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Transition-Metal-Free Direct Arylation of Anilines


  • 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.


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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.