刘文强, 李莉. 手性药物及其中间体拆分方法的研究进展J. 药学学报, 2018,53(1): 37-46. doi: 10.16438/j.0513-4870.2017-0616
引用本文: 刘文强, 李莉. 手性药物及其中间体拆分方法的研究进展J. 药学学报, 2018,53(1): 37-46. doi: 10.16438/j.0513-4870.2017-0616
LIU Wen-qiang, LI Li. Research progress of resolution of chiral drugs and their synthetic intermediatesJ. Acta Pharmaceutica Sinica, 2018,53(1): 37-46. doi: 10.16438/j.0513-4870.2017-0616
Citation: LIU Wen-qiang, LI Li. Research progress of resolution of chiral drugs and their synthetic intermediatesJ. Acta Pharmaceutica Sinica, 2018,53(1): 37-46. doi: 10.16438/j.0513-4870.2017-0616

手性药物及其中间体拆分方法的研究进展

Research progress of resolution of chiral drugs and their synthetic intermediates

  • 摘要: 与手性药物的外消旋体相比,单一光学异构体往往具有更强的选择性和较低的不良反应,已成为药物研发的热点。尽管不对称合成方法学研究蓬勃发展,手性拆分仍是获取手性药物的重要途径。本文重点介绍了手性药物及中间体拆分方法的最新研究进展,包括结晶拆分、化学拆分、动力学拆分等。将拆分与外消旋化过程结合,提高拆分效率,已成为手性拆分方法发展的趋势。此外,还介绍了手性萃取、膜拆分、纳米粒拆分等方法。

     

    Abstract: Compared with the racemate of chiral drugs, enantiopure chiral drugs have been the hot spot of drug research because of their higher selectivity and lower side-effects. Although remarkable progress of asymmetric synthesis has been achieved in the last decades, chiral resolution is regarded as an important approach to obtain chiral drugs. Recent research advancements in the field of chiral resolution of racemic drugs and intermediates are reviewed here. It is clear that combination of chiral separation and racemization to improve the resolution efficiency has become a trend of chiral resolution. In addition, we also introduce some novel resolution methods, such as chiral extraction, membrane resolution, and resolution using nanoparticles.

     

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