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Organocatalytic Enantioselective Aminoalkylation of Pyrazol-3-ones with Aldimines Generated in Situ from α‐Amido Sulfones

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Valencià Castellano

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Organocatalytic Enantioselective Aminoalkylation of Pyrazol-3-ones with Aldimines Generated in Situ from α‐Amido Sulfones

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Carceller-Ferrer, Laura; Vila Descals, Carlos; Blay Llinares, Gonzalo; Fernández Picot, Isabel; Muñoz, M. Carmen; Pedro, José Ramón

Aquest document és un/a article, creat/da en: 2019

Herein, an efficient asymmetric aminoalkylation of pyrazolones with α-amido sulfones catalyzed by a quinine-derived squaramide in dichloromethane/aqueous media has been established. A variety of chiral amines were obtained with high yields (up to 98%) and excellent enantioselectivities (up to 99% ee). The corresponding products are transformed into optically active acetylated pyrazoles after treatment with Ac2O/Et3N, because of the instability of some adducts. The reaction tolerates a wide range of α-amido sulfones and different pyrazolones.

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