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  • Title: A Novel Methodology for Synthesis of 1,5,6-Trisubstituted 2(1H)-Pyrazinones of Biological Interest.
    Author: Saijo R, Sekiya H, Tamai E, Kurihara KI, Maki J, Sakagami H, Kawase M.
    Journal: Chem Pharm Bull (Tokyo); 2017; 65(4):365-372. PubMed ID: 28381677.
    Abstract:
    In this report, we describe a new method for the synthesis of densely functionalized 2(1H)-pyrazinones. Treatment of mesoionic 1,3-oxazolium-5-olates with carbanions derived from activated methylene isocyanides (p-toluenesulfonylmethyl isocyanide (TosMIC) and ethyl isocyanoacetate) causes a novel ring transformation affording 2(1H)-pyrazinones in moderate to high yields. The cytotoxicity and antibacterial activity of some of the obtained products were studied and some of the products exhibited tumor-specific cytotoxicity.
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