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

Zhiyi Liu; Yijun Sun; Tianfei Liu

doi:10.3389/fchem.2022.883866

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

Front Chem. 2022 Apr 14:10:883866. doi: 10.3389/fchem.2022.883866. eCollection 2022.

Authors

Zhiyi Liu^{1

2}, Yijun Sun^{1

2}, Tianfei Liu^{1

2

3}

Affiliations

¹ State Key Laboratory of Elemento-Organic Chemistry, Department of Chemistry, Nankai University, Tianjin, China.
² The Haihe Laboratory of Sustainable Chemical Transformations, Nankai University, Tianjin, China.
³ Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, China.

Abstract

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.

Keywords: electrocatalysis; leaving functional groups; organic synthetic methodologies; photocatalysis; radiofluorination; transition metal catalysis.

Publication types

Review