One-pot homologation of boronic acids
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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.
Muir , C W , Vantourout , J C , Isidro-Llobet , A , Macdonald , S J F & Watson , A J B 2015 , ' One-pot homologation of boronic acids ' Organic Letters , vol 17 , no. 24 , pp. 6030-6033 . DOI: 10.1021/acs.orglett.5b03030
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This work was supported by the Engineering and Physical Sciences Research Council (EPSRC).
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