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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

18F-DOPA制备研究进展

贾丽娜1,2,3;张岚1,2,3   

  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

Abstract:

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

摘要:

6-[18F]氟-L-多巴(18F-DOPA)为神经系统疾病和脑部肿瘤的理想示踪剂,广泛用于神经内分泌瘤的显像。本文综述近几年亲电取代法和亲核取代法合成18F-DOPA取得的新进展,重点介绍新型标记前体和手性相转移催化剂在亲核取代法制备18F-DOPA中的应用。

关键词: 18F-DOPA, 亲核取代, 新型标记前体, 手性相转移催化剂