CN1889833A - N-芳基肼衍生物在动物中和动物上防治害虫的用途 - Google Patents
N-芳基肼衍生物在动物中和动物上防治害虫的用途 Download PDFInfo
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- CN1889833A CN1889833A CNA2004800361663A CN200480036166A CN1889833A CN 1889833 A CN1889833 A CN 1889833A CN A2004800361663 A CNA2004800361663 A CN A2004800361663A CN 200480036166 A CN200480036166 A CN 200480036166A CN 1889833 A CN1889833 A CN 1889833A
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- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
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- 239000002460 polyether antibiotic agent Substances 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
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- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 1
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- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 description 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical group [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
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- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 1
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- NWWZPOKUUAIXIW-FLIBITNWSA-N thiamethoxam Chemical compound [O-][N+](=O)\N=C/1N(C)COCN\1CC1=CN=C(Cl)S1 NWWZPOKUUAIXIW-FLIBITNWSA-N 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
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- 125000001544 thienyl group Chemical group 0.000 description 1
- DNVLJEWNNDHELH-UHFFFAOYSA-N thiocyclam Chemical compound CN(C)C1CSSSC1 DNVLJEWNNDHELH-UHFFFAOYSA-N 0.000 description 1
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- NKNFWVNSBIXGLL-UHFFFAOYSA-N triazamate Chemical compound CCOC(=O)CSC1=NC(C(C)(C)C)=NN1C(=O)N(C)C NKNFWVNSBIXGLL-UHFFFAOYSA-N 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 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
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
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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
- A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
- A01N37/52—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing groups, e.g. carboxylic acid amidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Environmental Sciences (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Dentistry (AREA)
- Engineering & Computer Science (AREA)
- Plant Pathology (AREA)
- Pest Control & Pesticides (AREA)
- Agronomy & Crop Science (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Tropical Medicine & Parasitology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pretreatment Of Seeds And Plants (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Catching Or Destruction (AREA)
- Pyridine Compounds (AREA)
Abstract
本发明涉及式(I)化合物在动物中和动物上防治寄生物的用途,其中Q为(II)、(III)或(IV);X1为氯、溴或氟;R1、R2各自独立地为H、烷基、链烯基、炔基或环烷基、烷基氨基、二烷基氨基、烷基羰基氨基、烷基磺酰基或烷基亚磺酰基,其中这些基团中的碳原子可以被取代,或R1和R2可以一起形成由结构(V)代表的环;p、m为1、2或3;X’为氧、硫、氨基、烷基氨基、苯基氨基或亚甲基;Z为烷基或苯基;R3为H、烷基、链烯基、炔基、环烷基,其中这些基团中的碳原子可以被取代;R、R4为H或烷基、烷氧羰基、烷基氨基羰基或二烷基氨基羰基,其中这些基团中的碳原子可以被取代;A为C-R5或N;B为C-R6或N;W为C-R7或N;条件是A、B和W中之一不为N;R5、R6、R7为H、卤素、硝基、氰基、氨基、巯基、羟基、烷基、链烯基、炔基、环烷基、烷氧基、烷基氨基、二烷基氨基、烷硫基、烷基磺酰基或烷基亚磺酰基,其中这些基团中的碳原子可以被取代,可以含有1-4个选自氧、硫和氮的杂原子且可以被取代的5-6元芳族环体系;Y为氢、卤素、氰基、硝基、氨基、羟基、巯基、烷基、链烯基、炔基、环烷基、烷氧基、烷基氨基、二烷基氨基、烷硫基、烷基磺酰基或烷基亚磺酰基,其中这些基团中的碳原子可以被取代;n为0、1或2。
Description
本发明涉及式I的肼衍生物或其对映异构体或非对映异构体、兽用可接受盐或酯在动物中和动物上防治寄生物的用途:
其中Q为:
X1为氯、溴或氟;
R1、R2各自独立地为氢、C1-C10烷基、C3-C10链烯基、C3-C10炔基或C3-C12环烷基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷基羰基氨基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被1-3个如下基团取代:卤素、羟基、硝基、氰基、氨基、巯基、C1-C6烷氧基、C1-C6卤代烷氧基、C1-C6烷硫基、C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6卤代烷基磺酰基、C1-C6卤代烷基亚磺酰基或可以被1-3个基团R#取代的C3-C6环烷基,或
R#为卤素、氰基、硝基、羟基、巯基、氨基、C1-C6烷氧基、C2-C6链烯氧基、C2-C6炔氧基、C1-C6卤代烷氧基、C1-C6烷硫基或C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷基羰基、C1-C6烷氧羰基或二(C1-C6烷基)氨基羰基;
甲酰基、C1-C6烷基羰基、C(=O)NRaRb、CO2Rc、Rd、Re、可以被1-3个基团R#取代的苯基或可以被1-3个基团R#取代的吡啶基,
Ra、Rb、Rc各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;
Rd为NRiRj或
Ri、Rj各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;
p、m各自独立地为0、1、2或3,条件是p和m不同时为0,
X为氧、硫、氨基、C1-C4烷基氨基或苯基氨基,或若p为0,则X还可以为苯氧基或C1-C6烷氧基;
r为0或1;
Re为
Rk、Rq各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;或
R1和R2可以一起形成如下结构代表的环:
p、m为1、2或3;
X’为氧、硫、氨基、C1-C4烷基氨基、苯基氨基或亚甲基;
Z为C1-C4烷基或苯基;
R3为氢、C1-C10烷基、C2-C10链烯基、C2-C10炔基、C3-C12环烷基,其中这些基团中的碳原子可以部分或完全被卤化或被1-3个如下基团取代:
氰基、硝基、羟基、巯基、氨基、C1-C6烷基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被如下基团取代:
1-3个卤原子,5-6元芳族环体系,该环体系可以含有1-4个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,或
苯氧基,其可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,或
3-6元饱和或部分不饱和环体系,该环体系含有1-3个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,
3-6元饱和或部分不饱和环体系,该环体系含有1-3个选自氧、硫和氮的杂原子且可以未被取代或被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、C1-C6卤代烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代;
R、R4各自独立地为氢或C1-C6烷基、C1-C6烷氧羰基、C1-C6烷基氨基羰基或二(C1-C6烷基)氨基羰基,其中这些基团中的碳原子可以被1-3个基团R#取代;
A为C-R5或N;
B为C-R6或N;
W为C-R7或N;
条件是A、B和W中的一个不为N;
R5、R6、R7各自独立地为氢、卤素、硝基、氰基、氨基、巯基、羟基、C1-C10烷基、C2-C10链烯基、C2-C10炔基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被1-3个基团R#取代,
5-6元芳族环体系,该环体系可以含有1-4个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6卤代烷基、C1-C6烷硫基、C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6卤代烷基磺酰基、C1-C6卤代烷基亚磺酰基、C1-C6烷氧基、C1-C6卤代烷氧基、巯基、羟基、氨基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个基团R#取代;
Y为氢、卤素、氰基、硝基、氨基、羟基、巯基、C1-C6烷基、C2-C10链烯基、C2-C10炔基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,
其中这些基团中的碳原子可以被1-3个基团R#取代;
n为0、1或2。
通常农学家和兽医的目标是在寄生物试图入侵或侵袭动物时有充分的方法防治它们。
本发明的目的是提供在动物中和动物上防治寄生物的新方法。本发明的另一目的是提供更安全的动物用杀虫剂。本发明的再一目的是提供与现有杀虫剂相比可以更低剂量使用的动物用杀虫剂。本发明的还一目的是提供能够对寄生物提供长期残留控制的动物用杀虫剂。
这些目的整体或部分由本发明满足。
本发明还涉及含有杀寄生物有效量的式I化合物和可接受载体的组合物,其用于在动物中和动物上防治寄生物。
本发明还提供了一种处理、防治、预防和保护动物免受寄生物侵染和感染的方法,包括对动物口服、局部或肠胃外给予或施用杀寄生物有效量的式I化合物或包含它的组合物。
本发明还提供了一种制备用于处理、防治、预防或保护动物免受寄生物侵染或感染的组合物的方法,该组合物包含杀寄生物有效量的式I化合物或包含它的组合物。
式I化合物中的一些在作物保护中的杀虫和杀螨活性已经描述于EP-A 604 798中以及J.A Furch等,“氨基腙:一类新的鞘翅目杀虫剂”,ACS Symposium Series 686,Am.Chem.Soc.,1998,第18章,第178页及随后各页和D.G.Kuhn等,“环烷基取代的氨基腙:一类新的昆虫防治剂”,ACS Symposium Series 686,Am.Chem.Soc.,1998,第19章,第185页及随后各页中。
化合物对农业害虫的活性并不暗示它们对于在动物中和动物上防治体内寄生物和体外寄生物的适用性,该适用性例如要求在口服情况下低的非呕吐剂量,与动物的代谢相容性,低毒性和安全处理。
惊人的是现已发现式I化合物适于在动物中和动物上防治体内寄生物和体外寄生物。
式I化合物可以根据在EP-A 604 798中描述或参考的制备方法或其改性形式制备。
在上式I的定义中,取代基具有下列含义:
“卤素”应理解为指氟、氯、溴和碘。
本文所用的术语“烷基”指具有1-10个碳原子的支化或未支化的饱和烃基,尤其是C1-C6烷基如甲基、乙基、丙基、1-甲基乙基、丁基、1-甲基丙基、2-甲基丙基、1,1-二甲基乙基、戊基、1-甲基丁基、2-甲基丁基、3-甲基丁基、2,2-二甲基丙基、1-乙基丙基、己基、1,1-二甲基丙基、1,2-二甲基丙基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、1,3-二甲基丁基、2,2-二甲基丁基、2,3-二甲基丁基、3,3-二甲基丁基、1-乙基丁基、2-乙基丁基、1,1,2-三甲基丙基、1,2,2-三甲基丙基、1-乙基-1-甲基丙基和1-乙基-2-甲基丙基。
本文所用术语“卤代烷基”指具有1-10个碳原子的直链或支化烷基(如上所述),其中这些基团中的一些或所有氢原子可以被上述卤原子替代,例如C1-C2卤代烷基如氯甲基、溴甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氯乙基、1-溴乙基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基和五氟乙基;
“烷氧基”指在烷基中的任何键处通过氧键键合的具有1-4或6个碳原子的直链或支化烷基(如上所述)。实例包括甲氧基、乙氧基、丙氧基和异丙氧基。
同样,术语“烷硫基”、“烷基氨基”、“二烷基氨基”、“烷基磺酰基”和“烷基亚磺酰基”指分别通过硫、-NH-、-N-、-S(=O)2-或S(=O)-键键合的具有1-4或6个碳原子的直链或支化烷基(如上所述)。
本文所用术语“链烯基”指具有3-10个碳原子和在任意位置的双键的支化或未支化不饱和烃基,例如C3-C6链烯基如1-丙烯基、2-丙烯基、1-甲基乙烯基、1-丁烯基、2-丁烯基、3-丁烯基、1-甲基-1-丙烯基、2-甲基-1-丙烯基、1-甲基-2-丙烯基、2-甲基-2-丙烯基、1-戊烯基、2-戊烯基、3-戊烯基、4-戊烯基、1-甲基-1-丁烯基、2-甲基-1-丁烯基、3-甲基-1-丁烯基、1-甲基-2-丁烯基、2-甲基-2-丁烯基、3-甲基-2-丁烯基、1-甲基-3-丁烯基、2-甲基-3-丁烯基、3-甲基-3-丁烯基、1,1-二甲基-2-丙烯基、1,2-二甲基-1-丙烯基、1,2-二甲基-2-丙烯基、1-乙基-1-丙烯基、1-乙基-2-丙烯基、1-己烯基、2-己烯基、3-己烯基、4-己烯基、5-己烯基、1-甲基-1-戊烯基、2-甲基-1-戊烯基、3-甲基-1-戊烯基、4-甲基-1-戊烯基、1-甲基-2-戊烯基、2-甲基-2-戊烯基、3-甲基-2-戊烯基、4-甲基-2-戊烯基、1-甲基-3-戊烯基、2-甲基-3-戊烯基、3-甲基-3-戊烯基、4-甲基-3-戊烯基、1-甲基-4-戊烯基、2-甲基-4-戊烯基、3-甲基-4-戊烯基、4-甲基-4-戊烯基、1,1-二甲基-2-丁烯基、1,1-二甲基-3-丁烯基、1,2-二甲基-1-丁烯基、1,2-二甲基-2-丁烯基、1,2-二甲基-3-丁烯基、1,3-二甲基-1-丁烯基、1,3-二甲基-2-丁烯基、1,3-二甲基-3-丁烯基、2,2-二甲基-3-丁烯基、2,3-二甲基-1-丁烯基、2,3-二甲基-2-丁烯基、2,3-二甲基-3-丁烯基、3,3-二甲基-1-丁烯基、3,3-二甲基-2-丁烯基、1-乙基-1-丁烯基、1-乙基-2-丁烯基、1-乙基-3-丁烯基、2-乙基-1-丁烯基、2-乙基-2-丁烯基、2-乙基-3-丁烯基、1,1,2-三甲基-2-丙烯基、1-乙基-1-甲基-2-丙烯基、1-乙基-2-甲基-1-丙烯基和1-乙基-2-甲基-2-丙烯基;
“环烷基”指3-6、3-8、3-10或3-12元饱和的碳原子单环,例如C3-C8环烷基如环丙基、环丁基、环戊基、环己基、环庚基和环辛基。
含有1-4个选自氧、硫和氮的杂原子的5-6元芳族环体系例如为含有1-4个氮原子或1-3个氮原子和1个硫或氧原子的5元杂芳基,例如呋喃基、噻吩基、吡咯基、异_唑基、异噻唑基、吡唑基、_唑基、噻唑基、咪唑基、_二唑基、噻二唑基、_二唑基、三唑基和四唑基;或含有1-4个氮原子或1-3个氮原子和1个氧或硫原子的6元杂芳基,例如2-吡啶基、3-吡啶基、4-吡啶基、3-哒嗪基、4-哒嗪基、2-嘧啶基、4-嘧啶基、5-嘧啶基、2-吡嗪基、1,3,5-三嗪-2-基和1,2,4-三嗪-3-基;
含有1-3个选自氧、硫和氮的杂原子的3-6元饱和或部分不饱和环体系例如指含有1-3个选自氮和氧的杂原子的饱和3-6元环体系,例如氮丙啶、吡咯烷、四氢呋喃、四氢吡喃或哌啶。
术语“兽用可接受盐”指本领域对于形成兽用盐是已知且被接受的阴离子的盐。例如由含碱性氮原子如氨基的式I化合物形成的合适酸加成盐包括与无机酸形成的盐,例如盐酸盐、硫酸盐、磷酸盐和硝酸盐,以及有机酸盐如乙酸盐、马来酸盐、马来酸氢盐、富马酸盐、富马酸氢盐、甲烷次磺酸盐、甲烷磺酸盐和琥珀酸盐。
对于式I化合物的意欲用途,特别优选取代基的下列含义,在每种情况下单独或组合:
优选其中A代表C-R5的式I化合物。
此外,还优选其中B代表C-R6的式I化合物。
还优选其中W代表C-R7的式I化合物。
特别优选其中A代表C-R5、B代表C-R6且W代表C-R7的化合物。
此外,还优选其中R5为卤素或C1-C6卤代烷基,最优选卤素,尤其是氯的式I化合物。
还优选其中R6为氢或卤素,尤其是氢的式I化合物。
此外,优选其中R7为卤素或C1-C6卤代烷基,优选C1-C6卤代烷基,尤其是三氟甲基的式I化合物。
此外,还优选其中Y位于邻位且为卤素或C1-C6卤代烷基的式I化合物。特别优选其中Y为卤素,尤其是氯的式I化合物。
优选其中n为1的式I化合物。
还优选其中Q代表-N=[C(NR1R2)R3]的式I化合物。
此外,还优选其中X1为氯的式I化合物。
还优选其中R代表C1-C6烷基或氢,优选氢的式I化合物。
还优选其中R1和R2各自独立地为氢、可以被C1-C4烷氧基取代的C1-C10烷基或可以被1-3个卤素取代的C3-C10环烷基的式I化合物。
此外,还优选其中R1和R2各自独立地为氢、C1-C4烷基或C3-C6环烷基的式I化合物。
尤其优选其中R1为氢且R2为可以被C1-C4烷氧基取代的C1-C10烷基或可以被1-3个卤素取代的C3-C10环烷基的式I化合物。尤其优选其中R1为氢且R2为C1-C4烷基或C3-C6环烷基的式I化合物。
此外,优选其中R3为未取代的C1-C10烷基或可以被1-5个卤原子和/或1-3个C1-C6烷基取代的C3-C10环烷基的式I化合物。
特别优选其中R3为叔丁基的式I化合物。
此外,特别优选其中R3为可以被C1-C6烷基或卤素取代的环丙基,尤其是1-甲基-2,2-二氯环丙基的式I化合物。
此外,还优选其中R4为氢或C1-C6烷基的式I化合物。
对于其应用,特别优选汇编在下表中的化合物I-A。此外,对表中取代基所提到的基团本身为所述取代基的特别优选实施方案,与其中提到它们的组合无关。
对于其应用,还特别优选下表的化合物的盐酸、马来酸、氢马来酸、富马酸、氢富马酸、甲烷次磺酸、甲烷磺酸和琥珀酸加合物。
一些式I化合物是新的。这些化合物也为本发明的主题。
表1
其中R3为甲基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表2
其中R3为乙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表3
其中R3为乙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表4
其中R3为丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表5
其中R3为异丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表6
其中R3为异丁基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表7
其中R3为叔丁基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表8
其中R3为新戊基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表9
其中R3为环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表10
其中R3为1,1-二甲基丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表11
其中R3为环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表12
其中R3为2,2-二氯环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表13
其中R3为2,2-二溴环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表14
其中R3为1-甲基环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表15
其中R3为1-甲基-2,2-二氯环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表16
其中R3为1-甲基-2,2-二溴环丙基且R1、R2、R5、R6、R7和Yn的组合在每种情况下对应于表A中的一行的式I-A化合物。
表A
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1 | H | H | Cl | H | H | H |
A-2 | CH3 | CH3 | Cl | H | H | H |
A-3 | CH2CH3 | CH2CH3 | Cl | H | H | H |
A-4 | CH3 | H | Cl | H | H | H |
A-5 | CH2CH3 | H | Cl | H | H | H |
A-6 | (CH2)2CH3 | H | Cl | H | H | H |
A-7 | CH(CH3)2 | H | Cl | H | H | H |
A-8 | CH2CF3 | H | Cl | H | H | H |
A-9 | C(CH3)3 | H | Cl | H | H | H |
A-10 | CH2CH(CH3)2 | H | Cl | H | H | H |
A-11 | CH(CH3)CH2CH3 | H | Cl | H | H | H |
A-12 | (CH2)2OCH3 | H | Cl | H | H | H |
A-13 | CH2CH(OCH3)2 | H | Cl | H | H | H |
A-14 | CH2CH(OCH2CH3)2 | H | Cl | H | H | H |
A-15 | CH2C6H5 | H | Cl | H | H | H |
A-16 | CH(CH3)C6H5 | H | Cl | H | H | H |
A-17 | (CH2)2OC6H5 | H | Cl | H | H | H |
A-18 | (CH2)2C6H5 | H | Cl | H | H | H |
A-19 | (CH2)2C6H4F | H | Cl | H | H | H |
A-20 | (CH2)2C6H4Cl | H | Cl | H | H | H |
A-21 | (CH2)2C6H4CN | H | Cl | H | H | H |
A-22 | (CH2)2C6H4CH3 | H | Cl | H | H | H |
A-23 | (CH2)2C6H4CF3 | H | Cl | H | H | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-24 | (CH2)2C6H4OCH3 | H | Cl | H | H | H |
A-25 | (CH2)2C6H4OCF3 | H | Cl | H | H | H |
A-26 | CH2CH=CH2 | H | Cl | H | H | H |
A-27 | 环-C3H5 | H | Cl | H | H | H |
A-28 | (CH2)2NHCH3 | H | Cl | H | H | H |
A-29 | H | H | F | H | H | H |
A-30 | CH3 | CH3 | F | H | H | H |
A-31 | CH2CH3 | CH2CH3 | F | H | H | H |
A-32 | CH3 | H | F | H | H | H |
A-33 | CH2CH3 | H | F | H | H | H |
A-34 | (CH2)2CH3 | H | F | H | H | H |
A-35 | CH(CH3)2 | H | F | H | H | H |
A-36 | CH2CF3 | H | F | H | H | H |
A-37 | C(CH3)3 | H | F | H | H | H |
A-38 | CH2CH(CH3)2 | H | F | H | H | H |
A-39 | CH(CH3)CH2CH3 | H | F | H | H | H |
A-40 | (CH2)2OCH3 | H | F | H | H | H |
A-41 | CH2CH(OCH3)2 | H | F | H | H | H |
A-42 | CH2CH(OCH2CH3)2 | H | F | H | H | H |
A-43 | CH2C6H5 | H | F | H | H | H |
A-44 | CH(CH3)C6H5 | H | F | H | H | H |
A-45 | (CH2)2OC6H5 | H | F | H | H | H |
A-46 | (CH2)2C6H5 | H | F | H | H | H |
A-47 | (CH2)2C6H4F | H | F | H | H | H |
A-48 | (CH2)2C6H4Cl | H | F | H | H | H |
A-49 | (CH2)2C6H4CN | H | F | H | H | H |
A-50 | (CH2)2C6H4CH3 | H | F | H | H | H |
A-51 | (CH2)2C6H4CF3 | H | F | H | H | H |
A-52 | (CH2)2C6H4OCH3 | H | F | H | H | H |
A-53 | (CH2)2C6H4OCF3 | H | F | H | H | H |
A-54 | CH2CH=CH2 | H | F | H | H | H |
A-55 | 环-C3H5 | H | F | H | H | H |
A-56 | (CH2)2NHCH3 | H | F | H | H | H |
A-57 | H | H | CF3 | H | H | H |
A-58 | CH3 | CH3 | CF3 | H | H | H |
A-59 | CH2CH3 | CH2CH3 | CF3 | H | H | H |
A-60 | CH3 | H | CF3 | H | H | H |
A-61 | CH2CH3 | H | CF3 | H | H | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-62 | (CH2)2CH3 | H | CF3 | H | H | H |
A-63 | CH(CH3)2 | H | CF3 | H | H | H |
A-64 | CH2CF3 | H | CF3 | H | H | H |
A-65 | C(CH3)3 | H | CF3 | H | H | H |
A-66 | CH2CH(CH3)2 | H | CF3 | H | H | H |
A-67 | CH(CH3)CH2CH3 | H | CF3 | H | H | H |
A-68 | (CH2)2OCH3 | H | CF3 | H | H | H |
A-69 | CH2CH(OCH3)2 | H | CF3 | H | H | H |
A-70 | CH2CH(OCH2CH3)2 | H | CF3 | H | H | H |
A-71 | CH2C6H5 | H | CF3 | H | H | H |
A-72 | CH(CH3)C6H5 | H | CF3 | H | H | H |
A-73 | (CH2)2OC6H5 | H | CF3 | H | H | H |
A-74 | (CH2)2C6H5 | H | CF3 | H | H | H |
A-75 | (CH2)2C6H4F | H | CF3 | H | H | H |
A-76 | (CH2)2C6H4Cl | H | CF3 | H | H | H |
A-77 | (CH2)2C6H4CN | H | CF3 | H | H | H |
A-78 | (CH2)2C6H4CH3 | H | CF3 | H | H | H |
A-79 | (CH2)2C6H4CF3 | H | CF3 | H | H | H |
A-80 | (CH2)2C6H4OCH3 | H | CF3 | H | H | H |
A-81 | (CH2)2C6H4OCF3 | H | CF3 | H | H | H |
A-82 | CH2CH=CH2 | H | CF3 | H | H | H |
A-83 | 环-C3H5 | H | CF3 | H | H | H |
A-84 | (CH2)2NHCH3 | H | CF3 | H | H | H |
A-85 | H | H | H | H | Cl | H |
A-86 | CH3 | CH3 | H | H | Cl | H |
A-87 | CH2CH3 | CH2CH3 | H | H | Cl | H |
A-88 | CH3 | H | H | H | Cl | H |
A-89 | CH2CH3 | H | H | H | Cl | H |
A-90 | (CH2)2CH3 | H | H | H | Cl | H |
A-91 | CH(CH3)2 | H | H | H | Cl | H |
A-92 | CH2CF3 | H | H | H | Cl | H |
A-93 | C(CH3)3 | H | H | H | Cl | H |
A-94 | CH2CH(CH3)2 | H | H | H | Cl | H |
A-95 | CH(CH3)CH2CH3 | H | H | H | Cl | H |
A-96 | (CH2)2OCH3 | H | H | H | Cl | H |
A-97 | CH2CH(OCH3)2 | H | H | H | Cl | H |
A-98 | CH2CH(OCH2CH3)2 | H | H | H | Cl | H |
A-99 | CH2C6H5 | H | H | H | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-100 | CH(CH3)C6H5 | H | H | H | Cl | H |
A-101 | (CH2)2OC6H5 | H | H | H | Cl | H |
A-102 | (CH2)2C6H5 | H | H | H | Cl | H |
A-103 | (CH2)2C6H4F | H | H | H | Cl | H |
A-104 | (CH2)2C6H4Cl | H | H | H | Cl | H |
A-105 | (CH2)2C6H4CN | H | H | H | Cl | H |
A-106 | (CH2)2C6H4CH3 | H | H | H | Cl | H |
A-107 | (CH2)2C6H4CF3 | H | H | H | Cl | H |
A-108 | (CH2)2C6H4OCH3 | H | H | H | Cl | H |
A-109 | (CH2)2C6H4OCF3 | H | H | H | Cl | H |
A-110 | CH2CH=CH2 | H | H | H | Cl | H |
A-111 | 环-C3H5 | H | H | H | Cl | H |
A-112 | (CH2)2NHCH3 | H | H | H | Cl | H |
A-113 | H | H | H | H | F | H |
A-114 | CH3 | CH3 | H | H | F | H |
A-115 | CH2CH3 | CH2CH3 | H | H | F | H |
A-116 | CH3 | H | H | H | F | H |
A-117 | CH2CH3 | H | H | H | F | H |
A-118 | (CH2)2CH3 | H | H | H | F | H |
A-119 | CH(CH3)2 | H | H | H | F | H |
A-120 | CH2CF3 | H | H | H | F | H |
A-121 | C(CH3)3 | H | H | H | F | H |
A-122 | CH2CH(CH3)2 | H | H | H | F | H |
A-123 | CH(CH3)CH2CH3 | H | H | H | F | H |
A-124 | (CH2)2OCH3 | H | H | H | F | H |
A-125 | CH2CH(OCH3)2 | H | H | H | F | H |
A-126 | CH2CH(OCH2CH3)2 | H | H | H | F | H |
A-127 | CH2C6H5 | H | H | H | F | H |
A-128 | CH(CH3)C6H5 | H | H | H | F | H |
A-129 | (CH2)2OC6H5 | H | H | H | F | H |
A-130 | (CH2)2C6H5 | H | H | H | F | H |
A-131 | (CH2)2C6H4F | H | H | H | F | H |
A-132 | (CH2)2C6H4Cl | H | H | H | F | H |
A-133 | (CH2)2C6H4CN | H | H | H | F | H |
A-134 | (CH2)2C6H4CH3 | H | H | H | F | H |
A-135 | (CH2)2C6H4CF3 | H | H | H | F | H |
A-136 | (CH2)2C6H4OCH3 | H | H | H | F | H |
A-137 | (CH2)2C6H4OCF3 | H | H | H | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-138 | CH2CH=CH2 | H | H | H | F | H |
A-139 | 环-C3H5 | H | H | H | F | H |
A-140 | (CH2)2NHCH3 | H | H | H | F | H |
A-141 | H | H | H | H | CF3 | H |
A-142 | CH3 | CH3 | H | H | CF3 | H |
A-143 | CH2CH3 | CH2CH3 | H | H | CF3 | H |
A-144 | CH3 | H | H | H | CF3 | H |
A-145 | CH2CH3 | H | H | H | CF3 | H |
A-146 | (CH2)2CH3 | H | H | H | CF3 | H |
A-147 | CH(CH3)2 | H | H | H | CF3 | H |
A-148 | CH2CF3 | H | H | H | CF3 | H |
A-149 | C(CH3)3 | H | H | H | CF3 | H |
A-150 | CH2CH(CH3)2 | H | H | H | CF3 | H |
A-151 | CH(CH3)CH2CH3 | H | H | H | CF3 | H |
A-152 | (CH2)2OCH3 | H | H | H | CF3 | H |
A-153 | CH2CH(OCH3)2 | H | H | H | CF3 | H |
A-154 | CH2CH(OCH2CH3)2 | H | H | H | CF3 | H |
A-155 | CH2C6H5 | H | H | H | CF3 | H |
A-156 | CH(CH3)C6H5 | H | H | H | CF3 | H |
A-157 | (CH2)2OC6H5 | H | H | H | CF3 | H |
A-158 | (CH2)2C6H5 | H | H | H | CF3 | H |
A-159 | (CH2)2C6H4F | H | H | H | CF3 | H |
A-160 | (CH2)2C6H4Cl | H | H | H | CF3 | H |
A-161 | (CH2)2C6H4CN | H | H | H | CF3 | H |
A-162 | (CH2)2C6H4CH3 | H | H | H | CF3 | H |
A-163 | (CH2)2C6H4CF3 | H | H | H | CF3 | H |
A-164 | (CH2)2C6H4OCH3 | H | H | H | CF3 | H |
A-165 | (CH2)2C6H4OCF3 | H | H | H | CF3 | H |
A-166 | CH2CH=CH2 | H | H | H | CF3 | H |
A-167 | 环-C3H5 | H | H | H | CF3 | H |
A-168 | (CH2)2NHCH3 | H | H | H | CF3 | H |
A-169 | H | H | Cl | H | Cl | H |
A-170 | CH3 | CH3 | Cl | H | Cl | H |
A-171 | CH2CH3 | CH2CH3 | Cl | H | Cl | H |
A-172 | CH3 | H | Cl | H | Cl | H |
A-173 | CH2CH3 | H | Cl | H | Cl | H |
A-174 | (CH2)2CH3 | H | Cl | H | Cl | H |
A-175 | CH(CH3)2 | H | Cl | H | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-176 | CH2CF3 | H | Cl | H | Cl | H |
A-177 | C(CH3)3 | H | Cl | H | Cl | H |
A-178 | CH2CH(CH3)2 | H | Cl | H | Cl | H |
A-179 | CH(CH3)CH2CH3 | H | Cl | H | Cl | H |
A-180 | (CH2)2OCH3 | H | Cl | H | Cl | H |
A-181 | CH2CH(OCH3)2 | H | Cl | H | Cl | H |
A-182 | CH2CH(OCH2CH3)2 | H | Cl | H | Cl | H |
A-183 | CH2C6H5 | H | Cl | H | Cl | H |
A-184 | CH(CH3)C6H5 | H | Cl | H | Cl | H |
A-185 | (CH2)2OC6H5 | H | Cl | H | Cl | H |
A-186 | (CH2)2C6H5 | H | Cl | H | Cl | H |
A-187 | (CH2)2C6H4F | H | Cl | H | Cl | H |
A-188 | (CH2)2C6H4Cl | H | Cl | H | Cl | H |
A-189 | (CH2)2C6H4CN | H | Cl | H | Cl | H |
A-190 | (CH2)2C6H4CH3 | H | Cl | H | Cl | H |
A-191 | (CH2)2C6H4CF3 | H | Cl | H | Cl | H |
A-192 | (CH2)2C6H4OCH3 | H | Cl | H | Cl | H |
A-193 | (CH2)2C6H4OCF3 | H | Cl | H | Cl | H |
A-194 | CH2CH=CH2 | H | Cl | H | Cl | H |
A-195 | 环-C3H5 | H | Cl | H | Cl | H |
A-196 | (CH2)2NHCH3 | H | Cl | H | Cl | H |
A-197 | H | H | F | H | Cl | H |
A-198 | CH3 | CH3 | F | H | Cl | H |
A-199 | CH2CH3 | CH2CH3 | F | H | Cl | H |
A-200 | CH3 | H | F | H | Cl | H |
A-201 | CH2CH3 | H | F | H | Cl | H |
A-202 | (CH2)2CH3 | H | F | H | Cl | H |
A-203 | CH(CH3)2 | H | F | H | Cl | H |
A-204 | CH2CF3 | H | F | H | Cl | H |
A-205 | C(CH3)3 | H | F | H | Cl | H |
A-206 | CH2CH(CH3)2 | H | F | H | Cl | H |
A-207 | CH(CH3)CH2CH3 | H | F | H | Cl | H |
A-208 | (CH2)2OCH3 | H | F | H | Cl | H |
A-209 | CH2CH(OCH3)2 | H | F | H | Cl | H |
A-210 | CH2CH(OCH2CH3)2 | H | F | H | Cl | H |
A-211 | CH2C6H5 | H | F | H | Cl | H |
A-212 | CH(CH3)C6H5 | H | F | H | Cl | H |
A-213 | (CH2)2OC6H5 | H | F | H | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-214 | (CH2)2C6H5 | H | F | H | Cl | H |
A-215 | (CH2)2C6H4F | H | F | H | Cl | H |
A-216 | (CH2)2C6H4Cl | H | F | H | Cl | H |
A-217 | (CH2)2C6H4CN | H | F | H | Cl | H |
A-218 | (CH2)2C6H4CH3 | H | F | H | Cl | H |
A-219 | (CH2)2C6H4CF3 | H | F | H | Cl | H |
A-220 | (CH2)2C6H4OCH3 | H | F | H | Cl | H |
A-221 | (CH2)2C6H4OCF3 | H | F | H | Cl | H |
A-222 | CH2CH=CH2 | H | F | H | Cl | H |
A-223 | 环-C3H5 | H | F | H | Cl | H |
A-224 | (CH2)2NHCH3 | H | F | H | Cl | H |
A-225 | H | H | Cl | H | F | H |
A-226 | CH3 | CH3 | Cl | H | F | H |
A-227 | CH2CH3 | CH2CH3 | Cl | H | F | H |
A-228 | CH3 | H | Cl | H | F | H |
A-229 | CH2CH3 | H | Cl | H | F | H |
A-230 | (CH2)2CH3 | H | Cl | H | F | H |
A-231 | CH(CH3)2 | H | Cl | H | F | H |
A-232 | CH2CF3 | H | Cl | H | F | H |
A-233 | C(CH3)3 | H | Cl | H | F | H |
A-234 | CH2CH(CH3)2 | H | Cl | H | F | H |
A-235 | CH(CH3)CH2CH3 | H | Cl | H | F | H |
A-236 | (CH2)2OCH3 | H | Cl | H | F | H |
A-237 | CH2CH(OCH3)2 | H | Cl | H | F | H |
A-238 | CH2CH(OCH2CH3)2 | H | Cl | H | F | H |
A-239 | CH2C6H5 | H | Cl | H | F | H |
A-240 | CH(CH3)C6H5 | H | Cl | H | F | H |
A-241 | (CH2)2OC6H5 | H | Cl | H | F | H |
A-242 | (CH2)2C6H5 | H | Cl | H | F | H |
A-243 | (CH2)2C6H4F | H | Cl | H | F | H |
A-244 | (CH2)2C6H4Cl | H | Cl | H | F | H |
A-245 | (CH2)2C6H4CN | H | Cl | H | F | H |
A-246 | (CH2)2C6H4CH3 | H | Cl | H | F | H |
A-247 | (CH2)2C6H4CF3 | H | Cl | H | F | H |
A-248 | (CH2)2C6H4OCH3 | H | Cl | H | F | H |
A-249 | (CH2)2C6H4OCF3 | H | Cl | H | F | H |
A-250 | CH2CH=CH2 | H | Cl | H | F | H |
A-251 | 环-C3H5 | H | Cl | H | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-252 | (CH2)2NHCH3 | H | Cl | H | F | H |
A-253 | H | H | F | H | F | H |
A-254 | CH3 | CH3 | F | H | F | H |
A-255 | CH2CH3 | CH2CH3 | F | H | F | H |
A-256 | CH3 | H | F | H | F | H |
A-257 | CH2CH3 | H | F | H | F | H |
A-258 | (CH2)2CH3 | H | F | H | F | H |
A-259 | CH(CH3)2 | H | F | H | F | H |
A-260 | CH2CF3 | H | F | H | F | H |
A-261 | C(CH3)3 | H | F | H | F | H |
A-262 | CH2CH(CH3)2 | H | F | H | F | H |
A-263 | CH(CH3)CH2CH3 | H | F | H | F | H |
A-264 | (CH2)2OCH3 | H | F | H | F | H |
A-265 | CH2CH(OCH3)2 | H | F | H | F | H |
A-266 | CH2CH(OCH2CH3)2 | H | F | H | F | H |
A-267 | CH2C6H5 | H | F | H | F | H |
A-268 | CH(CH3)C6H5 | H | F | H | F | H |
A-269 | (CH2)2OC6H5 | H | F | H | F | H |
A-270 | (CH2)2C6H5 | H | F | H | F | H |
A-271 | (CH2)2C6H4F | H | F | H | F | H |
A-272 | (CH2)2C6H4Cl | H | F | H | F | H |
A-273 | (CH2)2C6H4CN | H | F | H | F | H |
A-274 | (CH2)2C6H4CH3 | H | F | H | F | H |
A-275 | (CH2)2C6H4CF3 | H | F | H | F | H |
A-276 | (CH2)2C6H4OCH3 | H | F | H | F | H |
A-277 | (CH2)2C6H4OCF3 | H | F | H | F | H |
A-278 | CH2CH=CH2 | H | F | H | F | H |
A-279 | 环-C3H5 | H | F | H | F | H |
A-280 | (CH2)2NHCH3 | H | F | H | F | H |
A-281 | H | H | Cl | H | CF3 | H |
A-282 | CH3 | CH3 | Cl | H | CF3 | H |
A-283 | CH2CH3 | CH2CH3 | Cl | H | CF3 | H |
A-284 | CH3 | H | Cl | H | CF3 | H |
A-285 | CH2CH3 | H | Cl | H | CF3 | H |
A-286 | (CH2)2CH3 | H | Cl | H | CF3 | H |
A-287 | CH(CH3)2 | H | Cl | H | CF3 | H |
A-288 | CH2CF3 | H | Cl | H | CF3 | H |
A-289 | C(CH3)3 | H | Cl | H | CF3 | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-290 | CH2CH(CH3)2 | H | Cl | H | CF3 | H |
A-291 | CH(CH3)CH2CH3 | H | Cl | H | CF3 | H |
A-292 | (CH2)2OCH3 | H | Cl | H | CF3 | H |
A-293 | CH2CH(OCH3)2 | H | Cl | H | CF3 | H |
A-294 | CH2CH(OCH2CH3)2 | H | Cl | H | CF3 | H |
A-295 | CH2C6H5 | H | Cl | H | CF3 | H |
A-296 | CH(CH3)C6H5 | H | Cl | H | CF3 | H |
A-297 | (CH2)2OC6H5 | H | Cl | H | CF3 | H |
A-298 | (CH2)2C6H5 | H | Cl | H | CF3 | H |
A-299 | (CH2)2C6H4F | H | Cl | H | CF3 | H |
A-300 | (CH2)2C6H4Cl | H | Cl | H | CF3 | H |
A-301 | (CH2)2C6H4CN | H | Cl | H | CF3 | H |
A-302 | (CH2)2C6H4CH3 | H | Cl | H | CF3 | H |
A-303 | (CH2)2C6H4CF3 | H | Cl | H | CF3 | H |
A-304 | (CH2)2C6H4OCH3 | H | Cl | H | CF3 | H |
A-305 | (CH2)2C6H4OCF3 | H | Cl | H | CF3 | H |
A-306 | CH2CH=CH2 | H | Cl | H | CF3 | H |
A-307 | 环-C3H5 | H | Cl | H | CF3 | H |
A-308 | (CH2)2NHCH3 | H | Cl | H | CF3 | H |
A-309 | H | H | CF3 | H | Cl | H |
A-310 | CH3 | CH3 | CF3 | H | Cl | H |
A-311 | CH2CH3 | CH2CH3 | CF3 | H | Cl | H |
A-312 | CH3 | H | CF3 | H | Cl | H |
A-313 | CH2CH3 | H | CF3 | H | Cl | H |
A-314 | (CH2)2CH3 | H | CF3 | H | Cl | H |
A-315 | CH(CH3)2 | H | CF3 | H | Cl | H |
A-316 | CH2CF3 | H | CF3 | H | Cl | H |
A-317 | C(CH3)3 | H | CF3 | H | Cl | H |
A-318 | CH2CH(CH3)2 | H | CF3 | H | Cl | H |
A-319 | CH(CH3)CH2CH3 | H | CF3 | H | Cl | H |
A-320 | (CH2)2OCH3 | H | CF3 | H | Cl | H |
A-321 | CH2CH(OCH3)2 | H | CF3 | H | Cl | H |
A-322 | CH2CH(OCH2CH3)2 | H | CF3 | H | Cl | H |
A-323 | CH2C6H5 | H | CF3 | H | Cl | H |
A-324 | CH(CH3)C6H5 | H | CF3 | H | Cl | H |
A-325 | (CH2)2OC6H5 | H | CF3 | H | Cl | H |
A-326 | (CH2)2C6H5 | H | CF3 | H | Cl | H |
A-327 | (CH2)2C6H4F | H | CF3 | H | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-328 | (CH2)2C6H4Cl | H | CF3 | H | Cl | H |
A-329 | (CH2)2C6H4CN | H | CF3 | H | Cl | H |
A-330 | (CH2)2C6H4CH3 | H | CF3 | H | Cl | H |
A-331 | (CH2)2C6H4CF3 | H | CF3 | H | Cl | H |
A-332 | (CH2)2C6H4OCH3 | H | CF3 | H | Cl | H |
A-333 | (CH2)2C6H4OCF3 | H | CF3 | H | Cl | H |
A-334 | CH2CH=CH2 | H | CF3 | H | Cl | H |
A-335 | 环-C3H5 | H | CF3 | H | Cl | H |
A-336 | (CH2)2NHCH3 | H | CF3 | H | Cl | H |
A-337 | H | H | F | H | CF3 | H |
A-338 | CH3 | CH3 | F | H | CF3 | H |
A-339 | CH2CH3 | CH2CH3 | F | H | CF3 | H |
A-340 | CH3 | H | F | H | CF3 | H |
A-341 | CH2CH3 | H | F | H | CF3 | H |
A-342 | (CH2)2CH3 | H | F | H | CF3 | H |
A-343 | CH(CH3)2 | H | F | H | CF3 | H |
A-344 | CH2CF3 | H | F | H | CF3 | H |
A-345 | C(CH3)3 | H | F | H | CF3 | H |
A-346 | CH2CH(CH3)2 | H | F | H | CF3 | H |
A-347 | CH(CH3)CH2CH3 | H | F | H | CF3 | H |
A-348 | (CH2)2OCH3 | H | F | H | CF3 | H |
A-349 | CH2CH(OCH3)2 | H | F | H | CF3 | H |
A-350 | CH2CH(OCH2CH3)2 | H | F | H | CF3 | H |
A-351 | CH2C6H5 | H | F | H | CF3 | H |
A-352 | CH(CH3)C6H5 | H | F | H | CF3 | H |
A-353 | (CH2)2OC6H5 | H | F | H | CF3 | H |
A-354 | (CH2)2C6H5 | H | F | H | CF3 | H |
A-355 | (CH2)2C6H4F | H | F | H | CF3 | H |
A-356 | (CH2)2C6H4Cl | H | F | H | CF3 | H |
A-357 | (CH2)2C6H4CN | H | F | H | CF3 | H |
A-358 | (CH2)2C6H4CH3 | H | F | H | CF3 | H |
A-359 | (CH2)2C6H4CF3 | H | F | H | CF3 | H |
A-360 | (CH2)2C6H4OCH3 | H | F | H | CF3 | H |
A-361 | (CH2)2C6H4OCF3 | H | F | H | CF3 | H |
A-362 | CH2CH=CH2 | H | F | H | CF3 | H |
A-363 | 环-C3H5 | H | F | H | CF3 | H |
A-364 | (CH2)2NHCH3 | H | F | H | CF3 | H |
A-365 | H | H | CF3 | H | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-366 | CH3 | CH3 | CF3 | H | F | H |
A-367 | CH2CH3 | CH2CH3 | CF3 | H | F | H |
A-368 | CH3 | H | CF3 | H | F | H |
A-369 | CH2CH3 | H | CF3 | H | F | H |
A-370 | (CH2)2CH3 | H | CF3 | H | F | H |
A-371 | CH(CH3)2 | H | CF3 | H | F | H |
A-372 | CH2CF3 | H | CF3 | H | F | H |
A-373 | C(CH3)3 | H | CF3 | H | F | H |
A-374 | CH2CH(CH3)2 | H | CF3 | H | F | H |
A-375 | CH(CH3)CH2CH3 | H | CF3 | H | F | H |
A-376 | (CH2)2OCH3 | H | CF3 | H | F | H |
A-377 | CH2CH(OCH3)2 | H | CF3 | H | F | H |
A-378 | CH2CH(OCH2CH3)2 | H | CF3 | H | F | H |
A-379 | CH2C6H5 | H | CF3 | H | F | H |
A-380 | CH(CH3)C6H5 | H | CF3 | H | F | H |
A-381 | (CH2)2OC6H5 | H | CF3 | H | F | H |
A-382 | (CH2)2C6H5 | H | CF3 | H | F | H |
A-383 | (CH2)2C6H4F | H | CF3 | H | F | H |
A-384 | (CH2)2C6H4Cl | H | CF3 | H | F | H |
A-385 | (CH2)2C6H4CN | H | CF3 | H | F | H |
A-386 | (CH2)2C6H4CH3 | H | CF3 | H | F | H |
A-387 | (CH2)2C6H4CF3 | H | CF3 | H | F | H |
A-388 | (CH2)2C6H4OCH3 | H | CF3 | H | F | H |
A-389 | (CH2)2C6H4OCF3 | H | CF3 | H | F | H |
A-390 | CH2CH=CH2 | H | CF3 | H | F | H |
A-391 | 环-C3H5 | H | CF3 | H | F | H |
A-392 | (CH2)2NHCH3 | H | CF3 | H | F | H |
A-393 | H | H | CF3 | H | CF3 | H |
A-394 | CH3 | CH3 | CF3 | H | CF3 | H |
A-395 | CH2CH3 | CH2CH3 | CF3 | H | CF3 | H |
A-396 | CH3 | H | CF3 | H | CF3 | H |
A-397 | CH2CH3 | H | CF3 | H | CF3 | H |
A-398 | (CH2)2CH3 | H | CF3 | H | CF3 | H |
A-399 | CH(CH3)2 | H | CF3 | H | CF3 | H |
A-400 | CH2CF3 | H | CF3 | H | CF3 | H |
A-401 | C(CH3)3 | H | CF3 | H | CF3 | H |
A-402 | CH2CH(CH3)2 | H | CF3 | H | CF3 | H |
A-403 | CH(CH3)CH2CH3 | H | CF3 | H | CF3 | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-404 | (CH2)2OCH3 | H | CF3 | H | CF3 | H |
A-405 | CH2CH(OCH3)2 | H | CF3 | H | CF3 | H |
A-406 | CH2CH(OCH2CH3)2 | H | CF3 | H | CF3 | H |
A-407 | CH2C6H5 | H | CF3 | H | CF3 | H |
A-408 | CH(CH3)C6H5 | H | CF3 | H | CF3 | H |
A-409 | (CH2)2OC6H5 | H | CF3 | H | CF3 | H |
A-410 | (CH2)2C6H5 | H | CF3 | H | CF3 | H |
A-411 | (CH2)2C6H4F | H | CF3 | H | CF3 | H |
A-412 | (CH2)2C6H4Cl | H | CF3 | H | CF3 | H |
A-413 | (CH2)2C6H4CN | H | CF3 | H | CF3 | H |
A-414 | (CH2)2C6H4CH3 | H | CF3 | H | CF3 | H |
A-415 | (CH2)2C6H4CF3 | H | CF3 | H | CF3 | H |
A-416 | (CH2)2C6H4OCH3 | H | CF3 | H | CF3 | H |
A-417 | (CH2)2C6H4OCF3 | H | CF3 | H | CF3 | H |
A-418 | CH2CH=CH2 | H | CF3 | H | CF3 | H |
A-419 | 环-C3H5 | H | CF3 | H | CF3 | H |
A-420 | (CH2)2NHCH3 | H | CF3 | H | CF3 | H |
A-421 | H | H | Cl | Cl | Cl | H |
A-422 | CH3 | CH3 | Cl | Cl | Cl | H |
A-423 | CH2CH3 | CH2CH3 | Cl | Cl | Cl | H |
A-424 | CH3 | H | Cl | Cl | Cl | H |
A-425 | CH2CH3 | H | Cl | Cl | Cl | H |
A-426 | (CH2)2CH3 | H | Cl | Cl | Cl | H |
A-427 | CH(CH3)2 | H | Cl | Cl | Cl | H |
A-428 | CH2CF3 | H | Cl | Cl | Cl | H |
A-429 | C(CH3)3 | H | Cl | Cl | Cl | H |
A-430 | CH2CH(CH3)2 | H | Cl | Cl | Cl | H |
A-431 | CH(CH3)CH2CH3 | H | Cl | Cl | Cl | H |
A-432 | (CH2)2OCH3 | H | Cl | Cl | Cl | H |
A-433 | CH2CH(OCH3)2 | H | Cl | Cl | Cl | H |
A-434 | CH2CH(OCH2CH3)2 | H | Cl | Cl | Cl | H |
A-435 | CH2C6H5 | H | Cl | Cl | Cl | H |
A-436 | CH(CH3)C6H5 | H | Cl | Cl | Cl | H |
A-437 | (CH2)2OC6H5 | H | Cl | Cl | Cl | H |
A-438 | (CH2)2C6H5 | H | Cl | Cl | Cl | H |
A-439 | (CH2)2C6H4F | H | Cl | Cl | Cl | H |
A-440 | (CH2)2C6H4Cl | H | Cl | Cl | Cl | H |
A-441 | (CH2)2C6H4CN | H | Cl | Cl | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-442 | (CH2)2C6H4CH3 | H | Cl | Cl | Cl | H |
A-443 | (CH2)2C6H4CF3 | H | Cl | Cl | Cl | H |
A-444 | (CH2)2C6H4OCH3 | H | Cl | Cl | Cl | H |
A-445 | (CH2)2C6H4OCF3 | H | Cl | Cl | Cl | H |
A-446 | CH2CH=CH2 | H | Cl | Cl | Cl | H |
A-447 | 环-C3H5 | H | Cl | Cl | Cl | H |
A-448 | (CH2)2NHCH3 | H | Cl | Cl | Cl | H |
A-449 | H | H | Cl | F | Cl | H |
A-450 | CH3 | CH3 | Cl | F | Cl | H |
A-451 | CH2CH3 | CH2CH3 | Cl | F | Cl | H |
A-452 | CH3 | H | Cl | F | Cl | H |
A-453 | CH2CH3 | H | Cl | F | Cl | H |
A-454 | (CH2)2CH3 | H | Cl | F | Cl | H |
A-455 | CH(CH3)2 | H | Cl | F | Cl | H |
A-456 | CH2CF3 | H | Cl | F | Cl | H |
A-457 | C(CH3)3 | H | Cl | F | Cl | H |
A-458 | CH2CH(CH3)2 | H | Cl | F | Cl | H |
A-459 | CH(CH3)CH2CH3 | H | Cl | F | Cl | H |
A-460 | (CH2)2OCH3 | H | Cl | F | Cl | H |
A-461 | CH2CH(OCH3)2 | H | Cl | F | Cl | H |
A-462 | CH2CH(OCH2CH3)2 | H | Cl | F | Cl | H |
A-463 | CH2C6H5 | H | Cl | F | Cl | H |
A-464 | CH(CH3)C6H5 | H | Cl | F | Cl | H |
A-465 | (CH2)2OC6H5 | H | Cl | F | Cl | H |
A-466 | (CH2)2C6H5 | H | Cl | F | Cl | H |
A-467 | (CH2)2C6H4F | H | Cl | F | Cl | H |
A-468 | (CH2)2C6H4Cl | H | Cl | F | Cl | H |
A-469 | (CH2)2C6H4CN | H | Cl | F | Cl | H |
A-470 | (CH2)2C6H4CH3 | H | Cl | F | Cl | H |
A-471 | (CH2)2C6H4CF3 | H | Cl | F | Cl | H |
A-472 | (CH2)2C6H4OCH3 | H | Cl | F | Cl | H |
A-473 | (CH2)2C6H4OCF3 | H | Cl | F | Cl | H |
A-474 | CH2CH=CH2 | H | Cl | F | Cl | H |
A-475 | 环-C3H5 | H | Cl | F | Cl | H |
A-476 | (CH2)2NHCH3 | H | Cl | F | Cl | H |
A-477 | H | H | Cl | Cl | F | H |
A-478 | CH3 | CH3 | Cl | Cl | F | H |
A-479 | CH2CH3 | CH2CH3 | Cl | Cl | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-480 | CH3 | H | Cl | Cl | F | H |
A-481 | CH2CH3 | H | Cl | Cl | F | H |
A-482 | (CH2)2CH3 | H | Cl | Cl | F | H |
A-483 | CH(CH3)2 | H | Cl | Cl | F | H |
A-484 | CH2CF3 | H | Cl | Cl | F | H |
A-485 | C(CH3)3 | H | Cl | Cl | F | H |
A-486 | CH2CH(CH3)2 | H | Cl | Cl | F | H |
A-487 | CH(CH3)CH2CH3 | H | Cl | Cl | F | H |
A-488 | (CH2)2OCH3 | H | Cl | Cl | F | H |
A-489 | CH2CH(OCH3)2 | H | Cl | Cl | F | H |
A-490 | CH2CH(OCH2CH3)2 | H | Cl | Cl | F | H |
A-491 | CH2C6H5 | H | Cl | Cl | F | H |
A-492 | CH(CH3)C6H5 | H | Cl | Cl | F | H |
A-493 | (CH2)2OC6H5 | H | Cl | Cl | F | H |
A-494 | (CH2)2C6H5 | H | Cl | Cl | F | H |
A-495 | (CH2)2C6H4F | H | Cl | Cl | F | H |
A-496 | (CH2)2C6H4Cl | H | Cl | Cl | F | H |
A-497 | (CH2)2C6H4CN | H | Cl | Cl | F | H |
A-498 | (CH2)2C6H4CH3 | H | Cl | Cl | F | H |
A-499 | (CH2)2C6H4CF3 | H | Cl | Cl | F | H |
A-500 | (CH2)2C6H4OCH3 | H | Cl | Cl | F | H |
A-501 | (CH2)2C6H4OCF3 | H | Cl | Cl | F | H |
A-502 | CH2CH=CH2 | H | Cl | Cl | F | H |
A-503 | 环-C3H5 | H | Cl | Cl | F | H |
A-504 | (CH2)2NHCH3 | H | Cl | Cl | F | H |
A-505 | H | H | F | Cl | Cl | H |
A-506 | CH3 | CH3 | F | Cl | Cl | H |
A-507 | CH2CH3 | CH2CH3 | F | Cl | Cl | H |
A-508 | CH3 | H | F | Cl | Cl | H |
A-509 | CH2CH3 | H | F | Cl | Cl | H |
A-510 | (CH2)2CH3 | H | F | Cl | Cl | H |
A-511 | CH(CH3)2 | H | F | Cl | Cl | H |
A-512 | CH2CF3 | H | F | Cl | Cl | H |
A-513 | C(CH3)3 | H | F | Cl | Cl | H |
A-514 | CH2CH(CH3)2 | H | F | Cl | Cl | H |
A-515 | CH(CH3)CH2CH3 | H | F | Cl | Cl | H |
A-516 | (CH2)2OCH3 | H | F | Cl | Cl | H |
A-517 | CH2CH(OCH3)2 | H | F | Cl | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-518 | CH2CH(OCH2CH3)2 | H | F | Cl | Cl | H |
A-519 | CH2C6H5 | H | F | Cl | Cl | H |
A-520 | CH(CH3)C6H5 | H | F | Cl | Cl | H |
A-521 | (CH2)2OC6H5 | H | F | Cl | Cl | H |
A-522 | (CH2)2C6H5 | H | F | Cl | Cl | H |
A-523 | (CH2)2C6H4F | H | F | Cl | Cl | H |
A-524 | (CH2)2C6H4Cl | H | F | Cl | Cl | H |
A-525 | (CH2)2C6H4CN | H | F | Cl | Cl | H |
A-526 | (CH2)2C6H4CH3 | H | F | Cl | Cl | H |
A-527 | (CH2)2C6H4CF3 | H | F | Cl | Cl | H |
A-528 | (CH2)2C6H4OCH3 | H | F | Cl | Cl | H |
A-529 | (CH2)2C6H4OCF3 | H | F | Cl | Cl | H |
A-530 | CH2CH=CH2 | H | F | Cl | Cl | H |
A-531 | 环-C3H5 | H | F | Cl | Cl | H |
A-532 | (CH2)2NHCH3 | H | F | Cl | Cl | H |
A-533 | H | H | F | F | Cl | H |
A-534 | CH3 | CH3 | F | F | Cl | H |
A-535 | CH2CH3 | CH2CH3 | F | F | Cl | H |
A-536 | CH3 | H | F | F | Cl | H |
A-537 | CH2CH3 | H | F | F | Cl | H |
A-538 | (CH2)2CH3 | H | F | F | Cl | H |
A-539 | CH(CH3)2 | H | F | F | Cl | H |
A-540 | CH2CF3 | H | F | F | Cl | H |
A-541 | C(CH3)3 | H | F | F | Cl | H |
A-542 | CH2CH(CH3)2 | H | F | F | Cl | H |
A-543 | CH(CH3)CH2CH3 | H | F | F | Cl | H |
A-544 | (CH2)2OCH3 | H | F | F | Cl | H |
A-545 | CH2CH(OCH3)2 | H | F | F | Cl | H |
A-546 | CH2CH(OCH2CH3)2 | H | F | F | Cl | H |
A-547 | CH2C6H5 | H | F | F | Cl | H |
A-548 | CH(CH3)C6H5 | H | F | F | Cl | H |
A-549 | (CH2)2OC6H5 | H | F | F | Cl | H |
A-550 | (CH2)2C6H5 | H | F | F | Cl | H |
A-551 | (CH2)2C6H4F | H | F | F | Cl | H |
A-552 | (CH2)2C6H4Cl | H | F | F | Cl | H |
A-553 | (CH2)2C6H4CN | H | F | F | Cl | H |
A-554 | (CH2)2C6H4CH3 | H | F | F | Cl | H |
A-555 | (CH2)2C6H4CF3 | H | F | F | Cl | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-556 | (CH2)2C6H4OCH3 | H | F | F | Cl | H |
A-557 | (CH2)2C6H4OCF3 | H | F | F | Cl | H |
A-558 | CH2CH=CH2 | H | F | F | Cl | H |
A-559 | 环-C3H5 | H | F | F | Cl | H |
A-560 | (CH2)2NHCH3 | H | F | F | Cl | H |
A-561 | H | H | F | Cl | F | H |
A-562 | CH3 | CH3 | F | Cl | F | H |
A-563 | CH2CH3 | CH2CH3 | F | Cl | F | H |
A-564 | CH3 | H | F | Cl | F | H |
A-565 | CH2CH3 | H | F | Cl | F | H |
A-566 | (CH2)2CH3 | H | F | Cl | F | H |
A-567 | CH(CH3)2 | H | F | Cl | F | H |
A-568 | CH2CF3 | H | F | Cl | F | H |
A-569 | C(CH3)3 | H | F | Cl | F | H |
A-570 | CH2CH(CH3)2 | H | F | Cl | F | H |
A-571 | CH(CH3)CH2CH3 | H | F | Cl | F | H |
A-572 | (CH2)2OCH3 | H | F | Cl | F | H |
A-573 | CH2CH(OCH3)2 | H | F | Cl | F | H |
A-574 | CH2CH(OCH2CH3)2 | H | F | Cl | F | H |
A-575 | CH2C6H5 | H | F | Cl | F | H |
A-576 | CH(CH3)C6H5 | H | F | Cl | F | H |
A-577 | (CH2)2OC6H5 | H | F | Cl | F | H |
A-578 | (CH2)2C6H5 | H | F | Cl | F | H |
A-579 | (CH2)2C6H4F | H | F | Cl | F | H |
A-580 | (CH2)2C6H4Cl | H | F | Cl | F | H |
A-581 | (CH2)2C6H4CN | H | F | Cl | F | H |
A-582 | (CH2)2C6H4CH3 | H | F | Cl | F | H |
A-583 | (CH2)2C6H4CF3 | H | F | Cl | F | H |
A-584 | (CH2)2C6H4OCH3 | H | F | Cl | F | H |
A-585 | (CH2)2C6H4OCF3 | H | F | Cl | F | H |
A-586 | CH2CH=CH2 | H | F | Cl | F | H |
A-587 | 环-C3H5 | H | F | Cl | F | H |
A-588 | (CH2)2NHCH3 | H | F | Cl | F | H |
A-589 | H | H | Cl | F | F | H |
A-590 | CH3 | CH3 | Cl | F | F | H |
A-591 | CH2CH3 | CH2CH3 | Cl | F | F | H |
A-592 | CH3 | H | Cl | F | F | H |
A-593 | CH2CH3 | H | Cl | F | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-594 | (CH2)2CH3 | H | Cl | F | F | H |
A-595 | CH(CH3)2 | H | Cl | F | F | H |
A-596 | CH2CF3 | H | Cl | F | F | H |
A-597 | C(CH3)3 | H | Cl | F | F | H |
A-598 | CH2CH(CH3)2 | H | Cl | F | F | H |
A-599 | CH(CH3)CH2CH3 | H | Cl | F | F | H |
A-600 | (CH2)2OCH3 | H | Cl | F | F | H |
A-601 | CH2CH(OCH3)2 | H | Cl | F | F | H |
A-602 | CH2CH(OCH2CH3)2 | H | Cl | F | F | H |
A-603 | CH2C6H5 | H | Cl | F | F | H |
A-604 | CH(CH3)C6H5 | H | Cl | F | F | H |
A-605 | (CH2)2OC6H5 | H | Cl | F | F | H |
A-606 | (CH2)2C6H5 | H | Cl | F | F | H |
A-607 | (CH2)2C6H4F | H | Cl | F | F | H |
A-608 | (CH2)2C6H4Cl | H | Cl | F | F | H |
A-609 | (CH2)2C6H4CN | H | Cl | F | F | H |
A-610 | (CH2)2C6H4CH3 | H | Cl | F | F | H |
A-611 | (CH2)2C6H4CF3 | H | Cl | F | F | H |
A-612 | (CH2)2C6H4OCH3 | H | Cl | F | F | H |
A-613 | (CH2)2C6H4OCF3 | H | Cl | F | F | H |
A-614 | CH2CH=CH2 | H | Cl | F | F | H |
A-615 | 环-C3H5 | H | Cl | F | F | H |
A-616 | (CH2)2NHCH3 | H | Cl | F | F | H |
A-617 | H | H | F | F | F | H |
A-618 | CH3 | CH3 | F | F | F | H |
A-619 | CH2CH3 | CH2CH3 | F | F | F | H |
A-620 | CH3 | H | F | F | F | H |
A-621 | CH2CH3 | H | F | F | F | H |
A-622 | (CH2)2CH3 | H | F | F | F | H |
A-623 | CH(CH3)2 | H | F | F | F | H |
A-624 | CH2CF3 | H | F | F | F | H |
A-625 | C(CH3)3 | H | F | F | F | H |
A-626 | CH2CH(CH3)2 | H | F | F | F | H |
A-627 | CH(CH3)CH2CH3 | H | F | F | F | H |
A-628 | (CH2)2OCH3 | H | F | F | F | H |
A-629 | CH2CH(OCH3)2 | H | F | F | F | H |
A-630 | CH2CH(OCH2CH3)2 | H | F | F | F | H |
A-631 | CH2C6H5 | H | F | F | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-632 | CH(CH3)C6H5 | H | F | F | F | H |
A-633 | (CH2)2OC6H5 | H | F | F | F | H |
A-634 | (CH2)2C6H5 | H | F | F | F | H |
A-635 | (CH2)2C6H4F | H | F | F | F | H |
A-636 | (CH2)2C6H4Cl | H | F | F | F | H |
A-637 | (CH2)2C6H4CN | H | F | F | F | H |
A-638 | (CH2)2C6H4CH3 | H | F | F | F | H |
A-639 | (CH2)2C6H4CF3 | H | F | F | F | H |
A-640 | (CH2)2C6H4OCH3 | H | F | F | F | H |
A-641 | (CH2)2C6H4OCF3 | H | F | F | F | H |
A-642 | CH2CH=CH2 | H | F | F | F | H |
A-643 | 环-C3H5 | H | F | F | F | H |
A-644 | (CH2)2NHCH3 | H | F | F | F | H |
A-645 | H | H | Cl | Cl | CF3 | H |
A-646 | CH3 | CH3 | Cl | Cl | CF3 | H |
A-647 | CH2CH3 | CH2CH3 | Cl | Cl | CF3 | H |
A-648 | CH3 | H | Cl | Cl | CF3 | H |
A-649 | CH2CH3 | H | Cl | Cl | CF3 | H |
A-650 | (CH2)2CH3 | H | Cl | Cl | CF3 | H |
A-651 | CH(CH3)2 | H | Cl | Cl | CF3 | H |
A-652 | CH2CF3 | H | Cl | Cl | CF3 | H |
A-653 | C(CH3)3 | H | Cl | Cl | CF3 | H |
A-654 | CH2CH(CH3)2 | H | Cl | Cl | CF3 | H |
A-655 | CH(CH3)CH2CH3 | H | Cl | Cl | CF3 | H |
A-656 | (CH2)2OCH3 | H | Cl | Cl | CF3 | H |
A-657 | CH2CH(OCH3)2 | H | Cl | Cl | CF3 | H |
A-658 | CH2CH(OCH2CH3)2 | H | Cl | Cl | CF3 | H |
A-659 | CH2C6H5 | H | Cl | Cl | CF3 | H |
A-660 | CH(CH3)C6H5 | H | Cl | Cl | CF3 | H |
A-661 | (CH2)2OC6H5 | H | Cl | Cl | CF3 | H |
A-662 | (CH2)2C6H5 | H | Cl | Cl | CF3 | H |
A-663 | (CH2)2C6H4F | H | Cl | Cl | CF3 | H |
A-664 | (CH2)2C6H4Cl | H | Cl | Cl | CF3 | H |
A-665 | (CH2)2C6H4CN | H | Cl | Cl | CF3 | H |
A-666 | (CH2)2C6H4CH3 | H | Cl | Cl | CF3 | H |
A-667 | (CH2)2C6H4CF3 | H | Cl | Cl | CF3 | H |
A-668 | (CH2)2C6H4OCH3 | H | Cl | Cl | CF3 | H |
A-669 | (CH2)2C6H4OCF3 | H | Cl | Cl | CF3 | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-670 | CH2CH=CH2 | H | Cl | Cl | CF3 | H |
A-671 | 环-C3H5 | H | Cl | Cl | CF3 | H |
A-672 | (CH2)2NHCH3 | H | Cl | Cl | CF3 | H |
A-673 | H | H | CF3 | Cl | Cl | H |
A-674 | CH3 | CH3 | CF3 | Cl | Cl | H |
A-675 | CH2CH3 | CH2CH3 | CF3 | Cl | Cl | H |
A-676 | CH3 | H | CF3 | Cl | Cl | H |
A-677 | CH2CH3 | H | CF3 | Cl | Cl | H |
A-678 | (CH2)2CH3 | H | CF3 | Cl | Cl | H |
A-679 | CH(CH3)2 | H | CF3 | Cl | Cl | H |
A-680 | CH2CF3 | H | CF3 | Cl | Cl | H |
A-681 | C(CH3)3 | H | CF3 | Cl | Cl | H |
A-682 | CH2CH(CH3)2 | H | CF3 | Cl | Cl | H |
A-683 | CH(CH3)CH2CH3 | H | CF3 | Cl | Cl | H |
A-684 | (CH2)2OCH3 | H | CF3 | Cl | Cl | H |
A-685 | CH2CH(OCH3)2 | H | CF3 | Cl | Cl | H |
A-686 | CH2CH(OCH2CH3)2 | H | CF3 | Cl | Cl | H |
A-687 | CH2C6H5 | H | CF3 | Cl | Cl | H |
A-688 | CH(CH3)C6H5 | H | CF3 | Cl | Cl | H |
A-689 | (CH2)2OC6H5 | H | CF3 | Cl | Cl | H |
A-690 | (CH2)2C6H5 | H | CF3 | Cl | Cl | H |
A-691 | (CH2)2C6H4F | H | CF3 | Cl | Cl | H |
A-692 | (CH2)2C6H4Cl | H | CF3 | Cl | Cl | H |
A-693 | (CH2)2C6H4CN | H | CF3 | Cl | Cl | H |
A-694 | (CH2)2C6H4CH3 | H | CF3 | Cl | Cl | H |
A-695 | (CH2)2C6H4CF3 | H | CF3 | Cl | Cl | H |
A-696 | (CH2)2C6H4OCH3 | H | CF3 | Cl | Cl | H |
A-697 | (CH2)2C6H4OCF3 | H | CF3 | Cl | Cl | H |
A-698 | CH2CH=CH2 | H | CF3 | Cl | Cl | H |
A-699 | 环-C3H5 | H | CF3 | Cl | Cl | H |
A-700 | (CH2)2NHCH3 | H | CF3 | Cl | Cl | H |
A-701 | H | H | CF3 | Cl | F | H |
A-702 | CH3 | CH3 | CF3 | Cl | F | H |
A-703 | CH2CH3 | CH2CH3 | CF3 | Cl | F | H |
A-704 | CH3 | H | CF3 | Cl | F | H |
A-705 | CH2CH3 | H | CF3 | Cl | F | H |
A-706 | (CH2)2CH3 | H | CF3 | Cl | F | H |
A-707 | CH(CH3)2 | H | CF3 | Cl | F | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-708 | CH2CF3 | H | CF3 | Cl | F | H |
A-709 | C(CH3)3 | H | CF3 | Cl | F | H |
A-710 | CH2CH(CH3)2 | H | CF3 | Cl | F | H |
A-711 | CH(CH3)CH2CH3 | H | CF3 | Cl | F | H |
A-712 | (CH2)2OCH3 | H | CF3 | Cl | F | H |
A-713 | CH2CH(OCH3)2 | H | CF3 | Cl | F | H |
A-714 | CH2CH(OCH2CH3)2 | H | CF3 | Cl | F | H |
A-715 | CH2C6H5 | H | CF3 | Cl | F | H |
A-716 | CH(CH3)C6H5 | H | CF3 | Cl | F | H |
A-717 | (CH2)2OC6H5 | H | CF3 | Cl | F | H |
A-718 | (CH2)2C6H5 | H | CF3 | Cl | F | H |
A-719 | (CH2)2C6H4F | H | CF3 | Cl | F | H |
A-720 | (CH2)2C6H4Cl | H | CF3 | Cl | F | H |
A-721 | (CH2)2C6H4CN | H | CF3 | Cl | F | H |
A-722 | (CH2)2C6H4CH3 | H | CF3 | Cl | F | H |
A-723 | (CH2)2C6H4CF3 | H | CF3 | Cl | F | H |
A-724 | (CH2)2C6H4OCH3 | H | CF3 | Cl | F | H |
A-725 | (CH2)2C6H4OCF3 | H | CF3 | Cl | F | H |
A-726 | CH2CH=CH2 | H | CF3 | Cl | F | H |
A-727 | 环-C3H5 | H | CF3 | Cl | F | H |
A-728 | (CH2)2NHCH3 | H | CF3 | Cl | F | H |
A-729 | H | H | F | Cl | CF3 | H |
A-730 | CH3 | CH3 | F | Cl | CF3 | H |
A-731 | CH2CH3 | CH2CH3 | F | Cl | CF3 | H |
A-732 | CH3 | H | F | Cl | CF3 | H |
A-733 | CH2CH3 | H | F | Cl | CF3 | H |
A-734 | (CH2)2CH3 | H | F | Cl | CF3 | H |
A-735 | CH(CH3)2 | H | F | Cl | CF3 | H |
A-736 | CH2CF3 | H | F | Cl | CF3 | H |
A-737 | C(CH3)3 | H | F | Cl | CF3 | H |
A-738 | CH2CH(CH3)2 | H | F | Cl | CF3 | H |
A-739 | CH(CH3)CH2CH3 | H | F | Cl | CF3 | H |
A-740 | (CH2)2OCH3 | H | F | Cl | CF3 | H |
A-741 | CH2CH(OCH3)2 | H | F | Cl | CF3 | H |
A-742 | CH2CH(OCH2CH3)2 | H | F | Cl | CF3 | H |
A-743 | CH2C6H5 | H | F | Cl | CF3 | H |
A-744 | CH(CH3)C6H5 | H | F | Cl | CF3 | H |
A-745 | (CH2)2OC6H5 | H | F | Cl | CF3 | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-746 | (CH2)2C6H5 | H | F | Cl | CF3 | H |
A-747 | (CH2)2C6H4F | H | F | Cl | CF3 | H |
A-748 | (CH2)2C6H4Cl | H | F | Cl | CF3 | H |
A-749 | (CH2)2C6H4CN | H | F | Cl | CF3 | H |
A-750 | (CH2)2C6H4CH3 | H | F | Cl | CF3 | H |
A-751 | (CH2)2C6H4CF3 | H | F | Cl | CF3 | H |
A-752 | (CH2)2C6H4OCH3 | H | F | Cl | CF3 | H |
A-753 | (CH2)2C6H4OCF3 | H | F | Cl | CF3 | H |
A-754 | CH2CH=CH2 | H | F | Cl | CF3 | H |
A-755 | 环-C3H5 | H | F | Cl | CF3 | H |
A-756 | (CH2)2NHCH3 | H | F | Cl | CF3 | H |
A-757 | H | H | F | Cl | CF3 | H |
A-758 | CH3 | CH3 | F | Cl | CF3 | H |
A-759 | CH2CH3 | CH2CH3 | F | Cl | CF3 | H |
A-760 | CH3 | H | F | Cl | CF3 | H |
A-761 | CH2CH3 | H | F | Cl | CF3 | H |
A-762 | (CH2)2CH3 | H | F | Cl | CF3 | H |
A-763 | CH(CH3)2 | H | F | Cl | CF3 | H |
A-764 | CH2CF3 | H | F | Cl | CF3 | H |
A-765 | C(CH3)3 | H | F | Cl | CF3 | H |
A-766 | CH2CH(CH3)2 | H | F | Cl | CF3 | H |
A-767 | CH(CH3)CH2CH3 | H | F | Cl | CF3 | H |
A-768 | (CH2)2OCH3 | H | F | Cl | CF3 | H |
A-769 | CH2CH(OCH3)2 | H | F | Cl | CF3 | H |
A-770 | CH2CH(OCH2CH3)2 | H | F | Cl | CF3 | H |
A-771 | CH2C6H5 | H | F | Cl | CF3 | H |
A-772 | CH(CH3)C6H5 | H | F | Cl | CF3 | H |
A-773 | (CH2)2OC6H5 | H | F | Cl | CF3 | H |
A-774 | (CH2)2C6H5 | H | F | Cl | CF3 | H |
A-775 | (CH2)2C6H4F | H | F | Cl | CF3 | H |
A-776 | (CH2)2C6H4Cl | H | F | Cl | CF3 | H |
A-777 | (CH2)2C6H4CN | H | F | Cl | CF3 | H |
A-778 | (CH2)2C6H4CH3 | H | F | Cl | CF3 | H |
A-779 | (CH2)2C6H4CF3 | H | F | Cl | CF3 | H |
A-780 | (CH2)2C6H4OCH3 | H | F | Cl | CF3 | H |
A-781 | (CH2)2C6H4OCF3 | H | F | Cl | CF3 | H |
A-782 | CH2CH=CH2 | H | F | Cl | CF3 | H |
A-783 | 环-C3H5 | H | F | Cl | CF3 | H |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-784 | (CH2)2NHCH3 | H | F | Cl | CF3 | H |
A-785 | H | H | Cl | H | CF3 | 6-Cl |
A-786 | CH3 | CH3 | Cl | H | CF3 | 6-Cl |
A-787 | CH2CH3 | CH2CH3 | Cl | H | CF3 | 6-Cl |
A-788 | CH3 | H | Cl | H | CF3 | 6-Cl |
A-789 | CH2CH3 | H | Cl | H | CF3 | 6-Cl |
A-790 | (CH2)2CH3 | H | Cl | H | CF3 | 6-Cl |
A-791 | CH(CH3)2 | H | Cl | H | CF3 | 6-Cl |
A-792 | CH2CF3 | H | Cl | H | CF3 | 6-Cl |
A-793 | C(CH3)3 | H | Cl | H | CF3 | 6-Cl |
A-794 | CH2CH(CH3)2 | H | Cl | H | CF3 | 6-Cl |
A-795 | CH(CH3)CH2CH3 | H | Cl | H | CF3 | 6-Cl |
A-796 | (CH2)2OCH3 | H | Cl | H | CF3 | 6-Cl |
A-797 | CH2CH(OCH3)2 | H | Cl | H | CF3 | 6-Cl |
A-798 | CH2CH(OCH2CH3)2 | H | Cl | H | CF3 | 6-Cl |
A-799 | CH2C6H5 | H | Cl | H | CF3 | 6-Cl |
A-800 | CH(CH3)C6H5 | H | Cl | H | CF3 | 6-Cl |
A-801 | (CH2)2OC6H5 | H | Cl | H | CF3 | 6-Cl |
A-802 | (CH2)2C6H5 | H | Cl | H | CF3 | 6-Cl |
A-803 | (CH2)2C6H4F | H | Cl | H | CF3 | 6-Cl |
A-804 | (CH2)2C6H4Cl | H | Cl | H | CF3 | 6-Cl |
A-805 | (CH2)2C6H4CN | H | Cl | H | CF3 | 6-Cl |
A-806 | (CH2)2C6H4CH3 | H | Cl | H | CF3 | 6-Cl |
A-807 | (CH2)2C6H4CF3 | H | Cl | H | CF3 | 6-Cl |
A-808 | (CH2)2C6H4OCH3 | H | Cl | H | CF3 | 6-Cl |
A-809 | (CH2)2C6H4OCF3 | H | Cl | H | CF3 | 6-Cl |
A-810 | CH2CH=CH2 | H | Cl | H | CF3 | 6-Cl |
A-811 | 环-C3H5 | H | Cl | H | CF3 | 6-Cl |
A-812 | (CH2)2NHCH3 | H | Cl | H | CF3 | 6-Cl |
A-813 | H | H | Cl | H | F | 6-Cl |
A-814 | CH3 | CH3 | Cl | H | F | 6-Cl |
A-815 | CH2CH3 | CH2CH3 | Cl | H | F | 6-Cl |
A-816 | CH3 | H | Cl | H | F | 6-Cl |
A-817 | CH2CH3 | H | Cl | H | F | 6-Cl |
A-818 | (CH2)2CH3 | H | Cl | H | F | 6-Cl |
A-819 | CH(CH3)2 | H | Cl | H | F | 6-Cl |
A-820 | CH2CF3 | H | Cl | H | F | 6-Cl |
A-821 | C(CH3)3 | H | Cl | H | F | 6-Cl |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-822 | CH2CH(CH3)2 | H | Cl | H | F | 6-Cl |
A-823 | CH(CH3)CH2CH3 | H | Cl | H | F | 6-Cl |
A-824 | (CH2)2OCH3 | H | Cl | H | F | 6-Cl |
A-825 | CH2CH(OCH3)2 | H | Cl | H | F | 6-Cl |
A-826 | CH2CH(OCH2CH3)2 | H | Cl | H | F | 6-Cl |
A-827 | CH2C6H5 | H | Cl | H | F | 6-Cl |
A-828 | CH(CH3)C6H5 | H | Cl | H | F | 6-Cl |
A-829 | (CH2)2OC6H5 | H | Cl | H | F | 6-Cl |
A-830 | (CH2)2C6H5 | H | Cl | H | F | 6-Cl |
A-831 | (CH2)2C6H4F | H | Cl | H | F | 6-Cl |
A-832 | (CH2)2C6H4Cl | H | Cl | H | F | 6-Cl |
A-833 | (CH2)2C6H4CN | H | Cl | H | F | 6-Cl |
A-834 | (CH2)2C6H4CH3 | H | Cl | H | F | 6-Cl |
A-835 | (CH2)2C6H4CF3 | H | Cl | H | F | 6-Cl |
A-836 | (CH2)2C6H4OCH3 | H | Cl | H | F | 6-Cl |
A-837 | (CH2)2C6H4OCF3 | H | Cl | H | F | 6-Cl |
A-838 | CH2CH=CH2 | H | Cl | H | F | 6-Cl |
A-839 | 环-C3H5 | H | Cl | H | F | 6-Cl |
A-840 | (CH2)2NHCH3 | H | Cl | H | F | 6-Cl |
A-841 | H | H | F | H | Cl | 6-Cl |
A-842 | CH3 | CH3 | F | H | Cl | 6-Cl |
A-843 | CH2CH3 | CH2CH3 | F | H | Cl | 6-Cl |
A-844 | CH3 | H | F | H | Cl | 6-Cl |
A-845 | CH2CH3 | H | F | H | Cl | 6-Cl |
A-846 | (CH2)2CH3 | H | F | H | Cl | 6-Cl |
A-847 | C H(CH3)2 | H | F | H | Cl | 6-Cl |
A-848 | CH2CF3 | H | F | H | Cl | 6-Cl |
A-849 | C(CH3)3 | H | F | H | Cl | 6-Cl |
A-850 | CH2CH(CH3)2 | H | F | H | Cl | 6-Cl |
A-851 | CH(CH3)CH2CH3 | H | F | H | Cl | 6-Cl |
A-852 | (CH2)2OCH3 | H | F | H | Cl | 6-Cl |
A-853 | CH2CH(OCH3)2 | H | F | H | Cl | 6-Cl |
A-854 | CH2CH(OCH2CH3)2 | H | F | H | Cl | 6-Cl |
A-855 | CH2C6H5 | H | F | H | Cl | 6-Cl |
A-856 | CH(CH3)C6H5 | H | F | H | Cl | 6-Cl |
A-857 | (CH2)2OC6H5 | H | F | H | Cl | 6-Cl |
A-858 | (CH2)2C6H5 | H | F | H | Cl | 6-Cl |
A-859 | (CH2)2C6H4F | H | F | H | Cl | 6-Cl |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-860 | (CH2)2C6H4Cl | H | F | H | Cl | 6-Cl |
A-861 | (CH2)2C6H4CN | H | F | H | Cl | 6-Cl |
A-862 | (CH2)2C6H4CH3 | H | F | H | Cl | 6-Cl |
A-863 | (CH2)2C6H4CF3 | H | F | H | Cl | 6-Cl |
A-864 | (CH2)2C6H4OCH3 | H | F | H | Cl | 6-Cl |
A-865 | (CH2)2C6H4OCF3 | H | F | H | Cl | 6-Cl |
A-866 | CH2CH=CH2 | H | F | H | Cl | 6-Cl |
A-867 | 环-C3H5 | H | F | H | Cl | 6-Cl |
A-868 | (CH2)2NHCH3 | H | F | H | Cl | 6-Cl |
A-869 | H | H | Cl | H | Cl | 6-Cl |
A-870 | CH3 | CH3 | Cl | H | Cl | 6-Cl |
A-871 | CH2CH3 | CH2CH3 | Cl | H | Cl | 6-Cl |
A-872 | CH3 | H | Cl | H | Cl | 6-Cl |
A-873 | CH2CH3 | H | Cl | H | Cl | 6-Cl |
A-874 | (CH2)2CH3 | H | Cl | H | Cl | 6-Cl |
A-875 | CH(CH3)2 | H | Cl | H | Cl | 6-Cl |
A-876 | CH2CF3 | H | Cl | H | Cl | 6-Cl |
A-877 | C(CH3)3 | H | Cl | H | Cl | 6-Cl |
A-878 | CH2CH(CH3)2 | H | Cl | H | Cl | 6-Cl |
A-879 | CH(CH3)CH2CH3 | H | Cl | H | Cl | 6-Cl |
A-880 | (CH2)2OCH3 | H | Cl | H | Cl | 6-Cl |
A-881 | CH2CH(OCH3)2 | H | Cl | H | Cl | 6-Cl |
A-882 | CH2CH(OCH2CH3)2 | H | Cl | H | Cl | 6-Cl |
A-883 | CH2C6H5 | H | Cl | H | Cl | 6-Cl |
A-884 | CH(CH3)C6H5 | H | Cl | H | Cl | 6-Cl |
A-885 | (CH2)2OC6H5 | H | Cl | H | Cl | 6-Cl |
A-886 | (CH2)2C6H5 | H | Cl | H | Cl | 6-Cl |
A-887 | (CH2)2C6H4F | H | Cl | H | Cl | 6-Cl |
A-888 | (CH2)2C6H4Cl | H | Cl | H | Cl | 6-Cl |
A-889 | (CH2)2C6H4CN | H | Cl | H | Cl | 6-Cl |
A-890 | (CH2)2C6H4CH3 | H | Cl | H | Cl | 6-Cl |
A-891 | (CH2)2C6H4CF3 | H | Cl | H | Cl | 6-Cl |
A-892 | (CH2)2C6H4OCH3 | H | Cl | H | Cl | 6-Cl |
A-893 | (CH2)2C6H4OCF3 | H | Cl | H | Cl | 6-Cl |
A-894 | CH2CH=CH2 | H | Cl | H | Cl | 6-Cl |
A-895 | 环-C3H5 | H | Cl | H | Cl | 6-Cl |
A-896 | (CH2)2NHCH3 | H | Cl | H | Cl | 6-Cl |
A-897 | H | H | F | H | Cl | 6-F |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-898 | CH3 | CH3 | F | H | Cl | 6-F |
A-899 | CH2CH3 | CH2CH3 | F | H | Cl | 6-F |
A-900 | CH3 | H | F | H | Cl | 6-F |
A-901 | CH2CH3 | H | F | H | Cl | 6-F |
A-902 | (CH2)2CH3 | H | F | H | Cl | 6-F |
A-903 | CH(CH3)2 | H | F | H | Cl | 6-F |
A-904 | CH2CF3 | H | F | H | Cl | 6-F |
A-905 | C(CH3)3 | H | F | H | Cl | 6-F |
A-906 | CH2CH(CH3)2 | H | F | H | Cl | 6-F |
A-907 | CH(CH3)CH2CH3 | H | F | H | Cl | 6-F |
A-908 | (CH2)2OCH3 | H | F | H | Cl | 6-F |
A-909 | CH2CH(OCH3)2 | H | F | H | Cl | 6-F |
A-910 | CH2CH(OCH2CH3)2 | H | F | H | Cl | 6-F |
A-911 | CH2C6H5 | H | F | H | Cl | 6-F |
A-912 | CH(CH3)C6H5 | H | F | H | Cl | 6-F |
A-913 | (CH2)2OC6H5 | H | F | H | Cl | 6-F |
A-914 | (CH2)2C6H5 | H | F | H | Cl | 6-F |
A-915 | (CH2)2C6H4F | H | F | H | Cl | 6-F |
A-916 | (CH2)2C6H4Cl | H | F | H | Cl | 6-F |
A-917 | (CH2)2C6H4CN | H | F | H | Cl | 6-F |
A-918 | (CH2)2C6H4CH3 | H | F | H | Cl | 6-F |
A-919 | (CH2)2C6H4CF3 | H | F | H | Cl | 6-F |
A-920 | (CH2)2C6H4OCH3 | H | F | H | Cl | 6-F |
A-921 | (CH2)2C6H4OCF3 | H | F | H | Cl | 6-F |
A-922 | CH2CH=CH2 | H | F | H | Cl | 6-F |
A-923 | 环-C3H5 | H | F | H | Cl | 6-F |
A-924 | (CH2)2NHCH3 | H | F | H | Cl | 6-F |
A-925 | H | H | F | H | F | 6-Cl |
A-926 | CH3 | CH3 | F | H | F | 6-Cl |
A-927 | CH2CH3 | CH2CH3 | F | H | F | 6-Cl |
A-928 | CH3 | H | F | H | F | 6-Cl |
A-929 | CH2CH3 | H | F | H | F | 6-Cl |
A-930 | (CH2)2CH3 | H | F | H | F | 6-Cl |
A-931 | CH(CH3)2 | H | F | H | F | 6-Cl |
A-932 | CH2CF3 | H | F | H | F | 6-Cl |
A-933 | C(CH3)3 | H | F | H | F | 6-Cl |
A-934 | CH2CH(CH3)2 | H | F | H | F | 6-Cl |
A-935 | CH(CH3)CH2CH3 | H | F | H | F | 6-Cl |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-936 | (CH2)2OCH3 | H | F | H | F | 6-Cl |
A-937 | CH2CH(OCH3)2 | H | F | H | F | 6-Cl |
A-938 | CH2CH(OCH2CH3)2 | H | F | H | F | 6-Cl |
A-939 | CH2C6H5 | H | F | H | F | 6-Cl |
A-940 | CH(CH3)C6H5 | H | F | H | F | 6-Cl |
A-941 | (CH2)2OC6H5 | H | F | H | F | 6-Cl |
A-942 | (CH2)2C6H5 | H | F | H | F | 6-Cl |
A-943 | (CH2)2C6H4F | H | F | H | F | 6-Cl |
A-944 | (CH2)2C6H4Cl | H | F | H | F | 6-Cl |
A-945 | (CH2)2C6H4CN | H | F | H | F | 6-Cl |
A-946 | (CH2)2C6H4CH3 | H | F | H | F | 6-Cl |
A-947 | (CH2)2C6H4CF3 | H | F | H | F | 6-Cl |
A-948 | (CH2)2C6H4OCH3 | H | F | H | F | 6-Cl |
A-949 | (CH2)2C6H4OCF3 | H | F | H | F | 6-Cl |
A-950 | CH2CH=CH2 | H | F | H | F | 6-Cl |
A-951 | 环-C3H5 | H | F | H | F | 6-Cl |
A-952 | (CH2)2NHCH3 | H | F | H | F | 6-Cl |
A-953 | H | H | F | H | CF3 | 6-F |
A-954 | CH3 | CH3 | F | H | CF3 | 6-F |
A-955 | CH2CH3 | CH2CH3 | F | H | CF3 | 6-F |
A-956 | CH3 | H | F | H | CF3 | 6-F |
A-957 | CH2CH3 | H | F | H | CF3 | 6-F |
A-958 | (CH2)2CH3 | H | F | H | CF3 | 6-F |
A-959 | CH(CH3)2 | H | F | H | CF3 | 6-F |
A-960 | CH2CF3 | H | F | H | CF3 | 6-F |
A-961 | C(CH3)3 | H | F | H | CF3 | 6-F |
A-962 | CH2CH(CH3)2 | H | F | H | CF3 | 6-F |
A-963 | CH(CH3)CH2CH3 | H | F | H | CF3 | 6-F |
A-964 | (CH2)2OCH3 | H | F | H | CF3 | 6-F |
A-965 | CH2CH(OCH3)2 | H | F | H | CF3 | 6-F |
A-966 | CH2CH(OCH2CH3)2 | H | F | H | CF3 | 6-F |
A-967 | CH2C6H5 | H | F | H | CF3 | 6-F |
A-968 | CH(CH3)C6H5 | H | F | H | CF3 | 6-F |
A-969 | (CH2)2OC6H5 | H | F | H | CF3 | 6-F |
A-970 | (CH2)2C6H5 | H | F | H | CF3 | 6-F |
A-971 | (CH2)2C6H4F | H | F | H | CF3 | 6-F |
A-972 | (CH2)2C6H4Cl | H | F | H | CF3 | 6-F |
A-973 | (CH2)2C6H4CN | H | F | H | CF3 | 6-F |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-974 | (CH2)2C6H4CH3 | H | F | H | CF3 | 6-F |
A-975 | (CH2)2C6H4CF3 | H | F | H | CF3 | 6-F |
A-976 | (CH2)2C6H4OCH3 | H | F | H | CF3 | 6-F |
A-977 | (CH2)2C6H4OCF3 | H | F | H | CF3 | 6-F |
A-978 | CH2CH=CH2 | H | F | H | CF3 | 6-F |
A-979 | 环-C3H5 | H | F | H | CF3 | 6-F |
A-980 | (CH2)2NHCH3 | H | F | H | CF3 | 6-F |
A-981 | H | H | CF3 | H | F | 6-F |
A-982 | CH3 | CH3 | CF3 | H | F | 6-F |
A-983 | CH2CH3 | CH2CH3 | CF3 | H | F | 6-F |
A-984 | CH3 | H | CF3 | H | F | 6-F |
A-985 | CH2CH3 | H | CF3 | H | F | 6-F |
A-986 | (CH2)2CH3 | H | CF3 | H | F | 6-F |
A-987 | CH(CH3)2 | H | CF3 | H | F | 6-F |
A-988 | CH2CF3 | H | CF3 | H | F | 6-F |
A-989 | C(CH3)3 | H | CF3 | H | F | 6-F |
A-990 | CH2CH(CH3)2 | H | CF3 | H | F | 6-F |
A-991 | CH(CH3)CH2CH3 | H | CF3 | H | F | 6-F |
A-992 | (CH2)2OCH3 | H | CF3 | H | F | 6-F |
A-993 | CH2CH(OCH3)2 | H | CF3 | H | F | 6-F |
A-994 | CH2CH(OCH2CH3)2 | H | CF3 | H | F | 6-F |
A-995 | CH2C6H5 | H | CF3 | H | F | 6-F |
A-996 | CH(CH3)C6H5 | H | CF3 | H | F | 6-F |
A-997 | (CH2)2OC6H5 | H | CF3 | H | F | 6-F |
A-998 | (CH2)2C6H5 | H | CF3 | H | F | 6-F |
A-999 | (CH2)2C6H4F | H | CF3 | H | F | 6-F |
A-1000 | (CH2)2C6H4Cl | H | CF3 | H | F | 6-F |
A-1001 | (CH2)2C6H4CN | H | CF3 | H | F | 6-F |
A-1002 | (CH2)2C6H4CH3 | H | CF3 | H | F | 6-F |
A-1003 | (CH2)2C6H4CF3 | H | CF3 | H | F | 6-F |
A-1004 | (CH2)2C6H4OCH3 | H | CF3 | H | F | 6-F |
A-1005 | (CH2)2C6H4OCF3 | H | CF3 | H | F | 6-F |
A-1006 | CH2CH=CH2 | H | CF3 | H | F | 6-F |
A-1007 | 环-C3H5 | H | CF3 | H | F | 6-F |
A-1008 | (CH2)2NHCH3 | H | CF3 | H | F | 6-F |
A-1009 | H | H | CF3 | H | F | 6-CF3 |
A-1010 | CH3 | CH3 | CF3 | H | F | 6-CF3 |
A-1011 | CH2CH3 | CH2CH3 | CF3 | H | F | 6-CF3 |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1012 | CH3 | H | CF3 | H | F | 6-CF3 |
A-1013 | CH2CH3 | H | CF3 | H | F | 6-CF3 |
A-1014 | (CH2)2CH3 | H | CF3 | H | F | 6-CF3 |
A-1015 | CH(CH3)2 | H | CF3 | H | F | 6-CF3 |
A-1016 | CH2CF3 | H | CF3 | H | F | 6-CF3 |
A-1017 | C(CH3)3 | H | CF3 | H | F | 6-CF3 |
A-1018 | CH2CH(CH3)2 | H | CF3 | H | F | 6-CF3 |
A-1019 | CH(CH3)CH2CH3 | H | CF3 | H | F | 6-CF3 |
A-1020 | (CH2)2OCH3 | H | CF3 | H | F | 6-CF3 |
A-1021 | CH2CH(OCH3)2 | H | CF3 | H | F | 6-CF3 |
A-1022 | CH2CH(OCH2CH3)2 | H | CF3 | H | F | 6-CF3 |
A-1023 | CH2C6H5 | H | CF3 | H | F | 6-CF3 |
A-1024 | CH(CH3)C6H5 | H | CF3 | H | F | 6-CF3 |
A-1025 | (CH2)2OC6H5 | H | CF3 | H | F | 6-CF3 |
A-1026 | (CH2)2C6H5 | H | CF3 | H | F | 6-CF3 |
A-1027 | (CH2)2C6H4F | H | CF3 | H | F | 6-CF3 |
A-1028 | (CH2)2C6H4Cl | H | CF3 | H | F | 6-CF3 |
A-1029 | (CH2)2C6H4CN | H | CF3 | H | F | 6-CF3 |
A-1030 | (CH2)2C6H4CH3 | H | CF3 | H | F | 6-CF3 |
A-1031 | (CH2)2C6H4CF3 | H | CF3 | H | F | 6-CF3 |
A-1032 | (CH2)2C6H4OCH3 | H | CF3 | H | F | 6-CF3 |
A-1033 | (CH2)2C6H4OCF3 | H | CF3 | H | F | 6-CF3 |
A-1034 | CH2CH=CH2 | H | CF3 | H | F | 6-CF3 |
A-1035 | 环-C3H5 | H | CF3 | H | F | 6-CF3 |
A-1036 | (CH2)2NHCH3 | H | CF3 | H | F | 6-CF3 |
A-1037 | H | H | CF3 | H | CF3 | 6-F |
A-1038 | CH3 | CH3 | CF3 | H | CF3 | 6-F |
A-1039 | CH2CH3 | CH2CH3 | CF3 | H | CF3 | 6-F |
A-1040 | CH3 | H | CF3 | H | CF3 | 6-F |
A-1041 | CH2CH3 | H | CF3 | H | CF3 | 6-F |
A-1042 | (CH2)2CH3 | H | CF3 | H | CF3 | 6-F |
A-1043 | CH(CH3)2 | H | CF3 | H | CF3 | 6-F |
A-1044 | CH2CF3 | H | CF3 | H | CF3 | 6-F |
A-1045 | C(CH3)3 | H | CF3 | H | CF3 | 6-F |
A-1046 | CH2CH(CH3)2 | H | CF3 | H | CF3 | 6-F |
A-1047 | CH(CH3)CH2CH3 | H | CF3 | H | CF3 | 6-F |
A-1048 | (CH2)2OCH3 | H | CF3 | H | CF3 | 6-F |
A-1049 | CH2CH(OCH3)2 | H | CF3 | H | CF3 | 6-F |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1050 | CH2CH(OCH2CH3)2 | H | CF3 | H | CF3 | 6-F |
A-1051 | CH2C6H5 | H | CF3 | H | CF3 | 6-F |
A-1052 | CH(CH3)C6H5 | H | CF3 | H | CF3 | 6-F |
A-1053 | (CH2)2OC6H5 | H | CF3 | H | CF3 | 6-F |
A-1054 | (CH2)2C6H5 | H | CF3 | H | CF3 | 6-F |
A-1055 | (CH2)2C6H4F | H | CF3 | H | CF3 | 6-F |
A-1056 | (CH2)2C6H4Cl | H | CF3 | H | CF3 | 6-F |
A-1057 | (CH2)2C6H4CN | H | CF3 | H | CF3 | 6-F |
A-1058 | (CH2)2C6H4CH3 | H | CF3 | H | CF3 | 6-F |
A-1059 | (CH2)2C6H4CF3 | H | CF3 | H | CF3 | 6-F |
A-1060 | (CH2)2C6H4OCH3 | H | CF3 | H | CF3 | 6-F |
A-1061 | (CH2)2C6H4OCF3 | H | CF3 | H | CF3 | 6-F |
A-1062 | CH2CH=CH2 | H | CF3 | H | CF3 | 6-F |
A-1063 | 环-C3H5 | H | CF3 | H | CF3 | 6-F |
A-1064 | (CH2)2NHCH3 | H | CF3 | H | CF3 | 6-F |
A-1065 | H | H | CF3 | H | CF3 | 6-Cl |
A-1066 | CH3 | CH3 | CF3 | H | CF3 | 6-Cl |
A-1067 | CH2CH3 | CH2CH3 | CF3 | H | CF3 | 6-Cl |
A-1068 | CH3 | H | CF3 | H | CF3 | 6-Cl |
A-1069 | CH2CH3 | H | CF3 | H | CF3 | 6-Cl |
A-1070 | (CH2)2CH3 | H | CF3 | H | CF3 | 6-Cl |
A-1071 | CH(CH3)2 | H | CF3 | H | CF3 | 6-Cl |
A-1072 | CH2CF3 | H | CF3 | H | CF3 | 6-Cl |
A-1073 | C(CH3)3 | H | CF3 | H | CF3 | 6-Cl |
A-1074 | CH2CH(CH3)2 | H | CF3 | H | CF3 | 6-Cl |
A-1075 | CH(CH3)CH2CH3 | H | CF3 | H | CF3 | 6-Cl |
A-1076 | (CH2)2OCH3 | H | CF3 | H | CF3 | 6-Cl |
A-1077 | CH2CH(OCH3)2 | H | CF3 | H | CF3 | 6-Cl |
A-1078 | CH2CH(OCH2CH3)2 | H | CF3 | H | CF3 | 6-Cl |
A-1079 | CH2C6H5 | H | CF3 | H | CF3 | 6-Cl |
A-1080 | CH(CH3)C6H5 | H | CF3 | H | CF3 | 6-Cl |
A-1081 | (CH2)2OC6H5 | H | CF3 | H | CF3 | 6-Cl |
A-1082 | (CH2)2C6H5 | H | CF3 | H | CF3 | 6-Cl |
A-1083 | (CH2)2C6H4F | H | CF3 | H | CF3 | 6-Cl |
A-1084 | (CH2)2C6H4Cl | H | CF3 | H | CF3 | 6-Cl |
A-1085 | (CH2)2C6H4CN | H | CF3 | H | CF3 | 6-Cl |
A-1086 | (CH2)2C6H4CH3 | H | CF3 | H | CF3 | 6-Cl |
A-1087 | (CH2)2C6H4CF3 | H | CF3 | H | CF3 | 6-Cl |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1088 | (CH2)2C6H4OCH3 | H | CF3 | H | CF3 | 6-Cl |
A-1089 | (CH2)2C6H4OCF3 | H | CF3 | H | CF3 | 6-Cl |
A-1090 | CH2CH=CH2 | H | CF3 | H | CF3 | 6-Cl |
A-1091 | 环-C3H5 | H | CF3 | H | CF3 | 6-Cl |
A-1092 | (CH2)2NHCH3 | H | CF3 | H | CF3 | 6-Cl |
A-1093 | H | H | CF3 | H | Cl | 6-Cl |
A-1094 | CH3 | CH3 | CF3 | H | Cl | 6-Cl |
A-1095 | CH2CH3 | CH2CH3 | CF3 | H | Cl | 6-Cl |
A-1096 | CH3 | H | CF3 | H | Cl | 6-Cl |
A-1097 | CH2CH3 | H | CF3 | H | Cl | 6-Cl |
A-1098 | (CH2)2CH3 | H | CF3 | H | Cl | 6-Cl |
A-1099 | CH(CH3)2 | H | CF3 | H | Cl | 6-Cl |
A-1100 | CH2CF3 | H | CF3 | H | Cl | 6-Cl |
A-1101 | C(CH3)3 | H | CF3 | H | Cl | 6-Cl |
A-1102 | CH2CH(CH3)2 | H | CF3 | H | Cl | 6-Cl |
A-1103 | CH(CH3)CH2CH3 | H | CF3 | H | Cl | 6-Cl |
A-1104 | (CH2)2OCH3 | H | CF3 | H | Cl | 6-Cl |
A-1105 | CH2CH(OCH3)2 | H | CF3 | H | Cl | 6-Cl |
A-1106 | CH2CH(OCH2CH3)2 | H | CF3 | H | Cl | 6-Cl |
A-1107 | CH2C6H5 | H | CF3 | H | Cl | 6-Cl |
A-1108 | CH(CH3)C6H5 | H | CF3 | H | Cl | 6-Cl |
A-1109 | (CH2)2OC6H5 | H | CF3 | H | Cl | 6-Cl |
A-1110 | (CH2)2C6H5 | H | CF3 | H | Cl | 6-Cl |
A-1111 | (CH2)2C6H4F | H | CF3 | H | Cl | 6-Cl |
A-1112 | (CH2)2C6H4Cl | H | CF3 | H | Cl | 6-Cl |
A-1113 | (CH2)2C6H4CN | H | CF3 | H | Cl | 6-Cl |
A-1114 | (CH2)2C6H4CH3 | H | CF3 | H | Cl | 6-Cl |
A-1115 | (CH2)2C6H4CF3 | H | CF3 | H | Cl | 6-Cl |
A-1116 | (CH2)2C6H4OCH3 | H | CF3 | H | Cl | 6-Cl |
A-1117 | (CH2)2C6H4OCF3 | H | CF3 | H | Cl | 6-Cl |
A-1118 | CH2CH=CH2 | H | CF3 | H | Cl | 6-Cl |
A-1119 | 环-C3H5 | H | CF3 | H | Cl | 6-Cl |
A-1120 | (CH2)2NHCH3 | H | CF3 | H | Cl | 6-Cl |
A-1121 | H | H | CF3 | H | Cl | 6-CF3 |
A-1122 | CH3 | CH3 | CF3 | H | Cl | 6-CF3 |
A-1123 | CH2CH3 | CH2CH3 | CF3 | H | Cl | 6-CF3 |
A-1124 | CH3 | H | CF3 | H | Cl | 6-CF3 |
A-1125 | CH2CH3 | H | CF3 | H | Cl | 6-CF3 |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1126 | (CH2)2CH3 | H | CF3 | H | Cl | 6-CF3 |
A-1127 | CH(CH3)2 | H | CF3 | H | Cl | 6-CF3 |
A-1128 | CH2CF3 | H | CF3 | H | Cl | 6-CF3 |
A-1129 | C(CH3)3 | H | CF3 | H | Cl | 6-CF3 |
A-1130 | CH2CH(CH3)2 | H | CF3 | H | Cl | 6-CF3 |
A-1131 | CH(CH3)CH2CH3 | H | CF3 | H | Cl | 6-CF3 |
A-1132 | (CH2)2OCH3 | H | CF3 | H | Cl | 6-CF3 |
A-1133 | CH2CH(OCH3)2 | H | CF3 | H | Cl | 6-CF3 |
A-1134 | CH2CH(OCH2CH3)2 | H | CF3 | H | Cl | 6-CF3 |
A-1135 | CH2C6H5 | H | CF3 | H | Cl | 6-CF3 |
A-1136 | CH(CH3)C6H5 | H | CF3 | H | Cl | 6-CF3 |
A-1137 | (CH2)2OC6H5 | H | CF3 | H | Cl | 6-CF3 |
A-1138 | (CH2)2C6H5 | H | CF3 | H | Cl | 6-CF3 |
A-1139 | (CH2)2C6H4F | H | CF3 | H | Cl | 6-CF3 |
A-1140 | (CH2)2C6H4Cl | H | CF3 | H | Cl | 6-CF3 |
A-1141 | (CH2)2C6H4CN | H | CF3 | H | Cl | 6-CF3 |
A-1142 | (CH2)2C6H4CH3 | H | CF3 | H | Cl | 6-CF3 |
A-1143 | (CH2)2C6H4CF3 | H | CF3 | H | Cl | 6-CF3 |
A-1144 | (CH2)2C6H4OCH3 | H | CF3 | H | Cl | 6-CF3 |
A-1145 | (CH2)2C6H4OCF3 | H | CF3 | H | Cl | 6-CF3 |
A-1146 | CH2CH=CH2 | H | CF3 | H | Cl | 6-CF3 |
A-1147 | 环-C3H5 | H | CF3 | H | Cl | 6-CF3 |
A-1148 | (CH2)2NHCH3 | H | CF3 | H | Cl | 6-CF3 |
A-1149 | H | H | F | H | CF3 | 6-Cl |
A-1150 | CH3 | CH3 | F | H | CF3 | 6-Cl |
A-1151 | CH2CH3 | CH2CH3 | F | H | CF3 | 6-Cl |
A-1152 | CH3 | H | F | H | CF3 | 6-Cl |
A-1153 | CH2CH3 | H | F | H | CF3 | 6-Cl |
A-1154 | (CH2)2CH3 | H | F | H | CF3 | 6-Cl |
A-1155 | CH(CH3)2 | H | F | H | CF3 | 6-Cl |
A-1156 | CH2CF3 | H | F | H | CF3 | 6-Cl |
A-1157 | C(CH3)3 | H | F | H | CF3 | 6-Cl |
A-1158 | CH2CH(CH3)2 | H | F | H | CF3 | 6-Cl |
A-1159 | CH(CH3)CH2CH3 | H | F | H | CF3 | 6-Cl |
A-1160 | (CH2)2OCH3 | H | F | H | CF3 | 6-Cl |
A-1161 | CH2CH(OCH3)2 | H | F | H | CF3 | 6-Cl |
A-1162 | CH2CH(OCH2CH3)2 | H | F | H | CF3 | 6-Cl |
A-1163 | CH2C6H5 | H | F | H | CF3 | 6-Cl |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1164 | CH(CH3)C6H5 | H | F | H | CF3 | 6-Cl |
A-1165 | (CH2)2OC6H5 | H | F | H | CF3 | 6-Cl |
A-1166 | (CH2)2C6H5 | H | F | H | CF3 | 6-Cl |
A-1167 | (CH2)2C6H4F | H | F | H | CF3 | 6-Cl |
A-1168 | (CH2)2C6H4Cl | H | F | H | CF3 | 6-Cl |
A-1169 | (CH2)2C6H4CN | H | F | H | CF3 | 6-Cl |
A-1170 | (CH2)2C6H4CH3 | H | F | H | CF3 | 6-Cl |
A-1171 | (CH2)2C6H4CF3 | H | F | H | CF3 | 6-Cl |
A-1172 | (CH2)2C6H4OCH3 | H | F | H | CF3 | 6-Cl |
A-1173 | (CH2)2C6H4OCF3 | H | F | H | CF3 | 6-Cl |
A-1174 | CH2CH=CH2 | H | F | H | CF3 | 6-Cl |
A-1175 | 环-C3H5 | H | F | H | CF3 | 6-Cl |
A-1176 | (CH2)2NHCH3 | H | F | H | CF3 | 6-Cl |
A-1177 | H | H | F | H | F | 6-F |
A-1178 | CH3 | CH3 | F | H | F | 6-F |
A-1179 | CH2CH3 | CH2CH3 | F | H | F | 6-F |
A-1180 | CH3 | H | F | H | F | 6-F |
A-1181 | CH2CH3 | H | F | H | F | 6-F |
A-1182 | (CH2)2CH3 | H | F | H | F | 6-F |
A-1183 | CH(CH3)2 | H | F | H | F | 6-F |
A-1184 | CH2CF3 | H | F | H | F | 6-F |
A-1185 | C(CH3)3 | H | F | H | F | 6-F |
A-1186 | CH2CH(CH3)2 | H | F | H | F | 6-F |
A-1187 | CH(CH3)CH2CH3 | H | F | H | F | 6-F |
A-1188 | (CH2)2OCH3 | H | F | H | F | 6-F |
A-1189 | CH2CH(OCH3)2 | H | F | H | F | 6-F |
A-1190 | CH2CH(OCH2CH3)2 | H | F | H | F | 6-F |
A-1191 | CH2C6H5 | H | F | H | F | 6-F |
A-1192 | CH(CH3)C6H5 | H | F | H | F | 6-F |
A-1193 | (CH2)2OC6H5 | H | F | H | F | 6-F |
A-1194 | (CH2)2C6H5 | H | F | H | F | 6-F |
A-1195 | (CH2)2C6H4F | H | F | H | F | 6-F |
A-1196 | (CH2)2C6H4Cl | H | F | H | F | 6-F |
A-1197 | (CH2)2C6H4CN | H | F | H | F | 6-F |
A-1198 | (CH2)2C6H4CH3 | H | F | H | F | 6-F |
A-1199 | (CH2)2C6H4CF3 | H | F | H | F | 6-F |
A-1200 | (CH2)2C6H4OCH3 | H | F | H | F | 6-F |
A-1201 | (CH2)2C6H4OCF3 | H | F | H | F | 6-F |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1202 | CH2CH=CH2 | H | F | H | F | 6-F |
A-1203 | 环-C3H5 | H | F | H | F | 6-F |
A-1204 | (CH2)2NHCH3 | H | F | H | F | 6-F |
A-1205 | H | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1206 | CH3 | CH3 | Cl | Cl | Cl | 5,6-Cl2 |
A-1207 | CH2CH3 | CH2CH3 | Cl | Cl | Cl | 5,6-Cl2 |
A-1208 | CH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1209 | CH2CH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1210 | (CH2)2CH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1211 | CH(CH3)2 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1212 | CH2CF3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1213 | C(CH3)3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1214 | CH2CH(CH3)2 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1215 | CH(CH3)CH2CH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1216 | (CH2)2OCH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1217 | CH2CH(OCH3)2 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1218 | CH2CH(OCH2CH3)2 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1219 | CH2C6H5 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1220 | CH(CH3)C6H5 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1221 | (CH2)2OC6H5 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1222 | (CH2)2C6H5 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1223 | (CH2)2C6H4F | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1224 | (CH2)2C6H4Cl | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1225 | (CH2)2C6H4CN | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1226 | (CH2)2C6H4CH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1227 | (CH2)2C6H4CF3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1228 | (CH2)2C6H4OCH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1229 | (CH2)2C6H4OCF3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1230 | CH2CH=CH2 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1231 | 环-C3H5 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1232 | (CH2)2NHCH3 | H | Cl | Cl | Cl | 5,6-Cl2 |
A-1233 | H | H | F | F | F | 5,6-F2 |
A-1234 | CH3 | CH3 | F | F | F | 5,6-F2 |
A-1235 | CH2CH3 | CH2CH3 | F | F | F | 5,6-F2 |
A-1236 | CH3 | H | F | F | F | 5,6-F2 |
A-1237 | CH2CH3 | H | F | F | F | 5,6-F2 |
A-1238 | (CH2)2CH3 | H | F | F | F | 5,6-F2 |
A-1239 | CH(CH3)2 | H | F | F | F | 5,6-F2 |
编号 | R1 | R2 | R5 | R6 | R7 | Yn |
A-1240 | CH2CF3 | H | F | F | F | 5,6-F2 |
A-1241 | C(CH3)3 | H | F | F | F | 5,6-F2 |
A-1242 | CH2CH(CH3)2 | H | F | F | F | 5,6-F2 |
A-1243 | CH(CH3)CH2CH3 | H | F | F | F | 5,6-F2 |
A-1244 | (CH2)2OCH3 | H | F | F | F | 5,6-F2 |
A-1245 | CH2CH(OCH3)2 | H | F | F | F | 5,6-F2 |
A-1246 | CH2CH(OCH2CH3)2 | H | F | F | F | 5,6-F2 |
A-1247 | CH2C6H5 | H | F | F | F | 5,6-F2 |
A-1248 | CH(CH3)C6H5 | H | F | F | F | 5,6-F2 |
A-1249 | (CH2)2OC6H5 | H | F | F | F | 5,6-F2 |
A-1250 | (CH2)2C6H5 | H | F | F | F | 5,6-F2 |
A-1251 | (CH2)2C6H4F | H | F | F | F | 5,6-F2 |
A-1252 | (CH2)2C6H4Cl | H | F | F | F | 5,6-F2 |
A-1253 | (CH2)2C6H4CN | H | F | F | F | 5,6-F2 |
A-1254 | (CH2)2C6H4CH3 | H | F | F | F | 5,6-F2 |
A-1255 | (CH2)2C6H4CF3 | H | F | F | F | 5,6-F2 |
A-1256 | (CH2)2C6H4OCH3 | H | F | F | F | 5,6-F2 |
A-1257 | (CH2)2C6H4OCF3 | H | F | F | F | 5,6-F2 |
A-1258 | CH2CH=CH2 | H | F | F | F | 5,6-F2 |
A-1259 | 环-C3H5 | H | F | F | F | 5,6-F2 |
A-1260 | (CH2)2NHCH3 | H | F | F | F | 5,6-F2 |
对于本发明中的意欲用途,特别优选式I-B化合物或其对映异构体或兽用可接受盐:
其中
R7为氯或三氟甲基;
R5和Y各自独立地为氯或溴;
R2为C1-C6烷基、C3-C6链烯基、C3-C6炔基或可以被1-3个卤原子取代的C3-C6环烷基或被C1-C4烷氧基取代的C2-C4烷基;
R31和R32为C1-C6烷基或可以一起形成可以未被取代或被1-3个卤原子取代的C3-C6环烷基;
R33为氢或C1-C6烷基。
优选其中R7为三氟甲基的式I-B化合物。
此外还优选其中Y和R5均为氯的式I-B化合物。
此外,优选其中R2为C1-C6烷基,尤其是乙基的式I-B化合物。
此外还优选其中R31和R32均为甲基的式I-B化合物。
此外,优选其中R31和R32形成未被取代或被1-3个卤原子,尤其是氯和溴取代的环丙基环的式I-B化合物。
此外,特别优选其中R31和R32形成被2个卤原子取代的环丙基环的式I-B化合物。
此外,特别优选其中R31和R32形成被2个氯原子取代的环丙基环的式I-B化合物。
特别优选其中R31和R32形成2,2-二氯环丙基环的式I-B化合物。
此外还优选其中R33为C1-C6烷基,尤其是甲基的式I-B化合物。
特别优选其中R31、R32和R33全部为甲基的式I-B化合物。
此外,特别优选其中R31、R32和R33形成结构部分1-甲基-2,2-二氯环丙基的式I-B化合物。
此外还优选其中:
R7为三氟甲基;
Y和R5各自独立地为氯或溴;
R2为C1-C6烷基;
R31和R32为C1-C6烷基或可以一起形成被1-2个卤原子取代的C3-C6环烷基;
R33为C1-C6烷基;
的式I-B化合物或其对映异构体或兽用可接受盐。
特别优选N-乙基-2,2-二甲基丙酰胺-2-(2,6-二氯-α,α,α-三氟对甲苯基)腙和N-乙基-2,2-二氯-1-甲基环丙烷甲酰胺-2-(2,6-二氯-α,α,α-三氟对甲苯基)腙。
此外,对于本发明中的用途特别优选式I-1化合物(N-乙基-2,2-二甲基丙酰胺-2-(2,6-二氯-α,α,α-三氟对甲苯基)腙):
此外,对于在本发明中的用途优选式I-2化合物(N-乙基-2,2-二氯-1-甲基环丙烷甲酰胺-2-(2,6-二氯-α,α,α-三氟对甲苯基)腙):
式I化合物和含有它们的组合物优选用于防治和预防包括温血动物(包括人)和鱼在内的动物的侵染和感染。它们例如适于防治和预防在哺乳动物如牛、绵羊、猪、骆驼、鹿、马、小猪、家禽、兔、山羊、狗和猫、水牛、驴、黄鹿和驯鹿中以及在毛皮动物如水貂、灰鼠和浣熊,鸟类如母鸡、鹅、火鸡和鸭子以及鱼类如淡水鱼和咸水鱼,例如鲑鱼、鲤鱼和鳗鱼中的侵染和感染。
式I化合物和含有它们的组合物优选用于防治和预防家畜如狗和猫中的侵染和感染。
在温血动物和鱼类中的侵染包括但不限于虱、咬虱、壁虱、鼻蝇(nasalbots)、羊蜱蝇、叮咬蝇、家蝇(muscoid flies)、苍蝇、蝇疽病性苍蝇幼虫、恙螨、蚊(gnats)、蚊子(mosquitoes)和蚤。
式I化合物和含有它们的组合物适于内吸和/或非内吸防治体外寄生物和/或体内寄生物。它们对发育的所有阶段或一些阶段具有活性。
式I化合物尤其可用于防治体外寄生物。
式I化合物尤其可以用于防治分别属于下列目和种的寄生物:蚤(蚤目(Siphonaptera)),例如猫跳蚤(Ctenocephalides felis)、狗跳蚤(Ctenocephalides canis)、印鼠客蚤(Xenopsylla cheopis)、致痒蚤(Pulexirritans)、穿皮潜蚤(Tunga penetrans)和具带病蚤(Nosopsyllus fasciatus),蟑螂(蜚蠊目(Blattaria)-蜚蠊目(Blattodea)),例如德国小蠊(Blattellagermanica)、Blattella asahinae、美洲大蠊(Periplaneta americana)、日本蟑螂(Periplaneta japonica)、棕色蟑螂(Periplaneta brunnea)、Periplanetafuligginosa、澳洲大蠊(Periplaneta australasiae)和东方蜚蠊(Blattaorientalis),苍蝇、蚊子(双翅目(Diptera)),例如埃及伊蚊(Aedes aegypti)、白纹伊蚊(Aedes albopictus)、刺扰伊蚊(Aedes vexans)、墨西哥果蝇(Anastrephaludens)、五斑按蚊(Anopheles maculipennis)、Anopheles crucians、Anopheles albimanus、疟蚊(Anopheles gambiae)、Anopheles freeborni、白踝按蚊(Anopheles leucosphyrus)、微小按蚊(Anopheles minimus)、四斑按蚊(Anopheles quadrimaculatus)、红头丽蝇(Calliphora vicina)、蛆症金蝇(Chrysomya bezziana)、Chrysomya hominivorax、Chrysomyamacellaria、鹿蝇(Chrysops discalis)、Chrysops silacea、Chrysopsatlanticus、Cochliomyia hominivorax、Cordylobia anthropophaga、Culicoides furens、尖音库蚊(Culex pipiens)、斑蚊(Culex nigripalpus)、致倦库蚊(Culex quinquefasciatus)、媒斑蚊(Culex tarsalis)、Culiseta inornata、Culiseta melanura、Dermatobia hominis、小毛厕蝇(Fannia canicularis)、马蝇(Gasterophilus intestinalis)、刺舌蝇(Glossina morsitans)、须舌蝇(Glossina palpalis)、Glossina fuscipes、Glossina tachinoides、Haematobiairritans、Haplodiplosis equestris、Hippelates属、纹皮蝇(Hypodermalineata)、Leptoconops torrens、Lucilia caprina、铜绿蝇(Lucilia cuprina)、丝光绿蝇(Lucilia sericata)、Lycoria pectoralis、沼蚊属(Mansonia)、家蝇(Musca domestica)、厩腐蝇(Muscina stabulans)、羊狂蝇(Oestrus ovis)、Phlebotomus argentipes、Psorophora columbiae、Psorophora discolor、Prosimulium mixtum、红尾肉蝇(Sarcophaga haemorrhoidalis)、肉蝇属(Sarcophaga)、Simulium vittatum、厩螫蝇(Stomoxys calcitrans)、牛虻(Tabanus bovinus)、Tabanus atratus、红色原虻(Tabanus lineola)和Tabanus similis,虱(虱毛目(Phthiraptera)),例如人头虱(Pediculus humanus capitis)、人体虱(Pediculus humanus corporis)、耻阴虱(Pthirus pubis)、牛血虱(Haematopinus eurysternus)、猪血虱(Haematopinus suis)、牛腭虱(Linognathus vituli)、Bovicola bovis、鸡虱(Menopon gallinae)、Menacanthus stramineus和Solenopotes capillatus,壁虱和寄生螨(寄螨目(Parasitiformes):壁虱(蜱亚目(Ixodida),例如黑脚硬蜱(Ixodes scapularis)、全环硬蜱(Ixodes holocyclus)、太平洋硬蜱(Ixodespacificus)、棕色犬壁虱(Rhiphicephalus sanguineus)、安氏革螨(Dermacentor andersoni)、美洲大革螨(Dermacentor variabilis)、长星形壁虱(Amblyomma americanum)、Ambryomma maculatum、Ornithodorushermsi、Ornithodorus turicata以及寄生螨(甲螨亚目(Mesostigmata)),例如柏氏禽刺螨(Ornithonyssus bacoti)和鸡皮刺螨(Dermanyssus gallinae),辐螨亚目(Actinedida)(前气门亚目(Prostigmata)和粉螨亚目(Acaridida)(无气门目(Astigmata)),例如蜂盾螨属(Acarapis)、姬螯螨属(Cheyletiella)、Ornithocheyletia属、Myobia属、Psorergates属、蠕形螨属(Demodex)、恙螨属(Trombicula)、Listrophorus属、粉螨属(Acarus)、食酪螨属(Tyrophagus)、嗜木螨属(Caloglyphus)、Hypodectes属、Pterolichus属、Psoroptes属、痒螨属(Chorioptes)、耳痒螨属(Otodectes)、疥螨属(Sarcoptes)、茄螨属(Notoedres)、膝螨属(Knemidocoptes)、Cytodites属和Laminosioptes属,臭虫((Heteropterida):温带臭虫(Cimex lectularius)、热带臭虫(Cimexhemipterus)、Reduvius senilis、锥蝽属(Triatoma)、猎蝽属(Rhodnius)、Panstrongylus属和Arilus critatus,Anoplurida,例如血虱属(Haematopinus)、颚虱属(Linognathus)、虱属(Pediculus)、Phtirus属和管虱属(Solenopotes),Mallophagida(Arnblycerina和Ischnocerina亚目),例如Trimenopon属、鸡虱属(Menopon)、鸭虱属(Trinoton)、牛毛虱属(Bovicola)、Werneckiella属、Lepikentron属、啮毛虱属(Trichodectes)和猫毛虱属(Felicola),蛔虫线虫(Roundworms Nematoda):
Wipeworms和旋毛虫病(Trichinosis)(Trichosyringida),例如毛形虫科(Trichinellidae)(旋毛线虫属(Trichinella))、毛首科(Trichuridae)(毛首线虫属(Trichuris),毛细线虫属(Capillaria),小杆目(Rhabditida),例如小杆线虫属(Rhabditis)、Strongyloides属、Helicephalobus属,圆线虫目(Strongylida),例如圆线虫属(Strongylus)、Ancylostoma属、美洲钩虫(Necator americanus)、反刍兽钩虫属(Bunostomum)(钩虫)、毛圆线虫属(Trichostrongylus)、捻转血矛线虫(Haemonchus contortus)、Ostertagia属、库柏毛样线虫属(Cooperia)、细颈线虫属(Nematodirus)、网尾线虫属(Dictyocaulus)、盅口属(Cyathostoma)、猪结节虫属(Oesophagostomum)、猪肾虫(Stephanurus dentatus)、Ollulanus属、夏伯特属(Chabertia)、Stephanurus dentatus、气管开嘴虫(Syngamus trachea)、Ancylostoma属、弯口属(Uncinaria)、球首属(Globocephalus)、板口线虫属(Necator)、肺虫属(Metastrongylus)、毛细苗勒氏肺虫(Muellerius capillaris)、Protostrongylus属、Angiostrongylus属、Parelaphostrongylus属、Aleurostrongylus abstrusus和肾膨结线虫(Dioctophyma renale),肠圆虫(Intestinal roundworms)(蛔虫目(Ascaridida)),例如似蚓蛔线虫(Ascaris lumbricoides)、猪蛔虫(Ascaris suum)、鸡蛔虫(Ascaridia galli)、马副蛔虫(Parascaris equorum)、蠕形住肠线虫(Enterobiusvermicularis)(线虫),犬蛔虫(Toxocara canis)、Toxascaris leonine、Skrj abinema属和马尖尾线虫(Oxyuris equi),Camallanida,例如麦地那龙线虫(Dracunculus medinensis)(几内亚龙线虫)
旋尾目(Spirurida),例如吸吮线虫属(Thelazia)、丝虫属(Wuchereria)、Brugia属、Onchocerca属、Dirofilari属、Dipetalonema属、Setaria属、Elaeophora属、狼犬尾线虫(Spirocerca lupi)和柔线属(Habronema),棘头虫(棘头虫门(Acanthocephala)),例如Acanthocephalus属、猪巨吻棘头虫(Macracanthorhynchus hirudinaceus)和Oncicola属,涡虫类(Planarians)(Plathelminthes):
吸虫(吸虫纲(Trematoda)),例如Faciola属、大吸虫(Fascioloides magna)、Paragonimus属、双腔属(Dicrocoelium)、布氏姜片吸虫(Fasciolopsis buski)、华枝睾吸虫(Clonorchis sinensis)、Schistosoma属、毛毕属(Trichobilharzia)、Alaria alata、Paragonimus属和Nanocyetes属,Cercomeromorpha,尤其是绦虫纲(Cestoda(绦虫)),例如裂头绦虫属(Diphyllobothrium)、Tenia属、Echinococcus属、犬复孔绦虫(Dipylidiumcaninum)、Multiceps属、膜壳绦虫属(Hymenolepis)、Mesocestoides属、Vampirolepis属、Moniezia属、裸头绦虫属(Anoplocephala)、Sirometra属、裸头绦虫属(Anoplocephala)和膜壳绦虫属(Hymenolepis)。
式I化合物和含有它们的组合物特别可用于防治双翅目(Diptera)、蚤目(Siphonaptera)和蜱亚目(Ixodida)害虫。
此外,尤其优选式I化合物和含有它们的组合物在防治蚊子中的用途。
式I化合物和含有它们的组合物在防治苍蝇中的用途为本发明的另一优选实施方案。
此外,尤其优选式I化合物和含有它们的组合物在防治蚤中的用途。
式I化合物和含有它们的组合物在防治壁虱中的用途为本发明的另一优选实施方案。
式I化合物还尤其可用于防治体内寄生物(蛔虫线虫、棘头虫和涡虫类)。
给药可以以预防和治疗两种方式进行。
活性化合物的给药直接或以合适制剂形式口服、局部/皮肤或肠胃外进行。
为了对温血动物口服给药,可以将式I化合物配制成动物饲料、动物饲料预混物、动物饲料浓缩物、丸剂、溶液、糊、悬浮液、兽用顿服药、凝胶、片剂、大丸剂和胶囊。此外,式I化合物可以在动物的饮用水中对动物给药。对于口服给药,所选择的剂型应给动物提供0.01-100mg/kg动物体重/天的式I化合物,优选0.5-100mg/kg动物体重/天。
或者,式I化合物可以对动物肠胃外给药,例如通过腔内(intraruminal)、肌内、静脉内或皮下注射。式I化合物可以分散或溶于用于皮下注射的生理上可接受的载体中。或者可以将式I化合物配制成用于皮下给药的植入物。此外,式I化合物可以经皮对动物给药。对于肠胃外给药,所选择的剂型应给动物提供0.01-100mg/kg动物体重/天的式I化合物。
式I化合物还可以滴剂、粉剂、粉末、颈圈、medallions、喷雾剂、洗发水、点上(spot-on)或浇注配制剂以及软膏或水包油或油包水乳液的形式局部施用于动物。对于局部施用,滴剂和喷雾剂通常含有0.5-5,000ppm,优选1-3,000ppm的式I化合物。此外,式I化合物可以配制成用于动物,特别是四足动物如牛和绵羊的耳贴。
合适的制剂是:
-溶液如口服溶液、稀释后口服给药的浓缩物、用于皮肤上或用于体腔中的溶液、浇注配制剂、凝胶;
-口服或皮肤给药用乳液和悬浮液;半固体制剂;
-其中活性化合物在软膏基质中或在水包油或油包水乳液基质中处理的配制剂;
-固体制剂如粉末、预混物或浓缩物、颗粒、丸剂、片剂、大丸剂、胶囊;气溶胶和吸入剂以及含活性化合物的成型制品。
适于注射的组合物通过将活性成分溶于合适溶剂中并任选加入其他成分如酸、碱、缓冲盐、防腐剂和增溶剂而制备。过滤溶液并无菌填充。
合适的溶剂是生理上可耐受的溶剂如水,链烷醇如乙醇、丁醇、苄醇、甘油、丙二醇、聚乙二醇,N-甲基吡咯烷酮,2-吡咯烷酮及其混合物。
活性化合物可以任选溶于适于注射的生理上可耐受的植物油或合成油中。
合适的增溶剂是促进活性化合物在主溶剂中溶解或防止其沉淀的溶剂。实例是聚乙烯吡咯烷酮、聚乙烯醇、聚氧乙基化蓖麻油和聚氧乙基化脱水山梨糖醇酯。
合适的防腐剂是苄醇、三氯丁醇、对羟基苯甲酸酯和正丁醇。
口服溶液直接给药。浓缩物在预先稀释到使用浓度之后口服给药。口服溶液和浓缩物根据现有技术状态并如上面对注射溶液所述制备,杀菌程序并不是必需的。
将
用于皮肤上的溶液滴上、散布、擦入、洒上或喷上。
用于皮肤上的溶液根据现有技术状态和上面对注射溶液所述制备,杀菌程序并不是必需的。
其他合适的溶剂是聚丙二醇,苯基乙醇,苯氧基乙醇,酯如乙酸乙酯或乙酸丁酯、苯甲酸苄基酯,醚如亚烷基二醇烷基醚,例如二丙二醇单甲醚,酮类如丙酮、甲基乙基酮,芳族烃类,植物和合成油,二甲基甲酰胺,二甲基乙酰胺,transcutol,solketal,碳酸亚丙酯及其混合物。
可能有利的是在制备过程中加入增稠剂。合适的增稠剂是无机增稠剂如膨润土、胶态硅酸、单硬脂酸铝,有机增稠剂如纤维素衍生物、聚乙烯醇及其共聚物、丙烯酸酯和甲基丙烯酸酯。
将
凝胶施用于或散布于皮肤上或引入体腔中。凝胶通过用足以得到具有软膏状稠度的透明物质的增稠剂处理已经如在注射溶液情况下所述制备的溶液而制备。所用增稠剂是上面所给的增稠剂。
将
浇注配制剂浇注或喷雾于皮肤的限定区域,活性化合物渗透皮肤并内吸起作用。
浇注配制剂通过将活性化合物在合适的皮肤相容性溶剂或溶剂混合物中溶解、悬浮或乳化而制备。合适的话,加入其他助剂如着色剂、生物吸收促进物质、抗氧化剂、光稳定剂、粘合剂。
合适的溶剂是水,链烷醇,二醇,聚乙二醇,聚丙二醇,甘油,芳族醇如苄醇、苯乙醇、苯氧基乙醇,酯类如乙酸乙酯、乙酸丁酯、苯甲酸苄基酯,醚类如亚烷基二醇烷基醚如二丙二醇单甲醚、二甘醇单丁醚,酮类如丙酮、甲基乙基酮,环状碳酸酯如碳酸亚丙酯、碳酸亚乙酯,芳族和/或脂族烃类,植物或合成油,DMF,二甲基乙酰胺,正烷基吡咯烷酮如甲基吡咯烷酮、正丁基吡咯烷酮或正辛基吡咯烷酮,N-甲基吡咯烷酮,2-吡咯烷酮,2,2-二甲基-4-氧基-亚甲基-1,3-二氧戊环和甘油缩甲醛。
合适的着色剂是所有允许用于动物且可以溶解或悬浮的着色剂。
合适的吸收促进物质例如为DMSO,散布油如肉豆蔻酸异丙酯,壬酸二丙二醇酯,硅油及其与聚醚、脂肪酸酯、甘油三酯、脂肪醇的共聚物。
合适的抗氧化剂是亚硫酸盐或偏亚硫酸氢盐如偏亚硫酸氢钾、抗坏血酸、丁羟基甲苯、丁羟基茴香醚、生育酚。
合适的光稳定剂例如为novantisolic acid。
合适的粘合剂例如为纤维素衍生物,淀粉衍生物,聚丙烯酸酯,天然聚合物如藻酸盐、明胶。
乳液可以口服给药、皮肤给药或作为注射液给药。
乳液是油包水或水包油型中的任一种。
它们通过将活性化合物溶于疏水相或亲水相中并借助合适的乳化剂和合适的话其他助剂如着色剂、吸收促进物质、防腐剂、抗氧化剂、光稳定剂、粘度提高物质用其他相的溶剂均化而制备。
合适的疏水相(油)是:
-液体石蜡,硅油,天然植物油如芝麻油、杏仁油、蓖麻油,合成甘油三酯如辛酸/癸酸甘油二酯,链长为C8-C12的植物脂肪酸或其他精选天然脂肪酸的甘油三酯混合物,还可能含有羟基的饱和或不饱和脂肪酸的部分甘油酯混合物,C8-C10脂肪酸的甘油单酯和甘油二酯,
-脂肪酸酯如硬脂酸乙酯、己二酸二正丁基酯、月桂酸己酯、壬酸二丙二醇酯、中等链长的支化脂肪酸与链长为C16-C18的饱和脂肪醇的酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、链长为C12-C18的饱和脂肪醇的辛酸/癸酸酯、硬脂酸异丙酯、油酸油基酯、油酸癸基酯、油酸乙酯、乳酸乙酯、蜡状脂肪酸酯如合成鸭尾骨腺脂肪、邻苯二甲酸二丁酯、己二酸二异丙酯以及与后者相关的酯混合物,
-脂肪醇如异十三烷醇、2-辛基十二烷醇、鲸蜡基硬脂醇、油醇,和
-脂肪酸如油酸,和
-其混合物。
合适的亲水相是水,醇类如丙二醇、甘油、山梨醇及其混合物。
合适的乳化剂是:
-非离子表面活性剂,例如聚乙氧基化蓖麻油、聚乙氧基化脱水山梨糖醇单油酸酯、脱水山梨醇单硬脂酸酯、甘油单硬脂酸酯、聚氧乙基硬脂酸酯、烷基酚聚乙二醇醚;
-两性表面活性剂如N-月桂基对亚氨基二丙酸二钠或卵磷脂;
-阴离子表面活性剂,例如月桂基硫酸钠、脂肪醇醚硫酸盐、单/二烷基聚乙二醇醚正磷酸酯单乙醇铵盐;
-阳离子活性表面活性剂,例如鲸蜡基三甲基氯化铵。
合适的其他助剂是提高粘度并稳定乳液的物质,例如羧甲基纤维素、甲基纤维素和其他纤维素以及淀粉衍生物、聚丙烯酸盐、藻酸盐、明胶、阿拉伯胶、聚乙烯吡咯烷酮、聚乙烯醇、甲基乙烯基醚和马来酸酐的共聚物、聚乙二醇、蜡、胶态硅酸或上述物质的混合物。
悬浮液可以口服或局部/皮肤给药。它们通过将活性化合物悬浮于悬浮剂中而制备,合适的话加入其他助剂如润湿剂、着色剂、生物吸收促进物质、防腐剂、抗氧化剂、光稳定剂。
液体悬浮剂是所有均相溶剂和溶剂混合物。
合适的润湿剂(分散剂)是上面所给的乳化剂。
可以提到的其他助剂是上面所给的那些。
半固体制剂可以口服或局部/皮肤给药。它们与上述悬浮液和乳液的不同仅在于具有更高粘度。
为了生产固体制剂,将活性化合物与合适赋形剂混合,合适的话加入助剂,并制成所需形式。
合适的赋形剂是所有生理上耐受的固体惰性物质。所用的那些是无机和有机物质。无机物质例如为氯化钠,碳酸盐如碳酸钙,碳酸氢盐,氧化铝,钛氧化物,硅酸,泥质土(argillaceous earths),沉淀或胶态二氧化硅或磷酸盐。有机物质例如为糖、纤维素、食品和饲料如奶粉、动物粉、谷粉和碎片、淀粉。
合适的助剂是上面已经描述的防腐剂、抗氧化剂和/或着色剂。
其他合适的助剂是润滑剂和滑动剂如硬脂酸镁、硬脂酸、滑石、膨润土,崩解促进物质如淀粉或交联聚乙烯吡咯烷酮,粘合剂如淀粉、明胶或线性聚乙烯吡咯烷酮以及干粘合剂如微晶纤维素。
可以用于本发明中的组合物通常可以包含约0.001-95%式I化合物。
通常有利的是以0.5-100mg/kg/天,优选1-50mg/kg/天的总量使用式I化合物。
即用制剂以10ppm至80重量%,优选0.1-65重量%,更优选1-50重量%,最优选5-40重量%的浓度含有防治寄生物,优选体外寄生物的化合物。
在使用之前稀释的制剂以0.5-90重量%,优选1-50重量%的浓度含有防治体外寄生物的化合物。
此外,制剂以10ppm至2重量%,优选0.05-0.9重量%,非常特别优选0.005-0.25重量%的浓度包含防治体内寄生物的式I化合物。
在本发明的优选实施方案中,包含式I化合物的组合物皮肤/局部施用。
在进一步优选的实施方案中,局部施用以含有化合物的成型制品如颈圈、medallions、耳贴、固定在身体部分上的绑带以及粘合条和箔的形式进行。
通常有利的是施用固体配制剂,其以10-300mg/kg,优选20-200mg/kg,最优选25-160mg/kg被处理动物体重的总量在三周内释放式I化合物。
为了制备
成型制品,使用热塑性和柔性塑料以及弹性体和热塑性弹性体。合适的塑料和弹性体是与式I化合物充分相容的聚乙烯基树脂、聚氨酯、聚丙烯酸酯、环氧树脂、纤维素、纤维素衍生物、聚酰胺和聚酯。用于成型制品的塑料和弹性体以及制备程序的详细列举例如给于WO03/086075中。
活性化合物还可以作为与增效剂或防治病原性体内寄生物和体外寄生物的其他活性化合物的混合物使用。
下列本发明化合物可以与其一起使用的杀虫剂用来阐述可能的组合,而不施以任何限制:
有机磷酸酯类:高灭磷(Acephate)、毒虫畏(Chlorfenvinphos)、二嗪农(Diazinon)、敌敌畏(Dichlorvos)、百治磷(Dicrotophos)、乐果(Dimethoate)、乙硫磷(Ethion)、杀螟松(Fenitrothion)、倍硫磷(Fenthion)、异_唑磷(Isoxathion)、马拉硫磷(Malathion)、稻丰散(Phenthoate)、伏杀磷(Phosalone)、亚胺硫磷(Phosmet)、辛硫磷(Phoxim)、虫螨磷(Pirimiphos-methyl)、丙溴磷(Profenofos)、丙硫磷(Prothiofos)、乙丙硫磷(Sulprophos)、三唑磷(Triazophos)、敌百虫(Trichlorfon)、喹涕福(Quintiofos)、蝇毒磷(Coumaphos)、氯腈肟磷(Chlorphoxim)、乙基溴硫磷(Bromophos-ethyl)、2,3-对二氧杂环己烷二硫醇-S,S-二(O,O-二乙基连二硫酸磷酸酯(2,3-p-Dioxanedithiol-S,S-bis(O,O-diethylphosphorodithionat));
氨基甲酸酯类:棉铃威(Alanycarb)、丙硫克百威(Benfuracarb)、甲萘威(Carbaryl)、丁硫克百威(Carbosulfan)、双氧威(Fenoxycarb)、呋线威(Furathiocarb)、_二唑虫(Indoxacarb)、唑蚜威(Triazamate);
合成除虫菊酯类:甲体氯氰菊酯(alpha-Cypermethrin)、溴氰菊酯(Deltamethrin)、醚菊酯(Ethofenprox)、杀灭菊酯(Fenvalerate)、(RS)氯氟氰菊酯(Cyhalothrin)、氯氟氰菊酯(Lambda-Cyhalothrin)、氯菊酯(Permethrin)、灭虫硅醚(Silafluofen)、氟胺氰菊酯(Tau-Fluvalinate)、四溴菊酯(Tralomethrin)、己体氯氰菊酯(Zeta-Cypermethrin)、氟氯苯菊酯(Flumethrin)、氟氯氰菊酯(Cyfluthrin)及其对映异构体和立体异构体、氯氰菊酯(Cypermethrin);
节肢动物生长调节剂:a)几丁质合成抑制剂:苯甲酰脲类:定虫隆(Chlorfluazuron)、灭蝇胺(Cyromazine)、氟脲杀(Diflubenzuron)、氟螨脲(Flucycloxuron)、氟虫脲(Flufenoxuron)、氟铃脲(Hexaflumuron)、氟丙氧脲(Lufenuron)、双苯氟脲(Novaluron)、伏虫隆(Teflubenzuron)、杀虫隆(Triflumuron);噻嗪酮(Buprofezin)、_茂醚(Diofenolan)、噻螨酮(Hexythiazox)、特苯_唑(Etoxazole)、四螨嗪(Clofentazine);b)蜕皮激素拮抗剂:特丁苯酰肼(Halofenozide)、甲氧苯酰肼(Methoxyfenozide)、双苯酰肼(Tebufenozide);c)保幼激素类似物:蚊蝇醚(Pyriproxyfen)、蒙五一五(Methoprene)、双氧威(Fenoxycarb);d)类脂生物合成抑制剂:螺螨酯(Spirodiclofen);
新烟碱类:吡虫清(Acetamiprid)、噻虫胺(Clothianidin)、氟啶虫酰胺(Flonicamid)、吡虫啉(Imidacloprid)、硝胺烯啶(Nitenpyram)、噻虫啉(Thiacloprid)、噻虫嗪(Thiamethoxam);
合成球虫病化合物,聚醚抗菌素:氨丙啉(Amprolium)、Robenidin、百球清(Toltrazuril)、莫能霉素(Monensin)、盐霉素(Salinomycin)、马杜霉素(Maduramicin)、拉沙里菌素(Lasalocid)、甲基盐霉素(Narasin)、赛杜霉素(Semduramicin);
各种其它杀虫剂:齐墩螨素(Abamectin)、灭螨醌(Acequinocyl)、虫螨脒(Amitraz)、艾扎丁(Azadirachtin)、联苯肼酯(Bifenazate)、苏云金芽孢杆菌(Bacillus thuringiensis)、柯敌克菌(Bacillus subtilis)、杀螟丹(Cartap)、氟唑虫清(Chlorfenapyr)、杀虫脒(Chlordimeform)、灭蝇胺(Cyromazine)、杀螨硫隆(Diafenthiuron)、呋虫胺(Dinetofuran)、_茂醚(Diofenolan)、埃玛菌素(Emamectin)、硫丹(Endosulfan)、Epsiprantel、Ethiprole、喹螨醚(Fenazaquin)、锐劲特(Fipronil)、伐虫脒(Formetanate)、伐虫脒盐酸盐(Formetanate hydrochloride)、灭蚁腙(Hydramethylnon)、_二唑虫(Indoxacarb)、4-{(2Z)-2-({[4-(三氟甲氧基)苯胺基]羰基}亚肼基)-2-[3-(三氟甲基)苯基]乙基}苄腈、L-2,3,5,6-四氢-6-苯基咪唑并噻唑、保松噻(Levamisole)、米尔螨素(Milbemectin)、莫西菌素(Moxidectin)、吡喹酮(Praziquantel)、噻嘧啶(Pyrantel)、哒螨酮(Pyridaben)、拒嗪酮(Pymetrozine)、色拉菌素(Selamectin)、艾克敌105(Spinosad)、硫(Sulfur)、吡螨胺(Tebufenpyrad)和硫环杀(Thiocyclam)。
通常而言,“杀寄生物有效量”是指对生长获得可观察到的效果所需的活性成分量,所述效果包括坏死、死亡、延缓、预防和除去效果,破坏效果或目标生物体的出现和活动降低效果。对于用于本发明的各种化合物/组合物,杀寄生物有效量可以变化。组合物的杀寄生物有效量也可以根据主要条件如所需杀寄生物效果和持续时间、目标种类、施用方式等而改变。
对寄生物的作用实施例
1.经由玻璃接触测试对厩螫蝇、黄热病蚊、家蚊、疟蚊、猫跳蚤和棕色犬壁虱的接触活性的筛选方法
用0.5ml活性成分丙酮溶液处理玻璃小瓶(20ml闪烁小瓶)。将各小瓶开盖摇晃约10分钟以允许活性成分完全涂敷小瓶并使丙酮充分干燥。将昆虫或壁虱放入各小瓶中。将小瓶保持在22℃并在各时间间隔下观察处理效果。结果示于表I中。
2.经由水处理测试对黄热病蚊、南方家蚊和疟蚊幼虫的接触活性的筛选方法
将孔板用作测试场。将活性成分溶于丙酮中并用水稀释而得到所需浓度。将含有约1%丙酮的最终溶液放入各孔中。将在1ml水中的约10只蚊子幼虫(4龄幼虫)加入各孔中。幼虫每天进食一滴肝粉。将各盘覆盖并维持在22℃。每天记录死亡率并且每天取出死亡的幼虫和活或死的蛹。在试验结束时记录残留的活幼虫并计算百分死亡率。结果示于表I中。
各试验重复至少3次。
结果
使用式I-1和I-2化合物进行的试验呈现下列结果:
表I对各种物种的活性
害虫通用名 | 害虫拉丁名 | 施用率 | 达到100%死亡率的天数或小时数 |
经由玻璃接触测试接触活性的筛选方法 | |||
厩螫蝇 | 厩螫蝇(Stomoxys calcitrans) | 10ppm | 4小时 |
黄热病蚊 | 埃及伊蚊(Aedes aegypti) | 10ppm | 4小时 |
家蚊 | 致倦库蚊(Culexquinquefasciatus) | 0.5ppm | 4小时 |
小型赤家蚊 | Anopheles albimanus | 1ppm | 1天 |
猫跳蚤 | 猫跳蚤(Ctenocephalides felies) | 100ppm | 2天 |
棕色犬壁虱 | Rhipicephalus sanguineus | 10ppm | 3-5天 |
经由水处理测试接触活性的筛选方法 | |||
黄热病蚊 | 埃及伊蚊 | 10ppm | 2天 |
家蚊 | 致倦库蚊 | 10ppm | 1天 |
疟蚊 | Anopheles albimanus | 1.0ppm | 1天 |
3.在“人造狗”设备中对猫跳蚤的活性
将活性成分溶于丙酮中并与合适体积的已去纤维蛋白的牛血混合。将5ml已处理血倒入装有石蜡薄膜的进食室中。将带有已处理血的该室放于蚤进食室之上。对每个活性成分的5个剂量浓度的每个剂量浓度重复该试验。在各间隔下观察处理效果,包括击倒、24小时后不能进食、不能产卵等。用丙酮/血液混合物进行对照试验。
结果
用100ppm式I-1和I-2化合物进行的试验表明对猫跳蚤的杀灭率超过60%。
Claims (10)
1.式I的化合物或其对映异构体或非对映异构体、兽用可接受盐或酯在动物中和动物上防治寄生物的用途:
其中Q为:
X1氯、溴或氟;
R1、R2各自独立地为氢、C1-C10烷基、C3-C10链烯基、C3-C10炔基或C3-C12环烷基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷基羰基氨基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被1-3个如下基团取代:卤素、羟基、硝基、氰基、氨基、巯基、C1-C6烷氧基、C1-C6卤代烷氧基、C1-C6烷硫基、C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6卤代烷基磺酰基、C1-C6卤代烷基亚磺酰基或可以被1-3个基团R#代的C3-C6环烷基,或
R#为卤素、氰基、硝基、羟基、巯基、氨基、C1-C6烷氧基、C2-C6链烯氧基、C2-C6炔氧基、C1-C6卤代烷氧基、C1-C6烷硫基或C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷基羰基、C1-C6烷氧羰基或二(C1-C6烷基)氨基羰基;
甲酰基、C1-C6烷基羰基、C(=O)NRaRb、CO2Rc、Rd、Re、可以被1-3个基团R#取代的苯基或可以被1-3个基团R#取代的吡啶基,
Ra、Rb、Rc各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;
Rd为NRiRj或
Ri、Rj各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;
p、m各自独立地为0、1、2或3,条件是p和m不同时为0,
X为氧、硫、氨基、C1-C4烷基氨基或苯基氨基,或若p为0,则X还可以为苯氧基或C1-C6烷氧基;
r为0或1;
Re为
Rk、Rq各自独立地为氢或可以被1-3个基团R#取代的C1-C4烷基;
或
R1和R2可以一起形成如下结构代表的环:
p、m为1、2或3;
X’为氧、硫、氨基、C1-C4烷基氨基、苯基氨基或亚甲基;
Z为C1-C4烷基或苯基;
R3为氢、C1-C10烷基、C2-C10链烯基、C2-C10炔基、C3-C12环烷基,其中这些基团中的碳原子可以部分或完全被卤化或被1-3个如下基团取代:氰基、硝基、羟基、巯基、氨基、C1-C6烷基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被如下基团取代:
1-3个卤原子,5-6元芳族环体系,该环体系可以含有1-4个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,或
苯氧基,其可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,或
3-6元饱和或部分不饱和环体系,该环体系含有1-3个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代,
3-6元饱和或部分不饱和环体系,该环体系含有1-3个选自氧、硫和氮的杂原子且未被取代或被1-5个卤原子、1-3个C1-C6烷基、C1-C6烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6烷氧基、C1-C6卤代烷氧基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个卤原子取代;
R、R4各自独立地为氢或C1-C6烷基、C1-C6烷氧羰基、C1-C6烷基氨基羰基或二(C1-C6烷基)氨基羰基,其中这些基团中的碳原子可以被1-3个基团R#取代;
A为C-R5或N;
B为C-R6或N;
W为C-R7或N;
条件是A、B和W中的一个不为N;
R5、R6、R7各自独立地为氢、卤素、硝基、氰基、氨基、巯基、羟基、C1-C10烷基、C2-C10链烯基、C2-C10炔基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被1-3个基团R#取代,
5-6元芳族环体系,该环体系可以含有1-4个选自氧、硫和氮的杂原子且可以被1-5个卤原子、1-3个C1-C6烷基、C1-C6卤代烷基、C1-C6烷硫基、C1-C6卤代烷硫基、C1-C6烷基磺酰基、C1-C6烷基亚磺酰基、C1-C6卤代烷基磺酰基、C1-C6卤代烷基亚磺酰基、C1-C6烷氧基、C1-C6卤代烷氧基、巯基、羟基、氨基、硝基或氰基的任何组合取代,其中这些基团中的碳原子可以被1-3个基团R#取代;
Y为氢、卤素、氰基、硝基、氨基、羟基、巯基、C1-C6烷基、C2-C10链烯基、C2-C10炔基、C3-C6环烷基、C1-C6烷氧基、C1-C6烷基氨基、二(C1-C6烷基)氨基、C1-C6烷硫基、C1-C6烷基磺酰基或C1-C6烷基亚磺酰基,其中这些基团中的碳原子可以被1-3个基团R#取代;
n为0、1或2。
3.根据权利要求1或2的用途,其中式I化合物为式I-1化合物:
4.根据权利要求1或2的用途,其中式I化合物为式I-2化合物:
5.根据权利要求1-4中任一项的用途,其中所述寄生物选自双翅目、蚤目和蜱亚目。
6.根据权利要求1-5中任一项的用途,其中所述动物为猫或狗。
7.一种处理、防治、防止或保护动物免受寄生物侵染或感染的方法,包括对动物口服、局部或肠胃外给予或施用杀寄生物有效量的如权利要求1-4中任一项所定义的式I化合物。
8.如权利要求7所要求的方法,其中所述寄生物选自双翅目、蚤目和蜱亚目。
9.根据权利要求7或8的方法,其中所述动物为猫或狗。
10.一种制备用于处理、防治、防止或保护动物免受寄生物侵染或感染的组合物的方法,该组合物包含杀寄生物有效量的如权利要求1-4中任一项所定义的式I化合物。
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