Pd/Cu-cocatalyzed reigoselective arylation of thiazole derivatives at 2-position under ligand-free conditions

Abstract

An efficient protocol for regioselective arylation of thiazole derivatives at the 2-position via palladium- and copper-catalyzed C–H bond activation under ligand-free conditions has been developed. The reaction proceeds smoothly with 1% palladium catalyst in the presence of 20% Cu(TFA)₂ to furnish the desired products. The direct C–H arylation and no ligand made this method synthetically useful for the arylation of thiazoles at the 2-position.