Abstract

AbstractOxymorphone was converted to naltrexone in three steps by palladium‐catalyzed oxidative N‐demethylation and intramolecular acyl transfer from C‐14 hydroxy to N‐17. Vitride™ reduction of N‐acylamide to N‐alkylamine proceeded with concomitant reductive deprotection of C‐6 and O‐3 functionalities.

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