Studies on the Syntheses of N-Heterocyclic Compounds. VII. 2-Aryl-5,8-disubstitutedpyrimido [4,5-d] pyridazine

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概要

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• When 2-aryl-5,8-dichloropyrimido [4,5-d] pyridazine (1) was reacted with a variety of nucleophiles, such as amines, sodium methoxide, sodium azide, sodium sulfide etc., 5,8-disubstituted compounds (5) were obtained. Treatment of 2-phenyl-5-chloro-8-morpholinopyrimido [4,5-d] pyridazine (9,[chemical formula] : morpholino) or 2-phenyl-5-morpholino-8-chloropyrimido [4,55-d] pyridazine (10,[chemical formula] : morpholino) with nucleophiles gave the corresponding products with a different kind of substituents at 5-and 8-position (12 and 13). The phenyl group at 2-position seems to accelerate the substitution at position 5 and 8. The reaction of 2-phenyl-5,8-bis (substituted thio) pyrimido [4,5-d] pyridazine (5) with chlorine afforded the dichloride (1,Ar : phenyl). Among the synthesized disbstituted compounds, 5v, 5h, 5i, 5j, 5k, 5m, 5C, 5E, 5F, 5K, 5M and 5O showed diuretic activity.

• 公益社団法人日本薬学会の論文
• 1972-07-25

著者

• 万木 庄次郎

  武田薬品中研

• 川松 豊

  干寿製薬株式会社経営戦略室

• 冨本 光美

  京大(医)衛生学

• 杉原 弘貞

  Chemistry Research Laboratories, Takeda Chemical Industries, Ltd.,

• 杉原 弘貞

  Central Research Division Takeda Chemical Industries. Ltd.

• 川松 豊

  Chemical Research Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.

• 万木 庄次郎

  Chemical Research Laboratories, Research and Development Division, Takeda Chemical Industries, Ltd.

• 稗田 勝

  Chemical Research Laboratories, Research and Development Division, Takeda Chemical Industries, Ltd.

• 伏見 富吉

  Chemical Research Laboratories, Research and Development Division, Takeda Chemical Industries, Ltd.

• 冨本 光美

  Chemical Research Laboratories, Research and Development Division, Takeda Chemical Industries, Ltd.

• 稗田 勝

  武田薬品工業株式会社, 研究開発本部, 化学研究所

• 稗田 勝

  武田薬品工業株式会社 研究開発本部 化学研究所

• 伏見 富吉

  武田薬品工業株式会社 中央研究所 化学研究所

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