One pot synthesis of unsymmetrical ketones from carboxylic and boronic acids via PyClU-mediated acylative Suzuki coupling

Abstract

A synthetic procedure for the preparation of ketones from easily accessible carboxylic acids has been developed. This methodology proceeds via in situ activation of the carboxylic acid with PyClU, followed by the palladium-catalyzed acylative cross-coupling with boronic acids. The reaction is performed in one pot, without the need of phosphine ligands, at room temperature and in reaction times of 2h or less. The scope of the reaction is robust with aryl boronic and carboxylic acids.