光学活性棉酚衍生物的拆分及性质测定

Resolution of the optical active derivatives of gsssypol and the determination of its configuration

目的分离棉酚光学异构体。方法以L-(-)-1-(对硝基苯基)-1,3-二羟基丙胺-2为手性衍生化试剂,与消旋棉酚衍生化后生成一对非对映异构体,用常压柱色谱分离。结果棉酚消旋体经衍生化后,色谱图显示在tR=5.5min及tR=7.1min处有峰面积比为1∶1的两个色谱峰,分离度3.8。左旋棉酚衍生物在tR=5.5min处有单个色谱峰,右旋棉酚衍生物在tR=7.1min处有单个色谱峰。结论间接法—手性衍生化法可对棉酚衍生物进行拆分及性质测定,操作简单、重现性好。

[Objective] To separate enantiomers of gossypol. [Methods] L-threo（-）-1-（p-nitophenyl）-1, 3- dihydroxy propylamine-2 was found to be a useful resolving agent for racemic gossypol. In this paper column chromatography was used to separate enantiomer gossypols. [Results] The final product is identified by HPLC, IR,NMR,Melting point and optical rotation. [Conclusion] The method is simple and reproducible.