Site-Selective Azidation of Arenes via Hypervalent Iodine-Mediated C–H Functionalization

A hypervalent iodine-mediated C-H azidation is reported that enables direct, regioselective installation of azido groups onto diverse arenes. The method tolerates a wide range of functionalities and operates under mild conditions. Its value is demonstrated through late-stage azidation of drug intermediates and functional molecules, providing versatile azidoarenes that undergo efficient downstream transformations, including reduction and click conjugation. This concise and scalable strategy offers a practical platform for arene modification and rapid molecular diversification.