高等学校化学学报2012，Vol.33Issue(7)：1486-1489,4.DOI:10.3969/j.issn.0251-0790.2012.07.022
整合素αvβ3靶向PET探针18F-c(RGDfK)在Cu(I)催化体系中的点击合成
Synthesis of 18F-c(RGDfK) as Integrin αvβ3 Targeted PET Tracer via Click Chemsitry with Cu( I ) Catalyst Systems
摘要
Abstract
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-[ l8F]fluoroethyl azide( [ 18F]FEA) was synthesized by nucleophilic substitution of 18F-. Then, [l8F]fluoroethyl-1 H-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 [ 18F] FEA with propioloyl c( RGDfK). Three catalyst systems of click reaction were investigated: CuS04/NaVc, Cul(s) and CuI/NH4OH, the last two have been used in peptide-click-labeling for the first time. While CuS04/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.关键词
点击化学/18F标记/1,3-偶极环加成/叠氮化物/精氨酸-甘氨酸-天冬氨酸(RGD)序列Key words
Click chemistry/18F-labeling/ 1,3-Dipolar cycloaddition/ Azide/ RGD分类
化学化工引用本文复制引用
施玲丽,李剑波,王成,贾丽娜,汪勇先,张岚..整合素αvβ3靶向PET探针18F-c(RGDfK)在Cu(I)催化体系中的点击合成[J].高等学校化学学报,2012,33(7):1486-1489,4.基金项目
国家自然科学基金(批准号:10805069,10875163)资助. （批准号:10805069,10875163）
