New versatile Pd-catalyzed alkylation of indoles via nucleophilic allylic substitution: controlling the regioselectivity

Org Lett. 2004 Sep 2;6(18):3199-202. doi: 10.1021/ol048663z.

Abstract

[reaction: see text] A systematic study addressed toward the optimization of the Pd-catalyzed alkylation of indoles by allylic carbonates is presented. The protocol uses a catalytic amount of [PdCl(pi-allyl)](2)/phosphine as a promoting agent, providing allylindoles in excellent yields. The regioselectivity of the reaction can be controlled by a proper choice of the base and the reaction media. The method proved to be effective also for intramolecular allylic alkylations of indolyl carbonates, providing a flexible route to fused indole alkaloids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Carbonates / chemistry
  • Catalysis
  • Indole Alkaloids / chemical synthesis*
  • Indoles / analysis
  • Indoles / chemistry*
  • Molecular Structure
  • Palladium / chemistry*

Substances

  • Carbonates
  • Indole Alkaloids
  • Indoles
  • Palladium