4.8 Article

C8-Selective Acylation of Quinoline N-Oxides with α-Oxocarboxylic Acids via Palladium-Catalyzed Regioselective C-H Bond Activation

Journal

ORGANIC LETTERS
Volume 18, Issue 15, Pages 3722-3725

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b01746

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Funding

  1. NSF of China [21572072]
  2. Science and Technology Innovation Program of Universities in Henan Province [16HASTIT007]
  3. Zhengzhou University

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A facile and efficient protocol for palladium-catalyzed C8-selective acylation of quinoline N-oxides with alpha-oxocarboxylic acids has been developed. In this approach, N-oxide was utilized as a stepping stone for the remote C-H functionalization. The reaction proceeded efficiently under mild reaction conditions with excellent regioselectivity and broad functional group tolerance.

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