Department of Medicinal Chemistry, the University of Kansas, 1251 Wescoe Hall Dr., 4046A Malott Hall, Lawrence, KS 66045, USA.
Curr Top Med Chem. 2014;14(7):966-78. doi: 10.2174/1568026614666140202210850.
Fluorinated organic compounds have a long history in medicinal chemistry, and synthetic methods to access target fluorinated compounds are undergoing a revolution. One powerful strategy for the installation of fluorinecontaining functional groups includes decarboxylative reactions. Benefits of decarboxylative approaches potentially include: 1) readily available substrates or reagents 2) mild reaction conditions; 3) simplified purification. This focus review highlights the applications of decarboxylation strategies for fluorination reactions to access compounds with biomedical potential. The manuscript highlights on two general strategies, fluorination by decarboxylative reagents and by decarboxylation of substrates. Where relevant, examples of medicinally useful compounds that can be accessed using these strategies are highlighted.
含氟有机化合物在药物化学中有悠久的历史,将目标含氟化合物合成的方法正在经历一场革命。一种用于引入含氟官能团的有力策略包括脱羧反应。脱羧方法的优点可能包括:1)易于获得的底物或试剂;2)温和的反应条件;3)简化的纯化。本综述重点介绍了脱羧策略在氟代反应中的应用,以获得具有生物医学潜力的化合物。本文强调了两种一般策略,即用脱羧试剂进行氟代和用底物进行脱羧。在相关的情况下,突出了可以使用这些策略获得的具有药用价值的化合物的实例。