1. Improved synthesis of the peripheral benzodiazepine receptor ligand [11C]DPA-713 using [11C]methyl triflate
- Author
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Thominiaux, C., Dollé, F., James, M.L., Bramoullé, Y., Boutin, H., Besret, L., Grégoire, M.-C., Valette, H., Bottlaender, M., Tavitian, B., Hantraye, Ph., Selleri, S., and Kassiou, M.
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BENZODIAZEPINE receptors , *POSITRON emission , *POSITRON emission tomography , *DIAGNOSTIC imaging , *METHYL triflate - Abstract
Abstract: Recently, the pyrazolopyrimidine, [11C] N,N-Diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]acetamide (DPA-713) has been reported as a new promising marker for the study of peripheral benzodiazepine receptors with positron emission tomography. In the present study, DPA-713 has been labelled from the corresponding nor-analogue using [11C]methyl triflate (CH3OTf). Conditions for HPLC were also modified to include physiological saline (aq. 0.9% NaCl)/ethanol:60/40 as mobile phase making it suitable for injection. The total time of radiosynthesis, including HPLC purification, was 18–20min. This reported synthesis of [11C]DPA-713, using [11C]CH3OTf, resulted in an improved radiochemical yield (30–38%) compared to [11C]methyl iodide (CH3I) (9) with a simpler purification method. This ultimately enhances the potential of [11C]DPA-713 for further pharmacological and clinical evaluation. These improvements make this radioligand more suitable for automated synthesis which is of benefit where multi-dose preparations and repeated syntheses of radioligand are required. [Copyright &y& Elsevier]
- Published
- 2006
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