Simplified synthesis ofN-(3-[18F]fluoropropyl)-2β-carbomethoxy-3β-(4-fluorophenyl)nortropane ([18F]β-CFT-FP) using [18F]fluoropropyl tosylate as the labelling reagent
| Autor: | Tiina Lipponen, Jouko Vepsäläinen, Outi Perhola, Teija Koivula, Olof Solin, Eeva-Liisa Kämäräinen |
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| Rok vydání: | 2005 |
| Předmět: |
Chemistry
Organic Chemistry Radiochemistry Alkylation Biochemistry High-performance liquid chromatography Chemical synthesis 030218 nuclear medicine & medical imaging Analytical Chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Bromide Reagent Yield (chemistry) Labelling Drug Discovery Radioligand Organic chemistry Radiology Nuclear Medicine and imaging 030217 neurology & neurosurgery Spectroscopy |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 48:463-471 |
| ISSN: | 1099-1344 0362-4803 |
| DOI: | 10.1002/jlcr.943 |
| Popis: | A synthesis method has been developed for the labelling of N-(3-[18F]fluoropropyl)-2β-carbomethoxy-3β-(4-fluorophenyl)nortropane ([18F]β-CFT-FP), a potential radioligand for visualization of the dopamine transporters by positron emission tomography. The two-step synthesis includes preparation of [18F]fluoropropyl tosylate and its use without purification in the fluoroalkylation of 2β-carbomethoxy-3β-(4-fluorophenyl)nortropane (nor-β-CFT). The final product is purified by HPLC. Optimization of the two synthesis steps resulted in a greater than 30% radiochemical yield of [18F]β-CFT-FP (decay corrected to end of bombardment). The synthesis time including HPLC-purification was approximately 90 min. The radiochemical purity of the final product was higher than 99% and the specific radioactivity at the end of synthesis was typically 20 GBq/µmol. In comparison to alkylation by [18F]fluoropropyl bromide, the procedure described here results in an improved overall radiochemical yield of [18F]β-CFT-FP in a shorter time. Copyright © 2005 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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