Ionic-liquid-promoted dual hydrogen-bond activation strategy enabling the synthesis of diverse 2-pyridone-fused uracils

Abstract

The synthesis of diverse 2-pyridone-fused uracils has been accomplished using the ionic liquid [bmim]BF4 as a dual hydrogen-bond (HB) activator. A [4 + 2] annulation-dehydration cascade reaction between 6-methyluracil-5-carbaldehydes and isocyanates was promoted through a HB-mediated strategy based on non-covalent interactions (NCIs). This protocol provides an operationally simple procedure that eliminates the use of strong bases, enabling straightforward access to structurally intriguing 2-pyridone-fused uracils-valuable scaffolds with promising potential in drug discovery.