| 摘要 |
The invention comprises compounds of the general formula <FORM:1008639/C2/1> (wherein R1 represents a hydrogen atom, a C1- 4 alkyl group or a benzyl group, R2 represents a C2- 4 alkyl group, R3 represents a pentyl or cyclopentyl group, and R4 and R5 each represents a C1- 4 alkyl group or, together with the adjoining carbon atom, form a cyclopentyl or cyclohexyl group) and physiologically tolerable acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by (a) reducing an amine (I) of the formula <FORM:1008639/C2/2> in the presence of a ketone R6COR7 (wherein R6 represents a C1- 4 alkenyl group, or R6, R7 and the adjoining carbon atom together form a cyclopentyl or cyclohexyl group), or (b) reacting (I) with an alcohol R4R5CHOH or an ester of the alcohol, optionally followed in either case by dealkylation or debenzylation, alkaylation and/or salt formation. The amine starting materials are prepared by catalytic hydrogenation of the corresponding cyanides, and the latter are prepared by reacting the appropriately substituted benzyl cyanides with a pentyl or cyclopentyl halide and sodamide. The compounds of the invention are analgesics and may be administered enterally or parenterally in the form of pharmaceutical preparations (e.g. tablets, dragees, capsules, solutions, suspensions and suppositories) containing them together with a carrier. |
