1403497-66-4Relevant academic research and scientific papers
Ortho-stabilized 18F-azido click agents and their application in PET imaging with single-stranded DNA aptamers
Wang, Lu,Jacobson, Orit,Avdic, Din,Rotstein, Benjamin H.,Weiss, Ido D.,Collier, Lee,Chen, Xiaoyuan,Vasdev, Neil,Liang, Steven H.
, p. 12777 - 12781 (2015/10/28)
Azido 18F-arenes are important and versatile building blocks for the radiolabeling of biomolecules via Huisgen cycloaddition ("click chemistry") for positron emission tomography (PET). However, routine access to such clickable agents is challenged by inefficient and/or poorly defined multistep radiochemical approaches. A high-yielding direct radiofluorination for azido 18F-arenes was achieved through the development of an ortho-oxygen-stabilized iodonium derivative (OID). This OID strategy addresses an unmet need for a reliable azido 18F-arene clickable agent for bioconjugation reactions. A ssDNA aptamer was radiolabeled with this agent and visualized in a xenograft mouse model of human colon cancer by PET, which demonstrates that this OID approach is a convenient and highly efficient way of labeling and tracking biomolecules. Markedly apt: A high-yielding direct radiofluorination strategy via ortho-oxygen-substituted iodonium derivatives is described. A ssDNA aptamer (sgc8), labelled with the resulting 18F azido agent through click chemistry, was used for PET imaging and provides the first example for the noninvasive in vivo PET imaging of protein tyrosine kinase 7 (PTK-7).
Single-step radiosynthesis of "18F-labeled click synthons" from azide-functionalized diaryliodonium salts
Chun, Joong-Hyun,Pike, Victor W.
, p. 4541 - 4547,7 (2020/08/31)
Positron emission tomography (PET) is an increasingly important biomedical imaging technique that relies on the development of radiotracers labeled with positron emitters to achieve biochemical specificity. Fluorine-18 (t 1/2 = 109.7 min) is an
