Direct Catalytic Asymmetric Mannich-Type Reaction of α-N3 Amide.

ABSTRACT

An α-N3 7-azaindoline amide serves as a latent enolate to directly engage in an asymmetric Mannich-type reaction with N-thiophosphinoyl imines by the action of a cooperative catalyst. The thus-obtained highly enantioenriched anti-adduct was transformed into ß-amino-α-azido acid in high yield by simple acidic treatment.