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Synthesis of [14C]-labelled vardenafil hydrochloride and metabolites

✍ Scribed by D. Seidel; P. Brehmer; Y. Schoof; U. Weinberg; M. Nowakowski

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
179 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

For studies of pharmacokinetics and drug metabolism of the new orally active, selective phosphodiesterase type V (PDE V) inhibitor vardenafil (Levitra^®^), the ^14^C‐labelled version was synthesised. Starting from the cyanation of 2‐iodophenol with K^14^CN, an 8‐step synthesis led to two batches with 0.727 g (2.857 GBq) and 2.199 g (5.497 GBq) of [triazinone‐^14^C]vardenafil hydrochlo‐ride with different specific radioactivities. The label was located in position 2 of the imidazotriazinone moiety. Several carbon‐14 labelled metabolites were synthesised as reference compounds for metabolism studies. Copyright © 2003 John Wiley & Sons, Ltd.

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