Enantioselective synthesis of no-carrier added (NCA) 6-[18F]Fluoro-L-Dopa |
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| Authors: | Duanzhi Yin Lan Zhang Ganghua Tang Xiaolan Tang Yongxian Wang |
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| Institution: | (1) Shanghai Institute of Nuclear Research, Chinese Academy of Sciences, P.O. Box 800-204, Shanghai, 201800, P. R. China;(2) Nanfang PET Center, Nanfang Hospital, The First Military Medical University, Guangzhou, 510515, P. R. China;(3) Shanghai Institute of Nuclear Research, Chinese Academy of Sciences Shanghai Institute of Nuclear Research, P.O. Box 800-204, Shanghai, 201800, P. R. China;(4) Nanfang PET Center, Nanfang Hospital, The First Military Medical University, PRC |
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| Abstract: | 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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