C-14 OXIDATION OF MORPHINE DERIVATIVES

摘要

The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising rea cting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein R1 is (1C-7C) alkyl optionally substituted with one or more chlorines, butenyl, vinyl, benzyl, phenyl or naphthyl; and R2 is benzyl or benzyl substituted with one ore more (1C-6C) alkoxy group or benzyl substituted with one or more halogen. The process is very suitable in the production of noroxymorphone.