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

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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‐[14C] was converted to potassium thiocyanate‐[14C] 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‐[2H4]‐diammonium dichloride.

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