草酸依地普伦.pdf

年 月第 卷第 期 2010 2 7 6 ·综 述 · 艾司西酞普兰合成路线图解 1 2 2 2 2 师建华 ，王 梅 ，孟 歌 ，周 凯 ，赵桂兰 （ 西安交通大学继续教育学院，陕西西安 ； 西安交通大学医学院药学系，陕西西安 ） 1. 710061 2. 710061 摘要 本文综述了手性抗抑郁药物艾司西酞普兰的 条合成路线，主要分为拆分法和手性合成法两大类，这两类 [ ] 11 方法各有优势。 通过拆分法获得艾司西酞普兰原料成本较高，操作条件苛刻，且拆分过程复杂；而采用不对称法可 直接合成所要求的异构体，可明显提高药品质量和生产效率，降低终产物的生产成本。 两种方法各有特点，后一种 合成法则为优选方法。 关键词 艾司西酞普兰；合成路线；图解；拆分；手性合成 [ ] [中图分类号] R978.7 [文献标识码] A [文章编号] 1673-7210 （2010 ）02 （c ）-015－03 Graphical synthetic routes of Escitalopram 1 2 2 2 2 SHI Jianhua , WANG Mei , MENG Ge , ZHOU Kai , ZHAO Guilan (1.School of Continuing Education, Xian Jiaotong University, Xian 710061, China; 2.School of Medicine, Xian Jiaotong University, Xian 710061, China) [Abstract] Graphical synthetic routes of the chiral anti-depressant drug Escitalopram were reviewed in this article. These eleven kinds of methods could be divided into two main groups, including resolution methods and asymetric synthesis routes. Escitalopram could be obtained by resolution methods with high cost, harsh conditions and complex workups. Citalopram isomer with an improved quality could be produced through direct asymetric synthesis route by increasing the production efficiency and reducing the cost of the target molecule significantly. Each of them has different