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Updated: Jun 13, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Stereoselective construction of highly functionalized azetidines via a [2 + 2]-cycloaddition
Yang Ye1, Hua Wang, Renhua Fan
1Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433, China, and Shanghai Key Laboratory of Molecular Catalysts and Innovative Materials, Department of Chemistry, Fudan University, Shanghai 200433, China.
Abstract:
A facile stereoselective synthesis of highly functionalized azetidines from a novel [2 + 2]-cycloaddition of 2-aminomalonates to chalcones is reported. The desired four-membered ring construction proceeded via a grind-promoted solvent-free Michael addition and a PhIO/Bu(4)NI mediated oxidative cyclization and afforded azetidines in moderate to good yields with excellent diastereoselectivities.
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