Fused Pyrimidines. IV. Synthesis of 3-Alkyl (or Acyl)-aminopyrazolo [3,4-d] pyrimidine Derivatives from 6-Hydrazinouracils and Isothiocyanates

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概要

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• 1,3-Dialkyl-6-hydrazinouracils (I) reacted with alkyl and acyl isothiocyanates to yield 5,7-dialkyl-3-alkyl (or acyl) aminopyrazolo [3,4-d] pyrimidine-4,6 (5H, 7H)-diones (II). This reaction was investigated in detail and it was found that the first product was a 6-[4-alkyl (or acyl) thiosemicarbazido] uracil (IV), which cyclized to II through two pathways. Acylation of II afforded the corresponding 2-acyl derivatives. Treatment of 1,3-diethyl-6-hydrazinouracil (Ia) with phosgeneimmonium chloride afforded 5,7-diethyl-3-dimethylamino [3,4-d] pyrimidine-4,6 (5H, 7H)-dione (X).

• 公益社団法人日本薬学会の論文
• 1979-06-25

著者

• 古川 純康

  鹿児島大学工学部

• 古川 純康

  Medicinal Research Laboratories, Takeda Chemical Industries, Ltd.

• 仲 建彦

  創薬研究本部

• 仲 建彦

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

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• 解説 アンジオテンシン2受容体拮抗薬:カンデサルタン シレキセチルの創製
• カンデサルタン シレキセチル:新世代のアンジオテンシンII受容体拮抗薬の薬理特性と臓器保護作用
• 非ペプチド性アンジオテンシンII受容体拮抗薬の研究開発
• Fused Pyrimidines. V. Synthesis of 2-Aminopyrimido [4,5-e]-1,3,4-thiadiazine and Some Related Compounds from 6-Thiosemicarbazidouracils
• Fused Pyrimidines. IV. Synthesis of 3-Alkyl (or Acyl)-aminopyrazolo [3,4-d] pyrimidine Derivatives from 6-Hydrazinouracils and Isothiocyanates

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