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Synthesis of N-(3-[18F]Fluoropropyl)-2β-carbomethoxy-3β-(4-iodophenyl)nortropane ([18F]FP-β-CIT)

✍ Scribed by R. P. Klok; P. J. Klein; J. D. M. Herscheid; A. D. Windhorst

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
163 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

N-(3-[ 18 F]fluoropropyl)-2b-carbomethoxy-3b-(4-iodophenyl)nortropane ([ 18 F]FP-b-CIT) was synthesized in a two-step reaction sequence. In the first reaction, 1-bromo-3-(nitrobenzene-4-sulfonyloxy)-propane was fluorinated with no-carrieradded fluorine-18. The resulting product, 1-bromo-3-[ 18 F]-fluoropropane, was distilled into a cooled reaction vessel containing 2b-carbomethoxy-3b-(4-iodophenyl)-nortropane, diisopropylethylamine and potassium iodide. After 30 min, the reaction mixture was subjected to a preparative HPLC purification. The product, [ 18 F]FP-b-CIT, was isolated from the HPLC eluent with solid-phase extraction and formulated to yield an isotonic, pyrogen-free and sterile solution of [ 18 F]FP-b-CIT.

The overall decay-corrected radiochemical yield was 25 AE 5%. Radiochemical purity was >98% and the specific activity was 94 AE 50 GBq/mmol at the end of synthesis.

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