通过氟/氟同位素交换对[GaF(BnMe -tacn)]进行快速水相后期放射性标记：迈向新型正电子发射断层显像（PET）成像探针
Rapid Aqueous Late-Stage Radiolabelling of [GaF (BnMe -tacn)] by F/ F Isotopic Exchange: Towards New PET Imaging Probes.
作者信息
Monzittu Francesco M, Khan Imtiaz, Levason William, Luthra Sajinder K, McRobbie Graeme, Reid Gillian
机构信息
School of Chemistry, University of Southampton, Southampton (UK), SO17 1BJ, UK.
GE Healthcare, The Grove Centre, White Lion Road, Amersham (UK), HP7 9LL, UK.
出版信息
Angew Chem Int Ed Engl. 2018 May 28;57(22):6658-6661. doi: 10.1002/anie.201802446. Epub 2018 Apr 26.
A simple and rapid method for F radiolabelling of [GaF (BnMe -tacn)] by F/ F isotopic exchange is described. The use of MeCN/H O or EtOH/H O (75:25) and aqueous [ F]F (up to 200 MBq) with heating (80 °C, 10 min) gave 66±4 % F incorporation at a concentration of 268 nm, and 37±5 % F incorporation at even lower concentration (27 nm), without the need for a Lewis acid promoter. A solid-phase extraction method was established to give [Ga F F (BnMe -tacn)] in 99 % radiochemical purity in an EtOH/H O mixture.
描述了一种通过¹⁸F/¹⁹F同位素交换对[GaF₃(BnMe₃ - tacn)]进行¹⁸F放射性标记的简单快速方法。使用MeCN/H₂O或EtOH/H₂O（75:25）以及含水的[¹⁸F]F⁻（最高200 MBq）并加热（80°C，10分钟），在浓度为268 nM时可实现66±4%的¹⁸F掺入，在更低浓度（27 nM）时可实现37±5%的¹⁸F掺入，无需路易斯酸促进剂。建立了一种固相萃取方法，可在EtOH/H₂O混合物中以99%的放射化学纯度得到[GaF₂¹⁸F(BnMe₃ - tacn)]。
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