| 摘要 |
<p>2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: <IMAGE> [I] wherein R1 and R2 are each hydrogen or C1-C3 alkyl; and R3 is hydrogen, halogen or C1-C3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: <IMAGE> [II] wherein R1 and R2 are as defined above, with a reactive derivative of an alcohol compound of the formula: <IMAGE> [III] wherein X is an optionally protected carbonyl group; and R3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: <IMAGE> [IV] wherein R1, R2 and R3 are as defined above.</p> |
