Highly efficient production of [ 18F]fallypride using small amounts of base concentration

• Published in: Applied radiation and isotopes 2010-12, Vol.68 (12), p.2279-2284
• Main Authors: Seok Moon, Byung, Hyung Park, Jun, Jin Lee, Hong, Sun Kim, Ji, Sup Kil, Hee, Se Lee, Byoung, Yoon Chi, Dae, Chul Lee, Byung, Kyeong Kim, Yu, Eun Kim, Sang
• Format: Article
• Language: English
• Subjects: [ 18F]Fallypride; Automated radiosynthesis; Catalysis; Dopamine D 2/D 3 receptor; Fluorides - chemistry; PET
• ISSN: 0969-8043; 1872-9800
• DOI: 10.1016/j.apradiso.2010.06.016

To minimize the base concentration of a phase-transfer catalyst, [ 18F]fluoride was extracted from 18O-enriched water trapped on an activated ion exchange cartridge (Chromafix ® PS-HCO 3) using different concentrations of tetrabutylammonium bicarbonate (TBAHCO 3) or Kryptofix 2.2.2./K 2CO 3 in organic solvents such as CH 3CN/H 2O or MeOH/H 2O. The optimal labeling condition for [ 18F]fallypride with automated synthesis was that 2 mg of tosyl-fallypride in acetonitrile (1 mL) was heated at 100 °C for 10 min using 40% TBAHCO 3 (10 μL). [ 18F]Fallypride was obtained with a high radiochemical yield of approximately 68±1.6% (decay-corrected, n=42) with a total synthesis time of 51±1.2 min, including HPLC purification and solid-phase purification for the final formulation.