Towards chemical libraries based on heterocyclic scaffolds with monofluorinated and difluoroalkyl side chains

The preparation of focused chemical libraries, based on five- and six-membered heteroaromatic systems with mono- and gemdifluoroalkyl side chains, is described. Four heterocyclic scaffolds with a p-bromophenyl group have been easily prepared from readily available propargylic fluorides. Starting from these scaffolds, palladium-catalyzed reactions have been performed, including by automated procedures, to prepare libraries of molecules designed for biological applications.

Focused chemical libraries of heteroaromatic systems with mono- and gemdifluoroalkyl side chains have been prepared. Starting from corresponding scaffolds, Pd-catalyzed reactions have been performed, including by automated procedures, to afford libraries of molecules designed for biological applications.Figure optionsDownload as PowerPoint slideHighlights
► New developments in the chemistry of mono- and gemdifluoro propargylic derivatives.
► Design and synthesis of novel heterocyclic scaffolds with fluorinated side chains.
► Preparation, by automated procedures, of chemical libraries designed for biological applications.