Abstract: | The first direct enantioselective Friedel–Crafts reaction of indoles with isatins has been developed. The process is catalyzed by simple cupreine under mild reaction conditions and affords synthetically and biologically interesting, chiral 3‐indolyl‐3‐hydroxy‐2‐oxindoles in good yields (68–97%) and with high enantioselectivities (76–91%). |