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Synthesis of 2 H‐ and 14 C‐labeled fexinidazole and its primary metabolites labeled with 2 H
Author(s) -
Fontana E.,
Pignatti Alberto,
Venegoni Serena,
Bray Michael A.
Publication year - 2011
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1914
Subject(s) - chemistry , sulfoxide , cyanide , radiochemistry , mass spectrometry , sulfone , chromatography , potassium cyanide , chemical synthesis , high performance liquid chromatography , nuclear chemistry , organic chemistry , biochemistry , in vitro
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.