A Novel Methodology for Synthesis of 1,5,6-Trisubstituted 2(1H)-Pyrazinones of Biological Interest.

نویسندگان

  • Ryosuke Saijo
  • Hiroshi Sekiya
  • Eiji Tamai
  • Ken-Ichi Kurihara
  • Jun Maki
  • Hiroshi Sakagami
  • Masami Kawase
چکیده

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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عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 65 4  شماره 

صفحات  -

تاریخ انتشار 2017