• 首页期刊简介编委会刊物订阅专栏专刊电子刊广告合作联系我们English
引用本文:何光超,王均伟,管哲,朱启华,徐云根.盐酸绿卡色林的工艺研究[J].中国现代应用药学,2019,36(9):1067-1070.
HE Guangchao,WANG Junwei,GUAN Zhe,ZHU Qihua,XU Yungen.Practical Synthesis of Lorcaserin Hydrochloride[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(9):1067-1070.
【打印本页】   【HTML】   【下载PDF全文】   查看/发表评论  【EndNote】   【RefMan】   【BibTex】
←前一篇|后一篇→ 过刊浏览    高级检索
本文已被:浏览 2155次   下载 863 本文二维码信息
码上扫一扫!
分享到: 微信 更多
盐酸绿卡色林的工艺研究
何光超, 王均伟, 管哲, 朱启华, 徐云根
中国药科大学药学院, 南京 210009
摘要:
目的 研究减肥药盐酸绿卡色林(1)的合成工艺。方法N-烯丙基-N-[2-(4-氯苯基)乙基]氨基甲酸叔丁酯(3)为原料,经一步反应同时实现分子内的傅-克烷基化反应和脱Boc保护基反应,再经L-(+)-酒石酸手性拆分和成盐制备得到1结果 合成工艺总收率为24.7%,化学纯度为99.9%,光学纯度ee值>99.8%。各中间体和目标产物经1H NMR、13C NMR、ESI-MS表征。结论 所研制的合成工艺路线操作简便、经济实用,适合工业化生产。
关键词:  盐酸绿卡色林  合成工艺  减肥药
DOI:10.13748/j.cnki.issn1007-7693.2019.09.007
分类号:R914
基金项目:江苏省产学研前瞻性联合研究项目(BY2015072-02)
Practical Synthesis of Lorcaserin Hydrochloride
HE Guangchao, WANG Junwei, GUAN Zhe, ZHU Qihua, XU Yungen
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
Abstract:
OBJECTIVE To study the synthetic process of antiobesity drug lorcaserin hydrochloride(1). METHODS 1 was synthesized form N-allyl-N-[2-(4-chlorobenyl)ethyl]tert-butyl carbamate(3) in a three-step process via one-step intramolecular Friedel-crafts alkylation and deprotection, chiral resolution with L-(+)-tartaric acid, and the final salification. RESULTS In overall yield was 24.7% the purity was 99.9%, and excellent enantioselectivity(ee) >99.8%. The intermediates and target product were confirmed by 1H NMR, 13C NMR and ESI-MS. CONCLUSION This convenient and economical procedure is remarkably applicable for industry.
Key words:  lorcaserin hydrochloride  synthesis process  antiobesity drug
扫一扫关注本刊微信