Synthesis of (±)-Bisavenanthramide B-6 by an Anionic Anhydride Mannich Reaction

Org Lett. 2016 Apr 15;18(8):1740-3. doi: 10.1021/acs.orglett.6b00413. Epub 2016 Mar 29.

Abstract

Bisavenanthramide B-6 (2) is a highly substituted γ-lactam derived from oat leaves. Development of a new base-promoted anhydride Mannich reaction with N-sulfonylated imines that forms the core structure of 2 in a single step is presented. Further elaboration allows for a facile one-pot double Buchwald N-arylation to install the final rings onto the densely substituted γ-lactam core. This route provides the natural product in a longest linear sequence of nine steps.

Publication types

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

MeSH terms

  • Anhydrides / chemical synthesis*
  • Anhydrides / chemistry
  • Anions / chemistry*
  • Catalysis
  • Cyclization
  • Lactams / chemical synthesis*
  • Lactams / chemistry
  • Molecular Structure
  • Stereoisomerism

Substances

  • Anhydrides
  • Anions
  • Lactams
  • bisavenanthramide B-6