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目的优化L-2-氨基-4-叠氮基丁酸的合成工艺。方法以L-蛋氨酸为起始原料经硫甲基化、水解一锅法制得L-2-氨基-4-羟基丁酸(2),2在浓盐酸中环合得到重要中间体α-氨基-γ-丁内酯盐酸盐(3),3经溴代开环、成酯、叠氮化、水解4步反应得到目标产物。结果与结论以L-蛋氨酸为起始原料,经6步反应合成目标产物,其结构经1H-NMR和IR谱确证。该合成方法原料易得、条件温和、操作简单、易于中试放大。
Objective To optimize the synthesis of L-2-amino-4-azido butyric acid. Methods L-2-amino-4-hydroxybutyric acid (2) was prepared by thiomethylation of L-methionine in one-pot by hydrolysis, and cyclization of 2 in concentrated hydrochloric acid gave α-amino-γ - butyrolactone hydrochloride (3), 3 by brominated ring opening, ester formation, azidation, hydrolysis 4-step reaction to give the desired product. Results and Conclusion The target product was synthesized through 6 steps using L-methionine as starting material. Its structure was confirmed by 1H-NMR and IR. The synthesis method is easy to obtain raw materials, mild conditions, easy to operate, easy to enlarge pilot.