Recent Progress in the Synthesis and Application of 2-Acylaziridines

Abstract 2-Acylaziridines are versatile three-membered nitrogen heterocycles whose distinct reactivity stems from substantial ring strain and relatively weak C–N bonds. The appended acyl group exerts significant stereoelectronic influence and serves as a directing moiety, enabling stereoselective transformations that favor nucleophilic attack at the more substituted aziridine carbon and facilitate tandem cyclization processes. This review highlights recent advances over the past decade in the synthesis and applications of 2-acylaziridines, with an emphasis on innovative methodologies, detailed mechanistic studies, and practical implementations. It aims to inspire the development of advanced synthetic strategies and promote the broader use of these scaffolds in the construction of bioactive molecules and complex heterocyclic systems.