Fluoroprolines

Fluorinated prolines help improve the lipophilicity, conformation, and dynamic properties of drugs. The first fluoroproline-based drug molecule, danicopan, was approved by the FDA in March 2024. Prusogliptin, another drug candidate, has recently shown success in Phase 3 trials. In April 2024, Pfizer disclosed the second-generation inhibitor of the SARS-CoV-2 main protease containing trifluoromethylproline. In this molecule, the fluorination enhances the dynamics of the amide rotation, thereby eliciting beneficial effects on bioavailability. Enamine offers a broad and remarkably rich collection of fluorine-containing analogues of proline.