Enantioselective synthesis of no-carrier added (NCA) 6-[18F]Fluoro-L-Dopa

被引:0
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作者
Duanzhi Yin
Lan Zhang
Ganghua Tang
Xiaolan Tang
Yongxian Wang
机构
[1] Chinese Academy of Sciences,Shanghai Institute of Nuclear Research
[2] The First Military Medical University,Nanfang PET Center, Nanfang Hospital
[3] Chinese Academy of Sciences Shanghai Institute of Nuclear Research,Shanghai Institute of Nuclear Research
[4] The First Military Medical University,Nanfang PET Center, Nanfang Hospital
来源
Journal of Radioanalytical and Nuclear Chemistry | 2003年 / 257卷
关键词
Dopamine; Radiochemical Purity; Synthesis Route; Triflate; Radiochemical Yield;
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摘要
6-[18F]Fluoro-L-Dopa (6-FDOPA) is the analogue of L-Dopa, the biosynthesis precursor for dopamine. As a PET tracer, it was widely applied for the presynaptic dopamine function studies in human brain. The application of a chiral phase-transfer-catalyst (PTC) in enantioselective synthesis of N.C.A. 6-[18F]Fluoro-L-Dopa has been developed recently. An improved procedure was described in this study. The labeling precursor (6-Trimethylammoniumveratraldehyde Triflate) and PTC (O-Allyl-N-(9)-anthracenylcinchonidinium Bromide) were synthesized. A successful synthesis route was developed for the preparation of 6-[18F]Fluoro-L-Dopa with high radiochemical yields (4-9%, decay uncorrected) and short synthesis time(80min). The radiochemical purity was over 99% and no D-isomer was detected by HPLC analysis using a chiral mobile phase.
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页码:179 / 185
页数:6
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