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Synthesis of [ 3 H] vardenafil, Levitra ® , using a new labeling technique
Author(s) -
Pleiss U.
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.782
Subject(s) - chemistry , vardenafil , radiochemistry , specific activity , lithium (medication) , tritium , amide , aluminum hydride , nuclear chemistry , stereochemistry , enzyme , organic chemistry , sildenafil , tadalafil , medicine , physics , nuclear physics , catalysis , endocrinology , methoxide
Tritium was introduced into the new orally active, selective phosphodiesterase type V (PDE V) inhibitor vardenafil (Levitra ® ), by reduction of a suitable amide precursor with freshly prepared lithium aluminum tritide. A specific activity of 52.7 Ci/mmol (1.95 TBq/mmol) was achieved. In order to overcome the usual technical difficulties during the preparation of complex tritides a new and easy labeling technique which has considerable potential for various tritia‐tion procedures, was developed. Copyright © 2003 John Wiley & Sons, Ltd.