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346 条记录 (耗时 0.009 秒)

    Intermediates for producing semi-synthetic penicillins
    128.
    发明授权
    Intermediates for producing semi-synthetic penicillins 失效
    生产半合成青霉素的中间体

    公开(公告)号：US3912750A

    公开(公告)日：1975-10-14

    申请号：US44159374

    申请日：1974-02-11

    申请人： AMERICAN HOME PROD

    发明人： SELLSTEDT JOHN H

    IPC分类号： C07D499/12 ,  C07D501/06 ,  C07F9/6561 ,  C07D99/16 ,  C07D99/24

    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。

    Cephalosporins
    129.
    发明授权
    Cephalosporins 失效
    CEPHALOSPORINS

    公开(公告)号：US3904616A

    公开(公告)日：1975-09-09

    申请号：US27301972

    申请日：1972-07-18

    申请人： TAKEDA CHEMICAL INDUSTRIES LTD

    发明人： SUGIMOTO KEIICHI ,  KOBAYASHI KUNIO ,  NISHIJIMA KOJI ,  MORIMOTO SHIRO

    IPC分类号： C07D235/26 ,  C07D501/36 ,  C07D99/24

    CPC分类号： C07D235/26

    摘要： Novel cephalosporins of the formula

    WHEREIN R1 and R2 are, the same or different, hydrogen atom or an acyl group of the formula;

    WHEREIN R represents phenyl, phenylthio, thienyl, 2-oxoprimidin-4-ylthio, 2-chloro-pyrimidin-4-ylthio, pyridylthio or 2oxo-5-methyl-pyrimidin-4-ylthio and X represents hydrogen, carboxyl, carbamoyl, carbamolyoxy, amino, or sulfo and pharmaceutically acceptable salts thereof are stable against an acid and have a broad antimicrobial spectrum.

    {8 (Azidomethyl)thio{9 acetylcephalosporins
    130.
    发明授权
    {8 (Azidomethyl)thio{9 acetylcephalosporins 失效
    {8（叠氮甲基）硫代{9乙酰头孢菌素

    公开(公告)号：US3897422A

    公开(公告)日：1975-07-29

    申请号：US33780473

    申请日：1973-03-05

    申请人： SQUIBB & SONS INC

    发明人： BREUER HERMANN ,  TREUNER UWE D

    IPC分类号： C07D333/24 ,  C07D261/08 ,  C07D277/20 ,  C07D277/30 ,  C07D307/54 ,  C07D501/20 ,  C07D99/24

    CPC分类号： C07D501/20

    摘要： New ((azidomethyl)thio)acetylcephalosporins of the following general formula, and their salts,

    WHEREIN R is hydrogen, lower alkyl, aralkyl, tri(lower alkyl)silyl, a salt forming ion or the group

    R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl or a heterocyclic group; R3 is lower alkyl, aryl or aralkyl; and X is hydrogen, hydroxy, lower alkanoyloxy, lower alkoxy, lower alkylthio, lower alkylthiazolylthio, azido, the radical of a nitrogen base, or together X and R represent a bond linking carbon and oxygen in a lactone ring; are useful as antibacterial agents.

    摘要翻译： 新的具有下列通式的[（叠氮基甲基）硫代]乙酰头孢菌素及其盐，其中R是氢，低级烷基，芳烷基，三（低级烷基） - 甲硅烷基，成盐离子或基团R 1是氢或低级烷基; R2是氢，低级烷基，芳基或杂环基; R3是低级烷基，芳基或芳烷基; 和X是氢，羟基，低级烷酰氧基，低级烷氧基，低级烷硫基，低级烷基噻唑硫基，叠氮基，氮碱基，或一起X和R表示内酯环中碳和氧的连接键; 作为抗菌剂是有用的。