基于自动固相萃取法合成16α-[F]氟雌二醇，无需高效液相色谱纯化步骤。
Automated SPE-based synthesis of 16α-[F]fluoroestradiol without HPLC purification step.
作者信息
Fedorova Olga, Nikolaeva Viktoria, Krasikova Raisa
机构信息
N.P. Bechtereva Institute of the Human Brain Russian Academy of Sciences, (IHB RAS), 9, Pavlova str., 197376 Saint-Petersburg, Russia.
St.-Petersburg State University, 7-9, Universitetskaya nab., 199034 Saint-Petersburg, Russia.
出版信息
Appl Radiat Isot. 2018 Nov;141:57-63. doi: 10.1016/j.apradiso.2018.08.007. Epub 2018 Aug 10.
[F]fluoroestradiol ([F]FES) is well-established PET radiotracer for diagnosing and monitoring treatment of estrogen-positive breast cancer. The radiotracer is produced via one-pot two steps synthesis using cyclic sulfate precursor and is usually purified by semi-preparative HPLC. Here we suggested simple SPE purification procedure using OASIS WAX 3cc and Sep-Pak QMA light cartridges that afforded [F]FES in typically 15% RCY (corrected for decay) within 45 min formulated in 5% EtOH/saline. All purity parameters were well within specifications recommended in the Investigator's Brochure for [F]Fluoroestradiol.
[氟]氟雌二醇（[F]FES）是一种成熟的用于诊断和监测雌激素阳性乳腺癌治疗的正电子发射断层显像（PET）放射性示踪剂。该放射性示踪剂通过使用环状硫酸盐前体的一锅两步合成法制备，通常通过半制备高效液相色谱法进行纯化。在此，我们提出了一种简单的固相萃取（SPE）纯化方法，使用OASIS WAX 3cc和Sep-Pak QMA轻型柱，在45分钟内以5%乙醇/生理盐水配制，通常可获得15%的放射性化学产率（RCY，已校正衰变）的[F]FES。所有纯度参数均完全符合研究者手册中对[氟]氟雌二醇推荐的规格要求。
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