N-甲酰-α-L-天门冬氨酰-L-苯丙氨酸水相合成法

N-formyl alpha- L-aspartyl- L- phenylalanine synthesis in aqueous phase

将N-甲酰-α-L-天门冬氨酸酐和液碱分次加入L-苯丙氨酸的碱性水溶液中,实现N-甲酰-α-L-天门冬氨酸酐与L-苯丙氨酸的酰化反应,得到产物N-甲酰-α-L-天门冬氨酰-L-苯丙氨酸,产率达96%。该方法实现水相酰化,大幅降低生产成本,实现生产工艺的绿色化。

Usually acylation of N -- formyl alpha -- L -- aspartic anhydride and L - phenylalanine must be carried out in acetic acid, without water. We added N -- formyl alpha -- L -- aspartic anhydride and liquid alkali in alkaline aqueous solution with L--phenylalanine step by step to achieve acylation process of N -- formyl alpha -- L -- aspartic anhydride and L -- phenylalanine. The result showed that the productive rate of the target compound, N--formyl alpha -- L -- as- partyl -- L - phenylalanine, was 96%. The technology is eco--friendly.