One-pot homologation of boronic acids

Muir, Calum W.; Vantourout, Julien C.; Isidro-Llobet, Albert; Macdonald, Simon J. F.; Watson, Allan J. B.

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Date

18/12/2015

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Abstract

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.

Citation

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 . https://doi.org/10.1021/acs.orglett.5b03030

Publication

Organic Letters

Status

Peer reviewed

DOI

https://doi.org/10.1021/acs.orglett.5b03030

ISSN

1523-7060

Type

Journal article

Rights

© 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.

Description

This work was supported by the Engineering and Physical Sciences Research Council (EPSRC).

Collections

University of St Andrews Research

URI

http://hdl.handle.net/10023/12684