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Updated: Jun 21, 2025

Preparation of Contiguous Bisaziridines for Regioselective Ring-Opening Reactions
Published on: July 28, 2022
Radical meta-C-H Halogenation of Azines via N-Benzyl Activation Strategy
Juan Tang1, Shun Li1, Yihua Fu1
1Key Laboratory of Green Chemistry & Technology, Ministry of Education College of Chemistry, Sichuan University, Chengdu 610064, P. R. China.
Abstract:
Regioselective halogenation of six-membered N-heteroarenes is crucial for precise functional derivatization. We present a meta-selective halogenation method for pyridines, quinolines, and isoquinolines via electrophilic halogen radical addition utilizing an N-benzyl activation strategy. This method achieves C3- and C5-dihalogenation in pyridines, C3- and C6-dihalogenation in quinolines, and C3-monohalogenation in isoquinolines. The feasibility and potential applications of this method were validated through scale-up reactions and the bromination of quinoline derivatives with biomolecular fragments.
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