4.8 Article

FeCl3-Mediated Synthesis of 2-(Trifluoromethyl)quinazolin-4(3H)-ones from Isatins and Trifluoroacetimidoyl Chlorides

Journal

ORGANIC LETTERS
Volume 22, Issue 14, Pages 5567-5571

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c01927

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Funding

  1. National Natural Science Foundation of China [21772177]
  2. Natural Science Foundation of Zhejiang Province [LY19B020016]
  3. Fundamental Research Funds of Zhejiang Sci-Tech University [2019Q065]

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An FeCl3-mediated cascade coupling/decarbonylative annulation reaction for the efficient construction of 2-(trifluoromethyl)quinazolin-4(3H)-ones has been developed. This transformation employs readily available isatins and trifluoroace-timidoyl chlorides as the starting materials, providing a facile and practical route to diverse biologically relevant quinazolin-4(3H)one derivatives. A plausible reaction pathway has been proposed based on the mechanistic observations.

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