Potential Antimetabolites. I. Selective Thiation of Uracil and 1, 2, 4-Triazine-3, 5 (2<I>H</I>, 4<I>H</I>)-dione (6-Azauracil)

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  • 水野 義久
    Faculty of Pharmaceutical Sciences, School of Medicine, Hokkaido University
  • 池原 森男
    Faculty of Pharmaceutical Sciences, School of Medicine, Hokkaido University
  • 渡辺 恭一
    Faculty of Pharmaceutical Sciences, School of Medicine, Hokkaido University

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1, 2, 4-Triazine-3, 5 (2H, 4H)-dione (6-azauracil)(I; R =H) and uracil were partially thiated to afford 5-mercapto-1, 2, 4-triazin-3 (2H)-one (II; R H) and 4-mercapto-2 (1H)-pyrimidinone, respectively, in good yields by the use of limited amount of phosphorus pentasulfide. These are the first examples of the success of monothiation in triazine and pyrimidine series. The alkylation of 5-mercapto-1, 2, 4-triazin-3 (2H)-one gave the corresponding alkylthio derivatives (IV and V; R=H) from which 5-amino-1, 2, 4-triazin-3 (2H)-one (6-azacytosine)(III; R=H) was synthesized in an excellent yield.

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