183155-67-1Relevant articles and documents
Iododestannylation: An Improved Synthesis of Iodoproxyfan, a Specific Radioligand of the Histamine H3 Receptor
Krause, Michael,Stark, Holger,Schunack, Walter
, p. 601 - 606 (2007/10/03)
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 sodium iodide and chloramine-T to give tritylated 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; iodoproxyfan; histamine H3 receptor antagonist.