A simple and efficient protocol for a palladium-catalyzed ligand-free Suzuki reaction at room temperature in aqueous DMF

Abstract

A convenient, effective and mild protocol has been developed for the palladium-catalyzed ligand-free Suzuki reaction of aryl bromides with arylboronic acids in aqueous N,N-dimethylformamide (DMF) in the presence of K₂CO₃ and a catalytic amount of PdCl₂ in air at room temperature. It is noteworthy that the volume ratio of water–DMF and base play important roles in the reaction, and various functional groups are tolerated under the optimized conditions. Furthermore, this protocol could be extended to the cross-couplings of nitrogen-based heteroaryl halides with arylboronic acids in moderate to excellent yields.