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Org Lett. 2015 Dec 18;17(24):6030-3. doi: 10.1021/acs.orglett.5b03030. Epub 2015 Dec 3.

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

Author information

1
Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde , 295 Cathedral St., Glasgow, G1 1XL, U.K.
2
GlaxoSmithKline , Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.

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.

PMID:
26632981
DOI:
10.1021/acs.orglett.5b03030
[Indexed for MEDLINE]

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