Hydrates of beta-lactam antibiotic
    73.
    发明公开
    Hydrates of beta-lactam antibiotic 失效
    水合物β-内酰胺 - 抗生素。

    公开(公告)号:EP0369686A1

    公开(公告)日:1990-05-23

    申请号:EP89311636.8

    申请日:1989-11-10

    IPC分类号: C07D463/00 A61K31/435

    CPC分类号: C07D463/22

    摘要: The crystalline dihydrate and trihydrate forms of the antibiotic 7β-[2′-(R)-2′-phenyl-2′-amino­acetamido]-3-chloro-3-(1-carbadethiacephem)-4-carboxylic acid ("LY163892") are described. These hydrates are antibiotics in their own right, and are valuable inter­mediates to the corresponding monohydrate form of LY163892.

    摘要翻译: 结晶二水合物和三水合物形式的抗生素7β-[2分钟 - (R)-2分钟 - 苯基-2分钟 - 氨基乙酰氨基] -3-氯-3-(1-碳二乙炔基缩水甘油基)-4-羧酸(“ LY163892“)。 这些水合物本身就是抗生素,是相应的LY163892一水合物形式的有价值的中间体。

    Process for 1-carba(dethia) cephalosporins
    74.
    发明公开
    Process for 1-carba(dethia) cephalosporins 失效
    头孢西泮(dehia)Verfahren zur Herstellung von 1-Carba(dethia)头孢菌素。

    公开(公告)号:EP0359540A2

    公开(公告)日:1990-03-21

    申请号:EP89309281.7

    申请日:1989-09-13

    摘要: The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-­dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyl­tin hydride or actinic radiation at 40°C to 150°C to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

    摘要翻译: 本发明提供了一种用2-取代的甲基头孢菌素1,1-二氧化物制备1-咔(1-脱硫)头孢菌素抗生素的自由基方法,其中2-亚甲基上的取代基是自由基前体基团,例如苯基或烷基硒 组。 后者的二氧化物用自由基引发剂例如氢化三烷基锡或光化辐射在40℃至150℃下处理,得到1-咔唑-3-头孢烯和1-咔二-2-头孢烯产物。 本发明还提供了在该方法中形成为中间体的自由基化合物。

    Fluorinated cephalosporin antibiotics and their use for the treatment of mastitis
    79.
    发明公开
    Fluorinated cephalosporin antibiotics and their use for the treatment of mastitis 审中-公开
    氟尿嘧啶头孢菌素 - 抗生素和维他命

    公开(公告)号:EP0953570A1

    公开(公告)日:1999-11-03

    申请号:EP99303336.4

    申请日:1999-04-28

    CPC分类号: C07D501/00 C07D463/20

    摘要: The invention provides new fluorinated cephalosporin antibiotics of Formula I
    wherein

    R a , R b , R c , R d and R e , independently, are H, F or C 1 -C 6 alkyl-(Z) n - group having at least one fluorine substituent;
    X is O or S;
    Y is S, O, or -CH 2 -;
    Z is O, S, -SO-, or -SO 2 -;
    m and n independently are 0 or 1; and
    R 1 is H, C 1 -C 6 -alkyl, phenyl or benzyl, each of which may optionally have up to three substituents selected from halo, C 1 -C 4 -alkoxy, phenyl, NO 2 , C 1 -C 6 -alkanoyl, benzoyl, or C 1 -C 6 -alkanoyloxy;
    or a physiologically acceptable salt thereof;
    provided that:

    1) at least one of R a , R b , R c , R d or R e is other than hydrogen; and
    2) when R e is F, or one of R b or R d is CF, at least one of the remaining R a , R b , R c , R d or R e is other than hydrogen,
    processes for preparing these compounds and veterinary and pharmaceutical formulations containing a Formula I compound as an active ingredient.

    摘要翻译: 本发明提供了式I的新的氟化头孢菌素抗生素,其中R a,R b,R c,R d和R e独立地是H,F或C 1 -C 6烷基 - (Z)n-基团,具有至少一个氟取代基; X为O或S; Y是S,O或-CH 2 - ; Z是O,S,-SO-或-SO 2 - ; m和n独立地为0或1; R 1是H,C 1 -C 6 - 烷基,苯基或苄基,它们各自可以任选地具有最多三个选自卤素,C 1 -C 4 - 烷氧基,苯基,NO 2,C 1 -C 6 - 烷酰基,苯甲酰基, 或C 1 -C 6 - 烷酰氧基; 或其生理上可接受的盐; 条件是:1)R a,R b,R c,R d或R e中的至少一个不是氢; 和2)当R e为F或R b或R d中的一个为CF时,其中R a,R b,R c,R d, >或R e不是氢,制备这些化合物的方法和含有式I化合物作为活性成分的兽医和药物制剂。