Crystalline forms of cephaloridine
    65.
    发明授权
    Crystalline forms of cephaloridine 失效
    结晶形式的头孢哌啶

    公开(公告)号:US3887551A

    公开(公告)日:1975-06-03

    申请号:US22053772

    申请日:1972-01-24

    申请人: GLAXO LAB LTD

    IPC分类号: C07D501/46 C07D99/24

    CPC分类号: C07D501/46

    摘要: The invention is concerned with two novel crystalline forms of the antibiotic cephaloridine which are relatively non-hygroscopic compared with previously known forms of cephaloridine and hence possess important advantages in handling and formulation. The novel crystalline forms are characterised in particular by X-ray crystallographic data set out in detail in the following disclosure.

    摘要翻译: 本发明涉及两种新型的抗生素头孢哌啶的结晶形式,与先前已知的头孢噻吩形式相比,它们相对不吸湿,因此在处理和制剂方面具有重要的优点。 新颖的结晶形式特别表现在以下公开内容中详细列出的X射线晶体学数据。

    3-(Alpha-trifluoromethylarylacetamido)-1,4-cyclo(1,-carboxyl)alkylenethio)-azetidin-2-one derivatives
    67.
    发明授权
    3-(Alpha-trifluoromethylarylacetamido)-1,4-cyclo(1,-carboxyl)alkylenethio)-azetidin-2-one derivatives 失效
    3-(α-三氟甲基芳基乙酰氨基)-1,4-环(1'-羧基)亚烷基硫代) - 氮杂环丁-2-酮衍生物

    公开(公告)号:US3879385A

    公开(公告)日:1975-04-22

    申请号:US36085773

    申请日:1973-05-16

    CPC分类号: C07D499/00

    摘要: 3-( Alpha -Trifluoromethylarylacetamido)-1,4-(cyclo-(1''carboxy)alkylenethio)azetidin-2-one derivatives possessing antibacterial activity are produced by the reaction of 3,3,3trifluoro-2-phenylpropanoic acid or 3,3,3-trifluoro-2-phydroxyphenylpropanoic acid and a 3-amino-1,4-(cyclo(1''carboxy)alkylenethio)-azetidin-2-one derivative in the presence of a condensing agent or by conversion of the propanoic acid derivative to an acid halide.

    摘要翻译: 通过3,3,3-三氟-2-苯基丙酸的反应产生具有抗菌活性的3-(α-三氟甲基芳基乙酰氨基)-1,4- [环 - (1'-羧基)亚烷基硫代] 酸或3,3,3-三氟-2-对羟基苯基丙酸和3-氨基-1,4- [环(1'-羧基)亚烷基硫代] - 氮杂环丁-2-酮衍生物在缩合剂存在下 或通过将丙酸衍生物转化为酰卤。

    Intermediates for producing semi-synthetic cephalosporins and methods of production
    69.
    发明授权
    Intermediates for producing semi-synthetic cephalosporins and methods of production 失效
    生产半合成CEPHOROSPORINS的中间体和生产方法

    公开(公告)号:US3875152A

    公开(公告)日:1975-04-01

    申请号:US37830873

    申请日:1973-07-11

    发明人: SELLSTEDT JOHN H

    CPC分类号: C07F9/65611 Y02P20/55

    摘要: Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a salt thereof with a phosphorus halide in the presence of an acid acceptor and subsequently acylating the thus formed phosphorylated compound, to form a phosphorylated acylated derivative which upon hydrolysis with water splits off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalosporin having useful antibacterial activity.

    摘要翻译: 描述了新的6-APA,7-ACA和7-ADCA衍生物,其包含6-APA,7-ACA或7-ADCA的磷酸化衍生物及其相应的酰化衍生物。 该新化合物通过在酸受体存在下通过6-APA,7-ACA,7-ADCA或其盐与卤化磷的反应制备,随后酰化由此形成的磷酸化化合物,形成磷酸化酰化衍生物 其在用水分解保护基团时提供相应的具有有效抗菌活性的半合成青霉素或头孢菌素。