Catalytic Asymmetric Access to Noncanonical Chiral α-Amino Acids from Cyclic Iminoglyoxylates and Enamides.

Here we describe an enantioselective Mannich reaction of cyclic iminoglyoxylates with enamides by virtue of chiral phosphoric acid catalysis in a one-pot manner. The wide substrate scope, mild reaction conditions, and constantly excellent enantioselectivities (>95% ee in most cases) render this protocol highly practical for the rapid construction of valuable noncanonical chiral α-amino-acid building blocks.