1118608-64-2Relevant academic research and scientific papers
Automated synthesis of18F-labelled analogs of metomidate, vorozole and harmine using commercial platform
Rahman, Obaidur,Erlandsson, Maria,Blom, Elisabeth,Langstroem, Bengt
, p. 169 - 171 (2010)
Three 18F-labelled PET tracers, 2-[18F]fluoroethyl 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylate ([18F]FETO), 6-[(S)-(4-chlorophenyl)-( 1H)-1,2,4-triazol-1-yl)methyl]-1-(2-[ 18F]fluoroethyl)-1H-benzotriazole
18F-Labelled vorozole analogues as PET tracer for aromatase
Erlandsson, Maria,Karimi, Farhad,Takahashi, Kayo,Langstroem, Bengt
, p. 207 - 212 (2008/12/20)
One- and two-step syntheses for the 18F-labelling of 6-[(S)-(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-(2-[18F] fluoroethyl)-1H-benzotriazole, [18F]FVOZ, 1 and 6-[(S)-(4- chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-[2-(2-[18F] fluoroethoxy)ethyl]-1H-benzotriazole, [18F]FVOO, 2 were developed. In the two-step synthesis, the nucleophilic fluorination step was performed by reacting (S)-6-[(4-chlorophenyl)-(1H-1,2,4-triazol-1-yl)methyl]-1H-benzotriazole (VOZ) with either the 18F-labelled ethane-1,2-diyl bis(4-methylbenzenesulfonate) or the oxydiethane-2,1-diyl bis(4- methylbenzenesulfonate). The radiochemical yields were in the range of 9-13% after the 110-120 min total syntheses and the specific radioactivities were 175 ± 7 GBq/μmol and 56 GBq/μmol for compounds 1 and 2, respectively. In the one-step synthesis, the precursor 2-{6-[(4-chlorophenyl)(1H-1,2,4- triazol-1-yl)methyl]-1H-1,2,3-benzotriazol-1-yl}ethyl 4-methylbenzenesulfonate (7) or 1-[2-(2-bromoethoxy)ethyl]-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl) methyl]-1H-benzotriazole (8) was directly labelled via an 18F nucleophilic substitution to give the corresponding tracer. The labelled compounds were obtained in 36-99% radiochemical yield after 75-min syntheses. The specific radioactivities are 100 GBq/μmol for compound 1 and 80 GBq/μmol for compound 2. In vitro autoradiography using frozen rat brains illustrated specific binding in the medial amygdala, the bed nucleus of stria terminalis and the preoptic area, all of which corresponded well to the result of 11C-labelled vorozole. Copyright
