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Updated: May 31, 2026

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Synthesis of antitrypanosomal 1,2-dioxane derivatives based on a natural product scaffold
Harish Holla1, Mehdi Labaied, Ngoc Pham
1Eskitis Institute, Griffith University, Brisbane QLD4111, Australia.
Abstract:
A short practical synthesis of a new natural product based scaffold (6), based on antitrypanosomal and antimalarial compounds isolated from different Plakortis species is described. The scaffold contains a peroxide unit that is surprisingly stable to chemical manipulation elsewhere in the molecule, enabling it to be elaborated into a small library of derivatives. It is stable to ozonolysis, reductive work-up with dimethylsulfide and the Wittig reaction with stabilized phosphorus ylides. The scaffold along with its Wittig analogues has displayed low to sub-micro molar (0.2-3.3 microM) antitrypanosomal activity.
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