Difluoroalkylation of tertiary amides and lactams by an iridium-catalyzed reductive Reformatsky reaction



The synthesis of medicinally relevant α-difluoroalkylated amines by an iridium-catalyzed reductive alkylation of tertiary amides and lactams with difluoro-Reformatsky reagents, is described. This report features the introduction of various geminal difluoro-acetates and -acetamides as well as late stage derivatization of APIs, gram scale synthesis and downstream functionalizations.


Supplementary material

Supporting information
Full optimization details, synthesis and characterization of starting materials and products, NMR spectra of unknown compounds.