Benzdiaz[1,4]Epine Derivatives

摘要

1,165,112. Benzodiazepine derivatives. F. HOFFMANNLA ROCHE & CO. A.G. 19 April, 1968 [21 April, 1967; 23 Oct., 1967], No. 18512/68. Heading C2C. Compounds of the general Formula (I) (B = CO or CH 2 , R1 = C 1-7 alkyl, R2 = CN or CONH 2 , R3 = C 1-7 alkyl, OH or alkanoyloxy, R4 = halogen, C 1-7 alkyl, NO 2 , CN or CF 3 , R5 = phenyl, (C 1-7 alkyl) phenyl, halophenyl, nitrophenyl or pyridyl, n = 2-7 and the broken lines denote optional bonds), N4-oxides of those compounds in which a double bond is present in the 4,5-position and acid addition salts of the compounds and oxides are prepared by treating a compound of the Formula (II) (R6 = C 1-7 alkyl) or an N4-oxide thereof with a cyanogen halide, optionally followed by hydrolysis or treatment with a strong acid and/or salt formation. The preparation of 7-chloro-5-(2-fluorophenyl)- 1 ,3.dihydro-2H-benzdiaz[1 ,4]epinone- (2) 4-oxide 7 - chloro - 1 - (2 - diethylaminoethyl) - 5 - (2 - fluorophenyl) - 1,3 - dihydro - 2H - benzdiaz[1,4]epinone - (2) 4 - oxide and 3 - acetoxy - 7 - chloro - 1 - (2 - diethylaminoethyl) - 5 - (2 - fluorophenyl) - 1,3 - dihydro - 2H - benzdiaz[1,4]- epinone-(2) and its hydrochloride is described. Compounds (I), R2 = CN or CONH 2 , their N4-oxides and salts of the compounds and oxides are hypnotics, psychosedatives, anticonvulsants, sedatives and muscle relaxants and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier.