Pd(ii)-catalyzed synthesis of aryl ketones in water

Abstract

A mild and efficient Pd-catalyzed protocol has been developed for the direct synthesis of aryl ketones through a reaction of arylboronic acids (and their ester derivatives) with aromatic as well as aliphatic nitriles. The reaction operates under mild conditions using minimal amounts of PTSA as a cost-effective acid additive and water as the sole solvent, enhancing the sustainability of the process. This method exhibits excellent functional group tolerance and a broad substrate scope, delivering both diaryl and alkyl aryl ketones in moderate to excellent yields. Notably, the utility of this methodology is demonstrated via the synthesis of (4-methoxyphenyl)(3,4,5-trimethoxyphenyl)methanone (PHT), a pharmaceutically relevant compound, in a remarkable yield of 96%.