A practical synthesis of indoles via a Pd-catalyzed C-N ring formation

Org Lett. 2014 Aug 15;16(16):4114-7. doi: 10.1021/ol5018118. Epub 2014 Jul 28.

Abstract

A method for the synthesis of N-functionalized C2-/C3-substituted indoles via Pd-catalyzed C-N bond coupling of halo-aryl enamines is described. The general strategy utilizes a variety of amines and β-keto esters which are elaborated into halo-aryl enamines as latent precursors to indoles. The preferred conditions comprising the RuPhos precatalyst and RuPhos in the presence of NaOMe in 1,4-dioxane tolerate a variety of substituents and are scalable for the construction of indoles in multigram quantities.

MeSH terms

  • Amines / chemistry
  • Catalysis
  • Cyclization
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Molecular Structure
  • Palladium / chemistry*

Substances

  • Amines
  • Indoles
  • Palladium