136507-16-9Relevant academic research and scientific papers
Convergent18F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2Areceptor PET ligands
Petersen, Ida Nymann,Villadsen, Jonas,Hansen, Hanne Demant,Jensen, Anders A.,Lehel, Szabolcs,Gillings, Nic,Herth, Matthias M.,Knudsen, Gitte M.,Kristensen, Jesper L.
, p. 5353 - 5356 (2016)
Positron emission tomography (PET) investigations of the 5-HT2Areceptor (5-HT2AR) system can be used as a research tool in diseases such as depression, Alzheimer's disease and schizophrenia. We have previously developed a11C-labeled agonist PET ligand ([11C]Cimbi-36), and the aim of this study was to identify a18F-labeled analogue of this PET-ligand. Thus, we developed a convergent radiochemical approach giving easy access to 5 different18F-labeled ligands structurally related to Cimbi-36 from a common18F-labeled intermediate. After intravenous injection, all ligands entered the pig brain. However, since within-scan intervention with ketanserin, a known orthosteric 5-HT2Areceptor antagonist, did not result in significant blocking, the radioligands seem unsuitable for neuroimaging of the 5-HT2AR in vivo.
Fast and reliable method for the preparation of ortho- and para-[ 18F]fluorobenzyl halide derivatives: Key intermediates for the preparation of no-carrier-added PET aromatic radiopharmaceuticals
Lemaire, Christian,Libert, Lionel,Plenevaux, Alain,Aerts, Jo?l,Franci, Xavier,Luxen, André
experimental part, p. 48 - 55 (2012/06/18)
A fast and reliable method suitable for the automated preparation of (substituted) [18F]fluorobenzyl halides from several [ 18F]fluorobenzaldehydes was developed. Aromatic nucleophilic substitution of trimethylammonium benzaldehyde t
Effect of aldehyde and methoxy substituents on nucleophilic aromatic substitution by [18F]fluoride
Shen, Bin,L?ffler, Dirk,Zeller, Klaus-Peter,übele, Michael,Reischl, Gerald,Machulla, Hans-Jürgen
, p. 1461 - 1468 (2008/09/18)
For a series of benzaldehydes only with a leaving group or with both a leaving group and a single methoxy substituent 18F-fluorination via nucleophilic aromatic substitution (SNAr) was studied in DMF and Me2SO. In general, the radiochemical yields were clearly higher in DMF than in Me2SO. In the fluorodehalogenation reaction (leaving group: halogen = Br, Cl), extremely low radiochemical yields were observed in Me2SO (2SO (within 3 min reaction time, 90% of the precursor was consumed; radiochemical yield = 1.0 ± 0.5%); however, in DMF oxidation was always kept at a low level during the entire reaction (13C-NMR ppm values of the aromatic carbon atom bearing the leaving group.
