Cobalt(III)-Catalyzed C2-Selective C-H Alkynylation of Indoles

Org Lett. 2015 Aug 21;17(16):4094-7. doi: 10.1021/acs.orglett.5b02038. Epub 2015 Aug 11.

Abstract

A cobalt(III)-catalyzed C-2 selective C-H alkynylation of indoles using hypervalent iodine-alkyne reagents is described. A broad range of synthetically useful functional groups (-F, -Cl, -Br, -CO2Me, -CN) were tolerated, providing an efficient and robust protocol for the synthesis of C-2 alkynylated indoles. The pyrimidyl and silyl protecting groups could be easily removed to give the corresponding 2-ethynyl-1H-indole.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemical synthesis*
  • Alkynes / chemistry*
  • Catalysis
  • Cobalt / chemistry*
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Iodine / chemistry
  • Molecular Structure

Substances

  • Alkynes
  • Indoles
  • Cobalt
  • Iodine