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Radiosynthesis of 10-(2-[18F]fluoroethoxy)-20(S)-camptothecin as a potential positron emission tomography tracer for the imaging of topoisomerase I in cancers

Journal 2013 · IF 1.467 · 299(3): 1509-1515 · 发表于 2013 年 12 月 5 日
作者: Liu Zhen-feng,Wang Guo-lin,Dong Meng-jie,Jin Jian-wen,Li Jia-jun,Zhang Qian,Zhao Kui,Yang Shu-ye,Lin Xiang-tong
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摘要

The preparation of 10-(2-[ 18 F]fluoroethoxy)-20( S )-camptothecin, a potential positron emission tomography tracer for the imaging of topoisomerase I in cancers, is described. 10-(2-[ 18 F]Fluoroethoxy)-20( S )-camptothecin was synthesized by the [ 18 F]fluoroalkylation of the corresponding hydroxy precursor molecule with 2-[ 18 F]fluoroethyl bromide ([ 18 F]FEtBr) in dimethylsulfoxide (DMSO) at 55 °C for 20 min; this was followed by purification using high performance liquid chromatography (HPLC) with a total preparation time of 60 min. The overall radiochemical yield was approximately 5.4–12 % (uncorrected), and the radiochemical purity was above 96 %.

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