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Palladium-Catalyzed Asymmetric (4 + 2) Annulation of γ-Methylidene-δ-valerolactones with Alkenes: Enantioselective Synthesis of Functionalized Chiral Cyclohexyl Spirooxindoles

Zhi-Long Jia, Xian‐Tao An, Yu‐Hua Deng, Lin-Han Pang, Chunfang Liu, Le-Le Meng, Jia-Kun Xue, Xian‐He Zhao, Chun‐An Fan

2021Organic Letters39 citationsDOI

Abstract

An unprecedented asymmetric catalytic (4 + 2) annulation reaction of aryl-substituted γ-methylidene-δ-valerolactones (GMDVs) with isatin-derived para-quinone methides (p-QMs) has been developed under the catalysis of palladium(0) and (S,S,S)-(−)-Xyl-SKP, offering a new approach for the diastereo- and enantioselective synthesis of chiral cyclohexadienone-fused cyclohexyl spirooxindoles. Significantly, three highly congested contiguous tetrasubstituted carbon atoms embedded in bispirocyclic skeleton, of which two are vicinal quaternary stereogenic centers, are forged in an effective and selective manner (up to 99% yield, up to 95% ee, >20/1 dr). The current reaction represents the first exploration of enantioselective catalytic (4 + 2) annulation forming the six-membered carbocycles in the chemistry of both GMDVs and p-QMs.

Topics & Concepts

Enantioselective synthesisAnnulationStereocenterChemistryCatalysisPalladiumYield (engineering)IsatinVicinalArylCombinatorial chemistryStereochemistryMedicinal chemistryOrganic chemistryAlkylMetallurgyMaterials scienceSynthesis of Indole DerivativesAxial and Atropisomeric Chirality SynthesisAsymmetric Synthesis and Catalysis
Palladium-Catalyzed Asymmetric (4 + 2) Annulation of γ-Methylidene-δ-valerolactones with Alkenes: Enantioselective Synthesis of Functionalized Chiral Cyclohexyl Spirooxindoles | Litcius