Catalyst-free C–H methylation of heteroarenes enabled by electron donor–acceptor complex photoactivation†

Jiayang Wang , Baoer Shao , Haixia Ge , Huiyu Xue , Xiangyuan Ding , Yuqi Li , Peiyao Sheng
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Abstract

An efficient, additive- and catalyst-free, visible-light-driven radical C–H methylation of heteroarenes (including quinoxalinones, pyrazinones, quinolinones and coumarins) utilizing readily available methylamines as the methyl source has been developed. The transformation possesses the advantages of operational simplicity, mild reaction conditions and broad substrate scope. Mechanistic studies disclosed that a photoactive electron donor–acceptor (EDA) complex between methylamines and heteroarenes is crucial to this transformation.

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电子供体-受体复合物光活化催化杂环烯的无催化剂 C-H 甲基化反应
我们开发了一种高效、无添加剂和催化剂、可见光驱动的杂环戊烯(包括喹喔啉酮类、吡嗪酮类、喹啉酮类和香豆素类)自由基 C-H 甲基化反应,利用现成的甲基胺作为甲基源。这种转化方法具有操作简单、反应条件温和、底物范围广等优点。机理研究表明,甲胺和杂环戊烯之间的光活性电子供体-受体(EDA)复合物对这一转化至关重要。
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