4.3 Article

Copper-catalyzed tandem cyclization and vinylation for the synthesis of 2-trifluoromethyl benzofurans

Journal

JOURNAL OF FLUORINE CHEMISTRY
Volume 228, Issue -, Pages -

Publisher

ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2019.109418

Keywords

Trifluoromethyl; Benzofuran; Copper-catalyzed; C-O bonds formation; Tandem reaction

Funding

  1. Natural Science Foundation of Zhejiang Province [LR15B020002]
  2. Natural Science Foundation of Guangxi Province [2018GXNSFDA281011]

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A copper-catalyzed tandem cyclization and vinylation of 2-chloro-1-(2-bromoaryl)-3,3,3-trifluoropropenes with KOH has been developed for the synthesis of 2-trifluoromethyl benzofuran derivatives. The reaction involves dual C-O bonds formation and hydroarylation of aryl trifluoropropynes. This approach represents a simple and efficient one-pot synthesis of 2-trifluoromethy-3-vinylbenzofurans, which are potentially useful in drug design.

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