Synthesis of 3-[[4-(4-[18F] fluorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine

✍ Scribed by Olli Eskola; Jörgen Bergman; Pertti Lehikoinen; Merja Haaparanta; Tove Grönroos; Sarita Forsback; Olof Solin

• Publisher: John Wiley and Sons
• Year: 2002
• Tongue: French
• Weight: 114 KB
• Volume: 45
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.597

✦ Synopsis

Abstract

3‐[[4hyphen;(4‐[^18^F]fluorophenyl)piperazin‐1‐yl] methyl] ‐1__H__‐pyrrolo[2,3‐b]pyridine, acandidate to image dopamine D~4~ receptors, was synthesised via electrophilic fluorination of a trimethylstannyl precursor with high specific radioactivity [^18^F]F~2~. The precursor was obtained by a facile four‐step synthetic approach; the trimethylstannyl leaving group was introduced by displacement of iodine utilising palladium catalysis and hexamethyldistannane in an inert solvent. The total radiosynthesis time was 50 min, including purification and formulation for injection. Decay corrected radiochemical yield was <1% as calculated from the amount of [^18^F]F^−^ produced. Specific radioactivity at the end of synthesis was 12.8–16.4 GBq/μmol. Radiochemical purity was 88–92%. Ex vivo studies in rats showed homogeneous distribution of radioactivity within rat brain. Copyright © 2002 John Wiley & Sons, Ltd.