Copper-Mediated C4-H Sulfonylation of Indoles via a Transient Directing Group Strategy
Ming-Shun Mei1, Fanyi Meng1, Junhao Tang1
1School of Chemical Science and Engineering, Tongji University, Shanghai 200092, China.
None:
The synthesis of C4-decorated indoles is of great significance in the construction of bioactive and functional molecules. Currently, the late-stage C4-H functionalization of indole scaffolds largely relies on toxic and expensive 4d/5d transition metal catalysts and preinstalled directing groups, which considerably limits their practical applications. In this work, we report a copper-mediated C4-H sulfonylation of indoles via a transient directing group strategy. This method features high atom- and step-economy, outstanding regioselectivity, and broad functional group compatibility, providing a novel and practical solution for the C4-functionalization of indole cores.
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