Simple and efficient strategy for the synthesis of pyridone derivatives

Multicomponent reactions (MCRs) are useful methods in the sustainable and diversity-oriented synthesis of heterocyclic compounds, especially for the synthesis of heterocyclic drug-like compounds.Synthesis of heterocyclic compounds, especially an important class of biologically active nitrogen containing compounds, which present a wide range of therapeutic and pharmacological properties is finding out that currently available compounds could not responsive the needs of chemical drug-like compounds. Pyridone-based molecules have shown a broad range of biological properties such as antifungal, anti-HIV, antitumoral, anti-hepatitis B, anti-mycobacterium tuberculosis agents [1,2].In continuation of our interest in the application of 1,1-bis(methylthio)-2-nitroethene in organic synthesis [3], herein we report an efficient and simple synthesis of pyridone derivatives, via a one-pot four-component reaction of nitro ketene aminals derived from the addition of various 1,n-diamines 1 to 1,1-bis(methylthio)-2-nitroethene 2 with aryl glyoxal 3 and methyl cyanoacetate or ethyl cyanoacetate 4 in EtOH as safe solvent under reflux condition in good to excellent yields (Fig 1). This strategy has the advantages of easy workup, mild reaction conditions without using catalysts. All structures were determined by IR, MS, 1H- and 13C-NMR analysis.