Enantioselective synthesis of pyrazolone derivatives catalysed by a chiral squaramide catalyst?

RSC Advances Pub Date: 2014-03-11 DOI: 10.1039/C3RA45974H

Abstract

An efficient chiral squaramide-catalysed enantioselective Michael addition of pyrazolin-5-ones to β,γ-unsaturated α-ketoesters has been developed. The chiral pyrazolone derivatives were obtained in moderate to high yields (up to 99% yield) with high enantioselectivities (up to 96% ee) for most substrates. This catalytic asymmetric reaction provides valuable and easy access to chiral pyrazolone ketoester derivatives.

Graphical abstract: Enantioselective synthesis of pyrazolone derivatives catalysed by a chiral squaramide catalyst
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