关键词: 拉科酰胺, 癫痫, 半合成

Abstract: Lacosamide(LCM)，a novel antagonist of the glycinebinding site on N-methyl-D-aspartate（NMDA） receptors，is mainly applied to the treatment of epilepsy and neuropathic pain. This review is to introduce recent studies on the synthesis of Lacosamide through both total synthesis and semi-synthesis methods. For the semi-synthesis method，chemical resolution or enzymatic kinetic resolution is usually adopted for producing its precursor material R-serine and its derivatives，and then the final product Lacosamide is obtained by chemical synthesis. For the total synthesis method，benzyl alcohol is used as raw material，and the final product Lacosamide is then obtained through a series of reaction：condensation，catalyzed hydrolysis，substitution，protective oxidation，de-protective condensation. Furthermore，the advantages and disadvantages of both synthesis methods are analyzed：the advantages of semi-synthesis are that reactions are easy to be reached，and the synthesis procedure is short，but its disadvantages includes expensive reaction reagent，too many side-effects，low yield and so on；while total synthesis is featured as easy raw material obtaining and low cost，long reaction procedure and low resolution yield. Therefore，the future development of Lacosamide should follow a more suitable synthesis route and adopt the revised modern synthesis techniques. Besides，to reduce the industrial cost significantly，the resource of raw material should be improved and the cost of reaction reagent should be reduced also.

Key words: Lacosamide, epilepsy, semi-synthesis