| 摘要 |
Pyrimidin-2-yl-1-pyrazole compounds (I), are new. Pyrimidin-2-yl-1-pyrazole compounds of formula (I), are new. X : phenyl, 2-pyridyl, 3-pyridyl or 2-pyrimidinyl (all substituted with one or multiple substituents selected from halogen, alkyl, haloalkyl, alkoxy, alkoxyalkyl, cycloalkyl, alkenoxy, alkinoxy, benzyloxy, cycloalkylalkoxy, haloalkoxy, haloalkoxyalkyl, alkylsulfanyl or haloalkylsulfanyl), alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, cyano, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, carboxyl, carboxamide, dialkylcarboxamide, trialkylsilyl, nitro, amino, alkylamino, dialkylamino, alkylsulfonylamino, dialkylsulfonylamino, -CH=NO-H, -CH=NO-alkyl, -CH=NO-halolkyl, -C(CH 3)=NO-H, -C(CH 3)=NO-alkyl, -C(CH 3)=NO-haloalkyl, formyl or benzyl substituted with one or multiple halogen atoms, phenoxy or pyrid-2-yloxy; R 1>alkyl substituted with one or two substituents selected from alkoxy, haloalkoxy, alkylsulfanyl, haloalkylsulfanyl, alkylsulfinyl, haloalkylsulflnyl, alkylsulfonyl, haloalkylsulfonyl, alkylcarbonyl, alkoxycarbonyl, hydroxy, cycloalkyl, phenyl, heterocyclyl, haloalkyl substituted with alkoxy, cyano, formyl, -CH=NO-H, -CH=NO-alkyl, -CH=NO-haloalkyl, -C(CH 3)=NO-H, -C(CH 3)=NO-alkyl, -C(CH 3)=NO-halolkyl or benzyl if necessary substituted with one or multiple substituents selected from halogen, alkyl, haloalkyl or alkoxy; R 2>amine optionally substituted with alkyl, alkylcarbonyl, cycloalkyl, alkenyl, alkoxycarbonyl, alkenoxycarbonyl, alkinoxycarbonyl, alkoxycarbonylalkyl, benzyl or phenylcarbonyl, piperidine, pyrrolidine, morpholine or halogen; R 3>halogen, alkyl, haloalkyl, alkoxy or dialkylamine, and n : 0 or 1. provided that: if R 5>=benzyl, alkyl, alkoxycarbonyl, alkenoxycarbonyl, alkinoxycarbonyl or alkylcarbonyl then R 6>=benzyl, alkyl, alkoxycarbonyl, alkenoxycarbonyl, alkinoxycarbonyl or alkylcarbonyl. Independent claims are included for the preparation of (I). [Image] - ACTIVITY : Antiparasitic. - MECHANISM OF ACTION : Ryanodine receptor antagonist. |
