BENZOTHIAZEPINE DERIVATIVES AND PROCESS FOR THE MANUFACTURE THEREOF

摘要

Compounds of the general formula (wherein R and R1 each represent a halogen atom or a CF3 or akoxy group, R2 represents a phenyl, halophenyl, trifluoromethylphenyl, alkyl or pyridyl group, R3 and R4 each represent an alkyl group and the broken lines denote optional substituents) and 1-monoxides, 1,1-dioxides and 1,1,4-trioxides thereof and acid addition salts thereof are prepared (a) by the process shown in the following formula scheme: (wherein B represents the benzene or fused benz ring which may be substituted by R and/or R1, one of the symbols Y and Z represents a halogen atom and the other represents a mercapto group and Rb represents an amino or protected amino group) or (b) by a variant of process (a) in which there is used in the first stage an analogue of a ketone of Formula (II) which contains a single nitro group in the Y-substituted benzene ring, this analogue is reacted with a substituted ethane in which Rb represents a protected amino group, the nitro group in the product is reduced to an amino group, the latter is replaced by a halogen atom and the resulting halo-substituted ketone is cyclized by cleavage of the protecting group and heating, optionally followed in the case of either process by salt formation. The preparation of intermediates of the general formulae (wherein X represents BF4), and and of salts of compound of Formula (IV) is described. The compound of the invention are muscle relaxants and anticonvulsants and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier.