Studies on the Stability of Δ^2 and Δ^3 Cephem Esters. II.Comparative Stability Studies of Δ^2 and Δ^3 Cephems at Various pHs and the Degradation Process of Δ^2 Caphem Esters
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概要
- 論文の詳細を見る
The instability of Δ^2 cephem prodrug-type ester (5a) under acidic conditions prompted us to investigate the comparative stability of Δ^3 and Δ^2 cephems at various pHs. The Δ^2 cephem ester 5a was found to show marked instability under neutral (pH 7) and acidic conditions (1M HCl) compared with the Δ^3 cephem ester (4a). A comparative study between Δ^3 (4c) and Δ^2 cephem acid (5c) at pH 7 and in 1M HCl solution showed that the Δ^2 acid 5c was as stable as the Δ^3 acid 4c pH 7,while 5c was less stable than 4c in 1M HCl. Isolation of the degraded compounds demonstrated that the C-4 ester moiety was hydrolyzed in the initial stage to afford 5c, which was further degraded to more polar substances. This instability was observed in other types of Δ^2 cephem esters (5d-f). Here we report comparative stability studies and elucidation of the degradation products.
- 公益社団法人日本薬学会の論文
- 1995-11-15
著者
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南 法夫
Eisai Tsukuba Research Laboratories
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Negi S
Eisai Co. Ltd. Kashima Plant Process Chemistry Research Laboratories
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山中 基資
Eisai Tsukuba Research Laboratories
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Komatsu Y
National Institute Of Advanced Industrial Science And Technology
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小松 雄毅
Eisai Tsukuba Research Laboratories
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Tsukada Itaru
Tsukuba Research Laboratories Eisai Co. Ltd.
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塚田 格
Eisai Co. Ltd. Tsukuba Research Laboratories
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根木 茂人
Eisai Co., Ltd., Tsukuba Research Laboratories
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鶴岡 明彦
Eisai Co., Ltd., Tsukuba Research Laboratories
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根木 茂人
Eisai Co. Ltd. Kashima Plant Process Chemistry Research Laboratories
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山中 基資
Eisai Co. Ltd. Tsukuba Research Laboratories
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鶴岡 明彦
Tsukuba Research Laboratories Eisai Co. Ltd.
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Minami N
Research Division Teikoku Hormone Manufacturing Co. Ltd.
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根木 茂人
Eisai Co. Ltd. Tsukuba Research Laboratories
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