Abstract

This review provides a brief assessment of the methodological field of trifluoromethylation and its possible impact on the development of new CF3-containing pharmaceuticals. Structural aspects of five new drug-candidates, [tafenoquine (aromatic CF3), roniciclib (heteroaromatic CF3), BAY-38-7271 (aliphatic CF3), sonidegib (OCF3) and navitoclax (S-CF3)] currently under the development in phase II and III clinical studies, and their biological properties, therapeutic area and synthesis are critically discussed.