Simplified synthesis of N-(3-[18F]fluoropropyl)-2β-carbomethoxy-3β-(4-fluorophenyl)nortropane ([18F]β-CFT-FP) using [18F]fluoropropyl tosylate as the labelling reagent

✍ Scribed by Teija Koivula; Outi Perhola; Eeva-Liisa Kämäräinen; Tiina Lipponen; Jouko Vepsäläinen; Olof Solin

• Publisher: John Wiley and Sons
• Year: 2005
• Tongue: French
• Weight: 114 KB
• Volume: 48
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.943

✦ Synopsis

A synthesis method has been developed for the labelling of N-(3-[ 18 F]fluoropropyl)-2b-carbomethoxy-3b-(4-fluorophenyl)nortropane ([ 18 F]b-CFT-FP), a potential radioligand for visualization of the dopamine transporters by positron emission tomography. The two-step synthesis includes preparation of [ 18 F]fluoropropyl tosylate and its use without purification in the fluoroalkylation of 2b-carbomethoxy-3b-(4-fluorophenyl)nortropane (nor-b-CFT)

. The final product is purified by HPLC. Optimization of the two synthesis steps resulted in a greater than 30% radiochemical yield of [ 18 F]b-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/mmol. In comparison to alkylation by [ 18 F]fluoropropyl bromide, the procedure described here results in an improved overall radiochemical yield of [ 18 F]b-CFT-FP in a shorter time.