Regioselective functionalization of aryl azoles as powerful tool for the synthesis of pharmaceutically relevant targets

Aryl azoles are common scaffolds in pharmaceutically relevant molecules. Here, the authors report the mild and highly regioselective ortho magnesiation of aryl azoles using a tailored magnesium amide base in hydrocarbon solvents followed by an efficient Pd-catalyzed arylation.

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Bibliographic Details
Main Authors: Ferdinand H. Lutter, Lucie Grokenberger, Luca Alessandro Perego, Diego Broggini, Sébastien Lemaire, Simon Wagschal, Paul Knochel
Format: article
Language:EN
Published: Nature Portfolio 2020
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Online Access:https://doaj.org/article/c1c7da05e71b426d8d98fbff31589ad0
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Summary:Aryl azoles are common scaffolds in pharmaceutically relevant molecules. Here, the authors report the mild and highly regioselective ortho magnesiation of aryl azoles using a tailored magnesium amide base in hydrocarbon solvents followed by an efficient Pd-catalyzed arylation.