One-pot homologation of boronic acids
MetadataShow full item record
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
© 2015 American Chemical Society. This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
DescriptionThis work was supported by the Engineering and Physical Sciences Research Council (EPSRC).
Items in the St Andrews Research Repository are protected by copyright, with all rights reserved, unless otherwise indicated.