Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis

Org Lett. 2021 Mar 19;23(6):1996-2001. doi: 10.1021/acs.orglett.1c00100. Epub 2021 Mar 5.

Abstract

A practical approach toward the synthesis of 2-arylazoles via direct arylation is described. The transformation relies on a Pd/Cu cocatalyst system that operates with low catalyst loadings. The reaction conditions were found to be tolerant of a wide range of functional groups and nitrogen-containing heterocycles commonly employed in a drug discovery setting.

Publication types

  • Research Support, Non-U.S. Gov't