部中央橾隼扃.只工消費合作社印裝 R4a = Mc· R4b*Ei 且 R3 H 2-F 2-a 2-Br 2«CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-f-Bu 2-01204 2-CH2f 2-Ph 2-CHO 2-COMc 2-COOMe 3-a 3-Br 3-CF3 3-OCF3 3-CN 3·Ν〇2 3-OMe 3-Et 3-/i-Pr 3-i-Pr 3-/i-Bu 3-i-Bu 3-x-Bu 3-r-Bu 3-CH2F 3-CH0 3-C0Me 3-COOMe 3-Ph 3-(4-Cl.Ph) 3-(4-F-Ph) 3-CaCH 3-C-C5H9 3-SF5 3-CH2ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4-CH2CF3 4-/i-Bu 4-i-Bu 4-i-Bu 4-n-Pr 4-(-Pr 4-Et 4-Mc 4-CH=CH2 4-CaCH 4-CH«CHCl 4-CaC-CH2Cl 4-CH2〇Me 4-CH2SMc 4-CH2CN 4-CN 4-NO2 4-S〇2Mc 4-OMe 4-CHO 4-COMc 4-COOMc 4-S〇2NHMc 4-N(Me)2 4-SiMe3 4-SF5 4-CH2Ph 4-Ph 4-(4-Cl-Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3.〇CF2H 3-SCF2H 3-OPh 3-SPh 4-OEt .4-SMc 4-SEt 4.〇CF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3«CH2CN 3-SiMe3 3-N(Mc)2 4-r-Bu 4-CH2f 4-C-C5H9 4-C〇NHMe 4-(4-F-Ph) 2-C0Ph 3-C0Ph 4-COPh R4a = Mc, R4b=Ph 且r3 H 2-F 2-CI 2·Βγ 2>CF3 2-OCF3 2-CN 2-OMe 2-Me 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-i-Bu 2-i-Bu ^ch2cn 2-CH2F 2-Ph 2-CH0 2-C0Mc 2-COOMe 3-CI 3-Br 3-CF3 3.OCF3 3-CN 3-N〇2 3-0Me 3-Et 3-/i-Pr 3-i-Pr 3-/i-Bu 3-/-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CH0 3-C0Mc 3-COOMc 3-Ph 3-(4-CI-Ph) 3.(4-F-Ph) 3-CsCH 3-c-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3-CH=CH2 3-CH2SMe 4-F 4-C1 4-Br 4-CF3 4.OCF3 4-OCH2CF3 4.CH2CF3 4-n-Bu 4-j-Bu 4-λ-Ργ 4-i-Pr 4-Et 4-Me (請先閱讀背面之注*-事項再'填寫本頁) -装. τβ 丨線 本紙乐尺度適用中®囤家標隼(CNS ) Λ4蜆格(210X297公锋) 五、發明説明(·84) A7 B7 經濟部中央櫟华局只工消资合作杜印裝 4-CH=CH2 4-OCH 4-CH^CHCl 4-Ca〇-CH2CI 4-CH2〇Me 4-CH2SMe 4-CH2CN 4-CN 4-N〇2 4-SO^Me 4-OMe 4-CHO 4-COMc 4-COOMe 4.S〇2NHMe 4-N(Me)2 4-SiMe3 ‘sf5 4-CH2Ph 4-Ph 4-(4-CI-Ph) 2-OEt 2-SMc 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-〇CF2H 3-SCF2H 3-OPh -3-SPh 4-〇Et 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-〇Ph 4-SPh 2-N〇2 2-j-Bu 3-F 3-Me 3*CH2CN 3-SiMc3 3-N(Me)2 4-i-Bu 4-CH2f 4-C-C5H9 4-C〇NHMc 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh R4a = Me, R4b = CF3 且 R3= H 2-F 2-a 2-Br 2-CF3 2.OCF3 2-CN 2-OMe 2-Mc 2-Et 2-n-Pr 2-i-Pr 2-n-Bu 2-/_·Βιι 2-i,Bu 2-CH2CN 2-CH2F 2-Ph 2-CHO 2-COMc 2-COOMe 3-C1 3-Br 3-CF3 3-OCF3 3CN 3-N〇2 3-OMc 3-Et 3-n-Pr 3-ί-Ρτ 3*n-Bu 3-i-Bu 3-j-Bu 3-r-Bu 3-CH2F 3-CHO 3-COMe 3-COOMc 3-Ph 3-(4-C]-Ph) 3-(4-F-Ph) 3-CsCH 3-C-C5H9 3-SF5 3-CH2Ph 3-OCH2CF3 3*CH=CH2 3-CH2SMe 4-F 4-a 4-Br 4-CF3 4-OCF3 4-OCH2CF3 4-CH2CF3 4-n-Bu 4-i-Bu 4-5-Bu 4-n-Pr 4-i-Pr 4-Et 4-Me 4-CH=CH2 4-OCH 4CH=CHCI 4-C^-CH2Cl 4-CH2〇Mc 4-CH2SMe 4-CH2CN 4-CN 4-NO2 4-S02Mc 4-OMe 4-CHO 4-COMc 4-COOMc 4-S02NHMe 4-N(Mc)2 ‘SiMe3 4-SF5 4-CH2Ph 4-Ph 4.(4〇.Ph) 2-OEt 2-SMe 2-SEt 2-OCF2H 2-SCF2H 2-OPh 2-SPh 3-OEt 3-SMe 3-SEt 3-OCF2H 3-SCF2H 3-OPh 3-SPh 4-OEt 4-SMc 4-SEt 4-OCF2H 4-SCF2H 4-OPh 4-SPh 2-N〇2 2-s-Bn 3-F 3-Me 3-CH2CN 3-SiMe3 3-N(Mc)2 4-nBu 4-CH2F 4-c-CjHq 4-CONHMe 4-(4-F-Ph) 2-COPh 3-COPh 4-COPh __________裝------訂-----^ -線 (請先¾讀背面之注*·事項再填寫本頁) _ )錢格(21&297公廣)-87- 經濟部中夬榡率局員Η消贽合作ή印¾ A7 ____87_五、發明説明(85 ) 配方/用途 本發明之化合物通常與農業上適合之載劑一併用於製 成配方或組成物,該載劑包括至少一種液體稀釋劑,固體 稀釋劑或界面活性劑。此配方或組成物之組份的選擇係爲 了與下列因素配合一致:活性組份之生理特性,施藥模式 及環境因素諸如土壤種類,濕度與溫度》 實用的配方包括液體類,例如溶液(包括可乳化濃縮 液),懸浮液,乳液(包括微滴乳液及/或懸乳液)及其 它可任意增凝膠之液體。資用的配方另包括固體類,例如 粉劑,散劑,粒劑,丸劑,錠劑,薄膜類及可在水中分散 (^可濕化^ )或可溶水之其它固體。活性組份可被(微 )包入膠囊並進一步形成懸浮液或固體配方;或者具有活 性組份之完整配方可包入膠囊(或^塗覆表面^ )。包入 膠囊之作用可控制或緩釋活性組份》可噴霧配方可在適當 介質中擴展並以每公頃約1至數百公升之噴霧劑量使用。 高張組成物主要用於作爲其它配方之中間產物。 配方類通常含有有效量之活性組份,稀釋劑及界面活 性劑,其具有下列以重量百分比表示之大約範圍。 J 裝 訂I . 線 (請先閱讀背面之注意事項再略寫本頁) 本紙张尺度適用中阗國家標芈(CNS ) Λ4^烙(2丨0.<297公釐) _ 88 _ 五、發明説明(86 A7 B7 可分散水中及可水溶 的粒劑,錠劑及散劑 懸浮液,乳液,溶液 (包括可乳化濃縮液) 粉劑 粒劑與丸劑 重量百分比 活性組份 稀釋劑 界面活性劑 5-90 0-94 1-15 5-50 1-25 40-95 70-99 0.01-99 5-99.99 0-15 0-5 0-15 請 先 閲 讀 背 ιέ 之 注 意. 事 項 再 填* 馬 裝 本衣 頁 高張組成物 90-99 0 - 1 0 0 -2 傳統固體稀釋劑描述於Watkins, et al., Handbook of Insecticide Dust Diluents, and Carriers, 2nd Ed .,Dorland Books, Caldwell, New Jersey。傳統液體稀 釋劑描述於 Marsden, Solvents, Guide, 2nd Ed.,
Intersc i ence, New York, 1 9 5 0 e McCutcheon' s Detergents and Emulsifiers Annual, Allured Pub1. Corp., Ridgewood, New Jersey,與 Sisely and Wood, Encyclopedia of Surface Active Agents, Chemical Publ. Co., Inc., New York, 1964列示出界定活性劑及建 議用法。所有配方皆可含有少量添加劑以減少泡沫,結塊 ,侵蝕,微生物生長等等,或含有少量增稠劑以增加黏度 本紙悵尺度適用中國國家標準(CNS ) Λ4规格(2丨0X297公釐) 訂 經濟部中央標嗥局只工消#4'作社印狀 - 89 _ J8595 a7 B7___ 五、發明説明(87) 界面活性劑包括聚乙氧化醇類,聚乙氧化烷基酚類’ 聚乙氧化山梨糖醇酐脂肪酸酯類,二烷基硫代丁二酸類’ 烷基硫酸鹽類,烷基苯磺酸鹽類,有機矽化物類’ N ’ N 一二烷基牛磺酸鹽類(taurates),木質素磺酸鹽類’某 磺酸鹽類,甲醛冷凝物類,聚羧酸鹽類,及聚氧化乙烯/ 聚氧化丙烯成塊共聚物。固相稀釋劑,舉例而言,包括黏 土類例如膨潤土,蒙脫土,活性白土與高嶺土,澱粉’葡 萄糖,矽土,滑石,矽藻土,尿素,碳酸鈣,碳酸鈉及重 碳酸鹽,及硫酸鈉鹽。液體稀釋劑,舉例而言,包括水’ N,N —二甲基甲醯胺,二甲亞砚,N —烷基吡咯烷酮, 乙二醇,聚丙二醇,石蠟,烷基苯,烷基菓,橄欖油,箆 麻油,亞麻子油,桐油,玉米油,花生油,棉子油,大豆 油,油菜子油與椰子油,脂肪酸酯類,酮類〔諸如環己酮 ’ 2 —庚酮,異佛爾酮(isophorone),與4 —擬基—4 _甲基一2—戊酮〕,及醇類(諸如甲醇,環己醇,癸醇 及四氫糠醇)。 溶液(包括可乳化濃縮液)可藉由簡單混合組成份而 製得。粉劑與散劑之製備可藉由調和法且通常在鎚棒式磨 粉機或流力磨粉機中磨成粉。通常以濕磨法製備懸浮液, 例如,可參見美國專利案第3,060,084號。粒劑 與丸劑之製備可將活性物質噴霧在預成形之顆粒性載劑之 上’或者利用凝聚技術。請參見Br owning所著’ Agglomeration’ , Chemical Engineering, 1 9 6 7 年 12月 4 日,第147—148 頁:Perry's Chemical 本紙張尺度適甩t闽國家標準(CNS ) Λ4現格(21U x 297公釐)〇Λ I- I^ΪΤ--1--- (請先閱讀背面之注意事項再4'寫本頁) 經濟部中央標隼局si工消费合it权印掣 A7 __B7_ 五、發明説明(88 )
Engineer’s Handbook,第 4版,Me Graw-Hill, New York, 1963,第8 — 57頁及其後績發表文獻,以及 W 0 9 1/1 3546。丸劑之製備可根據美國專利案 第4,1 7 2,7 1 4號所述。製備可分散水中及可水溶 的顆粒可根據U · S · 4,144,050, U.S-3,920,422 與 DE 3 ,246 ,493教示者。製備錠劑可根據11· S-5,180,687,U-S_5,232,701 與U · S · 5 ,208,030教示者。製備薄膜可根據 〇82,095,558與1]-8-3,299,566 教示者。 有關配方此藝之其它資料,請參見美國專利案第 3 ,235 ,361號,第6欄第16行至第7欄第19 行與實施例10_41;美國專利案第 3 ,309 ,192號第5欄第43行至第7欄第62行 與實施例8,12,15,39,41,52,53, 58,132:138-140,162-164-166 ,167及169 — 182 ;美國專利案第 2 ,89 1 ,855號第3欄第66行至第5欄第17行 與實施例 1 — 4 ; Klingman, Weed Control as a Science, John Wiley and Sons, Inc., New York, 1961, pp81-96;及 Hance 氏等人,Weed Control
Handbook, 8th Ed. , Blackwell Scientific 本紙張尺度適用个囤國家標隼(CNS M4規格(210,<297公釐) -------(---^------ir--1---- '0 (請先閱讀背面之注€-.事項再贫寫本頁) ~ 91 A7 _________B7五、發明说明(89 ) Publications, Oxford,1989°下列實例中,所有百分比係按重計且所有配方係以習 知方法製備。化合物編號參見索引表A — C中的化合物。 tM_A_ 可濕化的散劑 化合物2 3 十二烷基酚•聚乙二醇醚 木質素磺酸鈉 矽鋁酸鈉 蒙脫石(經煅燒者) 賨例B 粒劑 化合物2 3 活性白土顆粒(低揮發性物質, 0.71/0. 30 毫米;U.S.S·編號 25-50 篩孔) 6 5.0%2.0% 4.0%6.0¾ 23.0¾ 10.0¾ 90.0% (請先閱讀背面之注*.事項再贫寫本頁} 裝·
-'D -線 經濟部中央標隼局Mx消费合作ΐ印彀
賨例C 模壓丸劑 化合物2 3 無水硫酸鈉 粗製木質素磺酸鈉 烷基某磺酸鈉 25. 〇% 10.0¾ 5.0¾ 1.0% 本紙張尺度適用中困國家標率(€地),\4現格(210,<297公釐) 經濟部中央標苹局只工消费合作杜印焚 A7 B7 五、發明説明(9〇) 鈣/鎂膨潤土 59.0% 窗例D 可乳化澹縮液 化合物2 3 20.0% 可溶油之磺酸鹽與 聚氧化乙烯醚類的混合物 10.0¾ 異佛爾酮 70.0¾ 本發明化合物呈現拮抗廣泛種類之食葉性’食果實性 ,食莖性或食根性,食種子性,水生性及土壤寄生性節肢 動物節肢動物〃乙詞包括昆蟲類蝨類及線蟲類)的活 性,這些節肢動物及生長中及保存下之裊作物,林業,溫 室農作物,景觀植物,曲圃農作物,保存食品及嫌維產物 ,家畜,家務,及公共衛生與動物健康的害蟲。熟悉此藝 之士將了解,並非所有的化合物與對抗所有害蟲之全部生 長期皆爲同等有效。然而,本發明之全部化合物呈現拮抗 下列害蟲之活性:鱗翅目之卵、幼蟲及成蟲,鞘翅目之卵 ,食葉性,食果實性,食根性及食種子性幼蟲與成蟲;半 翅目與同翅目之卵,未成熟幼蟲及成蟲;蟎目之卵,幼蟲 ,蛹及成蟲;雙尾目,直翅目與革翅目之卵,未成熟仔蟲 及成蟲;雙翅目之卵,未成熟仔蟲及成蟲;以及線蟲門之 卵,保幼蟲與成蟲。本發明之化合物亦對膜翅目等翅目, 蚤目,排蠊目,雙尾目,嚙蟲目害蟲:以及屬於蛛形網與 海明寬翅門(phylum platyhelminthes)之害蟲有捨抗活 本紙悵尺度通m阁家標準·( CNS ) Λ4规格(210X297公釐) -------「—裝------訂-----1 _線 (請先閱讀背面之注*.事項再#寫本頁) -93 - A7 經濟部中央標準局!工消費合作杜印製 B7五、發明説明(gi) 性〇詳言之,此化合物對下列有拮抗活性:南方玉米根蟲 (-f--星瓜葉甲 Diabrotica undecimpunctata howardi ) ,星葉蚱猛(Mascrosteles fascifons),英殼蛄蟹( A n t h ο η 〇 m u s g r a n d i s ) ’ 兩點細蛛 Sf ( T e t r a n y c h u s u r 1: i c a e ),秋兵蟲(草地黏蟲 S p o d o p t e r a f r u g i p e r d a ) ,黑豆财蟲(Aphis fabae),綠桃贬蟲(Myzus persica ),棉财蟲(Aphis gossypii),蘇俄麥贬蟲( Diuraphis noxia),英國穀物呀蟲(Sitobion avenae) ,煙草芽蟲(Heliothis virescens),水稻蛄蟹( Lissorhoptrus oryzophilus),稻葉甲蟲(Oulema oryzae),白背植物蚱猛(Sogatella furcifera),綠 葉蚱猛(Nephotettix cincticeps),棕色植物蚱猛( Nilapervata lugens),小掠色植物蚱猛(Laodelphax striatellus),稻莖鑭!孔蟲(Chilo suppressalis), 稻葉滾輪蟲(Cnaphalocrocis medinalis),黑稻臭蟲( Scotinophara lurida),稻臭蟲(Oebalus pugnax), 稻蟲(Leptocorisa chinensis),纖細稻蟲(Cletus puntiger),與南方綠臭蟲(Nezara viridula)。此化 合物對蝨類有掊抗活性,證實對葉蟎此科具殺卵,殺幼蟲 與化學消毒活性,包括由地凱葉蟎(Tetranychus urticae) ’ 米砂葉摘(Tetranychus cinnabarinus), 麥克旦葉蟎(Tetranychus mcdarieli),太平洋葉痛( Tetranychus pacificus) ,土格斯坦葉彌(Tetranychus turkestani) ’ Byrobia rubrio cuius,蘋果紅御蛛( 請 先 閲 讀 背 ιέ 之 注 項 募裝 訂 線 本紙張尺度if州中阈阈家標準(CNS ) Λ4規格(2ΚΓΧ 297公釐) 94 經濟部中央橾準局只工消費合if社印¾ A7 ___B7__ 五、發明説明(92 )
Panonychus ulmi),橘全爪痛(Panonychus citri), 鶴耳櫪東方葉瞒(Eotetranychus carpini borealis), 海可瑞東方葉锻(Eotetranychus hicoriae),六點東方 葉蟎(Eotetranychus sexmaculatus),由門西斯東方葉 畴(Eotetranychus yumensis),本可斯東方葉瞒( Eotetranychus banksi)與草地小爪瞒(Oligonychus pratensis);瞒科包括橘短須彌(Brevipalpus lewisi ),風尼西斯須痛(Brevipalpus phoenicis),加州須 瞒(Brevipalpus californicus)及卵圓短須瞒( Brevipalpus oboratus);瘿補科包括橘绣痛( Phyllocoptruta oleivora),影澳瞒(Eriophyes sheldoni),桃銀色刺澳瞒(Aculus cornutus),梨葉 绣蟎(Epitrimerus pyri)與孟格費勒澳畴(Eriophyes mangiferae)。有關害蟲說明之更詳細資料可參見W0 90/10623 與 W0 92/00673。 本發明之化合物亦可混合一種或一種以上的殺昆蟲劑 ,殺真菌劑,殺線蟲劑,殺菌劑,殺壁蝨劑,生長調節劑 ,化學消毒劑,半化學品,推進劑,誘引劑,費洛蒙,攝 食刺激劑或其它生物活性化合物,藉以形成多種組成份之 殺害蟲劑而提供較廣範圍之農業保護。這種與本發明化合 物混合而得之農業保護劑可調配爲:殺昆蟲劑,例如阿巴 麥克汀(abamect in ),乙醯胺基硫代二甲-磷酸鹽( Acephate),枯死靈(Azinphos-Methyl),坪芬辛( bifenthrin),布波费仁(buprofezin),卡波富蘭( 本紙張尺度適用中國國家標準(CNS ) Λ4坭格(210X 公埯) -------^---^------1T---^---: ▲ (請先閱讀背面之注意’事項再斯寫本頁) -95 - 翅濟部中央標準局Mx消費合作杜印取 A7 ________B7 五、發明説明(93) carbofuran),毒絲苯(chlorpyrifos),甲基毒絲苯( chlorpyrifosiethyl),塞佛辛(Cyfiuthrin),冷一 塞佛辛(beat-cyfluthrin),代耳它麥辛(delta methrin),代耳芬素隆(diafenthiuron),代艾辛濃( diazinon) ’代佛本夫隆(diflubenzuron),代美索艾 特(dimethoate) ’ 伊絲芬瓦勒瑞(esfenvalerate), 芬剖帕辛(fenpropathrin),瓦勒瑞(fenvaierate), 剖尼(fipronil) ’ 富塞辛南(flucythrinate) ,λγ — 福瓦林奈得(tau-fluvalinate),風那福(f〇n〇phos) ’大可洛派(imidacloprid) ’ 異芬風(isofenphos) ,馬拉松(malathion),聚乙醛(metaldehyde),美 沙米多風(methamidophos),美西達辛(methidathion )’索麥(methomyl),麥修普令(methoprene),甲 氧氯(methoxychlor) ’ 莫諾閱特風(monocrotophos) ’氨基乙二酿一巴拉松(oxamyl parathion),甲基巴拉 松’剖美辛(permethrin),福瑞特(phorate),佛殺 隆(phosalone),佛斯美(phosmet),佛斯法米冬( phosphamidon),比利米卡(priimicarb),波芬諾佛 (profenofos),魚藤酮(rotenone),沙波佛斯( snlprofos),布芬諾里(tebu fenozide),鐵佛辛( tefluthrin),特布風(terbufos),四氣賓福( tetrachlorvinphos),硫化二卡布(thiodicarb),托 羅美辛(tralomethrin),杜貢(Trichlorfon)與三氟 木隆(triflumuron):殺真菌劑,例如氧化偶氮斯冬賓 本紙張尺度通汨中阐國家標隼(CNS ) Λ4現格(210X 297公釐) 1 裝------訂-----^ ·線 (請先閱讀背面之注意事項再埃寫本頁) -96 - A 7 B7 經濟部中央樣準局工消舟分作社印紧 五、發明説明(94) (azoxystrobin, ICIA 5504) ’ 苯諾米(benomyl),巴 斯丁素—S (blasticidin-S) ’ 得克斯(Bordeaux)混 合物(三喊基硫酸銅),博木空納哩(bromuconazole) ,凱普它佛(captafol),凱普坦(capton),卡苯大辛 (carbendazim),氯奈布(chloroneb) ’ 克羅沙隆尼 (chlorothalonil) ’氣氧化亞銅’銅鹽,塞莫山尼( cymoxanil),塞波空那哩(cyproconazole),塞波地 尼(cyprodinil,CGA 219417),載可美辛( diclomezine),大可藍(dicloran),大分諾可那哩( difenoconazde),二甲莫(dimethomporph),大尼空 那嗤(diniconazole),大尼空那哩一M,多丁(dodine ),艾迪芬福(edifenphos),環氧可納唑( epoxyconazole, BAS 480F),菲那林莫(fenarimol), 芬布可納哩(fenbuconazole),芬批可隆尼( fenpiclonil),波批定(fenpropidin),芬波批模( fenpropi morph ),福昆可納哩(fluquinconazole ), 福斯拉哩(flusilazole),福托蘭尼(flutolanil ), 福差耳佛(flutriafol),福樂培(folpet),佛沙基銘 (fosetyl-aluminum),佛拉勒克基(furalaxyl),六 可納哇(hexaconazole),艾波可納哩(ipconazole ) ,伊波苯佛(iprobenfos),伊波二酮(iprodione), 異波塞歐蘭(isoprothio lane),卡蘇加徽素( kasugamycin),甲基克梭新(kresoxim-methyl,BAS 490F) ’ 曼可瑞(mancozeb),曼奈柏(maneb),美波 本紙張尺度通州中囤囤孓標準(CNS ) Λ*»坭咯(21UX2W公t ) (請先聞讀背面之注意事項再填寫本頁) 裝. 訂 ——線 經濟部中央樣隼局N工消費合作托印f A 7 B7_ 五、發明説明(95 ) 尼(m e p r ο n i 1 ) ’金屬拉克斯基(m e t a 1 a X y 1 ),曼托可 納唑(metconazole),麥可布丹尼(myciobutanil), 新-艾梭辛(neo-asozin,甲烷胂酸鐵),D等二克斯基( oxadixyl),片可納唑(penconaz〇ie),片塞苦隆( pencycuron),波苯納唑(pr〇benazole),波可洛拉( prochloraz),波比克納哩(propiconazole),社利费 諾(p y r i f e η ο X ),焦 _ 隆(p y r 〇 q u i 1 〇 η ),硫磺,特布 可諾唑(tebuconazole),四可納唑(tetraconazole) ’塞本大哩(thiabendazole) ’ 睡吩甲酯(thiophanate -in e t h y 1 ) ’ 捷絪(t h i r a m ),三阿 丁美風(t r i a d i m e f ο η ),三阿丁美諾(tricyclazole),三環哩( triticonazole),三特可納唑(triticonazole),單可 納唑(uniconazole),維力大黴素(validamycin)與文 可容林(vinclozol in );殺線蟲劑,例如阿打克卡( aldoxycarb)與芬納米風(fenamiphos);殺菌劑,例如 鍵撇素,殺壁蟲劑’例如阿米嗟(amitraz),辛若美塞 男(chinomethionat) ’ 氣苯日醋(chlorobenzilate) ,凱黑殺汀(cyhexatin),代可風(dicofol),代恩諾 闊(dienochlor) ’ 芬納者昆(fenazaquin),芬不特丁 (fenbutatin),氧化物’芬波帕辛(fenpropathrin) ,芬派洛辛美(f e n p y r ο X i m a t e ),海西塞容( hexyth i azox ),帕捷(proparg i te ),大苯(pyridaben )與布芬瑞得(tebu fen py rad ):以及生物製劑,例如蘇 雲金芽孢桿菌(Bacillus thuringiensis),蘇雲金芽孢 本紙張兄度通州中國國家標準(CNS ) A4规格(210x2V公釐) . 裝 訂 ^ —線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標弟局只工消费合作'ft印製 A7 __B7 _ 五、發明説明(90 ) 桿菌delta內毒素,杆狀病毒(baculovirus),及對蟲媒 致病之細菌,病毒與真菌。 有些情況下,與具有類似控制範圍但不同作用模式之 其它節肢動物殺除劑組合,將對抗藥性管理特別有利。 對控制害蟲(使用率或使用範圍)或抗薬性管理更好 的較佳者爲本發明之化合物與一種選自下列之節肢動物殺 除劑之混合物:阿巴麥克二了(abamectin),非剖芬剖 帕辛(fenpropathrin),非剖尼(fipronil),咪大可 洛派(imidacloprid),美索麥(methomyl),波帕捷( p r 〇 p a g i t e ) ,tt 大苯(p y r i d a b e η ),塔布芬諾里( tebufenozide)與特布芬瑞得(tebufenpyrad)。尤其佳 的混合物(化合物編號請參照索引表A - C)係選自下列 包括:化合物1與阿巴麥克汀;化合物1與非剖芬剖帕辛 ;化合物1與非剖尼;化合物1與咪大可洛派;化合物1 與美索麥;化合物1與波帕捷;化合物1與吡大苯;化合 物1與塔布芬諾里;化合物1與特布芬瑞得; 化合物7與阿巴麥克汀;化合物7與非剖芬剖帕辛; 化合物1與非剖尼;化合物7與咪大可洛派;化合物7與 美索麥;化合物7與波帕捷;化合物7與吡大苯:化合物 7與塔布芬諾里;化合物7與特布芬瑞得; 化合物1 5與阿巴麥克汀;化合物1 5與非剖芬剖帕 辛;化合物1 5與非剖尼;化合物1 5與咪大可洛派;化 合物1 5與美索麥;化合物1 5與波帕捷;化合物1 5與 吡大苯;化合物1 5與塔布芬諾里;化合物1 5與特布芬 本紙張尺度遇用中闽國家標準(CNS ) Λ4現格(210X 297公缓> _ % _ " '裝 訂 線 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標隼局.只工消费含作社印裝 A7 _ _B7__ 五、發明説明(97) 瑞得; 化合物1 9與阿巴麥克汀;化合物1 9與非剖芬剖帕 辛;化合物1 9與非剖尼;化合物1 9與咪大可洛派;化 合物1 9與美索麥;化合物1 9與波帕捷:化合物1 9與 吡大苯;化合物19與塔布芬諾里;化合物19與特布芬 瑞得: 化合物2 3與阿巴麥克汀;化合物2 3與非剖芬剖帕 辛;化合物2 3與非剖尼;化合物2 3與咪大可洛派;化 合物2 3與美索麥:化合物2 3與波帕捷;化合物2 3與 吡大苯;化合物2 3與塔布芬諾里;化合物2 3與特布芬 瑞得; 節肢動物害蟲受到控制且達成保護農藝,園藝,及特 級農作物,動物與人類健康,係藉由施用本發明有效量之 一種或一種以上的化合物至害蟲所處環境包括害蟲橫行之 農業區及/或非農業區,欲保護地區,或直接施用在欲控 制之害蟲身上。因此,本發明進一步包括一種方法,其係 用於控制寄生葉與土壤之節肢動物與線蟲害蟲及用於保護 農業與非農業作物,包括將一種或一種以上之本發明化合 物,或含有一種以上之道類化合物,以有效量施用至害蟲 所處環境,包括害蟲橫行之農業區或非裊業區,欲保護地 區’或者直接施用至害蟲身上。較佳應用方法係噴霧法》 或者’這些化合物之顆粒配方可施加至植物葉上或土壤。 其它應用方法包括直接並後遺式噴霧法,區域式噴霧法, 種子塗覆,微包囊法,全身攝入法,誘餌法,耳牌,大丸 _本紙張尺度適用中國國家樣隼(〇奶)八4現格(210:<297公釐)~ -100 - -------;---^------1T------- —0 (請先閱讀背面之注t-事項再填寫本頁) 經濟部中央標準局·負工消費合作让印裝 A7 B7 五、發明説明(9S ) 劑,家畜看護器,燻蒸消毒劑,噴霧殺蟲劑,粉劑等等。 這些化合物可併入透餌中而被節肢動物吃掉或置入捕捉節 肢動物之裝置中等等。 本發明之化合物可以純化狀態施用,但最常的應用是 製成配方,此配方含有一種或一種以上之化合物,以及適 合載劑,稀釋劑,及界面活性劑,可能與食物混合,須視 意欲之最終用途而定》較佳應用方法包括噴灑水懸浮液或 精製此化合物之油溶液。與噴霧用油類,噴霧用油之濃縮 ,噴霧器黏貼劑,佐劑,其它溶劑及諸如胡椒基丁醚之類 的增加劑混合,通常會增加化合物效力。 達到有效控制所需之施用率將由諸如下述之因子決定 :欲控制之節肢動物種類,害蟲生活史,生活週期,軀體 大小,所處位置,時間,宿主作物或動物,攝食行爲,交 配行爲,流通濕度,溫度等等》正常情況下,每公頃約 0. 01至2公斤活性組份之施用率足以控制農業環境系 統中的害蟲,但僅0. 001公斤/公頃即爲足夠或可能 需要高達8公斤/公頃。非裊業應用時,有效使用率介於 約1. 0至50毫克/平方公尺,但也許僅0. 01毫克 /平方公尺即已足夠或可能需要高達1 5 0毫克/平方公 尺。 下列試驗證實本發明化合物對特定害蟲之控制效力。 ^控制效力〃表示節肢動物發展(包括死亡率)之抑制作 用,此作用明顯造成攝食減少。然而,這些化合物提供之 害蟲控制性保護作用不受這些害蟲種類的限制。化合物說 本紙張尺度適用中國國家標準(CNS ) Λ4現格(210Xm公釐) ΓΓ~ -101 - (請先閱讀背面之注t事項月填寫本頁) --裝. -3 .U丨線 A7 B7
五、發明説明(99 ) 明可參見索引表A — C »下列縮寫係用於索引素中:t = 三級,Me=甲基,Et=乙基,Bu= 丁基,Ph=苯 基,OMe=甲氧基,OE t=乙氧基,CHO =甲醯基 ,CN=氣基,且TMS=三甲基甲矽烷基。索引# A
F
請 先 閱 讀 背 A 之 注 意 事 項 再 窝 本 頁 裝 化合物編號 編航 P ε! m.o. (00 1 Ex. 1 Η 4-CI 131-134 2 Η Η oil* 3 2-CI 4-C1 159-160 4 Η 4-r-Bu 154-155 5 Η 4-Ph 130-131 6 Η 4-Ph (£-isomer) 120-124 7 Η 4-CF3 160-161 8 3-CF3 4-OEt 147-148 訂 線 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家梯準(CNS ) A4規格(210X 297公釐) 102 - B7 五、發明説明(100) 9 Η 3-α 117-119 】0 3-F 4-F 170-171 11 Η 3-CF3 103-104 12 Η 3-F 107-109 13 Η 3-Br oil* 14 3-F 4-OEt 139-140 15 Η 4·(4·α-Ρ« 153-154 16 Η 2-(4-CI-Ph) 170-174 irh, \ Η 3-(4-Cl-Ph) oil· 18 Η 4-(3-Cl-4-F-Ph) 163-165 19 Η 4-(4-F.Ph) 160-161 20 Ex. 2 Η 4-1 165-167 21 Η 4-(3-CF3-Ph) 150-152 22 Η 4-(4.CF3-Ph) 194-196 23 Ex. 3 Η 4-(2,4-diCl-Ph) 151-153 24 Ex. 4 Η 4-C^:-TMS 123-124 25 Η 4-(2-F各 OMe-Ph) 155-158 26 Η 4-(4-CN-Ph) 179-180 27 Η 4-(2-CHO-Ph) oil* 1% Η 4-(4-F-3-Me-Ph) 96-99 29 Η 4-(2-F-Ph) 120-121 30 Η 4-(2-Cl-Ph) oil* 31 Η 4-(2-CF3-Ph) oil* 32 Η 4-(2-Mc-Ph) 90-92 33 Η 4-(l-naphthaIenyI) 168-169 34 Η 4-(4-F-2-OMe-Ph) oil* 35 Η 4-(2-CI-6-OMe-Ph) oil* 經濟部中央標隼局員工消費合作社印聚 a.除非另外陳明,所有化合物根據1H NMR數據而歸類爲Z-異構物類。 *參見索引素C之1H NMR數據。 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) ---------II------1Τ------ ά. (請先閱讀背面之注意事項再填寫本頁) — 103 - A7 B7 五、發明説明(1〇l)
索引表B
Q
Q
化合物編號a Q. 熔點(°C ) 36 2-棻基 油* 37 1-棻基 油* a.除非另外陳明,所有化合物根據1H NMR數據而歸類爲Z-構物類。 *參見索引素C之1H NMR數據。 --------—扣衣------ΪΤ-----Φ (請先閱讀背面之注意事項再略寫本頁) 經濟部中央標準局員工消費合作杜印製 本紙張尺度適用中國國家橾準(CNS ) Λ4規格(210X:297公釐) 經濟部中央標隼局員工消费合作社印裝 A7 _ B7___五、發明説明(102、 索引表c化合物 1 H NMR數據(除非特別指明,否則在CDC 1 3編號 溶液中)β 2 84.48 (m.lH), 4.68 (t,lH), 5.20 (dd,2H), 6.33 (s,lH), 6.55 (dd.lH), 7.02 (t.2H), 7.26 (t,lH). 7.35 (t,2H), 7.50 7.68 (d,2H). 13 54.47 (dd.lH), 4.68 (ι,ΙΗ), 5.45 (d,lH), 5.53 (d,lH), 6.24 (s,]H), 6.51 (dd.lH), 7.03 (t,2H), 7.21 7.37 (d,lH), 7.49 (m,2H). 7.87 (s,lH) 17 54.47 (m,lH), 4.68 5.46 (d,lH), 5.53 (d,lH). 6.38 (s,lH), 6.53 (m,lH), 7.02 (t,2H), 7.42 (m,5H). 7.51 (m,2H), 7.62 7.86 (s,lH) 27 δ 4.40 4.69 5.49 (d,lH), 5.56 (d.lH), 6.39 (s.lH), 6.55 (m,lH), 7.03 (t,2H), 7.36 (d,2H), 7.49 (m,3H), 7.64 (m,lH), 7.76 (d,2H),. 8.01 (d,lH), 10.01 (s,lH) 30 5 4.400 (m,lH), 4.687 5.530 (d,lH). 5.572 (d,lH), 6.391 (s.lH). 6.700 (m.lH), 7.026 (t,2H), 7.281 (m,5H). 7.488 (m,2H), 7.698 (m.2H) 31 5 4.477 (m,lH), 4.683 (m.lH), 5.459 (d,lH), 5.537 (d.lH), 6.381 (s.lH), 6.537 (m,lH), 7.022 (t,2H), 7.340 (m,3H), 7.482 (m,2H), 7.536 (m.lH), 7.695 (m,3H) 34 δ 3.80 (s,3H), 4.51 (τη,ΙΗ), 4.70 (m,lH), 5.45 (d,lH), 5.53 (d,lH), 6.36 (s,lH), 6.52 (m,lH), 6.72 (m,2H), 7.02 (m,2H), 7.27 (m,lH), 7.49 (m,3H), 7.69 (d,2H). 35 δ 3.73 (s,3H), 4.48 (m,lH), 4.68 (m,lH), 5.45 (d,lH), 5.53 (d,lH), 6.39 (S,1H), 6.53 (m.lH), 6.88 (d,lH), 7.03 (m,2H), 7 25 (m,3H), 7.49 (m,lH), 7.75 (d,lH) ---------餐------、訂-----^ ▲ (請先閱讀背面之注意事項再亦寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐> 105 - A7
3〇8S9S ___B7_ 五、發明説明(l〇3) e 1H NMR數據係以自四甲基甲矽烷向下算之ppm表示。成 對者表示爲(s)_單峰,(d)-雙峰,(t)-三峰,(m)-多峰,(dd) -成對雙峰》 本發明夕牛物奮施例 試驗A 秋兵蟲 製備測試單位,每單位含有16格之Η,I ,S,( 高壓縮苯乙烯)槽。將潮濕濾紙與約8平方公分之蚌形大 豆葉置入12個格子中。將一層0. 5公分之麥源供應食 品置入其餘4格。將1 5至2 3隻秋兵蟲(草地黏蟲)內 星幼蟲置入2 3 0毫升(8盎斯)塑膠杯中。將每一種測 試化合物之溶液(於7 5 : 2 5之丙酮—蒸餾水溶劑中) 噴瀾至槽中與杯中。完成噴灑作業係將置於運輸帶上的槽 與杯,直接通過平面風扇水力噴嘴的下方,此噴嘴放出的 噴霧率爲每公頃0. 5 5仟克之活性組份(約每英畝 0. 5磅),207KPa(30p. s. i)。將昆蟲
由230毫升杯轉移至Η· I. S.槽(每格一隻昆蟲) 。將槽加蓋並保留在2 7 °C與5 0%相對濕度下,歷4 8 小時,然後判讀蛘形大豆葉之1 2個格子。其餘4格在第 6 - 8天判讀,因爲要延遲毒性作用。所測試的化合物中 ,下列it电物表現8 0 %或8 0 %以上之控制效力:化合 f 物 2 0/V 兩點蜘蛛蝨 本紙張尺度過州中國國家標準(CNS ) A4規格(21〇Χ 297公釐) ------------私衣------iT------ ά. (請先閱讀背面之注t事項再奏寫本頁) 經濟部中央標準局員工消费合作社印繁 經濟部中央標準局Μ工消費合作杜印取 A7 _B7_五、發明説明(1〇4) 試驗B 多片腎豆葉,每片葉面稹約6 _ 5平方公分(1平方 英时)且事先在背面以2 5至3 0隻蝨成蟲( Tetranyehus urticae)感染’將葉背面朝向水力噴霧器 ’以含測試化合物(於7 5 : 2 5之丙酮—蒸餾水溶劑中 .)之溶液噴霧。噴灑完成係將置於輸送帶上的幼蟲直接通 過平面風扇水力噴嘴下方’該噴嘴之噴霧率爲每公頃 0. 55仟克活性組份(約每英畝〇. 5磅)’ 207KPa (30p. s. i)。葉小格再反面朝上置 於培養皿中濕棉花之上,以攝子將葉小格之半徑填塞至棉 花上方,如此蝨才不會逃逸至未處理的葉表面上。測試單 位保持在2 7 °C與5 0%相對濕度下,歷4 8小時’然後 進行死亡率的判讀。所測試的化合物中’下列化合物呈現 8 0%或8 0%以上的死亡率: 相同單位再保存5天並判讀殺幼蟲/殺卵之死亡率及 /或發展影響。這些化合物中,下列化合物呈現8 0 %或 8 0%以上的活性:化合物2 0。 試驗C 兩點細蛛S (Tetranychus urticae)幼蟲 製備測試化合物溶液’其係將測試化合物溶於極少量 丙酮,再添加含有濕化劑之水’直到化合物之濃度爲 5 0 p pm。令經兩點蜘蛛蝨卵感染之兩週齡紅腎豆植物 被測試溶液噴灑至溶液由植物流下(等於2 8克/公頃) -------;---^-------玎-----^ ▲ (請先閱讀背面之注*-事項再填寫本頁) 本紙張尺度適用中國國家標隼(CNS ) Λ4^格(210X37公;f ) 經濟部中夬橾率局只工消#合作杜印災 3〇S59s at __B7_ 五、發明説明(l〇5) ,其係使用可轉向的噴霧器。令植物保持在2 5 °C與5 0 %相對濕度的密閉室中。所測試的化合物中,噴灑後7天 ,下列化合物呈現8 0%或8 0%以上之殺幼蟲/殺卵活 性:化合物1,2,3,4,5,6,7,9,1〇, 11,15,17,18*,19*,20*,21*, 22*,23*,29*,31*,及 3 2'〇化合物以 5ppm測試(等於2. 8克/公頃)<7
試驗D 秋兵蟲全株植物測試法 製備測試化合物溶液,其係將測試化合物溶於極少量 丙酮,再添加含有濕化劑之水,直到化合物之濃度爲 1. OP pm。然後使用旋轉平台與自動噴霧器將測試化 合物噴灑至大豆植物上,至溶液自植物流下(等於5. 5 克/公頃)。令測試後的植物乾燥,令秋兵蟲(草地黏蟲 Spodoptera frugiperda)與經摘除且處理過的葉片接觸 。測試單位保持在2 7 °C與5 0%相對濕度下,在感染後 1 2 0小時評估幼蟲死亡率。所測試的化合物中,下列化 合物呈現80%或8 0%以上之死亡率:1 ,3 ,7*, 15,18,19,21,22,23,24,26, 2 8 及 3 1 » *化合物係以3 p p m測試(等於1 . 7克/公頃)。 本紙张尺度適用中國國家標準(CNS ) Λ4現格(21UX297公釐) -------;.丨^------iT------ -- (請先閱讀背面之注*-事項再填寫本頁)
Claims (1)
- 經濟部中央標準局員工消費合作社印製 其中: X 爲—(CH2) η — 0 - : Q爲選自下列群體之基團:棻基,未經取代之苯基, 經一或二個各選自下列群體之取代基所取代之苯基:鹵素 ,Ca— C6烷基,Ca— C4鹵烷基,Cx—Cw烷氧基,苯 基,C2— 〇4块基—二(Cl— C4垸基)砂院基,某基, 以及經一或二個各選自鹵素,Ci—C4烷基,Cl—C4烷 氧基,Ci— C4鹵烷基,CN與CHO之取代基所取代苯 基; R 1與R 2各爲鹵素: m爲1或2 ; η爲1或2。 2 .如申請專利範圍第1項之化合物,其中 歹时5扣丨喵/1 «修正 .¾.參j 喊?.-4補充 I | ' 1 *'"*"· -----——— --------—----- L.穴、甲請專利k圍 附件一 A : 第8 5 1 Q 5 4 2 2號專利申請案 中文申請專利範圍修正本 民國86年2月修正 1. 一種式I化合物,其N -氧化物類及農業上適合 之鹽類本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ί I....., - . —1-'ji j - -- -- -- - Hi - III、一OJ— l _ I - - - - i -------- I (請先閲讀背面之注意事項再填寫本頁)鹵素,Ci-C*烷基,Cx— C4烷氧基,Ci— C4鹵烷基 經濟部中央標準局員工消費合作社印袋 ,CN與CHO之取代基所取代苯基: m爲1 ; η爲1。 3 .如申請專利範圍第2項之化合物,其中 R 1係選自F與C β,且係位於2 -位置; 係選自F與Cj?,且係位於6 -位置。 4 .如申請專利範圍第3項之化合物,其係選自: (Z. ) — 5 -〔 (4 —氯苯基)伸甲基〕一3 —〔2 一(2 ,6 —二氟苯基)一 4 ,5 —二氣—4 一鳴哩基〕 一 4 _ Df唑啶酮; (Z)— 3-〔2— (2,6 —二氟苯基)—4 ,5 一二氮一 4 — D等哩基〕—5 —〔〔 4 —(二氣甲基)苯基 〕伸甲基〕一4 — U号唑啶酮; (Z ) - 5 - [ (4 / —氯〔1 ,1 ' 一聯苯基〕一 4 —基)伸甲基〕一3 —〔2_ (2 ’ 6 — —氣本基)一 4 ,5 —二氫—4 —噚唑基〕—4— _唑啶酮; (Z) - 3—〔2 — (2 ,6 - 二氟苯基)一4 ,5 一二氫—4 —噚唑基〕一 5-〔 (4 ——氟〔1 ,1 >一 聯苯基〕-4 —基)伸甲基〕-4 -曙唑碇酮:以及 (Z)— 5-〔 (2一,4 -二氯〔1 ,;[一 —聯苯 基〕一4 —基)伸甲基〕一3 — 〔2-(2 ,6—二氟苯 基)—4 ,5 —二M— 4 — _唑基〕-4 一曙唑啶酮。 - 二--- I I 1 - . -I --- - -XJ^—ml— - I I! I I— -I ». I - i -I- ili 1^-1 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐)—.' 1 扣心.. -—- 六、申請專利範圍 5 .—種殺除節肢動物之組成物,其含有殺除節肢動 物有效量之如申請專利範圍第1項的化合物,與至少一種 界面活性劑,固體稀釋劑或液體稀釋劑。 6 . —種控制節肢動物之方法,包括令節肢動物或# 所處環境與殺除節肢動物有效量之如申請專利範園第丨$ 的化合物接觸。 (請先聞讀背面之注意事項再填寫本頁j線- 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4规格(2丨0 x 297公康)
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AU (1) | AU5439196A (zh) |
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IL (1) | IL117513A0 (zh) |
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