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Updated: Jan 18, 2026

A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
Published on: January 21, 2020
Catálisis de Paladio(II) para la Aciloxilación Directa en C7 de Indoles
Xianyu Zhang1, Jingwen Wang1, Shengrong Chen1
1State Key Laboratory of Photocatalysis on Energy and Environment, College of Chemistry, Fuzhou University, Fuzhou 350116, China.
Abstract:
We report a palladium-catalyzed C-H acyloxylation of indoles that achieves excellent regioselectivity at the C7 position. The synergistic combination of a methylsulfonyl directing group and a pyridone-based ligand was crucial to overriding the inherent preference for functionalization at the C3 position. The reaction features a broad substrate scope and good functional group tolerance and provides direct access to valuable 7-acyloxylated indole derivatives.
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