A modern approach to the synthesis of 2-(4-chlorophenyl)[2- 14C]thiazol-4-ylacetic acid ([14C] fenclozic acid) and its acyl glucuronide metabolite
Article first published online: 11 JAN 2013
Copyright © 2013 John Wiley & Sons, Ltd.
Journal of Labelled Compounds and Radiopharmaceuticals
Volume 56, Issue 1, pages 17–21, January 2013
How to Cite
Killick, D. A. and Bushby, N. (2013), A modern approach to the synthesis of 2-(4-chlorophenyl)[2- 14C]thiazol-4-ylacetic acid ([14C] fenclozic acid) and its acyl glucuronide metabolite. J Label Compd Radiopharm, 56: 17–21. doi: 10.1002/jlcr.2985
- Issue published online: 24 JAN 2013
- Article first published online: 11 JAN 2013
- Manuscript Accepted: 17 OCT 2012
- Manuscript Revised: 23 AUG 2012
- Manuscript Received: 15 JUN 2012
- fenclozic acid;
- acyl glucuronide;
An updated approach to the 1960s synthesis of [14C] fenclozic acid from labelled potassium cyanide is presented. By employing modern synthetic methodology and purification techniques, many of the inherent hazards in the original synthesis are avoided or significantly reduced. The concomitant labelled stereoselective synthesis of the key acyl glucuronide metabolite (the 1-β-O-acyl glucuronide) is also described.