4.5 Article

Copper-Catalyzed Intramolecular Oxidative C(sp3)- H Amidation of 2-Aminoacetophenones: Efficient Synthesis of Indoline-2,3-diones

Journal

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2014, Issue 14, Pages 2878-2882

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201400012

Keywords

Nitrogen heterocycles; Fused-ring systems; Amidation; Copper; C-H activation

Funding

  1. National Natural Science Foundation of China (NSFC) [21202167, 21072190, 21272233]
  2. Guangdong Natural Science Foundation [S2011020000806]

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An efficient synthesis of diverse indoline-2,3-diones from 2-aminoacetophenones through copper-catalyzed intramolecular C(sp(3))-H amidation is developed. The reaction proceeds in DMSO by using O-2 as the sole oxidant to provide the desired products in moderate to good yields.

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