Highly Enantioselective Synthesis of 2,3-Dihydro‑1H‑imidazo[2,1‑a]isoindol-5(9bH)‑ones via Catalytic Asymmetric Intramolecular Cascade Imidization–Nucleophilic Addition–Lactamization

Highly enantioselective catalytic asymmetric intramolecular cascade imidization–nucleophilic addition–lactamization of N 1-alkylethane-1,2-diamine with methyl 2-formylbenzoate catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones with high yields and excellent enantioselectivities. This strategy has been shown to be quite general toward various methyl 2-formylbenzoates.