4.8 Article

Copper-Catalyzed Aerobic Oxidative Amination of sp3C-H Bonds: Efficient Synthesis of 2-Hetarylquinazolin-4(3H)-ones

Journal

ORGANIC LETTERS
Volume 16, Issue 14, Pages 3672-3675

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol501454j

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Funding

  1. NSFC [21172062, 21273067, 21373080]
  2. Fundamental Research Funds for the Central Universities (Hunan University)

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An efficient synthesis of 2-hetarylquinazolin-4(3H)-ones via copper-catalyzed direct aerobic oxidative amination of sp(3)C-H bonds has been developed. This tandem oxidation-amination-cyclization transformation represents a straightforward protocol to prepare 2-hetaryl-substituted quinazolinones from easily available 2-aminobenzamides and (2-azaaryl)methanes.

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