Enantioselective Organocatalytic Synthesis of Arylglycines via Friedel–Crafts Alkylation of Arenes with a Glyoxylate Imine

The enantioselective organocatalytic synthesis of arylglycines has been developed employing 1 mol% of an enantiopure N‐triflyl phosphoramide Brønsted acid as organocatalyst. Various differently substituted phenylglycine derivatives can be synthesized in good to excellent yields and enantiomeric excesses based on a Friedel–Crafts alkylation of electron‐rich arenes with a glyoxylate imine. A novel protocol for the deprotection of the N‐tert‐butylsulfonyl (Bus) group has also been developed.