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Updated: Jul 17, 2025

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Electrochemical Direct α-Arylation of Alkylamines with Sulfonylarenes
Kyohei Yonekura1, Mari Murooka1, Kohei Aoki1
1Department of Applied Chemistry for Environment, School of Biological and Environmental Sciences, Kwansei Gakuin University, Sanda, Hyogo 669-1330, Japan.
Abstract:
The electrochemical α-arylation of alkylamines with sulfonylarenes has been developed. Here, diverse trialkylamines and aryl(dimethyl)amines are applicable to the α-arylation with sulfonylarenes having an azole, azine, and benzene nucleus. The α-arylation was scaled up using an electrolysis flow cell. Mechanistic studies show that anodic oxidation of an alkylamine with a sulfinate as a mediator followed by deprotonation gives an α-aminoalkyl radical, which undergoes homolytic aromatic substitution (HAS) on a sulfonylarene to give the corresponding α-arylalkylamine.
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