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A process for the kinetic resolution of alcohols with one or more stereogenic centers

机译:具有一个或多个立体生成中心的醇的动力学拆分方法

摘要

The present invention relates to a process for the kinetic resolution of alcohols with one or more stereogenic centers. The present invention is in particular for the preparation of pharmaceutical active ingredients or crop protection agents applicable. In accordance with the invention, first racemic alcohols with fluorinated acylating agents transferred in racemic fluorinated carboxylic acid esters. Subsequently, by lipase-catalyzed reaction of the racemic fluorinated carboxylic acid ester with alcohols, the fluorous phase marking of the faster reacting enantiomer is canceled and that of the slower reacting enantiomer is maintained. Subsequently, the enantiomers by distribution between organic phase and fluorous phase extractively separated.
机译:本发明涉及具有一个或多个立体生成中心的醇的动力学拆分方法。本发明特别用于制备药物活性成分或适用的作物保护剂。根据本发明,首先将具有氟化酰化剂的外消旋醇转移到外消旋氟化羧酸酯中。随后,通过外消旋的氟化羧酸酯与醇的脂肪酶催化反应,反应较快的对映异构体的氟相标记被消除,反应较慢的对映异构体的氟相标记得以保持。随后,对映体通过在有机相和氟相之间的分布而萃取分离。

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