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

Abstract

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.