| 摘要 |
The invention is concerned with certain new 6,7-benzomorphan derivatives having pharmacological, in particular analgesic and/or morphine-antagonistic properties, of the formula <IMAGE> wherein R1 is a substituted or unsubstituted phenyl or heteroaryl group; R2 is a hydrogen or halogen atom, or a hydroxy, alkoxy or acyloxy group; R3 is an alkyl or alkenyl group; R4 is a hydrogen atom or a hydroxy, alkoxy or acyloxy group; and R5 is an alkyl group or, when R2 is hydrogen in a trans-position to R3, R5 is a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, or a substituted or unsubstituted phenylalkyl, heteroarylalkyl or heterocycloalkylalkyl group; optical isomers and pharmaceutically acceptable salts thereof. The preferred compound is the alpha -isomer of 2,5-dimethyl-2'-hydroxy-9-phenyl-6,7-benzomorphan, in particular its (+)-enantiomer. These compounds are prepared by total synthesis and are not derived from opium alkaloids.
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