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Online Short Courses

Radiosynthesis of 123I-labelled benzimidazoles as novel single-photon emission computed tomography tracers for the histamine H3 receptor

Author(s): S. Champion, J. Gross, A. J. Robichaud, S. Pimlott

The histamine H3 receptor is implicated in many neurological and psychological disorders and is therefore of interest as a target for pharmacological intervention. The drug development process can be facilitated by using a radiotracer for this receptor in conjunction with single-photon emission computed tomography or positron emission tomography imaging studies, such as drug occupancy studies. This study investigates methods for the radiosynthesis of three compounds to be evaluated as novel radiotracers for the histamine H3 receptor. The radiosyntheses of the three target compounds, (123)I-WYE230949, (123)I-WYE126734 and (123)I-WYE127044 were evaluated using electrophilic iododesilylation and iododestannylation of the corresponding trimethylsilyl and tributylstannyl precursors. All three compounds could be produced in high radiochemical yield by electrophilic iododestannylation. By contrast, only two of the three (WYE230949 and WYE126734) could be produced by electrophilic iododesilylation. This is because of the fact that the trimethylsilyl precursors are less reactive than the stannyl precursors. Electrophilic iododestannylation of the tributylstannyl precursors is therefore the method of choice for radiosynthesis of these compounds because all three target compounds could be produced in high radiochemical yield.

Full version: Available here

Click the link to go to an external website with the full version of the paper

ISBN: 0362-4803
Publication Year: 2011
Periodical: Journal of Labelled Compounds & Radiopharmaceuticals
Periodical Number: 9-10
Volume: 54
Pages: 674-677
Author Address: Champion, S Univ Glasgow, Western Infirm, Inst Neurosci & Psychol, Glasgow G11 6NT, Lanark, Scotland Univ Glasgow, Western Infirm, Inst Neurosci & Psychol, Glasgow G11 6NT, Lanark, Scotland Wyeth Res Chem Sci, Princeton, NJ 08551 USA Univ Glasgow, Sch Med, Glasgow G11 6NT, Lanark, Scotland