多手性中心药物色谱拆分研究进展

Progress on Stereoselective Separation of Multichiral Compounds by Chromatography

多手性中心药物具有多个立体异构体,空间构型的差异导致异构体之间生物活性差异较大,多手性中心药物的手性分离分析仍然是一个巨大的挑战。关于单手性中心化合物手性分离分析的报道很多,而关于多手性中心药物的手性分离却非常少。本文总结了近年来关于多手性中心化合物色谱手性分离研究进展,主要包括HPLC、GC、毛细管电泳、超临界流体色谱及逆流色谱等在多手性药物分离分析中应用。

Drugs with more than one chiral center are usually involved with different stereo-specific isomers and big difference in bioactivity due to different stereo-chemical structure, its separation and analysis is still a great challenge. There are lots of reports about enantioseparation of racemate with one chiral center, however, only a small fraction number of papers about stereoselective separation of racemate with multiple chiral center are available. In this paper, stereoselective separation of racemate with more than one chiral center by various chromatographic techniques, including HPLC, GC, capillary electrophoresis, supercritical fluid chromatography and countercurrent chromatography are reviewed.