4.7 Article

Copper-Catalyzed Regioselective sp3 C-H Azidation of Alkyl Substituents of Indoles and Tetrahydrocarbazoles

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 84, Issue 18, Pages 11885-11890

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.9b01742

Keywords

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Funding

  1. NSFC [21871296, 21907111]
  2. Guangdong Natural Science Founds for Distinguished Young Scholars [2017A030306017]
  3. Guangdong Provincial Key Laboratory of Construction Foundation [2017B030314030]

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An efficient regioselective sp(3) C-H azidation is developed using CuBr as the catalyst and Zhdankin azidoiodinane as the N-3 source. Under simple and mild reaction conditions, the azido group could be successfully incorporated into the sp(3) C-H alkyl substituents of indoles and tetrahydrocarbazoles.

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