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Separation of twelve posaconazole related stereoisomers by multiple heart-cutting chiral-chiral two-dimensional liquid chromatography.
Journal of Chromatography A ( IF 3.8 ) Pub Date : 2020-01-02 , DOI: 10.1016/j.chroma.2019.460845
Feng Xu 1 , Yao Xu 2 , Guizheng Liu 3 , Meng Zhang 3 , Shangshang Qiang 2 , Jingwu Kang 3
Affiliation  

Posaconazole represents a triazole antifungal agent which is used to treat various fungal infections. It contains four chiral centers leading to 16 stereoisomers. With the convergent synthesis route, only 11 related stereoisomeric impurities may potentially exist in the active pharmaceutical ingredient (API). It is a challenge to separate all the stereoisomers in one run. To address this problem, a multiple heart-cutting chiral-chiral two-dimensional liquid chromatography (2D-LC) method was developed. The multiple heart-cutting 2D-LC separation was implemented on 2D-LC system with three chiral columns with immobilized polysaccharide chiral stationary phases, namely Chiralpak IB, IC and IF3. In the system, the column Chiralpak IB was used as the 1D separation column and IC and IF3 columns were used parallelly for the 2D separation. The twelve stereoisomers were all well separated in one run by the multiple heart-cutting chiral-chiral 2D-LC system.

中文翻译:

通过多次心脏切割手性-手性二维液相色谱分离十二种泊沙康唑相关的立体异构体。

泊沙康唑代表用于治疗各种真菌感染的三唑抗真菌剂。它包含四个手性中心,形成16个立体异构体。通过收敛的合成路线,活性药物成分(API)中可能仅存在11种相关的立体异构杂质。一次运行分离所有立体异构体是一项挑战。为了解决这个问题,开发了多切心手性-手性二维液相色谱法(2D-LC)。在具有三个固定有多糖手性固定相的手性柱的手性色谱柱的二维液相色谱系统上进行了多次心脏切割二维液相色谱分离,分别为Chiralpak IB,IC和IF3。在系统中,Chiralpak IB色谱柱用作一维分离柱,而IC和IF3色谱柱则并行用于2D分离。
更新日期:2020-01-02
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