正电子显像剂2-[^(18)F]F-A-85380的制备工艺优化研究  

Improved synthetic procedure of the imaging agent 2-[^(18)F]F-A-85380

作　　者：张大龙 张廷剑[1] 孟繁浩[1] ZHANG Dalong;ZHANG Tingjian;MENG Fanhao(School of Pharmacy,China Medical University,Shenyang 110122,China;The First Hospital of China Medical University,Shenyang 110001,China)

机构地区：[1]中国医科大学药学院,辽宁沈阳110122 [2]中国医科大学附属第一医院,辽宁沈阳110001

出　　处：《中国药物化学杂志》2024年第4期324-328,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的优化正电子显像剂2-[^(18)F]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]+^(18)F-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。2-[^(18)F]F-A-85380 is a positron emission tomography(PET)imaging agent for the noninvasive study ofα4β2 nAChRs in the brain.In this study,an improved one-pot synthetic procedure of 2-[^(18)F]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-[^(18)F]F-A-85380 一管法 固相萃取 流程设计 

分 类 号：R914[医药卫生—药物化学]