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Electrochemical fluorodecarboxylation for the labelling of gem-difluoro(cyclo)alkanes/amines

Electrochemical fluorodecarboxylation for the labelling of gem-difluoro(cyclo)alkanes/amines
用于标记偕二氟(环)烷烃/胺的电化学氟脱羧
批准号:
EP/X02458X/1
负责人:
Long Yang
金额:
$26.0万
依托单位:
依托单位国家:
英国
项目类别:
Fellowship
财政年份:
2022
资助国家:
英国
项目状态:
未结题
起止时间:
2022 至 --

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中文摘要
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英文摘要
Positron emission tomography (PET) is a powerful molecular imaging modality for diagnosis, monitoring disease progression, studying biological processes in vivo, and investigating the efficacy of drugs. Among the radioisotopes employed for the preparation of PET probes, fluorine-18 is a widely used and clinically relevant radionuclide in part due to its favourable decay properties, and the numerous clinical applications. While radiochemists have in recent years focused their efforts on methods enabling 18F-labelled fluorination and trifluoromethylation of (hetero)arenes, 18F-radiolabelled gem-difluorinated reactions have been much less studied despite the importance of the gem-difluoromethylene group (CF2) in radioligand design for drug discovery programmes. Herein, we propose a solution merging electrochemistry and 18F radiochemistry with the development of a novel electrochemical fluorodecarboxylation process affording 18F-labelled gem-difluoro(cyclo)alkanes and (cyclo)amines including structurally complex pharmaceutical drugs.
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