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

Calum W. Muir | Zendy; Julien C. Vantourout | Zendy; Albert IsidroLlobet | Zendy; Simon J. F. Macdonald | Zendy; Allan J. B. Watson | Zendy

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

Author(s) -

Calum W. Muir,

Julien C. Vantourout,

Albert IsidroLlobet,

Simon J. F. Macdonald,

Allan J. B. Watson

Publication year - 2015

Publication title -

organic letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.94

H-Index - 239

eISSN - 1523-7060

pISSN - 1523-7052

DOI - 10.1021/acs.orglett.5b03030

Subject(s) - chemistry , context (archaeology) , boronic acid , combinatorial chemistry , suzuki reaction , bromodomain , organic chemistry , catalysis , biochemistry , palladium , epigenetics , paleontology , biology , gene

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.

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