C2-Benzylic C(sp 3 )–H Alkylation of Indoles Enabled by Photoinduced, EDA-Complex-Mediated Radical–Radical Cross-Coupling

作者：Yingying Hu, Zhilin Liu, Hao‐Yue Xiang, Xiaoqing Chen, Kai Chen, Hua Yang · 发表于：Organic Letters · 年份：2025 · DOI：10.1021/acs.orglett.5c03141 · 被引用次数：4 · 研究领域：Radical Photochemical Reactions、Catalytic C–H Functionalization Methods、Fluorine in Organic Chemistry

2-Alkylindoles are privileged motifs that serve as versatile intermediates and building blocks in synthetic and medicinal chemistry. Herein, we report a photoinduced, EDA-complex-enabled C2-benzylic C(sp 3 )–H alkylation of indoles with bromides through radical cross-coupling. This developed protocol provides facile access to 2-alkylindoles from structurally varied 2-methylindoles and bromides under mild reaction conditions with simple operation. Mechanistically, the well-designed EDA complex by rationally leveraging π-electron-rich indole and electron-deficient halide and electronically matched radical cross-coupling is crucial to the success of this new open-shell methodology in the functionalization of indoles.