Bu4NI-Catalyzed Traceless Coupling of Carboxylic acids and Amines

A one-pot procedure for amide bond formation has been developed in the presence of TBAI/TBHP. 1,4-Dioxane serves dual roles as both solvent and a traceless acyl-activating agent for the direct coupling of carboxylic acids with primary and secondary amines, affording the corresponding amides with good to excellent yields. Moreover, the versatility of this strategy is also highlighted by the synthesis of pharmaceutically valuable amide bond-containing molecules such as Moclobemide, Trimethobenzamide, Olaparib, Mitapivat.