Fluoroalkyl Motif for Enhanced Solubility

2,2-Difluorocyclobutyl is a recent and successful addition to the toolkit of fluoroalkyl groups. First introduced in 2019 by scientists at Enamine, it serves as an analogue to the more widely used 3,3-difluorocyclobutyl motif. The latter has been incorporated into one FDA-approved drug (Ivosidenib, Servier) and three other drugs that reached clinical trials. Unlike the 3,3-difluoro- variant, the 2,2-difluorocyclobutyl group is less symmetric, which typically enhances the solubility of compounds by over an order of magnitude. Discover our latest collection of 2,2-difluorocyclobutyl compounds, designed to deliver improved pharmacological properties.