One-pot homologation of boronic acids : a platform for diversity-oriented synthesis

Muir, Calum W. and Vantourout, Julien C. and Isidro-Llobet, Albert and Macdonald, Simon J. F. and Watson, Allan J. B. (2015) One-pot homologation of boronic acids : a platform for diversity-oriented synthesis. Organic Letters, 17 (24). 6030–6033. ISSN 1523-7060

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    Abstract

    Formal homologation of sp2-hybridized boronic acids is achieved via cross-coupling of boronic acids with conjunctive haloaryl BMIDA components in the presence of a suitably balanced basic phase. The utility of this approach to provide a platform for diversity-oriented synthesis in discovery medicinal chemistry is demonstrated in the context of the synthesis of a series of analogues of a BET bromodomain inhibitor.