Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis

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 hetero-cycles commonly employed in a drug discovery setting.

Automated summary

A practical method for the synthesis of 2-arylazoles via direct arylation using a Pd/Cu cocatalyst system with low catalyst loadings is described. The reaction conditions are tolerant of a wide range of functional groups and nitrogen-containing hetero-cycles commonly used in drug discovery.