Carbonylative N-Heterocyclization via Nitrogen-Directed C–C Bond Activation of Nonactivated Cyclopropanes

Under Rh-catalyzed conditions, secondary amines and anilines function as directing groups to facilitate regioselective C–C bond activation of nonactivated cyclopropanes. The resulting amino-stabilized rhodacycles undergo carbonylative C–N bond formation en route to challenging seven- and eight-membered lactams. The processes represent rare examples where C–C bond oxidative addition of nonactivated cyclopropanes is exploited in reaction design.