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Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter |
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| Authors: | Dr Carlos Vila Fares Ibrahim Amr Prof Dr Gonzalo Blay Prof Dr M Carmen Muñoz Prof Dr José R Pedro |
| Institution: | 1. Departament de Química Orgànica, Facultat de Química, Universitat de València, Burjassot, València, Spain;2. Departament de Física Aplicada, Universitat Politècnica de València, València, Spain;3. (+34)?963544328
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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. |
| Keywords: | asymmetric catalysis isatin-derived ketimines organocatalysis pyrazoles quaternary stereocenters |