普瑞巴林合成工艺的改进  

Improvement of Pregabalin Synthesis Process

作　　者：祁秀秀[1] 陈文华[1] 陈闻起[1] 尤海烽 王菲 张乔乔 Qi Xiuxiu;Chen Wenhua;Chen Wenqi;You Haifeng;Wang Fei;Zhang Qiaoqiao(Department of Chemical and Pharmaceutical Engineering,Changzhou 213164,China)

机构地区：[1]常州工程职业技术学院制药与生物工程技术系

出　　处：《宁夏大学学报（自然科学版）》2019年第4期366-369,共4页Journal of Ningxia University(Natural Science Edition)

基　　金：江苏省青蓝工程基金资助项目(2018-12);江苏省高等学校自然科学研究面上基金资助项目(17KJB350001);江苏省“双创计划”科技副总项目(FZ20190353)

摘　　要：以丙二酸和异戊醛为原料,经过缩合、酯化、加成、水解得到3-异丁基戊二酸,再经过环化、氨解、Hoffman重排降解得到(±)-3-氨甲基-5-甲基己酸,该消旋体经过(S)-(+)-扁桃酸拆分得到普瑞巴林.该合成工艺产物的总收率为32.7%,且操作简便,易于工业化生产.Taking malonic acid and isovaleraldehyde as raw materials,3-isobutyl glutaric acid was obtained by condensation,esterification,addition and hydrolysis.(±)-3-aminomethyl-5-methylhexanoic acid was then obtained by cyclization,ammonolysis and Hoffman rearrangement.Pregabalin is obtained by the separation of racemate by(s)-(+)-mandelic acid.The total yield of the product of the synthesis process is 32.7%,and the operation is simple and easy for industrial production.

关 键 词：丙二酸 异戊醛 3-异丁基戊二酸 普瑞巴林 合成 

分 类 号：O625.63[理学—有机化学] R917[理学—化学]