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

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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.

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Almond-Thynne, J., Blakemore, D. C., Pryde, D. C., & Spivey, A. C. (2016). Site-selective Suzuki-Miyaura coupling of heteroaryl halides-understanding the trends for pharmaceutically important classes. Chemical Science, 8(1), 40–62. https://doi.org/10.1039/C6SC02118B

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