Synthesis of 3-chloro-6-((4-(di-tert-butyl[18F]-fluorosilyl)-benzyl)oxy)-1,2,4,5-tetrazine ([18F]SiFA-OTz) for rapid tetrazine-based 18F-radiolabeling

被引：22
|
作者：
Zhu, Jun [1 ,2 ,3 ]
Li, Stephen [1 ,2 ,3 ]
Waengler, Carmen [4 ]
Waengler, Bjoern [5 ]
Lennox, R. Bruce [1 ,2 ]
Schirrmacher, Ralf [3 ,6 ]
机构：
[1] McGill Univ, Dept Chem, Montreal, PQ H3A 2K6, Canada
[2] McGill Univ, Ctr Self Assembled Chem Struct, Montreal, PQ H3A 2K6, Canada
[3] McGill Univ, Montreal Neurol Inst & Hosp, Montreal, PQ H3A 2B4, Canada
[4] Heidelberg Univ, Med Fac Mannheim, Dept Clin Radiol & Nucl Med, Biomed Chem, Mannheim, Germany
[5] Heidelberg Univ, Med Fac Mannheim, Dept Clin Radiol & Nucl Med, Mol Imaging & Radiochem, Mannheim, Germany
[6] Univ Alberta, Dept Oncol, Div Oncol Imaging, Edmonton, AB T6G 1Z2, Canada
来源：
CHEMICAL COMMUNICATIONS | 2015年 / 51卷 / 62期
基金：
加拿大自然科学与工程研究理事会;
关键词：
TRANS-CYCLOOCTENE; PEPTIDES; LIGATION; F-18; CHEMISTRY; PROTEINS;
D O I：
10.1039/c5cc03623b
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
An efficient method to prepare the F-18-labeled tetrazine-derivative [F-18]-SiFA-OTz for bioorthogonal radiochemistry was developed. [F-18]-SiFA-OTz can be synthesized with a radiochemical yield of 78 +/- 5% within 25 min and can quantitatively react with a model strained dienophile, trans-cyclooctenol.
引用
收藏
页码：12415 / 12418
页数：4
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