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Synthesis of 3H- and 14C-ketanserin

✍ Scribed by Cor G. M. Janssen; Herman A. C. Lenoir; Jos B. A. Thijssen; Alfons G. Knaeps; Willy L. M. Verluyten; Jozef J. P. Heykants

Publisher: John Wiley and Sons
Year: 1988
Tongue: French
Weight: 342 KB
Volume: 25
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580250712

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✦ Synopsis

Ketanserin. 3-~2-~4-~4-fluorobenzoyl~-l-piperidinyllethyll-2,4(1H,3H)-quinazol- inedione is a new serotonin S2-receptor blocking agent used in hypertension and related diseases. Pharmacokinetic studies required the synthesis of monolabelled 3H-and 14C-ketanserin tartrate. The tritium compound had the label placed at the fluorobenzoyl moiety, whereas for 14C-ketanserin the heterocyclic part of the quinazolinedione system was chosen. Receptor binding studies and application in radioimunoassay necessitated the synthesis of a molecule at higher specific activity, hence a dilabelled molecule was constructed with tritium atoms placed at opposite positions in the molecule. The title compounds were obtained at specific activities of 169.5, 4.66 and 34900 mCi/mmol, respectively and with HPLC purities of > 98%.

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