Strategic Incorporation of Fluorine for Drug Discovery and Development

The extraordinary potential of fluorine in therapeutic and diagnostic agents has been extensively studied and successfully exploited for the drug discovery and development in the past three decades. Accordingly, in the current drug design, fluorine is considered the second "favorite heteroatom" only after nitrogen. The strategic incorporation of fluorine(s) into biologically active compounds often brings about pharmacologically beneficial properties. ¹⁸F-positron emission tomographic (PET) imaging enables rapid and accurate assessment of biodistribution and metabolic profiles of drug candidates. Also, ¹⁸F-PET imaging can be used for diagnosing neurological disorders such as Alzheimer disease. In this chapter, selected new fluorine-containing drugs, which have recently been approved by the US Food and Drug Administration or evaluated in phase III clinical trials for the unmet medical needs, are described, wherein the significance of the strategic incorporation of fluorine(s) in these drugs, as well as the modern synthetic processes employed for the production of these drugs, is discussed.