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通过不对称转移氢化合成替诺福韦及其类似物。

The synthesis of tenofovir and its analogues via asymmetric transfer hydrogenation.

机构信息

Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, School of Chemistry and Chemical Engineering, Henan Normal University , Xinxiang, Henan 453007, P. R. China.

出版信息

Org Lett. 2014 Apr 4;16(7):2014-7. doi: 10.1021/ol500583d. Epub 2014 Mar 20.

DOI:10.1021/ol500583d
PMID:24650095
Abstract

A series of tenofovir analogues with potential antiviral and immunobiologically active compounds were synthesized through an asymmetric transfer hydrogenation reaction from achiral purine derivatives. Up to 97% ee and good to excellent yields were achieved under mild conditions through short reaction steps. The present report suggests an efficient process to acquire tenofovir and its analogues.

摘要

通过手性嘌呤衍生物的不对称转移氢化反应,合成了一系列具有潜在抗病毒和免疫生物活性的替诺福韦类似物。在温和的条件下,通过短的反应步骤,可获得高达 97%的对映体过量值和良好至优异的产率。本报告提出了一种获得替诺福韦及其类似物的有效方法。

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