Concise Synthesis of Lacosamide with High Chiral Purity

Abstract

An efficient synthesis process of an antiepileptic drug, lacosamide, with high chiral purity has been developed. A series of acids were screened to form salts with the key intermediate 4, and phosphoric acid, an inexpensive and achiral reagent, turned out to be the best counterion, which could enhance both chemical purity and chiral purity of the key intermediate 4. 4-Phosphate was used for the successful synthesis of lacosamide with high chemical and chiral purities.