Carboncarbon bond construction at the 2-position of polysubstituted pyrimidinones

A novel synthetic method to introduce a carboncarbon bond at the 2-position of pyrimidinones via nucleophilic addition of Grignard reagents to 2-cyano pyrimidinones at ambient conditions is disclosed. This unique approach leads to the preparation of such biologically important molecules as polysubstituted pyrimidinones in good to excellent yields.