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

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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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Authors and Affiliations

  1. Shanghai Institute of Nuclear Research, Chinese Academy of Sciences, P.O. Box 800-204, Shanghai, 201800, P. R. China

    Duanzhi Yin, Lan Zhang & Ganghua Tang

  2. Nanfang PET Center, Nanfang Hospital, The First Military Medical University, Guangzhou, 510515, P. R. China

    Xiaolan Tang

  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

    Yongxian Wang

  4. Nanfang PET Center, Nanfang Hospital, The First Military Medical University, PRC

    Yongxian Wang

Authors
  1. Duanzhi Yin
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  2. Lan Zhang
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  3. Ganghua Tang
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  4. Xiaolan Tang
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  5. Yongxian Wang
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Yin, D., Zhang, L., Tang, G. et al. Enantioselective synthesis of no-carrier added (NCA) 6-[18F]Fluoro-L-Dopa. Journal of Radioanalytical and Nuclear Chemistry 257, 179–185 (2003). https://doi.org/10.1023/A:1024734402290

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  • DOI: https://doi.org/10.1023/A:1024734402290

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