Rapid Construction of Hexahydro‐1H‐pyrrolo[3,2‐c]pyridines with Functionalized 1,3‐Enynes and Imines via Palladium Catalysis

Presented herein is a palladium catalyzed tandem reaction between 3‐aminoethyl group tethered 1,3‐enynes and imines, proceeding through a cascade vinylogous addition/reductive elimination/protonation/allylic amination and 1,3‐hydrogen transfer sequence. A collection of complex hexahydro‐1H‐pyrrolo[3,2‐c]pyridine architectures were straightforwardly constructed in moderate yields and diastereoselectivity. A tandem reaction between 2‐aminoethyl tethered 1,3‐enynes and imines was developed via palladium catalysis, which provided an efficient and economical access to biologically important hexahydro‐1H‐pyrrolo[3,2‐c]pyridines.