Preparation of the isomeric azaindoline family by intramolecular carbolithiation

Org Lett. 2008 Mar 20;10(6):1071-4. doi: 10.1021/ol702862d. Epub 2008 Feb 14.

Abstract

An operationally convenient, one-pot, three-step sequence has been developed that provides access to 3-substituted 4-, 5-, 6-, and 7-azaindolines (2,3-dihydro-1H-pyrollopyridines) via intramolecular carbolithiation of the aryllithium derived from an appropriate (N,N-diallylamino)bromopyridine. Whereas cyclization proceeds as expected to give 1-allyl-3-methyl-4-azaindoline and 1-allyl-3-methyl-6-azaindoline following protonation of the 3-CH2Li group of the azaindoline, the isomeric 3-methyl-5-azaindoline and 3-methyl-7-azaindoline are generated as 3-methyl-N-allyl anions prior to quench with MeOH.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aza Compounds / chemistry*
  • Indoles / chemistry*
  • Isomerism
  • Lithium / chemistry*

Substances

  • Aza Compounds
  • Indoles
  • indoline
  • Lithium