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Research Progress in the Preparation of 18F-DOPA

JIA Li-na1,2,3;ZHANG Lan1,2,3   

  1. 1.Department of Radiochemistry and Engineering, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China;2.CAS center for excellence TMSR energy system, Shanghai 201800, China;3. Key Laboratory of Nuclear Radiation and Nuclear Energy Technology, CAS, Shanghai 201800, China
  • Online:2017-02-20 Published:2017-03-06



  1. 1.中国科学院 上海应用物理研究所 放射化学与工程技术部,上海201800;2.中国科学院 钍基熔盐堆核能系统卓越创新中心,上海201800;3.中国科学院 核辐射与核能技术重点实验室,上海201800


18F]6-fluoro-3,4-dihydroxy-L-phenylalanine (18F-DOPA) has been known to be a useful radiotracer for neuropsychiatric diseases and brain malignancies, and it is also abundantly used for visualizing neuroendocrine tumors at present. However, its more widespread clinical use was hampered by the lack of a high specific activity, high yielding labeling method. This review mainly summarized new developments in the synthesis of 18F-DOPA with electrophilic reactions and nucleophilic substitution reactions in recent years. Among these, considerable advances in nucleophilic synthesis had been achieved by developing novel precursors and utilizing chiral phase-transfer catalysts (cPTC) mediated fluorinations allowing for the production of 18F-DOPA in high specific activity and high radiochemical yield.

Key words: 18F-DOPA, nucleophilic substitution, new precursor, chiral phase transfer catalyst



关键词: 18F-DOPA, 亲核取代, 新型标记前体, 手性相转移催化剂