摘要
R-2-羟基-4-苯基丁酸乙酯是制成血管紧张素转化酶抑制剂类药物的重要中间体,以廉价易得的DL-苹果酸为手性源,经过酐活化、付-克反应、拆分、常压催化氢解和酯化等成功地制得了R-2-羟基-4-苯基丁酸乙酯,为了工业化生产制备该类药物提供了一些可行的方法和途径。
R-2-hydroxy-4-phenyl ethyl butyrate is an important intermediate of an angiotension converting enzyme inhibitor. R-2-hydroxy-4-phenyl butyric acid and its ethyl ester was synthesized with DL-malic acid as starting material by a series reation, such as enzyme activity, resolution, Frieded-Crafts reaction, hydrogenolysis, esterification in general pressure. The study provided a practicable method for industrial production of this remedy.
出处
《四川大学学报(工程科学版)》
EI
CAS
CSCD
2003年第4期106-108,共3页
Journal of Sichuan University (Engineering Science Edition)
关键词
光学活性
拆分
包结拆分
不对称合成
R-2-羟基-4-苯基丁酸乙酯
optical activity
resolution
inclusion resolution
asymmetric synthesis
DL-malic acid
R-2-hydroxy-4-phenyl ethyl butyrate