制备S-(+)-2,2-二甲基环丙烷甲酸的研究进展  

Research progress on preparation of S-(+)-2,2-dimethylcyclopropanecarboxylic acid

作　　者：刘婧[1] 黄金[1] 钟成刚[1] 何军邀[1,2] 王普[1] 

机构地区：[1]浙江工业大学药学院,浙江杭州310032 [2]浙江医药高等专科学校,浙江宁波315100

出　　处：《齐鲁药事》2012年第5期283-286,共4页qilu pharmaceutical affairs

基　　金：浙江省科技厅重大科技攻关项目(2010C11040);浙江省级公益性技术应用研究计划项目(2011C33005);浙江省教育厅科研项目(Y201018521)

摘　　要：西司他丁与亚胺培南制成的复合剂泰能具有极强的广谱抗菌活性,是目前临床上治疗重症感染的首选药。西司他丁是肾脱氢二肽酶抑制剂,可以抑制亚胺培南在肾内的代谢,并增强其药效。S-(+)-2,2-二甲基环丙烷甲酸(酰胺)是合成西司他丁药物的关键手性中间体,目前有多种制备方法。本文主要从化学法和生物法两方面综述了通过不对称合成与拆分的方法制备S-(+)-2,2-二甲基环丙烷甲酸的研究进展,并对其制备方法进行了讨论和展望。Imipenem and cilastatin - tienam has a strong broad - spectrum antibacterial activity and has become the pref- erreddrug for clinical treatment of severe infections at present. Cilastatin functioning as an inhibitor of dehydropeptidase - I can inhibit the metabolism of imipenem and reinforce its effecfiveness in kidney. S - （ ＋ ） - 2,2 - dimethylcyclopropanecarboxylic acid （ amide ） is an important intermediate for the production of cilastatin and can be synthesized by various methods at present. Research progress in asymmetric synthesis and resolution by chemical catalysis and biocatalysis for the preparation of S - （ ＋ ） - 2,2 -dimethylcyclopropanecarboxylic acid was reviewed in this paper. The prospect of preparation methods of S- （ ＋ ） -2,2 - dimethylcyclopropanecarboxylic acid was also discussed and summaried.

关 键 词：西司他丁 S-(+)-2 2-二甲基环丙烷甲酸 不对称合成 拆分 

分 类 号：R914.5[医药卫生—药物化学]