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Copper-Catalyzed Aerobic Selective Oxidation of Tetrahydrocarbolines.

Jun ShiRui-An WangWei WuJun-Rong SongQin ChiWei-Dong PanHai Ren
Published in: Organic letters (2022)
We report a safe and convenient open-flask copper-catalyzed selective oxidation/functionalization methodology for tetrahydrocarbolines and tetrahydro-β-carbolines that employs atmospheric O 2 as the terminal oxidant. The system is applicable to oxidative rearrangement of tetrahydro-β-carbolines, tetrahydrocarboline oxidation to α-alkoxy carbazoles and spirooxindoles, and Witkop oxidation. Mechanistic experiments indicated that a single-electron oxidation process is responsible for the tunable selectivity control. This copper-catalysis protocol represents a significant advance in the field of indole oxidation.
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