发明名称 Verfahren zur Herstellung von Benzodiazepin-Derivaten
摘要 The invention comprises compounds of the general formula <FORM:1013229/C2/1> (wherein R1 represents an alkanoyl, aralkanoyl, aroyl or alkyl group, R2 represents a halogen atom or trifluoromethyl group, R3 represents a halogen atom or an alkyl, alkylthio, nitro or trifluoromethyl group, R4 represents an alkyl or alkenyl group, and the broken lines denote optional substituents) and acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by subjecting a compound of the formula <FORM:1013229/C2/2> to acylation with an aliphatic, araliphatic or aromatic carboxylic acid anhydride, sulphide or halide, optionally followed by (a) one or both of the steps of hydrolysis and reaction with an alkanol (consecutively or simultaneously when both steps are required), (b) introduction of the R4 group at any stage when not present in the starting material, and/or (c) acid addition salt formation at any suitable stage. The compounds of the invention are sedatives, anticonvulsants and muscle relaxants, and may be administered enterally or parenterally in the form of pharmaceutical preparations (e.g. tablets, dragees, suppositories, capsules, solutions, emulsions and suspensions) containing them, with or without other (unspecified) active ingredients, in association with a carrier. Specification 972,968 is referred to.
申请公布号 DE1545955(A1) 申请公布日期 1969.11.20
申请号 DE19631545955 申请日期 1963.02.23
申请人 F. HOFFMANN-LA ROCHE & CO AG 发明人 REEDER,EARL;STEMPEL,ARTHUR;HENRYK STERNBACH,LEO
分类号 A61K31/55;C07D243/18;C07D243/20;C07D243/24;C07D243/26 主分类号 A61K31/55
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