Isoxazolodihydropyridinones: 1,3-Dipolar Cycloaddition of Nitrile Oxides onto 2,4-Dioxopiperidines
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- 作者：Keith C. Coffman ; Timothy P. Hartley ; Jerry L. Dallas ; Mark J. Kurth
- 刊名：ACS Combinatorial Science
- 出版年：2012
- 出版时间：April 9, 2012
- 年：2012
- 卷：14
- 期：4
- 页码：280-284
- 全文大小：351K
- 年卷期：v.14,no.4(April 9, 2012)
- ISSN：2156-8944
文摘
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鈥揳lkyne 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.