Asymmetric indoline synthesis via intramolecular aza-Michael addition mediated by bifunctional organocatalysts

Org Lett. 2013 Jul 19;15(14):3658-61. doi: 10.1021/ol401538b. Epub 2013 Jul 11.

Abstract

A novel method for the asymmetric synthesis of 2-substituted indolines, employing bifunctional amino(thio)urea catalysts, was developed. The reaction proceeded via an intramolecular aza-Michael addition mediated by activation through hydrogen bonding. The catalytic process was shown to be highly versatile and applicable to a wide range of substrates due to the flexible catalytic mechanism utilizing a noncovalent interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Hydrogen Bonding
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Molecular Structure
  • Stereoisomerism
  • Thiourea / chemistry*

Substances

  • Indoles
  • indoline
  • Thiourea