Synthesis of 1,5-diaryl-2-fluoro-6,7-dioxabicyclo[3.2.2]nonanes with high antimalarial activity utilizing photoinduced electron-transfer oxygenation reactions

Masaki Kamata, Rie Maeda, Jun Hayakawa, Hye Sook Kim

Research output: Contribution to journalArticlepeer-review

Abstract

1,5-Diaryl-2-fluoro-6,7-dioxabicyclo[3.2.2]nonanes were synthesized from corresponding 3-fluoro-2,6-diarylhepta-1,6-dienes utilizing 2,4,6-triphenylpyrylium salt (TPPX: X = BF4, ClO4)-sensitized photoinduced electron-transfer (PET) oxygenation reactions, and their in-vitro antimalarial activity was evaluated. Results showed that these fluorinated bicyclic peroxides had higher antimalarial activity than their nonfluorinated parent bicyclic peroxides. In addition, it was shown that PET oxygenation reactions, particularly TPPX-biphenyl-cosensitized PET oxygenation reactions, are an efficient method for the construction of a C–O–O–C structure during the synthesis of fluorinated antimalarial bicyclic peroxides.

Original languageEnglish
Article number153752
JournalTetrahedron Letters
Volume96
DOIs
Publication statusPublished - Apr 27 2022

Keywords

  • Antimalarial activity
  • Fluorinated bicyclic peroxide
  • Photoinduced electron-transfer (PET) oxygenation
  • Triphenylpyrylium salt

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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