Silver/Rhodium Relay Catalysis Enables C-H Functionalization of In Situ Generated Isoquinolines with Sulfoxonium Ylides:Construction of Hexahydrodibenzo[a，g]quinolizine Scaffolds

摘要

Employing silver/rhodium relay catalysis strategy， an intramolecular electrophilic cyclization and C-H activation followed by cascade hydrogenation and reductive amination has been developed.The acylmethylated isoquinoline derivatives could be afforded with broad substrate scope in 23-88% yields， which could be further transformed to the core skeleton of hexahydrodibenzo[a，g] quinolizine as drug-candidates.Moreover， this reaction was achieved in a gram-scale.A reasonable reaction mechanism has been proposed based on a series of control and KIE experiments.