【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。更多还原

【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.更多还原