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Updated: Jan 13, 2026

Synthesis and Purification of Iodoaziridines Involving Quantitative Selection of the Optimal Stationary Phase for Chromatography
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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.
This study introduces a new hypervalent iodine method for direct C-H azidation of arenes. This efficient process allows for late-stage functionalization of drug molecules and diverse compounds.
Area of Science:
- Organic Chemistry
- Synthetic Methodology
Background:
- C-H functionalization is a key area in organic synthesis.
- Developing regioselective methods for installing functional groups like azides is crucial.
Purpose of the Study:
- To report a novel hypervalent iodine-mediated C-H azidation reaction.
- To enable direct and regioselective installation of azido groups onto arenes.
Main Methods:
- Utilizing hypervalent iodine reagents for C-H activation.
- Performing regioselective azidation under mild reaction conditions.
Main Results:
- Successful azidation of diverse arenes with high regioselectivity.
- Demonstrated tolerance of various functional groups.
- Application in late-stage azidation of drug intermediates and functional molecules.
Conclusions:
- The developed method provides a practical and scalable platform for arene modification.
- Generated azidoarenes are versatile intermediates for further transformations like reduction and click chemistry.
- Facilitates rapid molecular diversification.
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