Practical and efficient methods have been developed for the diversity-oriented synthesis of isoxazolodihydropyridinones via the 1, 3-dipolar cycloaddition of nitrile oxides onto 2, 4- dioxopiperidines. A select few of these isoxazolodihydropyridinones were further elaborated with triazoles by copper-catalyzed azide–alkyne cycloaddition reactions. A total of 70 compounds and intermediates were synthesized and analyzed for drug likeness. Sixty- ...
