Organocatalytic Enantioselective Conjugate Addition of Nitromethane to Benzylidene-2-Benzoyl Acetate: Asymmetric Synthesis of ABT – 627, an Endothelin Receptor Antagonist

oleh: Saumen Hajra, Sk Mohammad Aziz, Bibekananda Jana, Bibekananda Jana, Sunit Hazra

Format: Article
Diterbitkan: Frontiers Media S.A. 2020-03-01

Deskripsi

First catalytic and enantioselective conjugate addition of nitromethane to benzylidene-2-benzoyl acetate has been developed using dihydroquinine derived squaramide catalyst with moderate to high selectivities. Asymmetric total synthesis of ABT-627, a potent ETA receptor antagonist is accomplished utilizing the developed method in overall 15.7% yield.