Organic Process Research and Development p. 818 - 824 (2019)
Update date:2022-09-26
Topics:
Yang, Anjiang
Hu, Feifei
Li, Zhong
Chen, Mengdi
Cai, Jianguang
Wang, Linghui
Zhang, Tao
Zhao, Chuanmeng
Zhang, Fuli
An improved synthesis of Lacosamide 1 with high purity has been developed. Critical parameters of each step were identified as well as the impurities generated. Moreover, a creative method to improve chiral purity and stability of the key intermediate (R)-2-amino-N-benzyl-3-methoxypropionamide 10 by forming salt with an achiral acid (phosphoric acid) was discovered to ensure the chiral purity of (R)-Lacosamide. Phosphoric acid was further developed for the deprotection of the Boc group.
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