盐酸吡格列酮的合成  

Synthesis of pioglitazone hydrochloride

作　　者：楼晨光[1] 高丽梅[1] 宋丹青[1] 

机构地区：[1]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

出　　处：《中国新药杂志》2005年第10期1187-1189,共3页Chinese Journal of New Drugs

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。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, ^1 H-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.

关 键 词：盐酸吡格列酮 药物合成 糖尿病 

分 类 号：R977.15[医药卫生—药品] R914.5[医药卫生—药学]