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Updated: Jun 18, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Iron-Catalyzed Aerobic Oxidative Aromatic Coupling of Unprotected Primary Arylamines
Shaoshuai Ma1, Changyin Zhao1, Hongbin Liu2
1School of Chemistry and Chemical Engineering, Shandong University, Jinan, 250100, China.
Abstract:
A ligand-free, iron-catalyzed aerobic oxidative coupling of unprotected primary arylamines is reported. Utilizing inexpensive FeCl3 and ambient air as the terminal oxidant, this protocol enables chemoselective ortho-ortho C(sp2)-C(sp2) bond formation while bypassing traditional N-protection requirements. The method accommodates regioselective homo- and cross-coupling of primary arylamines, alongside heterocoupling with phenolic substrates, providing a protection-free platform for constructing complex biaryls directly from primary anilines.
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