Chiral Brønsted Acid‐Mediated Enantioselective Organocatalytic Three‐Component Reaction for the Construction of Trifluoromethyl‐Containing Molecules

In combination with the advantages of organocatalysis, we have developed a highly enantioselective Friedel–Crafts aminoalkylation of indoles with imines generated in situ from trifluoroacetaldehyde methyl hemiacetal and aniline. Novel chiral trifluoromethyl‐containing compounds were obtained in high yields with excellent enantioselectivities. This methodology was further extended to difluoroacetaldehyde methyl hemiacetal to demonstrate the broad scope of substrates.