4.8 Article

Direct Synthesis of Quinolines via Co(III)-Catalyzed and DMSO-Involved C-H Activation/Cyclization of Anilines with Alkynes

Journal

ORGANIC LETTERS
Volume 20, Issue 3, Pages 566-569

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b03673

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Funding

  1. National Natural Science Foundation of China [21502100, 81502909]
  2. Guangdong Natural Science Funds for Distinguished Young Scholar [2017A030306031]

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A unique Co(III)-catalyzed and DMSO-involved CH activation/cyclization of simple, cheap, and easily available anilines with alkynes for direct and highly efficient synthesis of privileged quinolines with exclusive regioselectivity and broad substrate/functional group tolerance and in good to excellent yields, Where DMSO was employed as both the solvent and the C-1 building block of quinoline products, is reported. Mechanistic experiments revealed that the versatile reaction might employ the 2-vinylbenzenamine species as the active intermediate.

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