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Synthesis and antimalarial activities of structurally simplified 1,2,4-trioxanes related to artemisinin
Authors:Gary H Posner  Chang H Oh  Lucia Gerena  Wilbur K Milhous
Abstract:Eleven derivatives of the clinically useful, antimalarial, 1,2,4-trioxane artemisinin have been synthesized in only several steps from commercial cyclohexanones. Of these simple, tricyclic 1,2,4-trioxanes, 10 showed considerable in vitro antimalarial activity, with one being as potent as artemisinin. Some structure-activity relationship generalizations are made from this series of artemisinin analogs. Triethylsilyl hydrotrioxide (Et3SiOOOH), prepared in situ from ozone and triethylsilane, is shown to be a mild, fastacting, and effective dioxetane-forming reagent with vinyl ethers and with a vinyl thioether on relatively small (50–100 mg) scale.
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