Process for preparing lacosamide

摘要

The present invention provides a process for the preparation of lacosamide in substantially optically pure form, which in one aspect comprises the following steps: (i) resolution of O-methyl-D,L-serine to provide O-methyl-D-serine in substantially optically pure form; (ii) acetylation of O-methyl-D-serine thereby obtained to provide the N-acetyl 10 derivative thereof in substantially optically pure form; (iii) activating the carboxy group of the compound thereby obtained; and (iv) reacting the compound thereby obtained with benzylamine.

主权项

1. A process for the preparation of lacosamide of formula (I): in at least 95% optically pure form, which process comprises,
(ii) acetylating O-methyl-D-serine of formula (III),  to provide the compound of formula (IV),  in at least 95% optically pure form;(iii) activating the carboxy group of the compound of formula (IV) thereby obtained to provide a compound of formula (V),  wherein Q1 is a carboxy activating group; and(iv) reacting the compound of formula (V) thereby obtained with benzylamine.