An asymmetric pericyclic cascade approach to 3-alkyl-3-aryloxindoles: generality, applications and mechanistic investigations

Org Biomol Chem. 2015 Feb 14;13(6):1807-17. doi: 10.1039/c4ob02526a.

Abstract

The reaction of L-serine derived N-arylnitrones with alkylarylketenes generates asymmetric 3-alkyl-3-aryloxindoles in good to excellent yields (up to 93%) and excellent enantioselectivity (up to 98% ee) via a pericyclic cascade process. The optimization, scope and applications of this transformation are reported, alongside further synthetic and computational investigations. The preparation of the enantiomer of a Roche anti-cancer agent (RO4999200) 1 (96% ee) in three steps demonstrates the potential utility of this methodology.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cyclization
  • Ethylenes / chemistry
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Ketones / chemistry
  • Molecular Structure
  • Nitrogen Oxides / chemistry
  • Oxindoles
  • Quantum Theory

Substances

  • Ethylenes
  • Indoles
  • Ketones
  • Nitrogen Oxides
  • Oxindoles
  • nitrones
  • 2-oxindole
  • ketene