格隆溴铵合成方法的改进Improvement of synthetic method of glycopyrrolate
王钝,侯利珂,吴丽容,于鑫
WANG Dun1,HOU Li-ke1,WU Li-rong1,YU Xin2(1.College of Pharmaceutical Engineering
摘要(Abstract)：
目的改进格隆溴铵的合成方法。方法苯乙酮酸经格氏反应、酯化反应制得α-环戊基扁桃酸甲酯,再与N-甲基吡咯烷-3-醇经酯交换、季铵化反应制得格隆溴铵。结果与讨论合成的格隆溴铵总收率为13.9%,其结构经过熔点测定及1H-NMR、13C-NMR确证。
Objective To improve the synthetic method of glycopyrrolate.Methods Glycopyrrolate was synthesized from benzoylformic acid by Grignard reaction and esterification to give methyl cyclopentylglycolate,which was subjected to transesterification with N-methyl-3-pyrrolidinol and then quaternization with bromomethane.Results and Conclusions The desired product is obtained in overall yield of 13.9%.Its structure is confirmed by melting point and 1H-NMR,13C-NMR.
关键词(KeyWords)：
格隆溴铵;合成;苯乙酮酸
glycopyrrolate;synthesis;benzoylformic acid
基金项目(Foundation):
作者(Author):
王钝,侯利珂,吴丽容,于鑫
WANG Dun1,HOU Li-ke1,WU Li-rong1,YU Xin2(1.College of Pharmaceutical Engineering
DOI: 10.14066/j.cnki.cn21-1349/r.2012.02.013
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