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

Calum W. Muir, Julien C. Vantourout, Albert Isidro-Llobet, Simon J. F. Macdonald, Allan J. B. Watson

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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.
Original languageEnglish
Pages (from-to)6030–6033
Number of pages4
JournalOrganic Letters
Issue number24
Publication statusPublished - 3 Dec 2015


  • boronic acids
  • chemical reactivity
  • organometallic reagents

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