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Synthesis of N‐(3‐[18F]Fluoropropyl)‐2β‐carbomethoxy‐3β‐(4‐iodophenyl)nortropane ([18F]FP‐β‐CIT)
Authors:R P Klok  P J Klein  J D M Herscheid  A D Windhorst
Institution:Nuclear Medicine and PET Research, VU University Medical Centre, De Boelelaan 1085c, 1081 HV Amsterdam, The Netherlands
Abstract:N‐(3‐18F]fluoropropyl)‐2β‐carbomethoxy‐3β‐(4‐iodophenyl)nortropane (18F]FP‐β‐CIT) was synthesized in a two‐step reaction sequence. In the first reaction, 1‐bromo‐3‐(nitrobenzene‐4‐sulfonyloxy)‐propane was fluorinated with no‐carrier‐added fluorine‐18. The resulting product, 1‐bromo‐3‐18F]‐fluoropropane, was distilled into a cooled reaction vessel containing 2β‐carbomethoxy‐3β‐(4‐iodophenyl)‐nortropane, diisopropylethylamine and potassium iodide. After 30 min, the reaction mixture was subjected to a preparative HPLC purification. The product, 18F]FP‐β‐CIT, was isolated from the HPLC eluent with solid‐phase extraction and formulated to yield an isotonic, pyrogen‐free and sterile solution of 18F]FP‐β‐CIT. The overall decay‐corrected radiochemical yield was 25 ± 5%. Radiochemical purity was > 98% and the specific activity was 94 ± 50 GBq/µmol at the end of synthesis. Copyright © 2006 John Wiley & Sons, Ltd.
Keywords:F‐18  [18F]FP‐β  ‐CIT  dopamine transporter  positron emission tomography
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