中文摘要：

通过2-叠氮乙基对甲苯磺酸酯的18F-亲核取代反应,制备了[18F]2-氟叠氮乙烷,并与丙炔酸修饰的c（RGDfK）反应,采用常用的CuSO4/NaVc催化体系,并尝试了CuI（s）和CuI/NH4OH 2种催化体系,通过点击化学方法合成了整合素αvβ3靶向PET探针[18F]氟乙基-1,4-取代1,2,3-三唑c（RGDfK）[18F-c（RGD-fK）].在CuSO4/NaVc的催化下,18F-c（RGDfK）的总合成时间约为60 min,总收率62%（从[18F]F-起计,经过衰变校正）.实验结果表明,点击化学方法高效便捷,适于多肽的18F标记.

英文摘要：

As one of the most important types of Click chemistry,copper-catalyzed 1,3-dipolar cycloaddition reaction has attracted great attention.In this study,2-fluoroethyl azide（FEA） was synthesized by nucleophilic substitution of 18F-.Then,fluoroethyl-1H-1,2,3-triazole-4-c（RGDfK）[18F-c（RGDfK）] was radio-synthesized as integrin αvβ3 targeted PET tracer fast and efficiently via Click reaction of FEA with propioloyl c（RGDfK）.Three catalyst systems of click reaction were investigated： CuSO4/NaVc,CuI（s） and CuI/NH4OH,the last two have been used in peptide-click-labeling for the first time.While CuSO4/NaVc catalysing the Click reaction,the total radio-chemistry yield of 18F-c（RGDfK） was 62% and the synthesis time was about 60 min（decay-corrected）.Click chemistry has demonstrated to be an extraordinarily efficient and convenient method for the preparation of 18F labeled peptides.