A new derivative detected in accelerated ageing of artesunate-amodiaquine fixed dose combination tablets


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Abstract

Graphical abstractHighlightsA new impurity formed during heating of Artesunate tablets was detected by HPLC.Impurity B was identified as a 9,10-dehydrotetrahydrofuranyl acetate derivative.The same compound was alternatively prepared from anhydrodihydroartemisinin + FeII salt.2-Deoxy-4α-hydroxy-9,10-anhydrodihydroartemisinin was also formed in this treatment.An unknown impurity detected in small amounts during the heat treatment of artesunate-amodiaquine bilayer tablets was purified by semipreparative HPLC and identified by MS and NMR as the tetrahydrofuranyl acetate-rearranged derivative of anhydrodihydroartemisinin. When anhydrodihydroartemisinin was treated with a FeII salt in acetonitrile–water solution, the same product was generated, together with an isomeric 2-deoxy-4α-hydroxy-anhydrodihydroartemisinin derivative, as expected from the usual homolytic radical opening of the endoperoxide bond previously described for other artemisinin derivatives.

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