𝔖 Bobbio Scriptorium
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Synthesis of labelled bioactive compounds. III. 2-(arylimino)-imidazolidine labeled with 14C, tritium and deuterium

✍ Scribed by M. Stiasni; H. Stähle

Publisher
John Wiley and Sons
Year
1978
Tongue
French
Weight
266 KB
Volume
14
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Five compounds of a group of 2‐(arylimino)‐imidazolidines, among them Clonidine (St 155), have been labeled with ^14^ in the following manner: Potassium cyanide‐[^14^C] was converted to potassium thiocyanate‐[^14^C] and subsequently to the N′‐phenylthiourea using benzoyl chloride and the corresponding aniline. The thiourea was saponified and reacted with methyl iodide to give the quaternary isothiourea derivative. Ring closure to the imidazolidine was achieved through condensation with ethylenediamine. ‐ Tritium labeled Clonidine was obtained by catalytic debromination of the 4‐bromoderivative with tritium gas. ‐ The starting material for deuteroclonidine was ethylene‐[^2^H~4~]‐diammonium dichloride.

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