Sodium dithionite-mediated reductive N-acetylation/formylation of nitroarenes employing DMAc/DMF as acetyl/formyl surrogates

Abstract

The present invention discloses a unified strategy for N-acetylation/formylation directly from nitroarenes employing solvents DMAc/DMF as the source of acetyl/formyl groups, with sodium dithionite serving as the sole reagent. Unlike the conventional N-acetylation/formylation of anilines, the method uses precursor nitroarenes to form acetanilides/formanilides via in situ reduction to anilines. The regioselectivity, application to drug molecules, tandem process, and dual role of the reagent are the key features of the method.