Rh-Catalyzed Asymmetric Hydrogenation of α-Aminomethyl Acrylates for Enantioselective Synthesis of Chiral β-Amino Propanoates

Rh-catalyzed asymmetric hydrogenation of α-aminomethyl acrylates has been successfully achieved. This process can produce a variety of chiral β-amino propanoates in high yield with excellent enantioselectivities (up to 99% ee). Moreover, high turnover numbers (TON up to 2000) can also be attained. Notably, the substrates without an acyl protecting group on the amino group have also been successfully hydrogenated, yielding the free chiral secondary β-amino propanoates with excellent enantioselectivities of up to 98% ee.