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Direct Electrochemical Synthesis of 2,3‐Disubstituted Quinoline <i>N‐</i>oxides by Cathodic Reduction of Nitro Arenes

J. Winter, Tobias Prenzel, Tom Wirtanen, Dieter Schollmeyer, Siegfried R. Waldvogel

2022Chemistry - A European Journal20 citationsDOIOpen Access PDF

Abstract

The use of electric current in synthetic organic chemistry offers a sustainable tool for the selective reductive synthesis of quinoline N-oxides starting from easily accessible nitro compounds. The reported method employs mild and reagent-free conditions, a simple undivided cell, and constant current electrolysis set-up which provides conversion with a high atom economy. The synthesis of 30 differently substituted quinoline N-oxides was successfully performed in up to 90 % yield. Using CV studies, the mechanism of the selective formation of the quinoline N-oxides was elucidated. The technical relevance of the described reaction could be shown in a 50-fold scale-up reaction.

Topics & Concepts

Cathodic protectionQuinolineNitroElectrochemistryChemistryReduction (mathematics)Medicinal chemistryOrganic chemistryElectrodeMathematicsPhysical chemistryAlkylGeometryRadical Photochemical ReactionsCatalytic C–H Functionalization MethodsSynthesis and Biological Evaluation
Direct Electrochemical Synthesis of 2,3‐Disubstituted Quinoline <i>N‐</i>oxides by Cathodic Reduction of Nitro Arenes | Litcius