Alkynylation of heterocyclic compounds using hypervalent iodine reagent

Abstract

The alkynylation of various nitrogen- and/or sulphur-containing heterocyclic compounds using hypervalent iodine TMS-EBX by utilization of tertiary amines under mild conditions is described. The developed metal-free methodology furnishes the corresponding alkynylated heterocycles bearing quaternary carbon in high yields.

Keywords

• structure-based design
• electrophilic alkynylation
• rhodanine derivatives
• conjugate addition
• endogenous opioids
• acid-derivatives
• inhibitors
• potent
• pyrazolones
• indole