Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H
Article first published online: 30 AUG 2011
Copyright © 2011 John Wiley & Sons, Ltd.
Journal of Labelled Compounds and Radiopharmaceuticals
Volume 54, Issue 11, pages 714–719, September 2011
How to Cite
Fontana, E., Pignatti, A., Venegoni, S. and Bray, M. A. (2011), Synthesis of 2H- and 14C-labeled fexinidazole and its primary metabolites labeled with 2H. J Label Compd Radiopharm, 54: 714–719. doi: 10.1002/jlcr.1914
- Issue published online: 13 OCT 2011
- Article first published online: 30 AUG 2011
- Manuscript Accepted: 23 JUN 2011
- Manuscript Revised: 23 MAY 2011
- Manuscript Received: 31 MAR 2011
- internal standard;
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.