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Updated: Jul 15, 2025

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Solvent-Free Mechanoradical-Mediated Minisci-Type C-H Alkylation of N-Heteroarenes
Xiang Gu1, Taoyong Wang1, KaKing Yan1
1School of Physical Science and Technology, ShanghaiTech University, 201210 Shanghai, China.
Abstract:
An environmentally friendly new C-H alkylation method of N-heteroarenes facilitated by mechanochemistry is described. Under solvent-free ball-milling, mechanoradicals (SO4•-) were generated from persulfate via in situ homolysis in the solid state, at as low as -50 °C. These highly oxidizing radicals readily transform alkyl trifluoroborate salts to their corresponding carbon-based radicals for subsequent C-C bond formation with N-heterocycles. Mechanistic studies unambiguously confirmed the involvement of both oxygen- and alkyl-radical-based intermediates.
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