Nandy S K, Rajan M G R
Radiation Medicine Centre, Bio-Medical Group, Bhabha Atomic Research Centre, TMH Annexe, Parel, Mumbai 400012, India.
Appl Radiat Isot. 2010 Oct;68(10):1944-9. doi: 10.1016/j.apradiso.2010.04.011. Epub 2010 Apr 29.
A novel fully automated radiosynthesis procedure for the fluorine-18 analog of 1-alpha-D-(5'-deoxy-5'-fluoro-(1S,2R,3S,4S) arabinofuranosyl)-2-nitroimidazole ([(18)F]FAZA) using a commercially available combination column - Chromabond Set V (FDG-base-hydrolysis) - for purification was developed. [(18)F]FAZA was prepared via a one-pot, two-step synthesis using a nuclear interface nucleophilic synthesis module. Nucleophilic fluorination of the precursor molecule, 1-(2,3-di-O-acetyl-5-O-tosyl-alpha-D-arabinofuranosyl)-2-nitroimidazole, with no-carrier added [(18)F]fluoride followed by hydrolysis of the protecting groups with 0.3M NaOH was performed. Purification was carried out using the Chromabond Set V column without any modifications. The overall radiochemical yield obtained was 21.98+/-1.40% (n=5, without decay correction) within a total synthesis period of 51+/-1 min. The radiochemical purity was greater than 95% and devoid of any other chemical impurities. The reported method can easily be adapted in any commercial FDG synthesis module.
开发了一种新型全自动放射性合成方法,用于制备1-α-D-(5'-脱氧-5'-氟-(1S,2R,3S,4S)阿拉伯呋喃糖基)-2-硝基咪唑([(18)F]FAZA)的氟-18类似物,该方法使用市售组合柱——Chromabond Set V(基于FDG-水解)进行纯化。[(18)F]FAZA通过一锅两步合成法,使用核接口亲核合成模块制备。用无载体添加的[(18)F]氟化物对前体分子1-(2,3-二-O-乙酰基-5-O-甲苯磺酰基-α-D-阿拉伯呋喃糖基)-2-硝基咪唑进行亲核氟化,然后用0.3M NaOH水解保护基团。使用Chromabond Set V柱进行纯化,无需任何修改。在51±1分钟的总合成时间内,获得的总放射化学产率为21.98±1.40%(n = 5,未进行衰变校正)。放射化学纯度大于95%,且无任何其他化学杂质。所报道的方法可轻松适用于任何商业FDG合成模块。