固定化脂肪酶手性拆分2-芳基丙酸类药物研究进展

Research Progress on Chiral Resolution of 2-Arylpropionic Acids by Immobilized Lipase

2-芳基丙酸(2-APA)类药物是一类重要的非甾体抗炎药,临床研究证实2-APA类药物对映体之间在药效上存在较大差异,因此光学纯2-APA类药物疗效更好、安全性更高。固定化脂肪酶在手性制备2-APA类化合物上具有绿色环保、立体选择性强、催化活性高等优势,展现出极大的市场应用潜力。本文分别从布洛芬、萘普生及其衍生物的手性制备方面综述了国内外研究进展,并指明该领域中亟待解决的关键问题,以期为后续固定化脂肪酶应用于手性拆分2-APA类化合物提供参考。

2-arylpropionic acid(2-APA) drugs is an important class of non-steroidal anti-inflammatory drugs. It has confirmed that the therapeutic effect of the two enantiomers of 2-APA drugs has great differences in clinical treatment, so it has better efficacy and safety for optically pure 2-APA drugs. There are many advantages of green environment protection, good stereoselectivity and excellent catalytic activity for immobilized lipase in enantioseparation of 2-APA compounds,which shows great market application potential. In this paper, the latest progresses about the chiral preparation of ibuprofen, naproxen and their derivatives have been reviewed, and we point out the problems to be solved urgently in order to provide a little inspiration and reference for the chiral resolution of 2-APA compounds by immobilized lipase in the future.