发明授权
US4439426A Semisynthetic macrolidic antibiotics, intermediate compounds for their
preparation and related pharmaceutical compositions containing them
失效
半合成大环内酯抗生素,其制备的中间体化合物和含有它们的相关药物组合物
- 专利标题: Semisynthetic macrolidic antibiotics, intermediate compounds for their preparation and related pharmaceutical compositions containing them
- 专利标题(中): 半合成大环内酯抗生素,其制备的中间体化合物和含有它们的相关药物组合物
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申请号: US338105申请日: 1982-01-08
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公开(公告)号: US4439426A公开(公告)日: 1984-03-27
- 发明人: Luciano Toscano , Leonardo M. Cappelletti
- 申请人: Luciano Toscano , Leonardo M. Cappelletti
- 申请人地址: ITX Napoli
- 专利权人: Pierrel S.p.A.
- 当前专利权人: Pierrel S.p.A.
- 当前专利权人地址: ITX Napoli
- 优先权: ITX19082A/81 19810109; ITX25344A/81 19811127; ITX25346A/81 19811127
- 主分类号: C07D313/00
- IPC分类号: C07D313/00 ; C07D493/08 ; C07D493/18 ; C07H17/08 ; C12P19/62 ; A61K31/71
摘要:
From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-O-mycarosyl-erythronolide B into the corresponding hermiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.
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