A Highly Efficient Cocatalytic System for Direct Arylation
of Heteroarenes

J. Huang; J. Chan; Y. Chen; C. J. Borths; K. D. Baucom; R. D. Larsen; M. M. Faul

doi:10.1055/s-0029-1219771

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Synfacts 2010(6): 0695-0695
DOI: 10.1055/s-0029-1219771

Metal-Mediated Synthesis

A Highly Efficient Cocatalytic System for Direct Arylation of Heteroarenes

Contributor(s): Paul Knochel, Stefan Wunderlich
J. Huang*, J. Chan, Y. Chen, C. J. Borths, K. D. Baucom, R. D. Larsen, M. M. Faul
Amgen. Inc, Thousand Oaks, USA

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Publication History

Publication Date:
20 May 2010 (online)

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Significance

A highly efficient palladium/copper catalyzed C-H arylation method for a range of heterocycles has been investigated. It turned out that the key step of this transformation is a combination of a palladium catalyst and the copper cocatalyst Cu(Xanthphos)I. The efficiency and low loadings of the catalyst (0.25 mol%) and the cocatalyst (1 mol%) in combination with practical reaction conditions demonstrate the utility of this method.