Synthesis of [ 14 C]‐labelled vardenafil hydrochloride and metabolites | Zendy

Seidel D. | Zendy; Brehmer P. | Zendy; Schoof Y. | Zendy; Weinberg U. | Zendy; Nowakowski M. | Zendy

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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.

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