发明公开
EP0185323A2 2',3'-Dideoxy-2'-fluorokanamycin A and 1-N-(alpha-hydroxy-omega-aminoalkanoyl) derivatives thereof
失效
2',3'-二脱氧-2'-氟卡那霉素-A和Seine 1-N-(α-羟基-ω-氨基烷酰基)-Derivate。
- 专利标题: 2',3'-Dideoxy-2'-fluorokanamycin A and 1-N-(alpha-hydroxy-omega-aminoalkanoyl) derivatives thereof
- 专利标题(中): 2',3'-二脱氧-2'-氟卡那霉素-A和Seine 1-N-(α-羟基-ω-氨基烷酰基)-Derivate。
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申请号: EP85115901.2申请日: 1985-12-13
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公开(公告)号: EP0185323A2公开(公告)日: 1986-06-25
- 发明人: Umezawa, Hamao , Umezawa, Sumio , Tsuchiya, Tsutomu , Takahashi, Yoshiaki
- 申请人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 申请人地址: 14-23, Kami Osaki 3-chome Shinagawa-ku, Tokyo 141 JP
- 专利权人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人: ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
- 当前专利权人地址: 14-23, Kami Osaki 3-chome Shinagawa-ku, Tokyo 141 JP
- 代理机构: Goddar, Heinz J., Dr.
- 优先权: JP263759/84 19841215; JP231027/85 19851018
- 主分类号: C07H15/236
- IPC分类号: C07H15/236 ; C07H15/234 ; A61K31/70
摘要:
New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(a-hydroxy-w-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryt)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as anti-bacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-0-protected-2,3-6-trideoxy-2-fluoro-a-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2',4',6'-tri-0- protected-3'-N-protected-3'-amino-3'-deoxy-α-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.
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