4.4 Article

Copper-mediated N-arylation of methyl 2-aminothiophene-3-carboxylate with organoboron reagents

Journal

TETRAHEDRON LETTERS
Volume 56, Issue 49, Pages 6839-6842

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2015.10.080

Keywords

Thiophene; Cross-coupling; Copper; Amine; Carboxylate; Aryltrifluoroborate

Funding

  1. Higher Education Commission (HEC), Pakistan [112-24510-2PS1-388]
  2. National Institute of General Medical Sciences [R01 GM-081376]

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A practical protocol for the synthesis of N-arylated methyl 2-aminothiophene-3-carboxylate has been developed via Chan Lam cross-coupling. The desired products were synthesized by cross-coupling of methyl 2-aminothiophene-3-carboxylate with both arylboronic acids and potassium aryltrifluoroborate salts in moderate to good yields. A broad range of functional groups was well tolerated. (C) 2015 Elsevier Ltd. All rights reserved.

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