Enantioselective Organocatalytic Synthesis of Arylglycines <i>via</i> Friedel–Crafts Alkylation of Arenes with a Glyoxylate Imine

Abstract

Abstract 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.