摘要
16α-[^(18)F]氟-17β-雌二醇(^(18)F-FES)作为一种雌激素受体显像剂,在原发性和转移性乳腺癌的诊断中具有重要的应用价值,但目前它的合成方法存在步骤复杂和耗时的缺点,不利于临床的推广与使用。为了解决这一问题且满足临床使用的迫切需求,我们基于国产[^(18)F]FDG合成模块,利用固相萃取(SPE)技术,成功开发了一种快速、高效的"一锅,两步"式全自动化放射合成^(18)F-FES方法。首先,干燥后的^(18)F-离子与3-O-(甲氧甲基)-16,17-O-磺酰基-16-表雌二醇(MMSE)发生[^(18)F]亲核氟化反应。随后,[^(18)F]氟化中间体无需分离直接在弱酸性条件下进行水解反应。最后,经过固相柱纯化后得到产品^(18)F-FES。^(18)F-FES的总放射合成时间为45 min,衰变校正后放射化学合成产率45%±4%(n=10),放射化学纯度大于98%。
16α-[^18F]fluoroestradiol （^18F-FES） is known as an estrogen receptor imaging tracer and has an very important role for imaging primary and metastatic breast cancers. However, the complicated and time-consuming synthetic protocol of the tracer doesn＇t meet the demands of clinical use, which limits its routine clinical use and medical research. To solve the problem, it is very important for the radio-chemists to explore the technological improvement for the radiosynthesis of ^18F-FES. In this work, ^18F-FES was synthesized from 3-O-methoxymethyl-16,17-O-sullhryl-16-epiestriol （MMSE） as starting material via a ＂two-step, one-pot＂ procedure, including [^18F]fluorination reaction of the commercial available precursor and acid hydrolysis of the [^18F]intermediate. Without HPLC purification, CI8 Cartridges were used for the purification of the 18F-FES. The decay-corrected radiochemical yield of 18F-FES was 45±4 % （n= 10）, the radiochemical purity was more than 98 %, and the total synthesis time was within 45 min. A rapid and efficient ＂two-step one-pot＂ automated synthesis method of ^18F-FES has been developed from MMSE via a solid phase extraction （SPE） procedure on a domestic commercial [^18F]FDG synthesizer.
作者
汤睿昆
刘少玉
唐刚华
Tang Ruikun;Liu Shaoyu;Tang Ganghua(Guangzhou Hightech Radiopharmaceutical Co., Ltd., Guangzhou 510663;Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, Department of Nuclear Medicine, The First Affiliated Hospital, SunYat-sen University, Guangzhou 510080, China)
出处
《广东化工》
CAS
2018年第11期61-63,共3页
Guangdong Chemical Industry
