Abstract
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-four of these novel compounds were submitted to the NIH Molecular Libraries Small Molecule Repository for high-throughput biological screening.
Original language | English (US) |
---|---|
Pages (from-to) | 280-284 |
Number of pages | 5 |
Journal | ACS Combinatorial Science |
Volume | 14 |
Issue number | 4 |
DOIs | |
State | Published - Apr 9 2012 |
Keywords
- 1,3-dipolar cycloaddition
- Cu(I)-catalyzed azide-alkyne cycloaddition
- heterocycle
- isoxazole, triazole
ASJC Scopus subject areas
- Chemistry(all)