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Potential synthetic codeine substitutes: (-)-3-O-aryl-N-methylmorphinans.

E Mohacsi·T Hayes·J Sepinwall
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Abstract

A series of novel O-aryl-N-methylmorphinans (7-19) were synthesized by the Ullmann reaction from levorphanol (4) in our search for a synthetic codeine (2) substitute with reduced addition liability. The compounds were evaluated for antinociceptive potency and receptor binding affinity. Among these compounds, (-)-3-phenoxy-N-methylmorphinan (7) is an orally active analgesic comparable in potency to codeine (2), which exhibits decreased physical dependence liability and longer duration of action.

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AnimalsKineticsMorphinansNociceptorsRatsReceptors, OpioidStructure-Activity RelationshipJournal Article

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E Mohacsi, T Hayes, J Sepinwall. 1984. Potential synthetic codeine substitutes: (-)-3-O-aryl-N-methylmorphinans.. https://doi.org/10.1021/jm00375a024

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