Regioselective metal-free one-pot synthesis of functionalized 2-aminothiophene derivatives

J Org Chem. 2015 May 1;80(9):4611-7. doi: 10.1021/acs.joc.5b00488. Epub 2015 Apr 23.

Abstract

A facile metal-free synthesis of 2-aminothiophene derivatives by the reaction of 2-ynals with thioamides in alcohols has been developed. This transformation allows the assembly of 2-aminothienyl ether derivatives via a well-designed aldol condensation/regioselective intramolecular cyclization/conjugate addition cascade reaction and provides a straightforward synthetic protocol for constructing 2,3,5-trisubstituted 2-aminothiophenes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemistry*
  • Molecular Structure
  • Stereoisomerism
  • Thioamides / chemistry*
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry

Substances

  • Alkynes
  • Thioamides
  • Thiophenes