Copper-catalyzed synthesis of 2,3-disubstituted indoles from ortho-haloanilines and β-keto esters/β-diketone

Abstract

Tetrazole-1-acetic acid was identified as an efficient ligand to promote copper-catalyzed domino reaction of ortho-iodo/bromo-anilines with β-keto esters/β-diketone for 2,3-disubstituted indoles' synthesis with high yields under mild conditions. The protocol, with easy-available catalytic system, shows good substrate tolerance towards various functional groups.