Synthesis of Imidazo[4,5-e][1,4]diazepine and Imidazo[4,5-e][1,4]-oxazepine Derivatives Using Caffeidine, a Hydrolysis Product of Caffeine

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概要

• 論文の詳細を見る

• Synthesis of imidazo[4,5-e][1,4]diazepines using caffeidine (1) was studied. Caffeidine was condensed with various α, β-unsaturated carboxylic acid derivatives to give N-(α, β-unsaturated acyl)caffeidines (4). Intramolecular Michael addition of 4 having an electron-withdrawing group at the β-position of the α, β-unsaturated acyl group afforded imidazo[4,5-e][1,4]diazepines (5,6). Compounds of the same type (14) were also prepared by treatment of N-(α-halogenoacyl)caffeidines (13) with EtONa in abs. EtOH. On the other hand, heating of 13 in H_2O gave imidazo[4,5-e][1,4]oxazepines (15). Compounds 5d, 15b, and 15c showed arterial relaxing activities.

• 公益社団法人日本薬学会の論文
• 1986-09-25

著者

• 植田 泰誠

  Faculty of Pharmaceutical Sciences, Nagoya City University

• 榊原 仁作

  名市大院薬

• 榊原 仁作

  Faculty Of Pharmaceutical Sciences Science University Of Tokyo

• 榊原 仁作

  Nagoya City Univ. Nagoya Jpn

• 浅野 正久

  Department of Pharmacology, Nagoya City University Medical School

• 栗木 武男

  ヘキストジャパン(株)

• 浅野 正久

  Department Of Pharmacology Nagoya City University Medical School

• 栗木 武男

  Research and Development Laboratories, Hoechst Japan Limited

• 大崎 勉

  Pharma Research And Development Division Hoechst Japan Limited

• 栗木 武男

  Research And Development Laboratories Hoechst Japan Limited

• 大崎 勉

  Research and Development Laboratories, Hoechst Japan Limited

• 植田 泰誠

  Faculty Of Pharmaceutical Sciences Nagoya City University

• 栗木 武男

  Pharma Research And Development Division Hoechst Japan Limited

• 榊原 仁作

  Faculty Of Pharmaceutical Sciences Nagoya City University

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