One-Pot Homologation of Boronic Acids: A Platform for Diversity-Oriented Synthesis

Article abstract of DOI:10.1021/acs.orglett.5b03030

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.