Process for the preparation of O-desmethyl venlafaxine and intermediate for use therein

摘要

The present invention relates to a compound of formula A, wherein R is alkyl.;;Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.

主权项

1. A process for preparing O-desmethyl venlafaxine (ODV) of formula Vcomprising converting a compound of formula Ato ODV, wherein R is an alkyl group, wherein converting the compound of Formula A to ODV comprises:
d) reacting compound A with a Grignard reagent in the presence of a cyclic or acyclic ether as a solvent to form 1-[1-(4-benzyloxy-phenyl)-2-dimethylamino-ethyl]-cyclohexanol of formula IV;and
e) deprotecting 1-[1-(4-benzyloxy-phenyl)-2-dimethylamino-ethyl]-cyclohexanol to form ODV.