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

Author:

Almond-Thynne Joshua1234,Blakemore David C.564,Pryde David C.564,Spivey Alan C.1234ORCID

Affiliation:

1. Department of Chemistry

2. Imperial College London

3. London

4. UK

5. Pfizer Worldwide Medicinal Chemistry

6. Cambridge

Abstract

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

Funder

Pfizer

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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5. Transition-State Metal Aryl Bond Stability Determines Regioselectivity in Palladium Acetate Mediated C–H Bond Activation of Heteroarenes

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