Research Progress in the Preparation of 18F-DOPA

doi:10.7538/tws.2017.30.01.0071

Abstract

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

JIA Li-na;ZHANG Lan. Research Progress in the Preparation of ¹⁸F-DOPA[J]. JOURNAL OF ISOTOPES, DOI: 10.7538/tws.2017.30.01.0071.

贾丽娜;张岚. ¹⁸F-DOPA制备研究进展[J]. 同位素, DOI: 10.7538/tws.2017.30.01.0071.

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Research Progress in the Preparation of ¹⁸F-DOPA

¹⁸F-DOPA制备研究进展

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