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Merging Aerobic Oxidation and Enamine Catalysis in the Asymmetric α‐Amination of β‐Ketocarbonyls Using N‐Hydroxycarbamates as Nitrogen Sources |
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| Authors: | Changming Xu Dr Long Zhang Prof?Dr Sanzhong Luo |
| Institution: | 1. Beijing National Laboratory for Molecular Sciences (BNLMS), CAS Key Laboratory for Molecular Recognition and Function, Institute of Chemistry, The Chinese Academy of Sciences, Beijing, 100190 (China) http://luosz.iccas.ac.cn;2. Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, 300071 (China) |
| Abstract: | We describe herein an unprecedented asymmetric α‐amination of β‐ketocarbonyls under aerobic conditions. The process is enabled by a simple chiral primary amine through the coupling of a catalytic enamine ester intermediate and a nitrosocarbonyl (generated in situ) derived from N‐hydroxycarbamate. The reaction features high chemoselectivity and excellent enantioselectivity for a broad range of substrates. |
| Keywords: | aerobic oxidation α ‐amination β ‐ketocarbonyls enamine catalysis organocatalysis |