Radiosyntheses of 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine
- 1. Chinese Academy of Sciences, Shanghai (China). Shanghai Inst. of Nuclear Research
Description
L-750,667 is a novel, high-affinity (Ki = 0.51 nmol/L) and selective D4 receptor ligand. A L-750,667 analogue, 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine, was prepared by reacting 3- (piperazin-1-yl)-methyl-1H-pyrrolo[2,3-b]pyridine with 4-[18F]fluorobenzaldehyde. The 4 -[18F] fluorobenzaldehyde was prepared by nucleophilic substitution using no carrier added [18F]fluoride from trimethylammonium- benzaldehyde triflate in DMSO. The radiochemical yield of 3-{[4-(4-[18F]fluorobenzyl)] piperazin-1-yl}methyl-1H-pyrrolo[2,3-b]pyridine was 12.0% (decay -corrected) with a radiochemical purity better than 98% and a specific activity greater than 37GBq/μmol, and the synthesis time including HPLC purification was 73 min. This labeled compound may be a useful PET tracer for dopamine D4 receptors
Additional details
Publishing Information
- Journal Title
- Nuclear Techniques
- Journal Volume
- 26
- Journal Issue
- 8
- Journal Page Range
- p. 628-632
- ISSN
- 0253-3219
INIS
- Country of Publication
- China
- Country of Input or Organization
- China
- INIS RN
- 35053636
- Subject category
- S62: RADIOLOGY AND NUCLEAR MEDICINE; S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY;
- Descriptors DEI
- DMSO; DOPAMINE; FLUORINE 18; LABELLED COMPOUNDS; LIGANDS; METHYL RADICALS; ORGANIC FLUORINE COMPOUNDS; PIPERAZINES; POSITRON COMPUTED TOMOGRAPHY; PURIFICATION; PYRIDINE; PYRROLES; RECEPTORS; SYNTHESIS; THERAPEUTIC USES
- Descriptors DEC
- ALKYL RADICALS; AMINES; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; AZINES; AZOLES; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CARDIOTONICS; CARDIOVASCULAR AGENTS; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; DRUGS; EMISSION COMPUTED TOMOGRAPHY; FLUORINE ISOTOPES; HETEROCYCLIC COMPOUNDS; HOURS LIVING RADIOISOTOPES; HYDROXY COMPOUNDS; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; LIGHT NUCLEI; MEMBRANE PROTEINS; NANOSECONDS LIVING RADIOISOTOPES; NEUROREGULATORS; NUCLEI; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; ORGANIC HALOGEN COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC SULFUR COMPOUNDS; PHENOLS; POLYPHENOLS; PROTEINS; PYRAZINES; PYRIDINES; RADICALS; RADIOISOTOPES; SULFOXIDES; SYMPATHOMIMETICS; TOMOGRAPHY; USES