| Literature DB >> 16427784 |
C Thominiaux1, F Dollé, M L James, Y Bramoullé, H Boutin, L Besret, M-C Grégoire, H Valette, M Bottlaender, B Tavitian, Ph Hantraye, S Selleri, M Kassiou.
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 18-20 min. 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.Entities:
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Year: 2006 PMID： 16427784 DOI： 10.1016/j.apradiso.2005.12.003
Source DB: PubMed Journal: Appl Radiat Isot ISSN： 0969-8043 Impact factor: 1.513