Lawesson's reagent-initiated domino reaction of aminopropenoyl cyclopropanes: synthesis of thieno[3,2-c]pyridinones

Org Biomol Chem. 2012 Feb 28;10(8):1639-44. doi: 10.1039/c2ob06709a. Epub 2012 Jan 11.

Abstract

A convenient and efficient synthesis of substituted 2,3-dihydrothieno[3,2-c]pyridin-4(5H)-ones has been developed and relies upon a domino reaction of dimethylaminopropenoyl cyclopropanes initiated by Lawesson's reagent. A mechanism involving regioselective thionation, ring-enlargement, and an intramolecular aza-cyclization sequence is proposed. This protocol was utilized as a one-pot route to thieno[3,2-c]pyridin-4(5H)-ones with DDQ as an oxidant.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry*
  • Amination
  • Cyclopropanes / chemistry*
  • Molecular Structure
  • Pyridones / chemical synthesis*

Substances

  • Alkenes
  • Cyclopropanes
  • Pyridones
  • propylene