Difluorination of α-(bromomethyl)styrenes <i>via</i> I(I)/I(III) catalysis: facile access to electrophilic linchpins for drug discovery
Joel Häfliger, Keith Livingstone, Constantin G. Daniliuc, Ryan Gilmour
Abstract
difluorination to occur, thereby providing a platform to generate multiply fluorinated scaffolds for further downstream derivatization. The method facilitates access to a tetrafluorinated API candidate for the treatment of amyotrophic lateral sclerosis. Preliminary validation of an enantioselective process is disclosed to access α-phenyl-β-difluoro-γ-bromo/chloro esters.
Topics & Concepts
ElectrophileCatalysisCombinatorial chemistryChemistryDrug discoveryNanotechnologyOrganic chemistryMaterials scienceBiochemistryFluorine in Organic ChemistryCarbohydrate Chemistry and SynthesisChemical Synthesis and Analysis