一种实用且高效的路线，用于美西律类似物以及新型β-噻吩氧基和吡啶基醚的高对映选择性合成。
A practical and efficient route for the highly enantioselective synthesis of mexiletine analogues and novel beta-thiophenoxy and pyridyl ethers.
作者信息
Huang Kun, Ortiz-Marciales Margarita, Stepanenko Viatcheslav, De Jesús Melvin, Correa Wildeliz
机构信息
Department of Chemistry, University of Puerto Rico-Humacao, CUH Station, Humacao, Puerto Rico.
出版信息
J Org Chem. 2008 Sep 5;73(17):6928-31. doi: 10.1021/jo801181d. Epub 2008 Aug 9.
Abstract
A practical and efficient procedure for the enantioselective synthesis of mexiletine analogues with use of 10% of spiroborate ester 6 as chirality transfer agent is presented. A variety of mexiletine analogues were prepared in good yield with excellent enantioselectivities (91-97% ee) from readily available starting materials. The developed methodology was also successfully applied for the synthesis of novel beta-amino ethers containing thiophenyl and pyridyl fragments.
摘要
本文介绍了一种实用且高效的方法，该方法使用10%的螺硼酸酯6作为手性转移剂对美西律类似物进行对映选择性合成。以容易获得的起始原料，以良好的收率和优异的对映选择性（91-97% ee）制备了多种美西律类似物。所开发的方法也成功应用于含噻吩基和吡啶基片段的新型β-氨基醚的合成。
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