Papers

May, 2003

Antimalarial activity of novel 1,2,5,6-tetraoxacycloalkanes and 1,2,5-trioxacycloalkanes

JOURNAL OF MEDICINAL CHEMISTRY
  • HS Kim
  • ,
  • E Begum
  • ,
  • N Ogura
  • ,
  • Y Wataya
  • ,
  • Y Nonami
  • ,
  • T Ito
  • ,
  • A Masuyama
  • ,
  • M Nojima
  • ,
  • KJ McCullough

Volume
46
Number
10
First page
1957
Last page
1961
Language
English
Publishing type
Research paper (scientific journal)
DOI
10.1021/jm020387b
Publisher
AMER CHEMICAL SOC

Photooxygenation of 2-phenylnorbornene 1 in the presence of 30% aqueous hydrogen peroxide afforded 1,2-bishydroperoxide 3, which could be cycloalkylated on treatment with silver oxide and a 1,omega-diiodoalkane to provide the tricyclic peroxides 12. Trimethylsilylation of 3 followed by TMSOTf-catalyzed cyclocondensation with carbonyl compounds led to the formation of the tricyclic peroxides 14 containing a 1,2,4,5-tetroxepane structure. Photooxygenation of 1 in the presence of either unsaturated hydroperoxides or unsaturated alcohols followed by bis(collidine)iodine hexafluorophosphate promoted cyclization gave the corresponding cyclic peroxides 15-17. Several of these cyclic peroxides showed substantial antimalarial activity particularly in vitro.

Link information
DOI
https://doi.org/10.1021/jm020387b
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000182709200019&DestApp=WOS_CPL
ID information
  • DOI : 10.1021/jm020387b
  • ISSN : 0022-2623
  • eISSN : 1520-4804
  • Web of Science ID : WOS:000182709200019

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