Total Synthesis of Chalaniline A: An Aminofulvene Fused Chromone from Vorinostat-Treated Fungus Chalara sp. 6661

J Org Chem. 2024 Oct 4;89(19):14601-14605. doi: 10.1021/acs.joc.4c01855. Epub 2024 Sep 23.

Abstract

Chalaniline A, an aminofulveno[1,2-b]chromone derivative previously isolated from a vorinostat-treated ascomycete Chalara sp., was prepared in nine steps from orcinol (3,5-dihydroxytoluene). In a key transformation, the tricyclic ring system of the target was generated by a pyrrolidine-catalyzed double annulation between α-(methylsulfinyl)-2,6-dihydroxy-4-methylacetophenone and the ketaldoester, methyl 2,5-dioxopentanoate. The resulting tertiary alcohol (coniochaetone H) was further converted to chalaniline A by operations including dehydration (to yield a hydroxyfulvene), Vilsmeier reaction, and enamine exchange.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Ascomycota* / chemistry
  • Chromones* / chemical synthesis
  • Chromones* / chemistry
  • Chromones* / pharmacology
  • Hydroxamic Acids / chemistry
  • Molecular Structure
  • Vorinostat* / chemistry
  • Vorinostat* / pharmacology

Substances

  • Chromones
  • Vorinostat
  • Hydroxamic Acids