Recent Advances in Synthetic Methodologies to Form C-18F Bonds

Frontiers in Chemistry

Tianfei Liu¹  Yijun Sun³  Zhiyi Liu³ 

[1] Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, China;State Key Laboratory of Elemento-Organic Chemistry, Department of Chemistry, Nankai University, Tianjin, China;The Haihe Laboratory of Sustainable Chemical Transformations, Nankai University, Tianjin, China;

关键词: radiofluorination;    organic synthetic methodologies;    leaving functional groups;    transition metal catalysis;    photocatalysis;    electrocatalysis;   

DOI  :  10.3389/fchem.2022.883866

来源: DOAJ

【 摘 要 】

Positron emission tomography (PET) is an important technique for the early diagnosis of disease. Due to the specific physical and chemical properties of Fluorine-18, this important isotope is widely used in PET for labelling and molecular imaging, and its introduction into medicine molecules could produce PET tracers. Developing with the development of organic synthetic methodologies, the introduction of Fluorine-18 into drug molecules efficiently and rapidly under mild conditions, and the formation of C-18F chemical bonds, has become one of the leading topics in both organic synthetic chemistry and radiochemistry. In this mini-review, we review a series of recent advances in the organic synthesis of C-18F bonds (2015–2021), including non-catalytic radiofluorinations via good leaving functional groups, transition metal-catalyzed radiofluorinations, and photo- or electro-catalytic synthetic radiofluorinations. As a result of the remarkable advancements in this field, organic synthetic methods for forming C-18F bonds are expected to continue growing.

【 授权许可】

Unknown