Transition-Metal-Free Direct Arylation of Anilines

Authors


  • We thank Regione Piemonte, DRUIDI project (visiting research fellowship to T.P.) and the EPSRC for funding (Leadership Fellowship to M.F.G.), and the EPSRC mass spectrometry service at the University of Swansea.

Abstract

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Aryne arylation: A new method of direct arylation is reported for aniline substrates. The reaction uses benzyne to synthesize a variety of aminobiaryls under mild conditions (see scheme), requiring no stoichiometric metalation or transition-metal catalysis. An ene mechanism is implicated, and conveys excellent functional group tolerance relative to metal-mediated processes.

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