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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 |
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| Authors: | Zhen-feng Liu Guo-lin Wang Meng-jie Dong Jian-wen Jin Jia-jun Li Qian Zhang Kui Zhao Shu-ye Yang Xiang-tong Lin |
| Institution: | 1. PET Center, the First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, 310003, China 2. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China 3. Department of Nuclear Medicine, Huashan Hospital, Fudan University, Shanghai, 200400, China |
| Abstract: | The preparation of 10-(2-18F]fluoroethoxy)-20(S)-camptothecin, a potential positron emission tomography tracer for the imaging of topoisomerase I in cancers, is described. 10-(2-18F]Fluoroethoxy)-20(S)-camptothecin was synthesized by the 18F]fluoroalkylation of the corresponding hydroxy precursor molecule with 2-18F]fluoroethyl bromide (18F]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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