PET是当前医学界公认的最先进的大型医疗诊断成像设备之一。PET成像的物质基础是正电子核素标记的放射性药物，放射性药物通常由独立的放射性核素或与有机分子结合的放射性同位素组成。研究表明相比于传统¹⁸F标记方法，近年来备受关注的铜介导的放射性氟化具有反应快速、氟化过程不受体系含水量影响等优点，被大量用于¹⁸F新型标记方法的开发。前列腺癌是人类泌尿系统最常见的癌症，PSMA是前列腺癌诊断和治疗的理想靶点。本研究设计了一类新型PSMA靶向探针，其前体以硼酸酯作为离去基团以便于使用铜介导方法进行¹⁸F标记；通过使用模型化合物及不带放射性的¹⁹F模拟标记过程，并对相转移催化剂种类、溶剂种类、前体与铜盐用量比、反应时间等影响放射化学产率的因素进行优化。从而摸索出所需时间短、放射化学产率高、适于临床自动化合成的标记方法用于后续评价实验，对新型¹⁸F标记的PSMA靶向探针的开发具有重要意义。实验得到最佳模拟标记条件是：前体:铜盐=5:1（n: n），使用K₂₂₂ /KHCO₃作为相转移催化剂，DMF作溶剂，在120℃下反应30 min，产率21.68%。

PET is one of the most advanced large-scale medical diagnostic imaging equipment. The basis of PET imaging is radiopharmaceuticals labeled with positron nuclides. Radiopharmaceuticals are composed of independent radionuclides or radioisotopes combined with organic molecules. Studies have shown that compared to traditional ¹⁸F labeling methods, copper-mediated radiofluorination, which has attracted much attention in recent years, has the advantages of rapid reaction and the fluorination process is not affected by the water content of the system. It has been widely used in the development of new ¹⁸F labeling methods. Prostate cancer is the most common cancer of the human urinary system, and PSMA is a good target for the diagnosis and treatment of prostate cancer. In this study, a new PSMA targeting probe was designed, the precursor used borate ether as the leaving group to facilitate the use of copper-mediated ¹⁸F labeling methods. Through the use of model compounds and non-radioactive ¹⁹F simulated labeling process, the factors that affect the radiochemical yield, such as the type of phase transfer catalyst, the type of solvent, the ratio of the amount of precursor to copper salt, and the reaction time, are optimized to find a labeling method that requires short time, high radiochemical yield, and is suitable for clinical automated synthesis for subsequent evaluation experiments is of great significance to the development of new ¹⁸F-labeled PSMA targeting probes. The best simulated labeling conditions obtained in the experiment are: precursor: copper salt = 5:1 (n: n), using K₂₂₂/KHCO₃ as the phase transfer catalyst, DMF as the solvent, reacting at 120℃ for 30 min, the yield is 21.68%.