手性药物拆分技术研究进展.pdf

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Chinese Journal of New Drugs 2005 ,Vol. 14 No. 8 中国新药杂志 2005 年第 14 卷第 8 期
手性药物拆分技术研究进展
李根容,李志良
(重庆大学化学化工学院,重庆 400044)
[摘要] 对外消旋体进行拆分是获得手性药物的重要方法。综述了手性拆分方法及其分类,分别为结晶拆分
法,包括直接结晶法、形成非对映体的结晶法、组合拆分法等;复合和包合拆分法,包括包结拆分法;色谱拆分法等,
并结合一些药物对新近发展起来的手性药物拆分技术做了介绍。
[关键词] 手性拆分;异构体;消旋体;复合和包结拆分;色谱拆分 2
[中图分类号] R914 5 ;R927 [文献标识码] A [文章编号] 1003 - 3734(2005) 08 - 0969 - 06
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Advances in the chiral drug resolutions
LI Gen rong , LI Zhi liang
( College of Chemistry and Chemical Engineering , Chongqing University , Chongqing 400044 , China)
[ Abstract ] Significant progresses in developing the techniques of chiral resolution offer possibilities in
the preparation of new pounds. This article reviews the methodology and classification of raceme
resolutions , including direct crystallization (spontaneous resolution , preferential crystallization , combinational
resolution and converse resolution) , inclusion resolution and chromatography. The direct crystallization is
currently the most popular due to its simplicity and easy manipulation. New technologies using chromatographic
resolution , combinational resolution and inclusion resolution may be expected to promote the development of
more effective chiral drugs.
[ Key words ] chiral resolution ; isomer ; raceme ; complex and inclusion resolution ; chromatographic
resolution
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