Haji Dheere Abdul Karim, Bongarzone Salvatore, Shakir Dinah, Gee Antony
Department of Chemistry and Biology, School of Biomedical Engineering and Imaging Sciences, King's College London, King's Health Partners, St. Thomas' Hospital, London, UK.
J Chem. 2018 Dec 10;2018:7641304. doi: 10.1155/2018/7641304.
A novel carbon-11 radiolabelling methodology for the synthesis of the dialkylcarbonate functional group has been developed. The method uses cyclotron-produced short-lived [C]CO (half-life 20.4 min) directly from the cyclotron target in a one-pot synthesis. Alcohol in the presence of base trapped [C]CO efficiently forming an [C]alkylcarbonate intermediate that subsequently reacted with an alkylchloride producing the di-substituted [C]carbonate (34% radiochemical yield, determined by radio-HPLC) in 5 minutes from the end of [C]CO cyclotron delivery.
已开发出一种用于合成碳酸二烷基酯官能团的新型碳-11放射性标记方法。该方法在一锅法合成中直接使用回旋加速器产生的来自回旋加速器靶的短寿命[C]CO(半衰期20.4分钟)。在碱存在下,醇有效地捕获[C]CO,形成[C]烷基碳酸酯中间体,该中间体随后与烷基氯反应,在[C]CO从回旋加速器输送结束起5分钟内生成二取代的[C]碳酸酯(放射化学产率34%,通过放射性高效液相色谱法测定)。