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1. 发明公开

KR1020120101338A 페닐피리(미)디닐아졸 无效
标题翻译： PHENYLPYRI（MI）DINYLAZOLES
公开(公告)号：KR1020120101338A
公开(公告)日：2012-09-13
申请号：KR1020127008037
申请日：2010-10-04
申请人： 바이엘 크롭사이언스 악티엔게젤샤프트
发明人： 수다우알렉산더 , 에스-사예드마젠 , 브라운크리스토프안드레아스 , 마이스너루쓰 , 시르방카트린느 , 벤팅위르겐 , 다멘페터 , 포르츠다니엘라 , 바헨도르프-노이만울리케 , 데스보르데스필리프 , 베나비사미르 , 캐서린크리스토퍼 , 레브스톡앤-소피 , 그로장-쿠노에마리-클레르 , 하다노히로유키 , 크노블로흐토마스 , 리놀피필리프
IPC分类号： C07D403/14 , C07D401/14 , C07D487/04 , A01N43/56
CPC分类号： A01N43/56 , A01N43/84 , A01N43/90 , A61K31/415 , A61K31/44 , A61K31/495 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D471/04 , C07D487/04 , C07F5/02 , C07F7/2212
摘要： Phenylpyri(mi)dinylpyrazole compounds (A) and their salts, are new. Phenylpyri(mi)dinylpyrazole compounds (A) of formulae (I) and (II), and their salts, are new. In formula (I): X1 : CH or N; R1 : e.g. 1-benzothiophen-4-yl, 1-benzothiophen-7-yl, 1-benzofuran-4-yl, 1-benzofuran-7-yl, 1,3-benzodioxol-4-yl or 1,3-benzodioxol-5-yl (all optionally one or more times substituted); R2 : e.g. CN, nitro, halo, 2-9C-heterocyclyl or H; R3 : e.g. 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl or 3-6C-cycloalkyl (all optionally one or more times substituted); R4 : e.g. 1-6C-alkyl, 3-8C-cycloalkyl, 2-6C-alkenyl, 6-14C-aryl, 2-9C-heterocyclyl or 2-9C-heteroaryl (all optionally one or more times substituted), H, halo or CN; and R5, R6 : e.g. 1-6C-alkyl, 6-14C-aryl, S-(1-4C-alkyl), S(O)-(1-6C-alkyl) or C(O)-(1-6C-alkyl) (all optionally one or more times substituted), H, F, Cl, Br, CN, nitro, OH or SH. In formula (II): e.g. X1 : CH or N; R1 : e.g. isoquinolin-5-yl, isoquinolin-8-yl, 1-benzothiophen-4-yl, 1-benzofuran-7-yl or 1,3-benzodioxol-5-yl (all optionally one or more times substituted); R2 : e.g. 1-6C-(halo)alkyl, 3-6C-(halo)cycloalkyl, 2-9C-heterocyclyl or H; R301 : e.g. 1-6C-alkyl, 2-6C-alkenyl, 3-6C-allenyl, 2-6C-alkynyl, 3-8C-cycloalkyl, 1-6C-alkoxy, 2-9C-heterocyclyl, 2-9C-oxo-heterocyclyl or heteroaryl (all optionally one or more times substituted); R401 : NR12R13 or C(O)NR12R13; R5, R6 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl, 2-6C-alkynyl, 6-14C-aryl, S(O)-(1-6C-alkyl) or C(O)-(1-6C-alkyl) (all optionally one or more times substituted); R12 : e.g. C(S)R15, C(O)R15 or SO 2R15; R13 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl or 2-9C-heteroaryl (all optionally one or more times substituted) or H; and R15 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl, 2-6C-alkynyl or 2-9C-heteroaryl (all optionally one or more times substituted), H or OH. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) (hetero)aryl-pyrazole compounds (X) of formulae (XA) and (XB) and their salts; (2) (hetero)aryl-pyrazole compounds (XI) of formulae (XIA) and (XIB) and their salts, where (XI) exclude 1-({4-[1-(2,2-difluoroethyl)-3-(t rimethylstannyl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-ol; and (3) (hetero)arylamine-pyrazole compounds (III) of formulae (IIIA) and (IIIB) and their salts, where (III) exclude 4-[3-(4-fluorophenyl)-5-m ethyl-1H-pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-chlorophenyl)-5-methyl -1H-pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-methoxyphenyl)-5-methyl-1H- pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]p yrimidin-2-amine, 4-(5-methyl-3-phenyl-1H-pyrazol-4-yl)pyrimidin-2-a mine and [4-(2-aminopyrimidin-4-yl)-3-(3-chloro-5-hydroxyphenyl)-1H-p yrazol-1-yl]acetonitrile. PG : tetrahydro-2H-pyran-2-yl; M3 : tributylstannyl, 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl; and PG1 : tetrahydro-2H-pyran-2-yl or 2-(trimethylsilyl)ethoxymethyl. [Image] [Image] [Image] - ACTIVITY : Fungicide; Antibacterial. - MECHANISM OF ACTION : None given. The fungicidal activity of (A) against Botrytis cinereawas tested in cucumber plants. The results showed that 4-[3-(4-fluorophenyl)-1-(2-methylpropyl)-1H-pyrazol-4-yl]pyridine (500 ppm) exhibited an activity of 70%.

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