Narcotic antagonists. Synthesis and evaluation of some substituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines

Journal of Medicinal Chemistry
1977.0

Abstract

A seres of (+/-)-N-substituted 6-ethyl-or -methyl-8-hydroxy-1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines has been prepared from 6 hydroxytropinone. The N-cyclopropylmethyl compounds 10a and 10b were found to be strong narcotic antagonists approximately equivalent to nalorphine. Only slight analgetic activity was found in any of these compounds including the two N-methyl analogues.

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