Chiral Bidentate Boryl Ligand Enabled Iridium-Catalyzed Enantioselective C(sp3)–H Borylation of Cyclopropanes

We herein report an Ir-catalyzed enantioselective C­(sp3)–H borylation of cyclopropanecarboxamides using a chiral bidentate boryl ligand for the first time. A variety of substrates with α-quaternary carbon centers could be compatible in this reaction to provide β-borylated products with good to excellent enantioselectivities. We have also demonstrated that the borylated products can be used as versatile precursors engaging in stereospecific transformations of C–B bonds, including the synthesis of a bioactive compound Levomilnacipran.