Studies on the Syntheses of N-Heterocyclic Compounds. XXII. The Reaction of Polyazanaphthalene Derivatives with Organometallic Reagents

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概要

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• Reaction of 5,8-dimorpholino-2-phenylpyrimido [4,5-d] pyridazine (I) with Grignard reagent or organolithium afforded 4-substituted-3,4-dihydro derivatives (II). The use of an excess of the reagent gave rise to further substitution at 8-position to afford 4,8-disubstituted-3,4-dihydro derivatives (III and VII). Similar results were observed in the reaction of Grignard reagents with analogous tetraazanaphthalene derivatives, 5,8-dimorpholino-2-phenylpyrimido [4,5-d] pyrimidine (XX) and 5,8-dimorpholino-2-phenyl-pyrazino [2,3-d] pyridazine (XXII), to afford 4-substituted-3,4-dihydro derivatives (XXI) and 3-substituted-3,4-dihydro derivatives (XXIII), respectively. Among the obtained derivatives, IIa and IIj exhibited significant diuretic activity.

• 公益社団法人日本薬学会の論文
• 1975-07-25

著者

• 伊藤 克己

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• 万木 庄次郎

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

• 岡 良和

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

• 万木 庄次郎

  武田薬品中研

• 伊藤 克已

  Central Research Division Takeda Chemical Industries Ltd.

• 多田 憲生

  Central Research Division, Takeda Chemical Industries, Ltd.

• 多田 憲生

  Central Research Division Takeda Chemical Industries Ltd.

• 多田 憲生

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

• 伊藤 克己

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

• 三宅 昭夫

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

• 三宅 昭夫

  Chemistry Laboratories Central Research Division Takeda Chemical Industries Ltd.

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