N-Trifluoromethylated amides are the new kid on the block in drug discovery, with the potential to combine the favourable characteristics of two important functional groups. Amides are present in more than 40% of bioactive molecules, while fluorine features in approximately 23% of pharmaceuticals, reflecting its longstanding success in improving key drug properties such as metabolic stability, potency and selectivity. Despite this promise, N-(trifluoromethyl)amides have been difficult to access and not much has been known about their pharmacokinetic properties until very recently. In a review recently accepted in Chemical Science, we highlight advances in the synthesis of N-(trifluoromethyl)amides and evaluate their physical properties and suitability as drug targets.
