反应详情

The (R)-2-amino-N-benzyl-3-methoxypropionamide solution prepared above was cooled to <5° C. and acetic anhydride (10 ml, 0.106 mol) added at <15° C. The reaction mixture is warmed to room temperature over 30 minutes and aged for a further 30 minutes. The mixture is then washed with water (44 ml), 8% sodium bicarbonate (44 ml) and water (44 ml). The methylene chloride was exchanged for ethyl acetate by distillation and the solution distilled to a volume of 115 ml. The product was crystallized by cooling the solution to 0-5° C. and the pure Lacosamide isolated by filtration (18.7 g, 69.8%) HPLC purity 99.98%, Chiral purity 99.8% ee.

1. temperatureabove was cooled to <5° C.
2. washThe mixture is then washed with water (44 ml), 8% sodium bicarbonate (44 ml) and water (44 ml)
3. distillationThe methylene chloride was exchanged for ethyl acetate by distillation
4. distillationthe solution distilled to a volume of 115 ml
5. customThe product was crystallized
6. temperatureby cooling the solution to 0-5° C.