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Nature Chemistry

Thursday, December 15, 2011

Transition-Metal-Free Direct Arylation of Anilines


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.

DOI: 10.1002/anie.201106150

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