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Synfacts 2007(9): 0977-0977  
DOI: 10.1055/s-2007-968825
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

Efficient Catalysts for Suzuki-Miyaura Cross-Coupling of Heteroaryl Chlorides

Contributor(s): Paul Knochel, Andrei Gavryushin
A. S. Guram*, X. Wang, E. E. Bunel, M. M. Faul, R. D. Larsen, M. J. Martinelli
Amgen Inc., Thousand Oaks, USA
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Publication History

Publication Date:
23 August 2007 (online)

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Significance

The Suzuki-Miyaura cross-coupling reaction of heteroaryl chlorides is of great interest for pharmaceutical industry due to the relatively low price of such chlorides, compared to the corresponding bromides, and the prevalence of heterobiaryls among the biologically relevant molecules. The new catalysts exceed the well-known biaryl phosphines in efficiency for the coupling of heterocyclic substrates. They are air-stable solids, easy to prepare and handle. The catalyst loadings as low as 0.01 mol% are efficient for many cases.