米格列奈钙二水合物的合成  

Synthesis of mitiglinide calcium salt dihydrate

作　　者：高丽梅[1] 李迎红[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11期1316-1318,共3页Chinese Journal of New Drugs

摘　　要：目的:合成米格列奈。方法:以丁二酸二乙酯和苯甲醛为原料,经Stobble缩合、水解、还原、成盐、酸化、酰化、酰化、水解、成盐等9步反应得到米格列奈。结果:目标化合物经核磁共振氢谱、质谱及红外等确证其化学结构,总收率为9%。结论:本路线操作简单,成本低。Objective： To synthesize mitiglinide. Methods： Starting from diethyl succinate and benzaldehyde, mitiglinide was obtained via 9 chain steps including Stobble condensation, hydrolyzation, reduction, salt formation, acidification, two acylations, hydrolyzation and salt formation. Results： The structure of mitiglinide was verified by ^1H-NMR, MS and IR. The total yield of mitiglinide was 9%. Conclusion： A simple, easily manipulated and cost saving process for the synthesis of mitiglinide was attainable.

关 键 词：米格列奈 药物合成 促胰岛素分泌剂 

分 类 号：R914.5[医药卫生—药物化学] R972.4[医药卫生—药学]