Preparation of 5-Aminothiazole-4-carboxylic Acid Derivatives

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概要

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• Cyclization of 2-acylamino-2-thiocarbamoylacetamides (Va, b) with acetic formic anhydride gave good yields of 5-formamidothiazole-4-carboxamides (VIa, b) which were converted to 5-aminothiazole-4-carboxamides (VIIa, b) by hydrolysis. For the purpose of the preparation of the free base (VIIa), however, cyclization of Va with polyphosphoric acid was proved to give better result, that is, heating of Va-c and ethyl 2-acylamino-2-thiocarbamoylacetates (Vd-f) in polyphosphoric acid gave VIIa-c and ethyl 5-aminothiazole-4-carboxylates (VIId-f) in excellent yields. 5-Aminothiazole-4-carbonitriles (VIIg, h) were prepared by treatment of Va, b with phosphorus oxychloride.

• 公益社団法人日本薬学会の論文
• 1971-01-25

著者

• 田村 恭光

  Faculty Of Pharmaceutical Sciences Osaka University

• 下岡 釿雄

  New Product Development Center, Pfizer Pharmaceutical Inc., Ltd.,

• 下岡 釿雄

  New Product Development Center Pfizer Pharmaceutical Inc. Ltd.

• 宮本 知久

  Faculty of Pharmaceutical Sciences, Osaka University

• 下岡 釿雄

  Faculty of Pharmaceutical Sciences, Osaka University

• 増井 武彦

  Faculty of Pharmaceutical Sciences, Osaka University

• 増井 武彦

  大阪大学薬学部

• 宮本 知久

  Faculty Of Pharmaceutical Sciences Osaka University

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