4.4 Article

Solvent-free mechanochemical Buchwald-Hartwig amination of aryl chlorides without inert gas protection

Journal

TETRAHEDRON LETTERS
Volume 59, Issue 23, Pages 2277-2280

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2018.04.078

Keywords

Mechanochemistry; Aryl chloride; Buchwald-Hartwig amination; Inert gas protection free

Funding

  1. Special Program for Key Basic Research of the Ministry of Science and Technology of the People's Republic of China [2014CB460608]
  2. National Natural Science Foundation of China [21376221, 21406201]
  3. Prominent Ph.D. Thesis Supporting Project of Zhejiang University of Technology

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A solvent-free Buchwald-Hartwig amination had been developed under high-speed ball-milling conditions, which afforded the desired products with moderate to high yields. The addition of sodium sulfate was found to be crucial for improving both the performance and the reproducibility. Comparative solvent-free stirring experiments implicated the importance of mechanical interaction for the transformation, and the inert gas was proved to be unnecessary for this amination. (C) 2018 Elsevier Ltd. All rights reserved.

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