4.4 Article

Palladium-catalyzed intramolecular aerobic C-H amination of enamines for the synthesis of 2-trifluoromethylindoles

Journal

TETRAHEDRON
Volume 74, Issue 7, Pages 720-725

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2017.12.047

Keywords

C-H functionalization; Oxidative amination; Trifluoromethyl; Indole; Enamine

Funding

  1. National Natural Science Foundation of China [21272177]
  2. Natural Science Foundation of Zhejiang Province [LR15B020002]

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A new palladium-catalyzed C-H amination of aryl enamines for the synthesis of trifluoromethylated indoles is established. The attractive features of this transformation are the use of atom-economical O-2 as the oxidant and easily prepared enamines as substrates. A variety of pharmaceutically important 2-trifluoromethyl indoles can be targeted in moderate to good yields with good functional compatibility. (C) 2017 Elsevier Ltd. All rights reserved.

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