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| Synthesis of F-18-c(RGDfK) as Integrin alpha(v)beta(3) Targeted PET Tracer via Click Chemsitry with Cu(I) Catalyst Systems | |
| Shi, LL（施玲丽）; Li, JB（李剑波）; Wang, C（王成）; Jia, LN（贾丽娜）; Wang, YX（汪勇先）; Zhang, L（张岚） | |
| 2012 | |
| Source Publication | CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 |
| ISSN | 0251-0790 |
| Volume | 33Issue:7 |
| 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-[F-18]fluoroethyl azide([F-18]FEA) was synthesized by nucleophilic substitution of F-18(-). Then, [F-18]fluoroethyl-1H-1,2,3-triazole-4-c(RGDfK) [F-18-c(RGDfK)] was radio-synthesized as integrin alpha(v)beta(3), targeted PET tracer fast and efficiently via Click reaction of [F-18]FEA with propioloyl c(RGDfK). Three catalyst systems of click reaction were investigated; CuSO4/NaVc, Cul(s) and CuI/NH2OH, 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 F-18-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 F-18 labeled peptides. |
| Language | 英语 |
| Funding Project | 应物所项目组 |
| WOS ID | WOS:000306880600022 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.sinap.ac.cn/handle/331007/13307 |
| Collection | 中科院上海应用物理研究所2011-2020年 |
| Recommended Citation GB/T 7714 | Shi, LL,Li, JB,Wang, C,et al. Synthesis of F-18-c(RGDfK) as Integrin alpha(v)beta(3) Targeted PET Tracer via Click Chemsitry with Cu(I) Catalyst Systems[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2012,33(7). |
| APA | Shi, LL,Li, JB,Wang, C,Jia, LN,Wang, YX,&Zhang, L.(2012).Synthesis of F-18-c(RGDfK) as Integrin alpha(v)beta(3) Targeted PET Tracer via Click Chemsitry with Cu(I) Catalyst Systems.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,33(7). |
| MLA | Shi, LL,et al."Synthesis of F-18-c(RGDfK) as Integrin alpha(v)beta(3) Targeted PET Tracer via Click Chemsitry with Cu(I) Catalyst Systems".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 33.7(2012). |
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| Synthesis of F-18-c(（680KB） | 开放获取 | CC BY-NC-SA | View Download | |||
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