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Visible-light-mediated Minisci C–H alkylation of heteroarenes with unactivated alkyl halides using O2 as an oxidant†‡
Chemical Science ( IF 8.4 ) Pub Date : 2018-11-27 00:00:00 , DOI: 10.1039/c8sc04892d
Jianyang Dong 1 , Xueli Lyu 1 , Zhen Wang 1 , Xiaochen Wang 1 , Hongjian Song 1 , Yuxiu Liu 1 , Qingmin Wang 1, 2
Affiliation  

Herein, we report a protocol for direct visible-light-mediated Minisci C–H alkylation of heteroarenes with unactivated alkyl halides using molecular oxygen as an oxidant at room temperature. This mild protocol is compatible with a wide array of sensitive functional groups and has a broad substrate scope. Notably, functionalization of (iso)quinolines, pyridines, phenanthrolines, quinazoline, and other heterocyclic compounds with unactivated primary, secondary, and tertiary alkyl halides proceeds smoothly under the standard conditions. The robustness of this protocol is further demonstrated by the late-stage functionalization of complex nitrogen-containing natural products and drugs.

中文翻译:

使用 O2 作为氧化剂,用未活化的卤代烷对杂芳烃进行可见光介导的 Minisci C-H 烷基化†‡

在此,我们报告了一种在室温下使用分子氧作为氧化剂,用未活化的卤代烷对杂芳烃进行直接可见光介导的 Minisci C-H 烷基化的方案。这种温和的方案与多种敏感官能团兼容,并且具有广泛的底物范围。值得注意的是,(异)喹啉、吡啶、菲咯啉、喹唑啉和其他杂环化合物与未活化的伯、仲和叔烷基卤化物的官能化在标准条件下顺利进行。复杂的含氮天然产物和药物的后期功能化进一步证明了该协议的稳健性。
更新日期:2018-11-27
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