通过全自动真空蒸馏法纯化[(¹⁸)F]2-氟乙基叠氮化物以改进[(¹⁸)F]FLETT的合成。
Improved synthesis of [(18)F]FLETT via a fully automated vacuum distillation method for [(18)F]2-fluoroethyl azide purification.
作者信息
Ackermann Uwe, Plougastel Lucie, Goh Yit Wooi, Yeoh Shinn Dee, Scott Andrew M
机构信息
Department of Nuclear Medicine and Centre for PET, Austin Health, Heidelberg, VIC, Australia; The University of Melbourne, Parkville, VIC, Australia; Ludwig Institute for Cancer Research, Melbourne Branch, VIC, Australia.
Ecole National Supérior de Chimie de Rennes, Rennes, France.
出版信息
Appl Radiat Isot. 2014 Dec;94:72-76. doi: 10.1016/j.apradiso.2014.07.009. Epub 2014 Jul 24.
The synthesis of [(18)F]2-fluoroethyl azide and its subsequent click reaction with 5-ethynyl-2'-deoxyuridine (EDU) to form [(18)F]FLETT was performed using an iPhase FlexLab module. The implementation of a vacuum distillation method afforded [(18)F]2-fluoroethyl azide in 87±5.3% radiochemical yield. The use of Cu(CH3CN)4PF6 and TBTA as catalyst enabled us to fully automate the [(18)F]FLETT synthesis without the need for the operator to enter the radiation field. [(18)F]FLETT was produced in higher overall yield (41.3±6.5%) and shorter synthesis time (67min) than with our previously reported manual method (32.5±2.5% in 130min).
使用iPhase FlexLab模块进行[(18)F]2-氟乙基叠氮化物的合成及其随后与5-乙炔基-2'-脱氧尿苷(EDU)的点击反应以形成[(18)F]FLETT。采用真空蒸馏法得到[(18)F]2-氟乙基叠氮化物，放射化学产率为87±5.3%。使用Cu(CH3CN)4PF6和TBTA作为催化剂，使我们能够完全自动化[(18)F]FLETT的合成，而无需操作人员进入辐射区域。与我们之前报道的手动方法(130分钟内产率为32.5±2.5%)相比，[(18)F]FLETT的总产率更高(41.3±6.5%)，合成时间更短(67分钟)。
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