## Abstract A new method is presented for the tritiation of aryl compounds with tritium gas which is conducted on the underivatized substrate. Combined directed ortho metallation and facile reduction of the carbonpotassium bond affords incorporation of tritium at high specific activity under mild c
Synthesis of [3H] vardenafil, Levitra®, using a new labeling technique
✍ Scribed by U. Pleiss
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- French
- Weight
- 133 KB
- Volume
- 46
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.782
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✦ Synopsis
Abstract
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.
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