Nature Communications (Sep 2020)

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

  • Ferdinand H. Lutter,
  • Lucie Grokenberger,
  • Luca Alessandro Perego,
  • Diego Broggini,
  • Sébastien Lemaire,
  • Simon Wagschal,
  • Paul Knochel

DOI
https://doi.org/10.1038/s41467-020-18188-z
Journal volume & issue
Vol. 11, no. 1
pp. 1 – 8

Abstract

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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.