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Updated: Sep 9, 2025

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Photoinduced EDA Complexes Enabled C3 (Hetero)arylation of Indoles Using Amine as a Transient Occupying Group
Anping Luo1, Wenjie Liu1, Jiaxin Yang1
1Green Pharmaceutical Technology Key Laboratory of Luzhou City, Central Nervous System Drug Key Laboratory of Sichuan Province, School of Pharmacy, Southwest Medical University, Luzhou 646000, People's Republic of China.
Abstract:
Herein, an EDA complex enabled selective C3 (hetero)arylation of indole was established, utilizing morpholine as the transient occupying group. This protocol is efficient, sustainable, and exhibits excellent substrate compatibility and functional group tolerance. Mechanistic studies revealed the binding of morpholine to the C2 position of the indole cation radical plays a key role in forming the transient radical at the C3 position. Furthermore, late-stage functionalization of biorelevant compounds and gram-scale synthesis demonstrate the utility of this protocol.
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