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Dynamic Kinetic Resolution of γ-Substituted Cyclic β-Ketoesters via Asymmetric Hydrogenation: Constructing Chiral Cyclic β-Hydroxyesters with Three Contiguous Stereocenters

Dan Yang, Wu Xiong, Xiaojie Zheng, Jian‐Hua Xie, Qi‐Lin Zhou

2021Organic Letters14 citationsDOI

Abstract

An efficient asymmetric hydrogenation of racemic γ-substituted cyclic β-ketoesters via dynamic kinetic resolution to provide chiral cyclic β-hydroxy esters with three contiguous stereocenters is reported. Using a chiral spiro iridium catalyst (R)-5 (Ir-SpiroSAP), a series of racemic γ-aryl/alkyl substituted cyclic β-ketoesters were hydrogenated to the corresponding chiral cyclic β-hydroxy esters in high yields (84–97%) with good to excellent enantioselectivities (69–>99% ee) and cis,cis-selectivities (up to >99:1).

Topics & Concepts

StereocenterChemistryKinetic resolutionCatalysisAsymmetric hydrogenationAlkylArylEnantioselective synthesisStereochemistryResolution (logic)Medicinal chemistryOrganic chemistryComputer scienceArtificial intelligenceAsymmetric Hydrogenation and CatalysisSurface Chemistry and CatalysisAsymmetric Synthesis and Catalysis