利用高速逆流色谱分离制备达托霉素

Preparation of daptomycin by high speed counter-current chromatography

达托霉素是一种重要的临床抗耐药菌抗生素,其分离纯化较困难。本文研究了利用高速逆流色谱法快速制备达托霉素纯品的方法。研究获得的两相系统为乙酸乙酯-正丁醇-水(2mmol/L TFA)(4:1:5 V/V),上相为固定相,下相为流动相。在该条件下通过高速逆流色谱收集纯化目标产物,并冻干后获得淡黄色的粉末,液相纯度大于95%。经UPLC-MS分析鉴定产物与达托霉素一致。该方法可以用于达托霉素纯品的快速制备。

Daptomycin is an anti-resistant antibiotics, which is difficult to separate from fermentation broth. In this paper, high speed counter-current chromatography （HSCCC） was applied to preparation of daptomycin. A biphasic solvent system composed of ethyl acetate-n-butanol-2mmol/L trifluoroacetie acid （4：1：5, volume ratio） was used. The top phase was chosen as the stationary phase, and the bottom phase was chosen as the mobile phase. The fractions purified and collected was analyzed by high-performance liquid chromatography. A pale yellow powder with purity above 95 percent was obtained through lyophilization. And the structure of fractions was identified by UPLC- MS Analysis as daptomycin.This method is convenient to obtain pure daptomycin.