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

✍ Scribed by E. Fontana; Alberto Pignatti; Serena Venegoni; Michael A. Bray

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
419 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

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. Copyright © 2011 John Wiley & Sons, Ltd.

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