国产氟多功能模块合成雌激素受体显像剂16α-[^(18)F]氟-17β-雌二醇  

Preparation of 16α[^(18)F]fluoro-17 β-fluoroestradiol on Domestic Synthesis Module

作　　者：孙传金[1] 朱虹[1] 方可元[2,3] 

机构地区：[1]南京军区南京总医院核医学科,江苏南京210002 [2]南京军区南京总医院回旋加速器中心 [3]南京江原安迪科正电子研究发展有限公司,江苏南京210002

出　　处：《同位素》2012年第3期155-159,共5页Journal of Isotopes

摘　　要：采用国产氟多功能模块,以3-甲氧基甲基-16,17-O-磺酰基-表雌三醇-O-环状砜(3-O-(Methoxymethyl)-16,17-O-sulfuryl-16-epiestriol,MMSE)为前体,在国产氟多功能合成模块的密封体系下,经18F标记合成雌激素受体显像剂16α-[18 F]氟-17β-雌二醇(18 F-FES)。结果显示:合成的18 F-FES,不校正合成效率为8.2%,校正合成效率为12.8%;合成时间约为70min,标记物18 F-FES放化纯度大于98%,体外稳定性良好。以上结果表明,国产氟多功能模块可制备18 F-FES溶液,制备的18 F-FES溶液符合放射性药物的质量要求。Abstract： To investigate the synthesis method of 16a-[-18F]fluoro-17β-fluoroestradiol on do- mestic synthesizing module, the automated synthesis was carried out through the reaction of 3-O-（methoxymethyl） -16,17-O-sulfuryl-16-epiestriol （MMSE, 1 mg） as precursor with 18F- at 105 ℃ for 15 min in sealed system on domestic synthesizer, then 0.8 mL 1 mol/L HCl dissolved in 7.2 mL acetonetrile was added in three parts to the reaction vessel for hy- drolysis and hydrolysis reaction was performed at 105 ℃ for 6 min. The final reaction solu-Total synthesis time was about 70 min and radiochemical purity was higher than 98%. The product had good stability at room temperatur, 18F-FES injection can be prepared on domes- tic synthesis module and the quality can meet the requirements of radiopharmaceuticals for clinical use.

关 键 词：18F-FES 雌激素受体显像剂 雌二醇 国产氟多功能合成模块 

分 类 号：R817-33[医药卫生—影像医学与核医学]