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盐酸吡格列酮的合成
引用本文:楼晨光,高丽梅,宋丹青.盐酸吡格列酮的合成[J].中国新药杂志,2005,14(10):1187-1189.
作者姓名:楼晨光  高丽梅  宋丹青
作者单位:中国医学科学院中国协和医科大学医药生物技术研究所,北京,100050
摘    要:目的:合成盐酸吡格列酮.方法:以2-(5-乙基-2-吡啶基)乙醇(5-EPE)为起始原料,经缩合、还原、重氮化、环化、水解及成盐等6步反应得到盐酸吡格列酮.结果:目标化合物经质谱、核磁共振氢谱、红外光谱及X-单晶衍射等确证其化学结构,总收率为12.8%.结论:本路线可简化实验操作,降低成本,适合工业化生产.

关 键 词:盐酸吡格列酮  药物合成  糖尿病
文章编号:1003-3734(2005)10-1187-03
收稿时间:2005-03-24
修稿时间:2005-03-24

Synthesis of pioglitazone hydrochloride
LOU Chen-guang,GAO Li-mei,SONG Dan-qing.Synthesis of pioglitazone hydrochloride[J].Chinese Journal of New Drugs,2005,14(10):1187-1189.
Authors:LOU Chen-guang  GAO Li-mei  SONG Dan-qing
Institution:Institute of Medicinal Biotechnology, China Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Abstract:Objective:To synthesize pioglitazone hydrochloride.Methods: The target compound was synthesized from 2-(5-ethyl-2-pyridyl)-ethanol as a starting material via six steps including condensation,reduction,diazotization,cyclization,hydrolysis and saltilization.Results: The structure of the target compound was confirmed by MS,()~1H-NMR,IR and X-ray crystal analysis.The total yield of pioglitazone hydrochloride was 12.8%.Conclusion: This cost-saving and simplified method can be used in the industrial manufacture.
Keywords:pioglitazone hydrochloride  synthesis  diabetic disease
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