title: One-Pot Homologation of Boronic Acids: A Platform for Diversity-Oriented Synthesis.
abstract: Formal homologation of sp(2)-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.
authors.affiliation: Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde , 295 Cathedral St., Glasgow, G1 1XL, U.K.
authors.forename: Calum W
authors.initials: CW
authors.lastname: Muir
authors.affiliation: Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde , 295 Cathedral St., Glasgow, G1 1XL, U.K.|GlaxoSmithKline , Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.
authors.forename: Julien C
authors.initials: JC
authors.lastname: Vantourout
authors.affiliation: GlaxoSmithKline , Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.
authors.forename: Albert
authors.initials: A
authors.lastname: Isidro-Llobet
authors.affiliation: GlaxoSmithKline , Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.
authors.forename: Simon J F
authors.initials: SJ
authors.lastname: Macdonald
authors.affiliation: Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde , 295 Cathedral St., Glasgow, G1 1XL, U.K.
authors.forename: Allan J B
authors.initials: AJ
authors.lastname: Watson
mesh_terms: D001897:Boronic Acids / Q000737:chemistry*; D002384:Catalysis; D015394:Molecular Structure
chemical_list: D001897:Boronic Acids