Organocatalytic Highly Enantio- and Diastereoselective Mannich Reaction of β-Ketoesters with N-Boc-aldimines

The catalytic enantioselective Mannich reaction promoted by chiral bifunctional organocatalysts is described. The treatment of beta-ketoesters with N-Boc-aldimines under mild reaction conditions afforded the corresponding beta-amino beta-ketoesters with excellent diastereoselectivities (up to 100:0 dr) and excellent enantioselectivities (up to 99% ee).