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[一种用于通过高效液相色谱法拆分胺类和醇类药物对映体的新型手性衍生试剂]

[A new chiral derivatizing reagent for the resolution of amine and alcohol drug enantiomers by HPLC].

作者信息

Zhou Y, Sun Z P

机构信息

National Institute for the Control of Pharmaceutical and Biological Products, Beijing.

出版信息

Yao Xue Xue Bao. 1991;26(9):701-4.

PMID:1821090
Abstract

A new chiral derivatizing reagent (s)-alpha-methoxybenzyl isocyanate (MIB) was prepared from (s)-(+)-mandelic acid with a practical method, and its ability of liquid chromatographic resolution for drug enantiomers by pre-column chiral derivatization was evaluated with racemic amphetamine and mexiletine as well as phenylpropanol. The operation is simple and rapid. Separation is good for the amine isomers, but poor for alcohols and extensive work remains to be done. The solution of derivatization was directly injected into the chromatograph. Conventional silica gel column was used with light petroleum as the mobile phase.

摘要

通过一种实用方法由(S)-(+)-扁桃酸制备了一种新型手性衍生试剂(S)-α-甲氧基苄基异氰酸酯(MIB),并以外消旋苯丙胺、美西律以及苯丙醇为对象,评估了其通过柱前手性衍生化实现药物对映体液相色谱分离的能力。该操作简单快速。对胺类异构体的分离效果良好,但对醇类的分离效果较差,仍有大量工作有待开展。衍生化溶液直接注入色谱仪。使用常规硅胶柱,以轻质石油为流动相。

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