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Synfacts 2007(12): 1298-1298  
DOI: 10.1055/s-2007-991321
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

Copper-Catalyzed Sulfonylation of Arylboronic Acids

Contributor(s): Paul Knochel, Andrei Gavryushin
A. Kar, I. A. Sayyed, W. F. Lo, H. M. Kaiser, M. Beller, M. K. Tse*
Leibniz-Institut für Katalyse e.V. and der Universität rostock and Universität Rostock, Germany
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Publication History

Publication Date:
22 November 2007 (online)

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Significance

Aryl sulfones are widely present among modern drugs and various biologically active compounds. Herein, the authors report a cata­lytic version of Cu-promoted sulfonylation of boronic acids with alkyl- and arylsulfinate salts. This method tolerates most functional groups, including free hydroxyl, and can be applied as well to heterocycles and alkenylboronic acids. The broad range of suitable substrates makes this protocol especially attractive for modular and combinatorial synthesis.