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草酸依地普仑的合成
引用本文:姚忠科,阚丽娟. 草酸依地普仑的合成[J]. 中国新药杂志, 2006, 15(2): 117-120
作者姓名:姚忠科  阚丽娟
作者单位:1. 首都师范大学化学系,北京,100037
2. 中国科学院动物研究所,北京,100080
摘    要:目的:合成草酸依地普仑。方法:以5-氰基苯酞为起始原料,经亲核加成、水解、化学拆分、环化和成盐等反应制得抗抑郁药草酸依地普仑。结果:以5-氰基苯酞计,总收率为13.6%。结论:该方法原料价廉易得,反应条件温和,操作简便,适合工业生产。

关 键 词:草酸依地普仑  5-HT选择性再摄取抑制剂  抗抑郁药  药物合成
文章编号:1003-3734(2006)02-0117-04
收稿时间:2005-07-19
修稿时间:2005-07-19

Synthesis of escitalopram oxadate
YAO Zhong-ke,KAN Li-juan. Synthesis of escitalopram oxadate[J]. Chinese Journal of New Drugs, 2006, 15(2): 117-120
Authors:YAO Zhong-ke  KAN Li-juan
Affiliation:1 Department of Chemistry, Capital Normal University, Beijing 100037, China; 2 Institute of Zoology, Chinese Academy of Sciences, Beijing 100080, China
Abstract:Objective:To synthesize escitalopram oxalate. Methods:Starting from 5-cyanophthalide, escitalopram oxalate was prepared via several steps including nucleophilic addition, hydrolysis, chemical separation, cyclization and salt formation. Results:A total yield of escitalopram oxalate was 13. 6% . Conclusion:This easily manipulated synthetic process is worthy to have further pilot manufacture.
Keywords:escitalopram oxadate  selective serotonin reuptake inhibitor (SSRI)  antidepressant  synthesis
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