Synthesis of Vitisins A and D Enabled by a Persistent Radical Equilibrium

J Am Chem Soc. 2020 Apr 8;142(14):6499-6504. doi: 10.1021/jacs.0c01714. Epub 2020 Mar 24.

Abstract

The first total synthesis of the resveratrol tetramers vitisin A and vitisin D is reported. Electrochemical generation and selective dimerization of persistent radicals is followed by thermal isomerization of the symmetric C8b-C8c dimer to the C3c-C8b isomer, providing rapid entry into the vitisin core. Computational results suggest that this synthetic approach mimics Nature's strategy for constructing these complex molecules. Sequential acid-mediated rearrangements consistent with the proposed biogenesis of these compounds afford vitisin A and vitisin D. The rapid synthesis of these complex molecules will enable further study of their pharmacological potential.

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

  • Benzofurans / chemical synthesis*
  • Humans
  • Molecular Structure
  • Phenols / chemical synthesis*

Substances

  • Benzofurans
  • Phenols
  • vitisin D
  • vitisin A