18F-DOPA制备研究进展

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。...

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Bibliographic Details
Published in同位素 Vol. 30; no. 1; pp. 71 - 77
Main Author 贾丽娜 张岚
Format Journal Article
LanguageChinese
Published 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 2017
中国科学院核辐射与核能技术重点实验室,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
Subjects
18F-DOPA
亲核取代
手性相转移催化剂
新型标记前体
亲核取代
新型标记前体
nucleophilic substitution
手性相转移催化剂
chiral phase transfer catalyst
new precursor
18F-DOPA
Online AccessGet full text
ISSN1000-7512
DOI10.7538/tws.2017.30.01.0071

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Summary: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。
Bibliography:11-2566/TL
18F-DOPA; nucleophilic substitution; new precursor; chiral phase transfer catalyst
[^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.
JIA Li-na1,2,3,ZHANG Lan1,2,3 （1.Department of Radiochemistry and Engineering, Shanghai Institute of Applied Physics, Chinese Academy of
ISSN:1000-7512
DOI:10.7538/tws.2017.30.01.0071