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Iodine-123 labeled derivatives of methylphenidate: Potential SPECT radiopharmaceuticals for brain dopamine transporters

✍ Scribed by D. Pan; S. J. Gatley; R. Chen; Y.-S. Ding

Book ID
101289875
Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
479 KB
Volume
38
Category
Article
ISSN
0022-2135

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✦ Synopsis

Since d-threo-[ "C]methylphenidate (Ritalin) and especially the more active enantiomer, drhreo-["C]methylphenidate, have favorable properties for PET studies,we prepared two radioiodinated analogs of methylphenidate, p-['UI]iodomethylphenidate and m-[ '231Jiod0p-hydroxymethylphenidate with a view to evaluating them as potential SPECT tracers. To prepare p-['UI]iodomethylphenidate, the p-tributyltin derivative was prepared from the previously reported p-bromomethylphenidate and reacted under acidic conditions w i t h I-123 iodide plus chloramine-T at room temperature for 90 seconds. The predominant radioactive product was obtained in 85% radiochemical yield and >10 CVpmol specific radioactivity after HPLC purification. It had the same HPLC retention time as a spectroscopically characterized non-radioactive p-iodomethylphenidate standard prepared via nitration of methylphenidate and diazotization, after protection of the secondary amino group by benzoylation. A second radioicdinated methylphenidate derivative, m-[l"I]iodop-hydroxymethylphenidate was prepared in 80% radiochemical yield by direct iodination of the known p-hydroxymethylphenidate. In this case the non-radioactive standard was prepared by iodination of p-hydroxyritalinic acid using 12 and iodic acid, followed by esterifkation.

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