Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H

Abstract

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.

Citation

Fontana, E.; Pignatti, A.; Venegoni, S.; Bray, M. A. Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H. Journal of Labelled Compounds and Radiopharmaceuticals (2011) 54 (11) 714-719. [DOI: 10.1002/jlcr.1914]

Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H

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