286368-53-4Relevant articles and documents
One-step, no-carrier-added, synthesis of a 18F-Labelled benzodiazepine receptor ligand
Jalilian, Amir Reza,Tabatabai, Sayyed Abbas,Shafiee, Abbas,Afarideh, Hossein,Najafi, Reza,Bineshmarvasti, Maria
, p. 545 - 555 (2000)
5-(2-Phenoxy)phenyl-1,3,4-oxadiazole-2-yl-4-fluorobenzoate, a non-classical benzodiazepine receptor ligand, has shown anticonvulsant activity against pentylenetetrazole-induced convulsion. In order to perform biological studies, we decided to label the compound with positron-emitting fluorine-18 (t( 1/2 ) = 109.7 min). The latter compound was prepared in no-carrier-added form from [18F]fluoride and 5-(2-phenoxy)phenyl-1,3,4-oxadiazole-2-yl-4-N,N,N-trimethylanilinium triflate in one step. The best results were obtained using Kryptofix2.2.2/[18F]fluoride with dimethylsulfoxide as the solvent at 90°C. Column chromatography afforded the desired compound in 15 min in an overall radiochemical yield of 70-75% corrected to the end of radionuclide production with a specific radioactivity of about 3000 Ci/mmol and a radiochemical purity of more than 95% and high chemical purity.