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R-(+)-兰索拉唑的合成研究
引用本文:杜有国,宗在伟,陈祥峰.R-(+)-兰索拉唑的合成研究[J].化工时刊,2010,24(7):17-18,24.
作者姓名:杜有国  宗在伟  陈祥峰
作者单位:江苏奥赛康药业有限公司,江苏,南京,211112
摘    要:2-氯甲基-3-甲基-4-(2,2,2-三氟乙氧基)吡啶盐酸盐经缩合兰索啦唑硫醚,再经不对称氧化制得R-兰索拉唑,粗品经纯化得到化学纯度99.6%,光学纯度99.8%的目标产物,总收率37.9%。反应条件温和,适合工业化生产。目标产物经元素分析、质谱、核磁共振及红外确认结构。

关 键 词:R-(+)-兰索拉唑  质子泵抑制剂  不对称氧化  合成

The Synthesis of R-(+)-lansoprazole
Du Youguo,Zong Zaiwei,Chen Xiangfeng.The Synthesis of R-(+)-lansoprazole[J].Chemical Industry Times,2010,24(7):17-18,24.
Authors:Du Youguo  Zong Zaiwei  Chen Xiangfeng
Affiliation:Du Youguo Zong Zaiwei Chen Xiangfeng (Jingsu Aosaikang Pharmaceutical CO. , LTD. Jiangsu Nanjing 211112)
Abstract:R - ( + ) - lansoprazole was synthesized from 2 - Chloromethyl - 3 - methyl - 4 - (2,2,2 - trifluoroethoxy) pyri - dine hydrochloride by condensation and asymmetric oxidation. By purifying, chemical purity of the product was 99.6% , optical purity was 99.8% , and with an overall yield of 37.9%. This synthetic process was under mild reactive conditions and with cheaper raw material. The process was suitable for industrial producing. The structure of R - ( + ) lansop - razole was confirmed by MS, ^1H - NMR, ^13 C - NMRand IR.
Keywords:R - ( + ) -lansoprazole proton pump inhibitor asymmetric oxidation synthesis
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