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Synfacts 2009(4): 0427-0427  
DOI: 10.1055/s-0028-1087825
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Copper-Facilitated Suzuki Cross-Coupling of 2-Heterocyclic Boronates

Contributor(s): Paul Knochel, Andrei Gavryushin
J. Z. Deng*, D. V. Paone*, A. T. Ginnetti, H. Kurihara, S. D. Dreher, S. A. Weissman, S. R. Stauffer, C. S. Burgey
Merck Research Laboratories, Westpoint and Rahway, USA
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Publication History

Publication Date:
23 March 2009 (online)

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Significance

Heterocyclic pinacolborates are stable and highly interesting intermediates, especially for the pharmaceutical industry. A copper-assisted cross-coupling of these derivatives with greatly enhanced yield is described. This protocol allows a smooth and modular preparation of a variety of arylated heterocycles using relatively mild conditions.