Total synthesis of aigialomycin D using a Ramberg-Bäcklund/RCM strategy

J Org Chem. 2009 Mar 20;74(6):2271-7. doi: 10.1021/jo802561s.

Abstract

The bioactive resorcylic acid lactone aigialomycin D (1) has been synthesized by a novel combination of ring-closing metathesis (RCM) and Ramberg-Bäcklund reactions. This synthetic strategy enables the C1'-C2' alkene to be masked as a sulfone during formation of the macrocycle by ring closing metathesis at the C7'-C8' olefin, thus avoiding competing formation of a cyclohexene. A subsequent Ramberg-Bäcklund reaction efficiently produces the C1'-C2' E-alkene. This combined RCM/Ramberg-Bäcklund reaction strategy should be widely applicable to the synthesis of macrocyclic dienes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry
  • Cyclization
  • Lactones / chemistry
  • Macrocyclic Compounds / chemical synthesis
  • Macrolides / chemical synthesis*
  • Sulfones / chemistry

Substances

  • Alkenes
  • Lactones
  • Macrocyclic Compounds
  • Macrolides
  • Sulfones
  • aigialomycin D