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Indoles Synthesized from Amines via Copper Catalysis

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journal contribution
posted on 05.04.2013, 00:00 authored by Ronald Besandre, Miguel Jaimes, Jeremy A. May
N-Substituted indoles are synthesized from primary amines through a tandem reaction sequence. Initial condensation of the amine with an α-(o-haloaryl)ketone or aldehyde is followed by intramolecular aryl amination catalyzed by CuI. A variety of anilines and alkyl amines, including those with significant steric demands, are converted to indoles in high yields and with varying indole substitution.