Abstract
AbstractThe novel morphinans 13–18, which carry amino acid substituents at C(6), with potentially limited access to the central nervous system were prepared in two steps from 14‐O‐methyloxymorphone (5). Reductive amination with amino acid tert‐butyl esters gave compounds 7–12, which were hydrolyzed with tetrafluoroboric acid. Structure elucidation (including X‐ray analysis), preliminary μ‐opioid receptor binding studies, and calculations of pharmacokinetic parameters were carried out.
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