Figure 4. Direct trifluoromethylation of biologically active molecules.

Subjecting common medicinal agents and other biologically active molecules to our standard photoredox protocol enables direct CF₃ installation selectively at metabolically susceptible positions of some molecules (a). Alternatively, C–H functionalization of more metabolically stable medicines occurs non-selectively, allowing for rapid access to drug analogues (b). The promiscuous modification of equally reactive π-systems, such as the arenes in Lipitor, may be followed by separation of isomers (for example, via supercritical fluid chromatography, SFC) for rapid screening of biological activity (c).