Total Syntheses of Lobaric Acid and Its Derivatives from the Antarctic Lichen Stereocaulon alpinum

J Nat Prod. 2018 Jun 22;81(6):1460-1467. doi: 10.1021/acs.jnatprod.8b00227. Epub 2018 Jun 7.

Abstract

The first total syntheses of the natural products lobaric acid (1) and its derivatives isolated from the Antarctic lichen Stereocaulon alpinum are reported in this study. Lobarin (3), with a pseudodepsidone structure, was synthesized first in 11 steps by utilizing an Ullmann aryl ether coupling reaction, and lobaric acid was synthesized in an additional three steps by a seven-membered lactonization reaction. Various derivatives were also obtained from the prepared lobaric acid, and the synthetic compounds exhibited significant PTP1B inhibitory activities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antarctic Regions
  • Ascomycota / chemistry*
  • Depsides / chemistry
  • Lactones / chemistry*
  • Lichens / chemistry*
  • Phenyl Ethers / chemistry*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors
  • Salicylates / chemistry*

Substances

  • Depsides
  • Lactones
  • Phenyl Ethers
  • Salicylates
  • lobarin
  • lobaric acid
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1