| 摘要 |
1,233,489. Benzodiazepine derivatives. F. HOFFMANNLA ROCHE & CO. A.G. 10 Oct., 1969 [18 Oct., 1968], No. 49746/69. Heading C2C. Compounds of the general formula (A = CH 2 , CO; Z = O, NH, N-(C 1-7 alkyl), N- acyl; R 1 = H, halogen, NO 2 , CF 3 , C 1-7 alkyl, C 1-7 alkylmercapto, C 1-7 alkoxy; R2 = H, C 1-7 alkyl, C 3-6 cycloalkyl, C 1-7 hydroxyalkyl; R 3 = H, C 1-7 alkyl; Y = (CH 2 ) 2 , 3 optionally substituted by C 1-7 alkyl, CH 2 Cl, CH 2 Br, C 1-7 alkoxy- (C 1-8 alkyl), di-(C 1-7 alkyl)aminomethyl; R 5 = H, C 1-7 alkyl, Py, Ph optionally substituted by halogen, NO 2 , CF 3 , C 1-7 alkyl) are prepared by (a) cyclizing a compound of the formula optionally followed by alkylation or acylation or (b) reacting a compound of the formula with oxirane or a derivative thereof in the presence of an acidic agent, optionally followed in either case by separation of an isomer mixture. The above compounds are sedatives, muscle relaxants and anticonvulsants, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier. |
