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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