Abstract
AbstractEmploying 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.magnified image
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