Synthesis and Antiallergy Activity of [1,3,4]Thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one Derivatives. I

  • 鈴木 範夫
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 三輪 保
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 相原 俊三
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 菅野 英幸
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 高森 秀男
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 坪川 政雄
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 両川 祐一
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 塚田 恒
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
  • 磯田 純郎
    Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,

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抄録

A series of 6-substituted [1,3,4]thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one derivatives 4a-z were synthesized from 5-substituted 1,3,4-thiadiazol-2-amines 5 by the following consecutive reactions : pyrimidine ring closure with bis(2,4,6-trichlorophenyl)malonate, nitration, chlorination, amination, hydrogenation and diazotization. The structure of 4 was confirmed by an alternate synthesis of 4,involving reaction of 5-subsituted 2-azido-1,3,4-thiadiazole 13 with ethyl cyanoacetate, followed by the Dimroth rearrangement and ring closure.The antiallergic activities (anti-passive peritoneal anaphylaxis, anti-passive cutaneous anaphylaxis and anti-slow reacting substance of anaphylaxis activities) of the products were evaluated.

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詳細情報 詳細情報について

  • CRID
    1571980077391890176
  • NII論文ID
    110003629766
  • NII書誌ID
    AA00602100
  • ISSN
    00092363
  • 本文言語コード
    en
  • データソース種別
    • CiNii Articles

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