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

页码：57 / 60

页数：4

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