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

摘要

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.