第 40 卷第 2 期Vol. 40 No. 2
2010 年 4 月Apr 2010

所属栏目:医药及中间体

甘氨熊去氧胆酸的合成
龚启明,欧阳贵平 (贵州大学 精细化工研究开发中心,贵州 贵阳 550025)
摘 要:以熊去氧胆酸为原料,先与氯甲酸乙酯形成混酐,再与甘氨酸乙酯反应合成甘氨熊去氧胆酸乙酯,最后水解得到甘氨熊去氧胆酸,产物结构经过IR、1H NMR确证。使用了廉价试剂,优化了合成方法,收率达到90.2%。
关键词:熊去氧胆酸;甘氨熊去氧胆酸;氯甲酸乙酯;甘氨酸乙酯;合成
中图分类号:R975+.5  文献标识码:A  文章编号:1009-9212(2010)02-0030-02
Synthesis of Glycoursodeoxycholic Acid
GONG Qi-ming,OUYANG Gui-ping (Center for Research and Development of Fine Chemicals,Guizhou University,Guiyang 550025,China)
Abstract:Glycoursodeoxycholic acid could be synthesized in an overall yield of 90.2% by the following procedures. Firstly,a mixed anhydride of ursodeoxycholic acid and ethyl chloroformate was synthesized. Secondly,reaction of the anhydride with ethyl glycinate hydrochloride afforded the ethyl ester of the ursodeoxycholic acid. Finally,hydrolysis of the ester in ethanolic sodium hydroxide produced the title compound. The product was confirmed with IR and 1H NMR.
Key words:ursodeoxycholic acid;glycoursodeoxycholic acid;ethyl chloroformate;ethyl glycinate;synthesis
基金项目:贵州大学人才科研项目基金资助(2008040)。
作者简介:龚启明(1987-),男,江苏靖江人,硕士研究生,研究方向:有机合成化学。
联 系 人:欧阳贵平,研究员。(E-mail:oygp710@163.com)
收稿日期:2010-03-15