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化学进展 2007, Vol. 19 Issue (11): 1746-1753 前一篇   后一篇

• 综述与评论 •

“Dutch”拆分研究进展

孙凤霞* 付德才 于奕峰 郭军永 张丽丽   

  1. (河北科技大学 化学与制药工程学院 石家庄 050018)
  • 收稿日期:2007-01-08 修回日期:2007-04-17 出版日期:2007-11-14 发布日期:2007-11-25
  • 通讯作者: 孙凤霞

Dutch Resolution

Sun Fengxia*;Fu Decai; Yu Yifeng; Guo Junyong; Zhang Lili   

  1. (College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology,Shijiazhuang 050018, China)
  • Received:2007-01-08 Revised:2007-04-17 Online:2007-11-14 Published:2007-11-25
  • Contact: Sun Fengxia
本文综述了第一代Dutch拆分、第二代Dutch拆分及反义Dutch拆分的拆分机理和研究进展,并展望了Dutch拆分的应用前景。Dutch拆分能以高收率和近于100%ee值与所有的实验消旋体迅速形成非对映体的结晶。第一代Dutch拆分中Family拆分试剂在形成非对映体晶体过程是典型的固溶体行为。在第二代Dutch拆分中,成核抑制剂改变了非对映异构体的亚稳区宽度,溶解度较大的非对映体盐比溶解度较小的非对映体盐的结晶温度下降得更多,使溶解度较小的非对映体盐更容易析出。
Developments and mechanism of the first generation Dutch resolution, the second generation Dutch resolution and reverse Dutch resolution are reviewed. Diastereomeric crystallization can be formed easily and rapidly with high yield and nearly 100% ee in Dutch resolution. Members of the family resolving agents show the solid solution behavior in the first generation Dutch resolution. In the first generation Dutch resolution, nucleation inhibitor widens the metastable zone of diastereoisomers, and the nucleation temperature of the more soluble diastereomeric salt drops more than that of the less soluble diastereomeric salt. So the less soluble diastereomeric salt can crystallize easily. The application and outlook of Dutch resolution are presented in the end of this paper.

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摘要

“Dutch”拆分研究进展