Department of Chemistry, University of California, Davis, California 95616, United States.
ACS Comb Sci. 2012 Apr 9;14(4):280-4. doi: 10.1021/co200200u. Epub 2012 Mar 16.
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.
已开发出实用且高效的方法，通过腈氧化物与 2,4-二氧代哌啶的 1,3-偶极环加成，实现异噁唑二氢吡啶酮的多样性导向合成。通过铜催化的叠氮化物-炔烃环加成反应，对其中少数几个异噁唑二氢吡啶酮进行了进一步的三唑修饰。共合成并分析了 70 种化合物和中间体，以评估其类药性。这些新型化合物中的 64 种已提交给 NIH 分子库小分子库进行高通量生物筛选。
