Asymmetric Organocatalytic Tandem Reaction to Chiral Pyrimidinone Derivatives using Urea as Dinitrogen Source

A facile method for the asymmetric synthesis of pyrimidinone derivatives was developed via an organocatalytic tandem aza-Michael addition hemiammal formation dehydroxylation reaction, using N,N'-dialkyloxyurea as dinitrogen source (up to 97% ee). The transformations of hemiaminal intermediates to pyrimidinones with more complex structures have been also investigated.