Process for the preparation of 1-aminomethyl-1-cyclohexaneacetic acid

摘要

The invention relates to a novel embodiment of the Michael addition in the preparation of aminomethyl-1-cyclohexaneacetic acid (gabapentin), starting from cyclohexanone. By the use of KOH in the first reaction step, reaction with nitromethane in DMSO with alkali metal carbonate catalysis and reduction of the introduced nitro group at elevated temperature, the yield is raised and the safety of the preparation process is substantially increased.