3-Mercaptopropionic acid as a new reagent for the industrially applicable synthesis of highly pure O-desmethylvenlafaxine from venlafaxine

摘要

3-Mercaptopropionic acid was introduced as a cheap new O-demethylating agent as exemplified by its application in the synthesis of antidepressant O-desmethylvenlafaxine from venlafaxine. The application of 3-mercaptopropionic acid allowed high conversion of venlafaxine to O-desmethylvenlafaxine and a facile workup, which enabled the isolation of the desired O-desmethylvenlafaxine with a high >99.8% chromatographic purity and 76% yield by a simple extractive workup followed by the precipitation.