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Updated: Aug 16, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Directing Group Migration Strategy: Ru(II)-Catalyzed Domino C-H Functionalization toward the Synthesis of
Saiprasad Nunewar1, Animesh Kumar Pushparaj2, Vinaykumar Kanchupalli2,1
1Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Hyderabad, Telangana500037, India.
Abstract:
Directing group (DG) migration strategies originating from transition-metal-catalyzed C-H functionalization have recently attracted considerable attention. Herein, we report a Ru(II)-catalyzed domino process that involves C-H functionalization, DG-migration, and a subsequent 1,6-aza-conjugate addition between N-carbamoyl indoles and alkynylated p-quinone methides (p-QMs), providing an efficient route to 1,4-dihydroisoquinolin-3(2H)-one-based bisheterocycles. Notably, the protocol exhibits a broad substrate scope, delivers moderate to excellent yields, and is amenable to late-stage functionalization of structurally diverse biologically active molecules and natural products.
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