The one-pot direct N-acylation of NH sulsoximines with carboxylic acids is described. The method can be performed under mild low-temperature reaction conditions and exhibits a wide substrate scope (> 60 examples). The present method is operationally simple, scalable, and practical; thus, it can find wide applications in both academic and industrial laboratories.

This report describes a general and simple method for the one-pot direct N-acylation of sulfoximines with carboxylic acids using the previously developed 4-(N,N-dimethylamino)pyridine N-oxide (DMAPO)/di-tert-butyl dicarbonate (Boc₂O) system. The method can be performed under mild low-temperature reaction conditions and has a wide substrate scope. The present method is operationally simple, scalable, and practical; thus, it can find wide applications in both academic and industrial laboratories.