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Diastereodivergent Formal 1,3‐Dipolar Cycloaddition of 5‐alkenyl thiazolones to Access Stereochemically Diverse Pyrrolidinyl Spirooxindoles

Yu He, Yue Liu, Yu Liu, Xin‐Xin Kou, Qing‐Zhu Li, Jiahong Li, Jiahong Li, Hezhong Jiang, Hai‐Jun Leng, Cheng Peng, Jun‐Long Li, Jun‐Long Li

2020Advanced Synthesis & Catalysis31 citationsDOI

Abstract

Abstract We report here a stereoselective [3+2] cyclization of 5‐alkenyl thiazolones and ketimines that allows the assembly of three diastereoisomers through the combination of stereodivergent organocatalysis and the following diastereoselective transformation of products. A broad spectrum of pyrrolidinyl spirooxindoles featuring stereochemical diversity has been synthesized through organocatalytic formal 1,3‐dipolar cycloadditions with up to 98% yield, >20:1 dr and 99:1 er. magnified image

Topics & Concepts

ChemistryDiastereomerStereoselectivityOrganocatalysisYield (engineering)StereochemistryCycloadditionEnantioselective synthesisTransformation (genetics)Combinatorial chemistryCatalysisOrganic chemistryGeneMetallurgyMaterials scienceBiochemistryAsymmetric Synthesis and CatalysisFluorine in Organic ChemistrySynthesis and Catalytic Reactions