PROCESS FOR PREPARING 4,5-DIHYDRO-AND 4,5,6,7-TETRAHY-DROPYRAZOLO ]1,5-A PYRIMIDINES

摘要

A compound of the formula: wherein --- may represent the presence of a double bond between the C6 and C7 position, Ia, or the absence of a double bond between the C6 and C7 position, Ib; R1 is hydrogen, bromo, chloro, carbamoyl, carboxamido, ethylcarboxylate, carboxyl, carboxyalkoxyl where alkoxy is (C1-C3), cyano, -CO-CF3, COONa, -CO-C(CH3)3, or where X is hydrogen, cyano, halogen or nitro; R2, R4 and R5 are hydrogen or lower alkyl(C1-C3); R3 ia hydrogen, alkyl(C1-C3), where R7 and R8 may be the same or different and are hydrogen, halogen, alkyl(C1-C3), nitro, alkoxy(C1-C3), trifluoromethyl, N-alkyl(C1-C3)- N-alkanoxyl(C1-C3)- amino, acetylamino or N-alkylacetylamino where alkyl is (C1-C3), and R3 may be a monovalent radical of 3-thienyl, 2-pyridinyl, 3-pyridinyl or 4-pyridinyl, either of said pyridinyl radicals being optionally substituted with an alkyl radical R9, where alkyl is (C1-C4), and the structures of the monovalent 2-pyridinyl, 3-pyridinyl and 4-pyridinyl moieties are depicted respectively as: R6 is hydrogen, alkyl (C1-C3) or , where n is an integer from 1 to 4 inclusive; and Z is CH-, N- and -O- such that when Z is -CH, R10 is hydrogen, ethoxycarbonyl, phenyl, phenylmethyl, phenylmethyl(C1-C6)alkylenyl, when z is -O-, R10 is nil and when Z is N-, R10 is hydrogen, alkyl- (C1-C3), alkenyl(C2-C3), alkynyl(C2-C3), cycloalkyl(C3-C6), dimethylaminoalkyl(C1-C3), hydroxyalkyl(C1-C3), ethylcarboxylate, alkyl(C1-C3)carbonyl, phenyl, benzyl, mono- or disubstituted benzyl [wherein the substituents are halogen, alkoxy(C1-C3), alkyl (C1-C3), and trifluoromethyl], benzoyl, 4-chlorophenylmethyl, 1,3-benzodioxol-5-yl-methyl, 1,3-benzodioxol-5-yl, 2-furanylcarboxyl, 2-pyrimidinyl, 2-pyridinyl, 4-morpholinyl-2-oxoethyl, N-(1-methylethyl)-2-oxoethyl, 1-pyrrolidinyl-2-oxoethyl, bis(4-fluorophenyl)-methyl, 2-cyclohexylethyl, phenylcarboxamido, mono- and di-substituted phenylcarboxamido [wherein the substituents are trifluoromethyl, halogen and alkyl (C1-C3)], adamantanoyl, 3-phenoxypropyl, mono- and disubstituted phenyl [wherein the substituents are halogen, trifluoromethyl, alkoxy(C1-C3) and alkyl(C1-C3)], 5-chloro-2-methoxy phenylacetamide and (2-oxo-1-pyrrolidinyl)-2-butynyl and the pharmacologically acceptable acid addition salts thereof.