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Synthesis of [ 14 C]‐labelled vardenafil hydrochloride and metabolites
Author(s) -
Seidel D.,
Brehmer P.,
Schoof Y.,
Weinberg U.,
Nowakowski M.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.736
Subject(s) - vardenafil , chemistry , cyanation , moiety , pharmacokinetics , stereochemistry , metabolism , bioavailability , hydrochloride , pharmacology , biochemistry , sildenafil , tadalafil , medicine , catalysis
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.