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
スポンサーリンク
概要
- 論文の詳細を見る
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.
- 公益社団法人日本薬学会の論文
- 1992-02-25
著者
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磯田 純郎
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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鈴木 範夫
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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鈴木 範夫
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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相原 俊三
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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菅野 英幸
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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三輪 保
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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塚田 恒
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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高森 秀男
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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坪川 政雄
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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両川 祐一
Exploratory Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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塚田 恒
第一製薬 探索第三研究所
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相原 俊三
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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相原 俊三
第一製薬 探索第三研究所
-
三輪 保
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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高森 秀男
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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坪川 政雄
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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両川 祐一
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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