西司他丁钠的合成  

Systhesis of Cilastatin sodium

作　　者：欧阳罗[1] 陈瑞业[1] 柏一慧[1] 李新生[1] 徐东成[1] 

机构地区：[1]浙江师范大学化学与生命科学学院,浙江金华321004

出　　处：《浙江师范大学学报（自然科学版）》2011年第3期317-322,共6页Journal of Zhejiang Normal University:Natural Sciences

基　　金：浙江省科技厅科研项目(2008C21041)

摘　　要：(R)-1,1′-联萘酚((R)-BINOL)与2,2-二甲基环丙烷甲酰氯反应,高收率地得到2个非对映体单酯,柱色谱分离出单一对映体,氨解得到光学纯的S构型的2,2-二甲基环丙烷甲酰胺;半胱氨酸甲酯盐酸盐和7-氯-2-((1S)-2,2-二甲基环丙烷甲酰胺)-2-庚烯酸乙酯在不同的条件下反应,得到了合成西司他丁钠的较优路线.（S）-2,2-dimethylcyclopropane carboxamide was prepared by ammonification of the corresponding chiral BINOL monoester,which was obtained by resolution of the diastereomeric with column chromatography.The reaction of the amide and 7-chloro-2-oxoheptanoate gave the enamide ester,which reacted with cysteine ester under different conditions,including different solvents,bases,ratio of the substrates and reaction temperature.An effective method for synthesis of Cilastatin sodium with good yield under mild condition was developed.

关 键 词：西司他丁钠 2 2-二甲基环丙烷甲酰胺 联萘酚单酯 合成 拆分 

分 类 号：R914.5[医药卫生—药物化学]