Total Synthesis of (±)-Kuwanol E

J Nat Prod. 2016 Oct 28;79(10):2495-2503. doi: 10.1021/acs.jnatprod.6b00350. Epub 2016 Sep 22.

Abstract

The total synthesis of the Diels-Alder-type adducts (±)-kuwanol E and the heptamethyl ether derivative of (±)-kuwanon Y has been accomplished via a convergent strategy involving 2'-hydroxychalcone 6 or 9 and dehydroprenylstilbene 7, in nine steps. The synthesis features, as a key step, a Lewis acid-mediated biomimetic intermolecular Diels-Alder [4+2] cycloaddition for the construction of the cyclohexene skeleton with three stereogenic centers. Notably, the endo/exo diastereoselectivity of the reaction proved to be temperature-controlled.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chalcones
  • Cyclohexenes
  • Flavonoids / chemical synthesis*
  • Flavonoids / chemistry
  • Models, Molecular
  • Molecular Structure
  • Stereoisomerism
  • Temperature

Substances

  • Chalcones
  • Cyclohexenes
  • Flavonoids
  • kuwanol E
  • cyclohexene
  • 2'-hydroxychalcone