D. Seidel, M. Conrad, Y. Schoof
Nov 1, 2002
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0
Influential Citations
3
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
For studies of pharmacokinetics and drug metabolism of the new 5-HT1A agonist repinotan, the 14C-labelled version was synthesized. Starting from [U-14C]phenol, a 10-step synthesis led to 457 mg (1.58 GBq) of [U-14C]repinotan hydrochloride, labelled uniformly in the aromatic ring of the chromane moiety. For a study in man, a mono-carbon-14 labelled substance was required. Therefore a 7-step synthesis was performed starting from [carbonyl-14C]2-hydroxy-acetophenone. The yield was 106 mg (0.396 GBq) of [4-chromane-14C]repinotan hydrochloride. The carbon-14 labelled major metabolite, hydroxylated in the 6-position of the chromane moiety, was synthesised as reference compound. Copyright © 2002 John Wiley & Sons, Ltd.