CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES

摘要

Described herein is an efficient, cost-effective, one-pot process that affordshighdiastereomeric purity of N-alkyl morphinan-6-ols from morphinan-6-ones. Inparticular,the process comprises contacting a compound of Formula (II) with a boron-basedreducing agent and a carbonyl compound to form a compound of Formula (I):(see formula I)wherein L is absent, n is 1, R25 is OH, and R1, R2, R3, R10, R11, and R14 areas definedherein.