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~(18)F-DOPA制备研究进展
引用本文:贾丽娜,张岚.~(18)F-DOPA制备研究进展[J].同位素,2017,30(1):71-77.
作者姓名:贾丽娜  张岚
作者单位: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;中国科学院钍基熔盐堆核能系统卓越创新中心,上海201800;中国科学院核辐射与核能技术重点实验室,上海201800
基金项目:国家自然科学基金(11505269)
摘    要:6-~(18)F]氟-L-多巴(~(18)F-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~(18)F-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~(18)F-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

Research Progress in the Preparation of 18F-DOPA
JIA Li-na,ZHANG Lan.Research Progress in the Preparation of 18F-DOPA[J].Isotopes,2017,30(1):71-77.
Authors:JIA Li-na  ZHANG Lan
Affiliation: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
Abstract:18F]6-fluoro-3,4-dihydroxy-L-phenylalanine (18 F-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 18 F-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.
Keywords:18F-DOPA  nucleophilic substitution  new precursor  chiral phase transfer catalyst
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