Journal of labelled compounds and radiopharmaceuticals p. 601 - 606 (1997)
Update date:2022-08-11
Topics:
Krause, Michael
Stark, Holger
Schunack, Walter
<125I>Iodoproxyfan, a specific radioligand of histamine H3 receptors, was synthesized in 60percent yield under very mild conditions from a tributylstannyl precursor.The arylstannane, which was obtained in a palladium-catalyzed reaction of arylbromide and hexabutylditin, smoothly underwent radioiodination with <125I>sodium iodide and chloramine-T to give tritylated <125I>iodoproxyfan.Final detritylation was achieved with formic acid 90percent at room temperature.Compared to the original copper(I)-mediated halogen exchange this procedure has major advantages in terms of cost and ease of use. - Key Words: Iodine-125; iododestannylation; <125I>iodoproxyfan; histamine H3 receptor antagonist.
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