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

被引：0

作者：

A. R. Jalilian

M. Sheikhha

M. Mirzaei

G. R. Aslani

A. Shafiee

机构：

[1] Research Center for Agriculture and Medicine,Cyclotron Department

[2] Tehran University of Medical Sciences,Department of Chemistry, Faculty of Pharmacy

来源：

Journal of Radioanalytical and Nuclear Chemistry | 2004年 / 260卷

关键词：

Triflate; Trifluoromethane Sulfonate; Fluoride Anion; Anhydrous Dichloromethane; Potassium Fluoride;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

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 [18F]-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 °C in Kryptofix 2.2.2/[18F] 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%.

引用

页码：373 / 377

页数：4

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