Enantioselective Addition of Pyrazoles to Dienes

Abstract

We report the first enantioselective addition of pyrazoles to 1,3-dienes. Secondary and tertiary allylic pyrazoles can be generated with excellent regioselectivity. Mechanistic studies support a pathway distinct from previous hydroaminations: a Pd(0)-catalyzed ligand-to?ligand hydrogen transfer (LLHT). This hydroamination tolerates a range of functional groups and provides a breakthrough in hydrofunctionalization of dienes. <br>