A novel and convenient method for the synthesis of substituted naphthostyrils

3-Pyrrolyl-6-fluoro-naphthostyril 13 was synthesized via a base-catalyzed intramolecular cyclization of oxindole precursor 2 (Y=H). Derivatization of 2 (Y=I) through a one-pot reaction give 5-substituted naphthostyrils. This method allows convenient access to 3,5,6-trisubstituted naphthostyrils which may serve as a new template for CDK2 inhibition.