Novel Synthesis of Antiobesity Drug Lorcaserin Hydrochloride
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- 作者：Qihua Zhu ; Junwei Wang ; Xueguo Bian ; Lingzhi Zhang ; Ping Wei ; Yungen Xu
- 刊名：Organic Process Research & Development
- 出版年：2015
- 出版时间：September 18, 2015
- 年：2015
- 卷：19
- 期：9
- 页码：1263-1267
- 全文大小：286K
- ISSN：1520-586X
文摘
A novel synthesis of antiobesity drug lorcaserin hydrochloride was accomplished in six steps. N-protection of 2-(4-chlorophenyl)ethanamine with di-tert-butyl dicarbonate, N-alkylation with allyl bromide, deprotection, intramolecular Friedel鈥揅rafts alkylation, chiral resolution with l-(+)-tartaric acid, and the final salification led to the target molecule lorcaserin hydrochloride in 23.1% overall yield with 99.9% purity and excellent enantioselectivity (>99.8% ee). This convenient and economical procedure is remarkably applicable for scale-up production.