Advances in One‐Pot Construction of Complex Ring Systems via Aziridine‐Based Strain‐Release Strategy

ABSTRACT Aziridines, with their inherent strain energy and high reactivity, serve as pivotal building blocks for constructing complex polycyclic systems. This review focuses on recent advances (2015–2025) in one‐pot ring‐expansion reactions of aziridine derivatives, enabling efficient synthesis of heteroatom‐containing polycycles. Compared to conventional multi‐step strategies, these methodologies exhibit superior atom economy and enhanced environmental compatibility, offering novel synthetic routes to pharmaceutically relevant scaffolds.