Design and synthesis of fluorine aromatic scaffolds containing drugs approved by the US FDA from 2002 to 2022

Abstract

There are totally 93 fluorine aromatic scaffolds containing drugs approved by U.S. Food and Drug Administration from 2002 to 2022. The proportion of drugs containing fluorinated aromatic skeleton in approved drugs is increasing in recent ten years, which indicates the unique and important attributes of the fluorine atom. The introduction of fluorinated fragments into molecules can influence structure conformation, intrinsic potency and selectivity and pharmacokinetic properties productively. Additionally, 18F has been applied as a significant and useful positron emission tomography isotope for in vivo imaging technology. This review is mainly concentrated on the application and synthesis methods of 93 fluorine aromatic scaffolds containing drugs approved by the US FDA from 2002 to 2022. We hoped that this deep insight perspective into the synthetic methods for the delivery of these fluorine aromatic scaffolds containing drugs could offer practical and creative inspirations for the application and development of fluorine atom in new drug discovery.