Pd/Xiang-Phos-catalyzed enantioselective intermolecular carboheterofunctionalization under mild conditions

A mild and practical Pd/Xiang-Phos-catalyzed enantioselective intermolecular carboheterofunctionalization reaction of 2,3-dihydrofurans is developed, leading to various optically active fused furoindolines and tetrahydrofurobenzofurans. The key to this transformation is employing two newly modifiedN-Me-Xiang-Phos ligands ((S,R-S)-N-Me-X4/X5) as chiral ligands under mild conditions. Moreover, this synthetic methodology can be efficiently applied to a variety of complex polysubstituted heterocycles with high chemo-, regio-, and enantio-selectivitiesviaintroducing diverse substituents on furan rings, which were hard to access by other routes.