Synthesis of Indole-2-carboxylate Derivatives via Palladium-Catalyzed Aerobic Amination of Aryl C-H Bonds

Org Lett. 2016 Aug 5;18(15):3586-9. doi: 10.1021/acs.orglett.6b01592. Epub 2016 Jul 12.

Abstract

A direct oxidative C-H amination affording 1-acetyl indolecarboxylates starting from 2-acetamido-3-arylacrylates has been achieved. Indole-2-carboxylates can be targeted with a straightforward deacetylation of the initial reaction products. The C-H amination reaction is carried out using a catalytic Pd(II) source with oxygen as the terminal oxidant. The scope and application of this chemistry is demonstrated with good to high yields for numerous electron-rich and electron-poor substrates. Further reaction of selected products via Suzuki arylation and deacetylation provides access to highly functionalized indole structures.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amination
  • Catalysis
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Molecular Structure
  • Organometallic Compounds / chemistry*
  • Palladium / chemistry*

Substances

  • Indoles
  • Organometallic Compounds
  • indole-2-carboxylate
  • Palladium