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A Highly Efficient Palladium/Copper Cocatalytic System for Direct Arylation of Heteroarenes: An Unexpected Effect of Cu(Xantphos)I

Jinkun Huang*, Johann Chan, Ying Chen, Christopher J. Borths, Kyle D. Baucom, Robert D. Larsen and Margaret M. Faul

*Chemical Process Research and Development, Amgen Inc., Thousand Oaks, California 91320, Email:

J. Huang, J. Chan, Y. Chen, C. J. Borths, K. D. Baucom, R. D. Larsen, M. M. Faul, J. Am. Chem. Soc., 2010, 132, 3674-3675.

DOI: 10.1021/ja100354j


A highly efficient Pd/Cu-catalyzed C-H arylation method for a range of heterocycles has been discovered. The efficiency and low loading of a combination of a palladium catalyst and a well-defined copper cocatalyst together with the mild reaction conditions demonstrate this method to be practically useful and mechanistically interesting.

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proposed mechanism

Key Words

Benzothiazoles, Benzoxazoles

ID: J48-Y2010-0600