Radiosynthesis of (18)F -5- 2-(2-chlorophenoxy)phenyl -1,3,4-oxadiazole-2-yl-4-fluorobenz oate: A labeled ligand for benzodiazepine receptors

Journal of Radioanalytical and Nuclear Chemistry

Volume 2 - Number

Article Type: ---- Unspecified ----
Abstract:

5-[2-(2-Chlorophenoxy)phenyl]-1,3,4-oxadiazole-2-yl-4-fluorobenzoate 6a, the non-classic benzodiazepine ligand, has been shown to elicit a significant anticonvulsant activity against pentylenetetrazole-induced convulsion. In order to perform biological studies, we decided to prepare the [(18)F]-labeled compound. This compound was prepared in no-carrier-added (n.c.a) form from 5-[2-(2-chlorophenoxy)phenyl]-1,3,4-oxadiazole-2-yl-4-N,N,N-trimethylanilinium triflate 5 in one step at 125 degreesC in Kryptofix 2.2.2/[(18)F] and DMSO as the solvent followed by column chromatography. The synthesis took 20 minutes with an overall radiochemical yield of 70-75% (EOS) and a specific activity about 74 GBq/mmole and chemical-radiochemical purity more than 95%.