Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter

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Abstract

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 Ac2O/Et3N. The corresponding pyrazoles were afforded in high yields and excellent enantioselectivities. Four's a charm: In an efficient one-pot asymmetric synthesis, pyrazoles bearing a chiral quaternary stereocenter are synthesized by enantioselective addition of pyrazolones to isatin-derived ketimines. The reaction is catalyzed by quinine-derived thiourea, and the corresponding acetylated pyrazoles are obtained in high yields and excellent enantioselectivities after in situ treatment with Ac2O/Et3N.

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Vila, C., Amr, F. I., Blay, G., Muñoz, M. C., & Pedro, J. R. (2016). Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter. Chemistry - An Asian Journal, 11(10), 1532–1536. https://doi.org/10.1002/asia.201600325

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