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Updated: Jan 13, 2026

Synthesis and Purification of Iodoaziridines Involving Quantitative Selection of the Optimal Stationary Phase for Chromatography
Published on: May 16, 2014
Site-Selective Azidation of Arenes via Hypervalent Iodine-Mediated C-H Functionalization
Ziyang Zhang1, Jiajin Weng1, Yanchuan Zhao1
1State Key Laboratory of Fluorine and Nitrogen Chemistry and Advanced Materials and Shanghai Hong Kong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, University of the Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China.
None:
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.
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