Rhodium-catalyzed aminoacylation of alkenes via carbonylative C–H activation toward poly(hetero)cyclic alkylarylketones†

The well-developed carbonylative synthesis of varied and useful complex molecules with CO is very efficient and attractive. Herein, rhodium-catalyzed modular carbonylative aminobenzoylation of alkenes with a pendant acylaniline enabled by dual cleavage of N–H bonds and C–H bonds under ambient pressure of CO/O₂ was developed. Various poly(hetero)cyclic alkylarylketones were obtained in moderate-to-high yields. The logical synthetic transformations of products were also explored.