Approaches to polycyclic 1,4-dioxygenated xanthones. Application to total synthesis of the aglycone of IB-00208

Org Lett. 2015 Jan 2;17(1):114-7. doi: 10.1021/ol503336t. Epub 2014 Dec 16.

Abstract

Hexacyclic xanthone natural products such as IB-00208 present a formidable challenge in organic synthesis. A new approach to polycyclic 1,4-dioxygenated xanthones from benzocyclobutenones has been developed and applied to the first total synthesis of the aglycone of IB-00208. The 22-step synthesis features an acetylide stitching process that joins an aryl aldehyde with an angularly fused benzocyclobutenone, which was prepared by a ring-closing metathesis reaction. The resulting acetylenic benzocyclobutenone diol underwent a Moore rearrangement to give an intermediate that was further elaborated to the aglycone of IB-00208 as a mixture of hydroquinone-quinone tautomers.

Publication types

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

MeSH terms

  • Alcohols / chemistry
  • Biological Products / chemical synthesis*
  • Biological Products / chemistry
  • Glucosides / chemical synthesis*
  • Glucosides / chemistry
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Xanthenes / chemical synthesis*
  • Xanthenes / chemistry
  • Xanthones / chemistry*

Substances

  • Alcohols
  • Biological Products
  • Glucosides
  • IB 00208
  • Xanthenes
  • Xanthones