H8-BINOL chiral imidodiphosphoric acid catalyzed highly enantioselective aza-Friedel–Crafts reactions of pyrroles and enamides/imines

Abstract

The first enantioselective aza-Friedel–Crafts reaction between pyrroles and enamides has been achieved by using a novel H₈-BINOL-type imidodiphosphoric acid catalyst. This methodology was also applied to the highly enantioselective aza-Friedel–Crafts reaction between pyrroles and imines. The catalyst loadings in these two reactions are low (0.3–2 mol%). Both processes are amenable to gram scales.