Study On The Synthesis Of Antiepileptic Drugs Lacosamide

Objective To synthesize of antiepileptic drugs lacosamide and studies the synthetic process of lacosamide.Methods Lacosamide was prepared by acrylic acid and benzylamine as raw materials through six steps including mixed carbonic anhydride method,difunctionalization of C-C double Bond,substitution,reduction,acetylation and chiral separation.The synthesis process of lacosamide was improved and optimized by single factor and orthogonal design through solvents,catalysts,reaction time and reaction temperature.The target structure was confirmed by IR,¹ H-NMR,¹³C-NMR and MS.Results The synthetic process of lacosamide was studied.The target product was obtained with a total yield of 25.7%,verify the purity of 99.8%and optical purity of 95.7%.The structure of lacosamide was determined by IR,¹H-NMR,¹³C-NMR and MS.The purity was determined by HPLC.Conclusions Designed the synthesis route of lacosamide.The reaction conditions of each intermediate was optimized from the obtained lacosamide synthesis process.The synthesis process had many advantages such as raw materials cheap,operation simple and better yeild to provide a reference for better industrial production.