Direct C2-Alkylation of Azoles with Alcohols and Ethers through Dehydrogenative Cross-Coupling under Metal-Free Conditions
Direct C2-Alkylation of Azoles with Alcohols and Ethers through Dehydrogenative Cross-Coupling under Metal-Free Conditions
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DOI：
10.1021/ol201779n
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发表时间：
2011-10-07
期刊：
影响因子：
5.2
通讯作者：
Wang, Min
中科院分区：
文献类型：
--
作者：
He, Tao;Yu, Lin;Wang, Min
基于氧化C-H活化过程，开发了一种无金属的新颖、简单且高效的唑类与醇和醚直接C2烷基化方法。醇和醚中的α位sp(3) C-H与唑类中的2位sp(2) C-H的脱氢C-C交叉偶联反应在叔丁基过氧化氢(TBHP)存在下在纯净的反应条件下顺利进行，并以良好的收率生成了相应的产物。
A metal-free novel, simple, and highly efficient method for the direct C2-alkylation of azoles with alcohols and ethers has been developed on the basis of an oxidative C-H activation process. The dehydrogenative C-C cross-coupling reactions of alpha-position sp(3) C-H in alcohols and ethers with the 2-position sp(2) C-H in azoles proceeded smoothly in the presence of tert-butyl hydroperoxide (TBHP) under neat reaction conditions, which generated the corresponding products in good yields.