“Dutch”拆分研究进展.pdfVIP

19 11 化 学 进 展 Vol.19No.11 2007 11 PROGRESS IN CHEMISTRY Nov., 2007 / Dutch0拆分研究进展 * 孙凤霞 付德才 于奕峰 郭军永 张丽丽 (河北科技大学 化学与制药工程学院 石家庄050018) 本 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 Dutch拆分 手性 反义拆分 第一代Dutch 拆分 第二代Dutch 拆分 + : O62113 4; O656 : A : 1005-281X(2007) 11-1746-08 Dutch Resolution * Sun Fengx ia Fu Decai Yu Yfi eng Guo Junyong Zhang Lili (College of Chemical andPharmaceutical Engineering, HebeiUniversity of Science andTechnology, Shijiazhuang 050018, China) Abstract Developments and mechanism of the first generation Dutch resolution, the second generation Dutch resolution and reverse Dutch resolution are reviewed. Diastereomeric crystallization canbe formed easily and rapidlywith highyield and nearly 100 ee in Dutch resolution. Members of the family resolving agents show the solid solution behavior inthe first generation Dutch resolution. Inthe secondgeneration Dutch resolution, nucleation inhibitorwidens the metastable zoneof diastereoisomers, andthe nucleationtemperatureof themore solublediastereomericsalt dropsmore than that of the less soluble diastereomeric salt. So the less soluble diastereomeric salt can crystallize easily. The application andoutlookof Dutch resolutionare presented in the endof this paper. Key words Dutch resolution; chirality;