A fast, simple, and reproducible automated synthesis of [18F]FPyKYNE-c(RGDyK) for αvβ3 receptor positron emission tomography imaging

被引：16
|
作者：
Valdivia, Ana C. [1 ]
Estrada, Miriam [1 ]
Hadizad, Tayebeh [1 ]
Stewart, Duncan J. [1 ,2 ,3 ]
Beanlands, Rob S. [1 ,2 ,3 ]
DaSilva, Jean N. [1 ,2 ,3 ]
机构：
[1] Univ Ottawa, Inst Heart, Natl Cardiac PET Ctr, Ottawa, ON K1Y 4W7, Canada
[2] Univ Ottawa, Div Cardiol, Dept Med, Ottawa, ON K1Y 4W7, Canada
[3] Univ Ottawa, Dept Cellular & Mol Med, Ottawa, ON K1Y 4W7, Canada
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2012年 / 55卷 / 02期
关键词：
av ss 3 integrin receptors; 18F-labeling; 18F]-FPyKYNE; c(iRGDyK); PET; BRAIN-TUMOR ANGIOGENESIS; RGD PEPTIDE; F-18-LABELED RGD; CLICK CHEMISTRY; BREAST-CANCER; IN-VIVO; EXPRESSION; MICROPET; F-18; F-18-GALACTO-RGD;
D O I：
10.1002/jlcr.1948
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
[18?F]FPyKYNE-c(RGDyK) was successfully synthesized by the Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition of alkynes to azides using [18?F]FPyKYNE as a prosthetic group in an overall radiochemical yield of 12%18% (decay-corrected) and >99.5% chemical and radiochemical purities in 125?min including quality control. This simple, fully automated two-step, two-reactor approach consists of a quick and convenient purification of the prosthetic group using silica gel cartridges and its subsequent use for the labeling of the azido-c(RGDyK) peptide via click chemistry.
引用
收藏
页码：57 / 60
页数：4
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