Modular Synthesis of 3,3-Disubstituted Azetidines via Azetidinylation Reagents

Azetidines represent an attractive and emerging design option in medicinal chemistry owing to their small size and polar nature, as well as their potential to significantly impact the physicochemical properties of drug molecules. However, traditional methods for the synthesis of 3,3-disubstituted azetidines usually require higher step counts or exhibit poor functional group compatibility. Herein, we report a modular synthesis strategy for 3,3-disubstituted azetidines based on azetidinylation reagents. The practicality of this method is further exemplified by the use of readily available starting materials, mild reaction conditions, and a very broad substrate scope.