A biomimetic strategy to access the silybins: total synthesis of (-)-isosilybin A

Org Lett. 2015 Jan 2;17(1):98-101. doi: 10.1021/ol503303w. Epub 2014 Dec 17.

Abstract

We report the first asymmetric, total synthesis of (-)-isosilybin A. A late-stage catalytic biomimetic cyclization of a highly functionalized chalcone is employed to form the characteristic benzopyranone ring. A robust and flexible approach to this chalcone provides an entry to the preparation of the entire isomeric family of silybin natural products.

Publication types

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

MeSH terms

  • Biological Products / chemical synthesis*
  • Biological Products / chemistry
  • Catalysis
  • Chalcone / chemistry
  • Cyclization
  • Molecular Structure
  • Silybum marianum / chemistry
  • Silymarin / analogs & derivatives*
  • Silymarin / chemical synthesis
  • Silymarin / chemistry
  • Stereoisomerism

Substances

  • Biological Products
  • Silymarin
  • Chalcone
  • isosilybin A