We have developed a one-pot, three-component strategy for the Friedel-Crafts arylation of α-imino ketones with imidazopyridines under catalyst-free conditions. The reaction did not require any inert conditions and proceeded at room temperature in the open flask.

Abstract

We report here a catalyst-free, (sp²)C−H imination reaction of in-situ formed imidazo[1,2-a]pyridines and α-iminoketones. This one-pot, multicomponent, and atom economic reaction is performed at moderate to room temperature without the need for any catalyst and inert conditions. The reaction showed good substrate tolerance with appreciable yields. Gram-scale synthesis and post-synthetic modifications to obtain 1,2-diketones are also described.