Organocatalytic asymmetric Michael addition of pyrazoleamides to β-phthalimidonitroethene

Abstract A highly organocatalyzed asymmetric Michael addition reaction of pyrazoleamides to β -phthalimidonitroethene has been developed with a chiral bifunctional thiourea-tertiary amine as the catalyst. A wide range of γ -nitro β -amino amides were readily obtained in good to excellent yields with high diastereo- and enantioselectivities (up to 99% yield, 99% ee and >20:1 dr). The large scale experiment and transformation of the product have also been demonstrated.