No-carrier-added fluorine-18-labeled N-methylspiroperidol: synthesis and biodistribution in mice
No-carrier-added fluorine-18- (18F) labeled N-methylspiroperidol (4) was synthesized from four different substrates: p-nitrobenzonitrile (1), cyclopropyl p-nitrophenyl ketone (2A), p-cyclopropanoyl-N,N,N-trimethylanilinium iodide (2B) and p-cyclopropanoyl-N,N,N-trimethylanilinium perchlorate (2C) using the nucleophilic aromatic substitution reaction. Radiochemical yield, synthesis time, experimental simplicity, and specific activity were compared. In addition, factors which influence the yield of the nucleophilic aromatic substitution were studied. Based on these studies, the synthesis of 4 from 2A maximizes product specific activity and experimental simplicity and provides 4 in 10-15% radiochemical yield (based on (18F-) with a mass of less than 2 nmol and a specific activity of greater than 10 Ci/mumol (EOB)). The synthesis of 4 from 8-(4-(4-nitrophenyl)-4-oxobutyl)-3-methyl-1-phenyl-1,3,8-triazaspiro+ ++ (4.5)decan-4-one (5) and Cs(18F) using the nucleophilic aromatic substitution reaction gave unacceptably low and erratic yields. The biodistribution of 4 in mice showed a maximum brain uptake of 1.1% of the administered dose at 5 min and declined to approximately 0.6% at 120 min.
- Research Organization:
- Brookhaven National Lab., Upton, NY
- OSTI ID:
- 5232886
- Journal Information:
- J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 2; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMICAL PREPARATION
CHEMISTRY
DISTRIBUTION
FLUORINE 18
FLUORINE ISOTOPES
HOURS LIVING RADIOISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LABELLING
LIGHT NUCLEI
MAMMALS
MICE
NERVOUS SYSTEM
NUCLEI
ODD-ODD NUCLEI
ORGANS
RADIOCHEMISTRY
RADIOISOTOPES
RODENTS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
VERTEBRATES