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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 PublicationCHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
ISSN0251-0790
Volume33Issue:7
AbstractAs 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 IDWOS:000306880600022
Citation statistics
Document Type期刊论文
Identifierhttp://ir.sinap.ac.cn/handle/331007/13307
Collection中科院上海应用物理研究所2011-2019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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