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Enantioselective Organocatalytic Three-Component Vinylogous Michael/Aldol Tandem Reaction among 3-Alkylidene oxindoles, Methyleneindolinones, and Aldehydes

Jing-Xiang Xu, Yi-Syun Jiang, Chih‐Hao Chen, Nadaraj Sathishkumar, Kai‐Ti Chu, Ming‐Hsi Chiang, Hsin‐Tsung Chen, Jeng‐Liang Han

2021The Journal of Organic Chemistry13 citationsDOI

Abstract

We reported a one-pot enantioselective three-component vinylogous Michael/aldol tandem reaction of prochiral 3-alkylidene oxindoles with methyleneindolinones and aldehydes using bifunctional organocatalysts. A variety of enantioenriched 3,3-disubstituted oxindoles 3 and spirolactones 4 were generated in moderate yields (up to 78%) with high stereoselectivities (up to >20:1 dr, >99% ee). Intriguingly, we observed that the aldol reaction with paraformaldehyde generates 3,3-disubstituted oxindoles 3 bearing a hydroxymethyl group, while the reaction with aliphatic aldehydes generates spirolactones 4.

Topics & Concepts

Aldol reactionChemistryEnantioselective synthesisBifunctionalTandemHydroxymethylCascade reactionOrganic chemistryMichael reactionOrganocatalysisAldehydeCatalysisStereochemistryComposite materialMaterials scienceAsymmetric Synthesis and CatalysisSynthetic Organic Chemistry MethodsOxidative Organic Chemistry Reactions
Enantioselective Organocatalytic Three-Component Vinylogous Michael/Aldol Tandem Reaction among 3-Alkylidene oxindoles, Methyleneindolinones, and Aldehydes | Litcius