Substituted 4-alkoxy- and 4-hydroxyquinolin-2(1H)-ones 1 (Fig. 1) such as glycocitlones A–C (2–4) 1 are widely found among quinoline alkaloids of rutaceous plants. 2 Compound 1 also form a valuable class of biologically active molecules, 3 including human immunodeficiency virus type 1 (HIV-1) integrase inhibitors 3a and hepatitis C virus (HCV) inhibitors. 3b and 3e Therefore, a diversity-oriented strategy 4 for the preparation of this class of compounds in ...