Catalytic Amidation of Carboxylic Acids Using ortho-Aminophenylboronic Acids

Abstract

ortho-Substituted boronic acids have demonstrated significant potential as catalysts for direct amidation reactions, providing a sustainable alternative to conventional coupling reagents. We report the screening of ortho-functionalized arylboronic acids, including four literature benchmarks, as catalysts for the direct condensation of amines and carboxylic acids. The commercially available ortho-aminophenylboronic acids, specifically (2-(piperidin-1-yl)phenyl)boronic acid (2-PPBA), emerge as the optimal catalyst, providing amides from a range of carboxylic acids and amines.