正电子显像剂2-[18F]F-A-85380的制备工艺优化研究
Improved synthetic procedure of the imaging agent 2-[18F]F-A-85380
张大龙 1张廷剑 2孟繁浩2
作者信息
- 1. 中国医科大学药学院,辽宁沈阳 110122;中国医科大学附属第一医院,辽宁沈阳 110001
- 2. 中国医科大学药学院,辽宁沈阳 110122
- 折叠
摘要
目的 优化正电子显像剂2-[18F]F-A-85380的制备工艺,采用雄性SD大鼠进行脑Micro-PET静态显像.方法 以{3-[(2S)-N-(叔丁氧羰基)氮杂环丁烷-2-基]甲氧基吡啶-2-基}三甲基铵三氟甲磺酸盐为起始原料,与[K/222]+18F-经亲核取代反应合成中间体3,3经固相萃取技术提纯后由盐酸水解制得目标化合物.结果与结论 目标化合物未经衰减矫正的放射化学收率为34％,产品的放射化学纯度大于95％,该方法具有利用设备少、操作简单、用时短等优势.大鼠Micro-PET显像显示此方法制备的显像剂特异性好,体内结合稳定性高,适合医疗机构制备以供临床使用.
Abstract
2-[18F]F-A-85380 is a positron emission tomography(PET)imaging agent for the noninvasive study of a4β2 nAChRs in the brain.In this study,an improved one-pot synthetic procedure of 2-[18F]F-A-85380 was designed.With(2-trimethylammonium-3-(1-tert-butoxycarbonyl-2(S)-azetidinylmethoxy)-pyridine trifluoromethanesulfonate as starting material,the target compound was obtained by the substitution and hydrolysis.The uncorrected yield was 34％with a mean radiochemical purity of more than 95％.The improved procedure has advantages of simple operation and avoiding HPLC-equipment.It is more suitable for medical institutions production.
关键词
2-[18F]F-A-85380/一管法/固相萃取/流程设计Key words
2-[18F]F-A-85380/one-pot/solid phase extraction/procedure design引用本文复制引用
出版年
2024
NETL
NSTL
万方数据