Total Synthesis of Hyperforin

J Am Chem Soc. 2015 Aug 26;137(33):10516-9. doi: 10.1021/jacs.5b06939. Epub 2015 Aug 13.

Abstract

A 10-step total synthesis of the polycyclic polyprenylated acylphloroglucinol (PPAP) natural product hyperforin from 2-methylcyclopent-2-en-1-one is reported. This route was enabled by a diketene annulation reaction and an oxidative ring expansion strategy designed to complement the presumed biosynthesis of this complex meroterpene. The described work enables the preparation of a highly substituted bicyclo[3.3.1]nonane-1,3,5-trione motif in only six steps and thus serves as a platform for the construction of easily synthesized, highly diverse PPAPs modifiable at every position.

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

  • Chemistry Techniques, Synthetic
  • Oxidation-Reduction
  • Phloroglucinol / analogs & derivatives*
  • Phloroglucinol / chemical synthesis
  • Phloroglucinol / chemistry
  • Terpenes / chemical synthesis*
  • Terpenes / chemistry

Substances

  • Terpenes
  • Phloroglucinol
  • hyperforin