Improved methodologies for the preparation of highly substituted pyridines

Two separate strategies have been developed for the preparation of highly substituted pyridines from 1,2,4-triazines via the inverse-electron-demand Diels-Alder reaction: a microwave-promoted. Both routes avoid the need solvent-free procedure and a tethered imine-enamine (TIE) approach for a discrete aromatization step and offer significant advantages over the classical methods, giving a wide variety of tri-, tetra-, and penta-substituted pyridines in high, optimized yields.