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Organocatalytic Asymmetric Three-Component Povarov Reactions of Anilines and Aldehydes

Jun-Xiang Huang, Ke‐Qiang Hou, Qi-Long Hu, Xueping Chen, Jian Li, Albert S. C. Chan, Xiao‐Feng Xiong

2020Organic Letters32 citationsDOI

Abstract

We report the first highly enantio- and diastereoselective three-component Povarov reaction between anilines and aldehydes catalyzed by a chiral amine catalyst. A wide variety of substituted tetrahydroquinolines were obtained with moderate to good yields and excellent enantioselectivity and diastereoselectivity (up to 99% ee and >95:5 dr) under the reaction conditions. Furthermore, the reaction intermediates could be efficiently converted to other valuable building blocks.

Topics & Concepts

ChemistryCatalysisComponent (thermodynamics)Amine gas treatingOrganic chemistryReaction conditionsOrganocatalysisCombinatorial chemistryEnantioselective synthesisThermodynamicsPhysicsAsymmetric Synthesis and CatalysisSynthetic Organic Chemistry MethodsOxidative Organic Chemistry Reactions
Organocatalytic Asymmetric Three-Component Povarov Reactions of Anilines and Aldehydes | Litcius