Recent advances in the synthesis and reactivity of azetidines: strain-driven character of the four-membered heterocycle

Azetidines represent one of the most important four-membered heterocycles used in organic synthesis and medicinal chemistry. The reactivity of azetidines is driven by a considerable ring strain, while at the same the ring is significantly more stable than that of related aziridines, which translates into both facile handling and unique reactivity that can be triggered under appropriate reaction conditions. Recently, remarkable advances in the chemistry and reactivity of azetidines have been reported. In this review, we provide an overview of the synthesis, reactivity and application of azetidines that have been published in the last years with a focus on the most recent advances, trends and future directions. The review is organized by the methods of synthesis of azetidines and the reaction type used for functionalization of azetidines. Finally, recent examples of using azetidines as motifs in drug discovery, polymerization and chiral templates are discussed.

Automated summary

Azetidines, as one of the most important four-membered heterocycles, are widely used in organic synthesis and medicinal chemistry due to their considerable ring strain and unique reactivity. Recent advancements in the research of azetidines focus on synthesis, reactivity, and applications, with discussions on trends and future directions. Notable examples include the use of azetidines in drug discovery, polymerization, and chiral templates.