4.8 Article

Intramolecular, Site-Selective, Iodine-Mediated, Amination of Unactivated (sp3)C-H Bonds for the Synthesis of Indoline Derivatives

Journal

ORGANIC LETTERS
Volume 19, Issue 11, Pages 2793-2796

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b00846

Keywords

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Funding

  1. Natural Science Foundation of China [21373003, 21676076]
  2. Natural Science Foundation of Hunan Province, China [2016JJ3034]
  3. Hunan Youth Talent [2016RS3023]
  4. Chinese Scholarship Council
  5. Grants-in-Aid for Scientific Research [16H06039] Funding Source: KAKEN

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The Iodine-mediated oxidative intramolecular amination of anilines via cleavage of unactivated (sp(3))C-H and N-H borids for the production of indolines is described, This transition-metal-free approach provides a straightforward strategy for producing (Sp(3))C-N bonds for use in the preferential functionalization of unactivated (sp(3))C-H bonds Over (sp(2))C-H bonds. The reaction could be performed on a gram scale for the synthesis of functionalized indolines.

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