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Separation of enantiomers of drugs by capillary electrophoresis with permethyl-gamma-cyclodextrin as chiral solvating agent

机译：separation of enantiomers of drugs by capillary electrophoresis with permethyl-gamma-cyclodextrin as chiral solvating agent

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摘要

High-throughput screening is a promising new approach in analytical chemistry. Within the framework of an extended screening program (The German-Chinese Drug Screening Program), the enantioseparation of 86 drugs was investigated by capillary zone electrophoresis in the presence of the chiral solvating agent (CSA) octakis-(2,3,6-tri-O-methyl)-gamma-cyclodextrin (TM-gamma-CD). By this means, 15 drugs could be separated into enantiomeric pairs. Approximate measures for the degree of interaction (migration retardation factor, R-m) and for the degree of enantiomer recognition (migration separation factors, alpha(m)) revealed intriguing patterns that were compared with those found for native gamma-cyclodextrin (gamma-CD). Although there is a distinct influence of the analyte structure on the electrophoretic data, interpretation remains difficult. Most remarkably, permethylation of gamma-CD leads neither to a higher affinity nor to better chiral recognition, in contrast to the findings with alpha-CD.
机译：高通量筛选是分析化学中有希望的新方法。在扩展的筛选程序（德中药品筛选程序）的框架内，在手性溶剂化剂（CSA）octakis-（2,3,6-tri）存在下，通过毛细管区带电泳研究了86种药物的对映体分离-O-甲基）-γ-环糊精（TM-γ-CD）。通过这种方式，可以将15种药物分为对映体对。相互作用程度（迁移阻滞因子，Rm）和对映体识别程度（迁移分离因子，α（m））的近似量度显示出与天然γ-环糊精（γ-CD）相比有趣的模式。 。尽管分析物结构对电泳数据有明显的影响，但解释仍然很困难。最明显的是，与α-CD的发现相反，γ-CD的全甲基化既不会导致更高的亲和力也不会导致更好的手性识别。

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