用于A₃腺苷受体PET成像的新型碳-11标记的1,2,4-三唑并[4,3-a]喹喔啉-1-酮衍生物的简便合成
Simple synthesis of new carbon-11-labeled 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives for PET imaging of A₃ adenosine receptor.
作者信息
Gao Mingzhang, Gao Andy Chufan, Wang Min, Zheng Qi-Huang
机构信息
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-202, Indianapolis, IN 46202, USA.
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-202, Indianapolis, IN 46202, USA.
出版信息
Appl Radiat Isot. 2014 Sep;91:71-8. doi: 10.1016/j.apradiso.2014.05.005. Epub 2014 May 21.
The reference standards 4a-b, 6a-b, 7a-c, and desmethylated precursors 9a-b, 10a-b, 8a-c were synthesized from 4-methoxyaniline, ethyl 2-chloro-acetoacetate and substituted benzene-1,2-diamines with 3, 5, 6 steps in 61-67%, 34-41%, 23-31%, and with 4, 6, 7 steps in 49-57%, 28-35%, 20-27% overall chemical yield, respectively. The target tracers [(11)C]4a-b, [(11)C]6a-b, [(11)C]7a-c were synthesized from their corresponding precursors with [(11)C]CH3OTf through O-[(11)C]methylation and isolated by simplified SPE in 40-60% decay corrected radiochemical yields at EOB, with 185-370 GBq/μmol specific activity at EOS.
参考标准品4a-b、6a-b、7a-c以及去甲基化前体9a-b、10a-b、8a-c分别由4-甲氧基苯胺、2-氯乙酰乙酸乙酯和取代苯-1,2-二胺合成，分别经过3步、5步、6步以及4步、6步、7步反应，总化学产率分别为61-67%、34-41%、23-31%以及49-57%、28-35%、20-27%。目标示踪剂[(11)C]4a-b、[(11)C]6a-b、[(11)C]7a-c由其相应前体通过用[(11)C]CH3OTf进行O-[(11)C]甲基化反应合成，并通过简化的固相萃取法分离，在EOB时衰变校正放射化学产率为40-60%，在EOS时比活度为185-370 GBq/μmol。
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