Phthalimidine Synthesis\nvia Iridium-Catalyzed Reductive\nLactamization

Herein, we report a sustainable and efficient method\nfor the synthesis\nof structurally diverse phthalimidines from 2-formylbenzoic acid and\nprimary amines using an iridium-catalyzed reductive lactamization\nstrategy. The advantages of this method, such as the use of water–ethanol\nas a solvent, broad substrate scope, high catalyst efficiency (<i>S</i>/<i>C</i> up to 10000), good scalability, and\neasy purification, enable it to be a practical approach to phthalimidines.\nIt is suggested that iridium hydride formation is involved in the\nrate-limiting step. Synthetic applications for the late-stage functionalization\nof medicinally relevant molecules are also demonstrated.