Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter.
Carlos VilaFares Ibrahim AmrGonzalo BlayM Carmen MuñozJosé R PedroPublished in: Chemistry, an Asian journal (2016)
An efficient one-pot asymmetric synthesis of pyrazoles bearing a chiral quaternary stereocenter has been developed. Quinine-derived thiourea catalyzed the enantioselective addition of pyrazolones to isatin-derived ketimines, providing the corresponding acetylated pyrazoles after in situ treatment with Ac2 O/Et3 N. The corresponding pyrazoles were afforded in high yields and excellent enantioselectivities.
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