Fluorine in health care: Organofluorine containing blockbuster drugs

Organic fluorine compounds have had a profound impact on the development of bioactives for the modern pharmaceuticals market. It is estimated that up to 20% of pharmaceuticals prescribed or administered in the clinic contain a fluorine atom and 30% of the leading 30 blockbuster drugs by sales contain a fluorine. In this Highlight review, the top 10 fluorine containing pharmaceuticals (by US Sales in 2008) are highlighted. By this measure, these are currently the most significant fluorinated compounds impacting on health care. They embrace statins (Lipitor, Crestor, Vytorin, Zetia/Ezetimibe), anti-inflammatories (fluticasone propionate, Celebrex), antacids (Prevacid), antidepressants (Lexapro), neuroleptics (Risperdal) and antibiotics (Levaquin). In each case the structures and modes of action of these important drugs compounds are reviewed and representative synthetic routes are highlighted.

Graphical abstractOrganofluorine compounds have had a significant impact in the development of pharmaceutical products. The structures, modes of action and synthesis of the leading blockbuster pharmaceuticals of this class are highlighted. Currently 30% of the top thirty drugs by sales contain a fluorine atom.Figure optionsDownload full-size imageDownload as PowerPoint slide