4.8 Article

One-Pot Approach to 8-Acylated 2-Quinolinones via Palladium-Catalyzed Regioselective Acylation of Quinoline N-Oxides

Journal

ORGANIC LETTERS
Volume 18, Issue 10, Pages 2411-2414

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00923

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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 one-pot facile and efficient protocol for 8-acylated 2-quinolinones has been developed through palladium-catalyzed acylation of quinoline N-oxides, which proceeds with high selectivity at the C8-position. The desired products were isolated in up to 95% yield and good functional group tolerance. A palladacycle was isolated from the catalytic process and proposed as a key intermediate.

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