Chemical Modification of Antitumor Alkaloids, 20(S)-Camptothecin and 7-Ethylcamptothecin : Reaction of the E-Lactone Ring Portion with Hydrazine Hydrate

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概要

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• The structure of the N-amino pyridone (4a) obtained by the reaction of camptothecin (1a) with hydrazine was determined by X-ray crystallography. A mixture of 7-etylcamptothecin (1b) and hydrazine hydrate was stirred at room temperature, and the hydrazide (2b) was isolated as its diacetate 2c. Treatment of the 17-O-acetyl amide (5a) with hydrazine gave 1b (74% yield) and the N-amino lactam 6 (11% yield). Compounds with bulky acyl groups, 5c-e, gave 6 in modest yields. The N-amino lactam 6 was smoothly dehydrated into the pyridone 4d by refluxing in hydrazine hydrate.

• 社団法人日本薬学会の論文
• 1993-05-15

著者

• 宮坂 貞

  School of Pharmaceutical Sciences, Showa University

• 八重樫 隆

  Yakult Central Institute of Microbiological Research

• 澤田 誠吾

  Yakult Central Institute of Microbiological Research

• 山口 健太郎

  School of Pharmaceutical Sciences, Showa University

• 澤田 誠吾

  ヤクルト本社中央研究所

• 山口 健太郎

  School Of Pharmaceutical Sciences Showa University

• 横倉 輝男

  ヤクルト中央研究所

• 横倉 輝男

  Yakult Central Institute for Microbiological Research

• 沢田 誠吾

  Yakult Central Institute for Microbiological Research

• 古田 富雄

  Yakult Central Institute for Microbiological Research

• 横倉 輝雄

  Yakult Institute for Microbiological Research

• Sawada S

  Yakult Central Institute Of Microbiological Research

• 宮坂 貞

  School Of Pharmaceutical Sciences Showa University

• 横倉 輝男

  ヤクルト本社 中研

• 横倉 輝男

  Yakult Central Institute

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