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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。
The combination of cilastatin and imipenem has strong antimicrobial activity and is the drug of choice for the treatment of severe infections clinically. Cilastatin is a renal dehydrogenase inhibitor that inhibits imipenem metabolism in the kidney and enhances its efficacy. S - (+) - 2,2-dimethylcyclopropanecarboxylic acid (amide) is a key chiral intermediate in the synthesis of cilastatin drugs. There are various methods of preparation. This review summarizes the progress in the preparation of S - (+) - 2,2-dimethylcyclopropanecarboxylic acid by asymmetric synthesis and resolution from both chemical and biological aspects, and discusses its preparation And outlook.