4.7 Article

Copper-Catalyzed Azidative Multifunctionalization of Alkynes

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JOURNAL OF ORGANIC CHEMISTRY
卷 82, 期 23, 页码 12813-12820

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.7b02148

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  1. National NSF of China [21372041]
  2. Changbai Mountain Scholarship Program
  3. Fundamental Research Funds for the Central Universities [2412016KJ006]

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A facile and efficient copper-catalyzed azidative multifunctionalization of alkynes has been developed by using N-fluorobenzenesulfonimide (NFSI) as both nitrogen source and aryl source and trimethylsilyl azide (TMSN3) as azido source. This transformation proceeds under mild conditions, providing a series of alpha-azido-alpha-aryl imine in good yields by a single operation starting from a wide range of alkynes. The prepared alpha-azido-alpha-aryl imines could be easily converted into 1,5-piperizine-fused 1,2,3-triazoles and azido enamines.

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