电化学部分氟化芳基研究进展

含氟芳香化合物具有生物活性好、稳定性高、易被生物体代谢等优点,在医药和农药领域有着广泛的用途。目前芳基部分氟化的方法主要分为依赖于氟化试剂的亲电氟化方法以及反应条件苛刻甚至需要过渡金属催化的亲核氟化方法,这些方法操作繁琐并且污染环境。电化学氟化将"电能"作为一种"强氧化剂"来实现氟化反应,是一种直接、绿色且温和的氟化手段,避免了危险强氧化剂的使用,是现代氟化学发展的重要方向之一。本文重点介绍电化学部分氟化方法在不同类型芳香化合物中的应用,讨论有机溶剂对部分氟化的产率和区域选择性的影响,并介绍了利用电化学手段进行芳香化合物的;F标记的应用。

Progress on Electrochemical Partial Fluorination of Aryls

Biologically active, stable and metabolizable aryl fluorides are widely used as pharmaceuticals and agrochemicals. At present, the methods of partial fluorination of aryl groups are mainly divided into electrophilic fluorination methods relying on fluorination reagents and nucleophilic fluorination methods with harsh reaction conditions and even transition metal catalysis. These methods feature environmental pollution and complicated multi-step reaction operations. Electrochemical fluorination is a direct green synthesis method with electrical energy to replace the powerful oxidants, which provides milder and safer fluorination. This review discusses the methodologies of electrochemical partial fluorination of aryls, the effects of different electrolytic solvents on the fluorination yields and site-selectivity, as well as the electrochemical 18F-labeling of aromatic compounds.