【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%。更多还原

【Abstract】 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.更多还原