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

doi:10.1002/JLCR.597

Paper

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

Published May 27, 2002 · O. Eskola, J. Bergman, P. Lehikoinen

Journal of Labelled Compounds and Radiopharmaceuticals

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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.

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Animal Study

Study Snapshot

This study successfully synthesized 3-[[4-(4-[18F]fluorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine, a potential imaging agent for dopamine D4 receptors, with high specific radioactivity and

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

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

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References

Citations

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Carbon-11-labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide] shows potential as a PET tracer for dopamine D(4) receptors, with nanomolar affinity and

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