Wang Hongliang, Guo Xinyan, Jiang Shende, Tang Ganghua
Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, China.
Appl Radiat Isot. 2013 Jan;71(1):41-6. doi: 10.1016/j.apradiso.2012.09.014. Epub 2012 Sep 28.
An automated synthesis procedure of [(18)F]Florbetaben ([(18)F]BAY94-9172), a radiolabeled imaging agent in phase III study for in vivo mapping of fibrillar amyloid β (Aβ) with PET, was developed using the commercial PET-MF-2V-IT-1 synthesizer. The automated radiosynthesis was carried out via a one-step nucleophilic fluorination of methanesulfonic acid 2-[2-(2-{4-[2-(4-methylamino-phenyl)-vinyl]-phenoxy}-ethoxy)-ethoxy]-ethyl ester, as a new precursor, and separation with semi-preparative high performance liquid chromatography (HPLC). The total synthesis time amounted to 50 min with 20-25% yield (uncorrected for decay) and radiochemical purities of more than 95% in all runs. The described automated radiosynthesis allows the production of [(18)F]Florbetaben using a commercial radiosynthesis module and enables clinical trials of this compound.
利用商用PET-MF-2V-IT-1合成仪，开发了[(18)F]氟贝他宾（[(18)F]BAY94-9172）的自动化合成程序。[(18)F]氟贝他宾是一种用于正电子发射断层扫描（PET）体内绘制纤维状淀粉样β蛋白（Aβ）的放射性标记成像剂，处于III期研究阶段。自动化放射性合成通过对一种新前体2-[2-(2-{4-[2-(4-甲氨基苯基)-乙烯基]-苯氧基}-乙氧基)-乙氧基]-乙基甲磺酸酯进行一步亲核氟化反应来进行，并采用半制备高效液相色谱（HPLC）进行分离。总合成时间为50分钟，产率为20 - 25%（未校正衰变），且所有批次的放射化学纯度均超过95%。所描述的自动化放射性合成能够使用商用放射性合成模块生产[(18)F]氟贝他宾，并使该化合物能够进行临床试验。
