Site-Selective Azidation of Arenes via Hypervalent Iodine-Mediated C–H Functionalization
Abstract
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.
Fields of Study & Subjects
Catalytic C–H Functionalization Methods
Oxidative Organic Chemistry Reactions
Radical Photochemical Reactions
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 2
- Pages
- 788–793
- Publication date
- 6 January 2026
- Language
- EN