4.6 Article

Ready synthesis of free N-H 2-arylindoles via the copper-catalyzed amination of 2-bromo-arylacetylenes with aqueous ammonia and sequential intramolecular cyclization

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 9, Issue 13, Pages 4983-4986

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05549f

Keywords

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Funding

  1. National Natural Science Foundation of China [20876021, 20923006]
  2. Education Department of Liaoning Province [2009S021]
  3. Program for Changjiang Scholars and Innovative Research Team in University [IRT0711]

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A wide range of free N-H 2-arylindoles were synthesised via the copper(II)-catalyzed amination of 2-bromo-arylacetylenes with aqueous ammonia and sequential intramolecular cyclization. The convenience and atom economy of aqueous ammonia, and the low cost of the copper catalytic system make this protocol readily superior in practical application.

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