Modular Construction of Chiral Aminopiperidine via Palladium-Catalyzed Hydroamination of 1,2-Dihydropyridine.

In this study, we describe a generally straightforward methodology for the catalytic synthesis of chiral aminopiperidine from pyridine and azoles. The key step was the palladium-catalyzed regioselective N-H insertion into the double bond of 1,2-dihydropyridine. This hydroamination exhibits a wide substrate scope and functional group compatibility.