In conclusion, we have developed an electrophilic azetidinylation protocol based on the underexplored reagents, azetidinyl trichloroacetimidates. This method enables the direct installation of the azetidine ring onto over 20 classes of nucleophiles at any stage of synthesis. Our approach simplifies the synthesis of known compounds, facilitates the access to bioactive molecules, and offers a convenient pathway to azetidine analogues for piperidine-containing drugs. The broad applicability and practical benefits of this protocol are anticipated to create compelling opportunities in medicinal chemistry.