Abstract：
An efficient method for the continuous separation of Voriconazole enantiomers was developed using sulfobutyl ether-β-cyclodextrin (SBE-β-CD) as a chiral selector in high-speed countercurrent chromatography (HSCCC) with different types. The separation was performed using a two-phase solvent system consisting of n-hexane/ethyl acetate/100 mmol/L phosphate buffer solution (pH = 3.0, containing 50 mmol/L SBE-β-CD) (1.5:0.5:2, v/v/v). A fast and predictable scale-up process was achieved using an analytical DE HSCCC instrument. The optimized parameters were subsequently applied to a preparative Tauto HSCCC instrument, resulting in consistent separation time and enantiomeric purity, with throughput boosted by a remarkable 11-fold. Preparative HSCCC successfully separated 506 mg of the racemate, delivering enantiomers exceeding 99% purity as confirmed by high-performance liquid chromatography analysis. This investigation presents an effective methodology for forecasting the HSCCC scale-up process and attaining continuous separation of chiral drugs.
摘要：
在不同类型的高速逆流色谱（HSCCC）中，使用磺丁基醚-β-环糊精（SBE-β-CD）作为手性选择剂，开发了一种连续分离伏立康唑对映体的有效方法。使用由正己烷/乙酸乙酯/100mmol/L磷酸盐缓冲溶液(pH=3.0,含有50mmol/LSBE-β-CD)(1.5:0.5:2,v/v/v)组成的两相溶剂系统进行分离。使用分析DEHSCCC仪器实现了快速且可预测的放大过程。随后将优化的参数应用于制备型TautoHSCCC仪器，导致一致的分离时间和对映体纯度，吞吐量提高了11倍。制备HSCCC成功分离出506mg的外消旋体，提供超过99％纯度的对映异构体，如高效液相色谱分析所证实。这项研究提供了一种有效的方法来预测HSCCC的放大过程并实现手性药物的连续分离。
