Metal-Free C-2-H Alkylation of Quinazolin-4-ones with Alkanes via Cross-Dehydrogenative Coupling
Metal-Free C-2-H Alkylation of Quinazolin-4-ones with Alkanes via Cross-Dehydrogenative Coupling
复制标题
喹唑啉-4-酮与烷烃通过交叉脱氢偶联进行无金属 C-2-H 烷基化
DOI：
10.1021/acs.orglett.9b00638
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发表时间：
2019-04-05
期刊：
影响因子：
5.2
通讯作者：
Zhang, San-Qi
中科院分区：
文献类型：
--
作者：
Mao, Shuai;Luo, Kaixiu;Zhang, San-Qi
报道了一种实用的喹唑啉-4-酮与简单非活性烷烃交叉偶联反应的方法。产物在温和的反应条件下，在室温下在短的反应时间内顺利形成。在喹唑啉-4-酮的贫电子C-2位形成了新的Csp（3）-Csp（2）键。该方法有可能成为高级合成中间体后期功能化的重要工具，并可能在药物化学中找到许多应用。
A practically useful approach for the cross-dehydrogenative coupling of quinazolin-4-one with simple nonactivated alkanes is reported. The products were smoothly formed under mild reaction conditions, within short reaction time at ambient temperature. The formation of new Csp(3)-Csp(2) bonds occurred at the electron-poor C-2 position of quinazolin-4-one. The approach has the potential to be an important tool for the late-stage functionalization of advanced synthetic intermediates and may find many applications in medicinal chemistry.