Process for the preparation of lacosamide and its novel intermediate

摘要

An improved, cost effective process for the preparation of Lacosamide is disclosed. A novel intermediate of formula (IV) and a process for preparation of the novel intermediate is also disclosed.;
wherein, X is halogen.

主权项

1. A process for the preparation of Lacosamide of formula (I) which comprises: i). regioselective ring opening of compound of formula (II) in presence of water, followed by oxidation with an oxidising agent to obtain compound of formula (III) wherein, X is halogen; ii). reaction of compound of formula (III) with benzyl amine in presence of a base and coupling agent to obtain a compound of formula (IV); iii). reaction of compound of formula (IV) with a base in alcohol solvent to obtain a compound of formula (V); iv). protection of hydroxyl group of compound of formula (V) with Tosyl chloride in presence of dimethyl amino pyridine, dichloromethane and triethyl amine to obtain compound of formula (VI); v). reacting compound of formula (VI) with sodium azide in presence of dimethyl formamide and water to obtain compound of formula (VII); vi). reducing compound of formula (VII) with H2 in the presence of organic solvent and catalyst to obtain compound of formula (VIII); vii). acylation of compound of formula (VIII) with aceticanhydride in presence of dimethyl amino pyridine and anhydrous methylene dichloride to obtain Lacosamide of formula (I); optionally, recrystalizing Lacosamide in ethyl acetate to give pure Lacosamide of formula (I).