Liu Zhiyi, Sun Yijun, Liu Tianfei
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.
Front Chem. 2022 Apr 14;10:883866. doi: 10.3389/fchem.2022.883866. eCollection 2022.
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-F 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-F 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-F bonds are expected to continue growing.
正电子发射断层扫描（PET）是疾病早期诊断的一项重要技术。由于氟-18具有特定的物理和化学性质，这种重要的同位素在PET中被广泛用于标记和分子成像，将其引入药物分子可制备PET示踪剂。随着有机合成方法的发展，在温和条件下高效、快速地将氟-18引入药物分子并形成碳-氟化学键，已成为有机合成化学和放射化学的前沿课题之一。在本综述中，我们回顾了碳-氟键有机合成（2015-2021年）的一系列最新进展，包括通过良好离去官能团的非催化放射性氟化、过渡金属催化的放射性氟化以及光催化或电催化合成放射性氟化。由于该领域的显著进展，形成碳-氟键的有机合成方法有望持续发展。
