Synthesis and narcotic agonist-antagonist evaluation of some 2,6-methano-3-benzazocine-11-propanols. Analogs of the ring C bridged oripavine-7-methanols

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Abstract
A general synthesis of variously substituted 2,6-methano-3-benzazocine-11-propanols is described. Nine N-CH3 derivatives and their corresponding N-cyclopropylmethyl counterparts were prepared and studied in the mouse acetylcholine-induced writhing and rat phenazocine antagonism tests. The results are compared with literature information on the bridged oripavine methanols. The synthetic analogues have a different structure-activity profile, in general being weak agonists but potent antagonists.