N-琥珀酰亚胺4-[^(18)F]氟苯甲酸酯的合成  

Synthesis of N-succinimidyl-4-[^(18)F]fluorobenzoate

作　　者：程登峰[1] 尹端沚[1] 王明伟[1] 李谷才[1] 周伟[1] 汪勇先[1] 

机构地区：[1]中国科学院上海应用物理研究所放药中心,上海201800

出　　处：《核技术》2006年第12期917-920,共4页Nuclear Techniques

基　　金：中国科学院知识创新工程重大项目(KJCX-SW-08);国家自然科学基金(30371634)资助

摘　　要：合成了18F标记多肽和蛋白类药物中常用的中间体N-琥珀酰亚胺-4-[18F]氟苯甲酸酯([18F]SFB)。由于[18F]SFB能和生物分子结合达到较高的标记率以及具有较好的体内稳定性,成为一种最适宜的氟-18标记试剂。本工作首先合成标记前体乙基-4-三甲胺苯甲酸酯-三氟磺酸盐,接下来经三步放射合成,然后经Sep-PakC18柱分离可得[18F]SFB,并对第一步的18F标记反应进行了优化。合成时间约1h;放化产率约50%;经放射性TLC和HPLC分析,放化纯度大于98%。We have synthesized ^18F-labeled prosthetic group, N-succinimidyl 4-[^18F]fluorobenzoate （[^18F]SFB） for fluorine-18 labeling peptides and proteins. [^18F]SFB seems to be the most suitable ^18F-labeling agent because of its higher labeling yield and better stability of the conjugates in vivo. Labeling prosthetic group, triflate salt of ethyl p-trimethylammonium benzoate, was synthesized first, then the radio-synthesis with three steps was carried out, and the first step about ^18F -labeling was optimized. After purifying through Sep-Pak C18 cartridge, [^18F]SFB was produced with the decay-corrected radiochemical yield of 50% within 1 hour.The radiochemical purity was more than 98% by using radio-TLC and HPLC.

关 键 词：^18F N-琥珀酰亚胺4-[^18F]氟苯甲酸酯([^18F]SFB) 放射性合成 

分 类 号：O621.3[理学—有机化学]