摘要 |
<p>1-Aryl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-ones of the general formula <IMAGE> I. wherein: R1 is hydrogen, lower alkyl, preferably of 1-3 carbons, or unsaturated lower alkyl preferably of 2-3 carbons R2, R3, R4, R5 are the same or different and are each hydrogen, halogen, lower alkyl, preferably methyl, lower alkoxy, preferably methoxy, or trifluoromethyl, and R6, R7, R8, R9 are the same or different and are each hydrogen or lower alkyl, preferably methyl. The compounds are prepared by dehydrohalogenating substituted 2-(3'-halogenopropionylamino)-diphenyl amines of the general formula <IMAGE> II. wherein R2 to R9 are the same as defined above and X is halogen, in the presence of a solvent and a base, to cyclize the amines and then alkylating to introduce the unsaturated lower alkyl radical R1 on the nitrogen in the 5 position, if necessary. The compounds possess anticonvulsant, sedative and muscle relaxant properties.</p> |