Studies on the Stability of Δ^2 and Δ^3 Cephem Esters. I. Marked Difference in Stability between Δ^2 and Δ^3 Cephem Prodrug Esters and Application to the Preparation of Key Intermediates for Oral Cephem Synthesis

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概要

• 論文の詳細を見る

• The esterification of Δ^3-cephem-4-carboxylic acid sodium salt (1) with 1-iodoethyl isopropyl carbonate always afforded the Δ^2 cephem ester (3) as an inseparable minor component. However, in the course of formamido cleavage reaction, the 7-amino-Δ^2-cephem ester (5) was observed to be less stable than the Δ^3 cephem ester (4), which led us to develop a practical synthetic process for Δ^3 cephem esters, including a key intermediate of E1101,a new oral cephalosporin.

• 公益社団法人日本薬学会の論文
• 1995-11-15

著者

• 南 法夫

  Eisai Tsukuba Research Laboratories

• Negi S

  Eisai Co. Ltd. Kashima Plant Process Chemistry Research Laboratories

• 山中 基資

  Eisai Tsukuba Research Laboratories

• Komatsu Y

  National Institute Of Advanced Industrial Science And Technology

• 小松 雄毅

  Eisai Tsukuba Research Laboratories

• Tsukada Itaru

  Tsukuba Research Laboratories Eisai Co. Ltd.

• 塚田 格

  Eisai Co. Ltd. Tsukuba Research Laboratories

• 根木 茂人

  Eisai Co., Ltd., Tsukuba Research Laboratories

• 鶴岡 明彦

  Eisai Co., Ltd., Tsukuba Research Laboratories

• 根木 茂人

  Eisai Co. Ltd. Kashima Plant Process Chemistry Research Laboratories

• 山中 基資

  Eisai Co. Ltd. Tsukuba Research Laboratories

• 鶴岡 明彦

  Tsukuba Research Laboratories Eisai Co. Ltd.

• Minami N

  Research Division Teikoku Hormone Manufacturing Co. Ltd.

• 根木 茂人

  Eisai Co. Ltd. Tsukuba Research Laboratories

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