N-甲基-D-天冬氨酸的合成工艺优化  

Synthesis of N-Methyl-D-aspartic Acid and Optimization of the Technological Conditions

作　　者：朱高峰[1] 赖明友 曹俊[1] 李永[1] 樊玲玲[1] 汤磊[1] 

机构地区：[1]贵州医科大学药学院,贵州贵阳550004

出　　处：《化学试剂》2016年第3期280-282,286,共4页Chemical Reagents

基　　金：贵州省高等学校化学药物研发工程中心项目(黔教合KY字[2014]219);贵阳医学院药物化学重点实验室项目(GYZD[2014]001);贵州省科技厅-贵州医科大学联合基金(黔科合LH字[2015]7340)

摘　　要：以D-天冬氨酸为原料,依次通过酯化、酰化、N-甲基化和水解四步反应制得标题化合物,并对酯化和N-甲基化的反应条件进行了考察和优化,使反应总产率达到82.1%,并且产品的纯度与光学纯度均高于98%,从而避免了手性拆分,降低了生产成本,更适合工业化生产。N-methyl-D-aspartic acid was prepared through a four-step reaction of esterification,acylation,methylation and hydrolysis from D-aspartic acid used as a starting material. The reaction conditions of esterification and N-methylation were investigated and optimized. The overall yield of this method was 82. 1% and HPLC purity（ including optical purity） more than 98%,which can avoid chiral resolution and reduce the production cost. Therefore,this method is more suitable for industrial production.

关 键 词：N-甲基-D-天冬氨酸 合成 工艺优化 

分 类 号：O626[理学—有机化学]