Issue 1, 2017
From the journal:

Chemical Science

Site-selective Suzuki–Miyaura coupling of heteroaryl halides – understanding the trends for pharmaceutically important classes†

Joshua Almond-Thynne,a   David C. Blakemore,b   David C. Prydeb  and  Alan C. Spivey ORCID logo *a  

* Corresponding authors

a Department of Chemistry, Imperial College London, South Kensington Campus, London, UK
E-mail: a.c.spivey@imperial.ac.uk
Fax: +44 (0)1474 813219

b Pfizer Worldwide Medicinal Chemistry, The Portway Building, Granta Park, Great Abington, Cambridge, UK

Abstract

Suzuki–Miyaura cross-coupling reactions of heteroaryl polyhalides with aryl boronates are surveyed. Drawing on data from literature sources as well as bespoke searches of Pfizer's global chemistry RKB and CAS Scifinder® databases, the factors that determine the site-selectivity of these reactions are discussed with a view to rationalising the trends found.

Graphical abstract: Site-selective Suzuki–Miyaura coupling of heteroaryl halides – understanding the trends for pharmaceutically important classes

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Article information

DOI
https://doi.org/10.1039/C6SC02118B
Article type
Perspective
Submitted
13 May 2016
Accepted
04 Aug 2016
First published
09 Aug 2016
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2017,8, 40-62

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Site-selective Suzuki–Miyaura coupling of heteroaryl halides – understanding the trends for pharmaceutically important classes

J. Almond-Thynne, D. C. Blakemore, D. C. Pryde and A. C. Spivey, Chem. Sci., 2017, 8, 40 DOI: 10.1039/C6SC02118B

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