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Synfacts 2009(6): 0669-0669  
DOI: 10.1055/s-0029-1216687
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Nickel-Catalyzed Biaryl Coupling of Heteroarenes and Aryl Halides/Triflates

Contributor(s): Paul Knochel, Andreas J. Wagner
J. Canivet, J. Yamaguchi, I. Ban, K. Itami*
Nagoya University and PRESTO, Japan Science and Technology Agency, Nagoya, Japan
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Publication History

Publication Date:
25 May 2009 (online)

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Significance

A nickel-based catalytic system for the arylation of heteroarenes with aryl halides and triflates is reported herein. While aryl bromides and iodides are readily coupled using Ni(OAc)2/bipy, Ni(OAc)2/dppf is effective for aryl chlorides or triflates. The coupled products are obtained in good to very good yields and the authors make use of this procedure in a rapid synthesis of febuxostat, a drug for hyperuricemia and gout.