动态拆分技术在手性药物及手性化合物制备中的应用
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Application of dynamic resolution technology in the preparation of chiral drugs and chiral compounds
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    摘要:

    动态拆分技术是获得单一手性化合物的一种主要途径,近几年得到了较为深入的研究。动态拆分技术是将拆分反应与现场消旋化反应相结合的技术。该技术的关键是在拆分反应进行的同时,通过现场发生的快速消旋化反应,使慢拆分反应的对映体完全消旋化,并通过快拆分反应转化另一(非)对映体的反应产物的过程。动态拆分技术在理论上可以获得产率100%的光学纯的单一对映异构体。通常说来,实现高效的动态拆分技术的关键在于找到合适的并能与拆分反应条件兼容的消旋化反应条件。本文概述了动态拆分技术(动态动力学拆分和动态热力学拆分)及其在手性药物制备中的应用实例。

    Abstract:

    Dynamic resolution technology is one of the main approaches to obtain the single chiral compounds and has attracted much research interest.Dynamic resolution technology combines the resolution with racemization in situ.The key feature of this technology is the rapid racemization in situ of the unreactive enantiomer in the resolution of the racemic substrates.In this way,all the substrates could be converted into a single product isomer with a 100% theoretical yield.Generally speaking,in order to achieve high efficiency,the key point is to find the appropriate recemization conditions which are compatible with the resolution conditions.The dynamic resolution technology including dynamic kinetic resolution and dynamic thermodynamic resolution is summarized in this review and the latest research progress as well as the application in preparation of chiral drugs and chiral compounds are also presented.

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引用本文

张艳艳,尤启冬.动态拆分技术在手性药物及手性化合物制备中的应用[J].中国药科大学学报,2011,42(1):1-8.
Cite:ZHANG Yan-yan, YOU Qi-dong. Application of dynamic resolution technology in the preparation of chiral drugs and chiral compounds[J]. J China Pharm Univ,2011,42(1):1-8.

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