首页|正电子显像剂2-[18F]F-A-85380的制备工艺优化研究

正电子显像剂2-[18F]F-A-85380的制备工艺优化研究

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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.
Improved synthetic procedure of the imaging agent 2-[18F]F-A-85380
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.

2-[18F]F-A-85380one-potsolid phase extractionprocedure design

张大龙、张廷剑、孟繁浩

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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-[18F]F-A-85380 一管法 固相萃取 流程设计

2024

中国药物化学杂志
沈阳药科大学,中国药学会

中国药物化学杂志

CSTPCD
影响因子:0.463
ISSN:1005-0108
年,卷(期):2024.34(4)
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