Progress toward the total synthesis of N-methylwelwitindolinone B isothiocyanate

Org Lett. 2014 Sep 5;16(17):4460-3. doi: 10.1021/ol5020043. Epub 2014 Aug 15.

Abstract

Progress toward the welwitindolinone alkaloid N-methylwelwitindolinone B isothiocyanate is reported. A key reaction to synthesize the [4.3.1] bicycle embedded in the core of the molecule is a furan type 2 intramolecular Diels-Alder reaction with a tetrasubstituted dienophile, which sets the two vicinal quaternary centers present in the natural product. The sterically encumbered cycloaddition precursor was synthesized using a Horner-Wadsworth-Emmons reaction followed by a Suzuki cross-coupling reaction. Finally, introduction of the secondary alkyl chloride was achieved by a regio- and diastereoselective opening of a [2.2.1] oxobicycloheptane functionality.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyanobacteria / chemistry
  • Indole Alkaloids / chemical synthesis*
  • Indole Alkaloids / chemistry
  • Molecular Structure

Substances

  • Indole Alkaloids
  • N-methylwelwitindolinone B isothiocyanate
  • welwitindolinone B isothiocyanate