4.4 Article

Copper-catalyzed annulation of 2-bromobenzoic esters with terminal alkynes towards 3-substituted isocoumarins

Journal

TETRAHEDRON LETTERS
Volume 58, Issue 25, Pages 2433-2437

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2017.05.019

Keywords

Isocoumarins; Copper catalysis; Terminal alkynes; 2-Bromobenzoic esters

Funding

  1. National NSF of China [21573065, 21172062, 21273066]
  2. NSF of Hunan Province [2016JJ1007]

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An efficient method for the synthesis of 3-substituted isocoumarins that are an important class of biologically active scaffolds via annulation of 2-bromobenzoic esters with terminal alkynes by copper catalyzed is described. The advantages of this method include mild reaction conditions, high yield and regioselectivity, and wide tolerance toward functional groups. (C) 2017 Elsevier Ltd. All rights reserved.

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