O. Eskola, J. Bergman, P. Lehikoinen
May 27, 2002
Citations
0
Influential Citations
10
Citations
Quality indicators
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
3-[[4hyphen;(4-[18F]fluorophenyl)piperazin-1-yl] methyl] -1H-pyrrolo[2,3-b]pyridine, acandidate to image dopamine D4 receptors, was synthesised via electrophilic fluorination of a trimethylstannyl precursor with high specific radioactivity [18F]F2. 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 [18F]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.