Azabicyclo[1.1.0]butyl‐Substituted Sulfonimidoyl Fluoride: Electrophilic Hub Bridging Late‐Stage Azetidine Incorporation with Sufex Chemistry

The development of electrophilic strained small motifs is of increasing importance for chemical biology and drug discovery, enabling precise, late‐stage functionalization and targeted covalent inhibition. In this work, we report the efficient synthesis of a novel azabicyclo[1.1.0]butyl‐substituted sulfonimidoyl fluoride, a bench‐stable electrophilic hub combining strain‐release reactivity and SuFEx chemistry. The dual reactivity of this motif was demonstrated through selective ABB ring‐opening reactions, and SuFEx‐mediated ligations with diverse nucleophiles, including pharmaceutically relevant derivatives. Further derivatization of the resulting sulfonimidates and sulfonimidamides showcased the synthetic versatility of this system. These findings open avenues for the development of modular, multifunctional platforms in drug discovery.