Organocatalytic Asymmetric Three-Component Povarov Reactions of Anilines and Aldehydes

作者：Jun-Xiang Huang, Ke‐Qiang Hou, Qi-Long Hu, Xueping Chen, Jian Li, Albert S. C. Chan, Xiao‐Feng Xiong · 发表于：Organic Letters · 年份：2020 · DOI：10.1021/acs.orglett.0c00206 · 被引用次数：32 · 研究领域：Asymmetric Synthesis and Catalysis、Synthetic Organic Chemistry Methods、Oxidative Organic Chemistry Reactions

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.