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E. Fontana, Alberto Pignatti, Serena Venegoni and Michael A. Bray Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H Journal of Labelled Compounds and Radiopharmaceuticals 54

Version of Record online: 30 AUG 2011 | DOI: 10.1002/jlcr.1914

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The preparation of deuterium labeled fexinidazole, a 5-nitroimidazole drug candidate for the treatment of Human African Trypanosomiasis, and its two main metabolites (fexinidazole sulfoxide and fexinidazole sulfone) for use as internal standards for liquid chromatography-mass spectrometry are reported. Additionally, the synthesis of a 14 C-labeled version of fexinidazole for absorption, distribution, metabolism, and excretion studies is also described via a five-step procedure starting from commercially available potassium [14 C]cyanide.

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