Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis

• DOI: 10.1021/acs.orglett.1c00100
• Publication Date: 2021-03-05T17:13:58Z
• Authors: Tiffany Piou; Yuriy Slutskyy; Nancy J. Kevin; Zhongxiang Sun; Dong Xiao; Jongrock Kong
• Keywords: catalyst loadings; Chemical Sciences not elsewhere classified; synthesis; Science Policy; transformation; approach; nitrogen-containing heterocycles; Biochemistry; 01 natural sciences; Catalysi; drug discovery; 0104 chemical sciences; reaction conditions; 2- arylazoles; Space Science; Azoles Enabled; cocatalyst; Medicine; Pd; Direct Arylation; arylation; Biotechnology; Biological Sciences not elsewhere classified

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.