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    Process for cephalosporanic acid derivatives and intermediate therefor
    3.
    发明授权
    Process for cephalosporanic acid derivatives and intermediate therefor 失效
    头孢烷酸衍生物及其中间体的方法

    公开(公告)号：US4503221A

    公开(公告)日：1985-03-05

    申请号：US505807

    申请日：1983-06-20

    申请人： Hans Fliri ,  Helmut Hamberger

    发明人： Hans Fliri ,  Helmut Hamberger

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D231/12 ,  C07D501/36 ,  C07D417/12 ,  C07D501/04

    CPC分类号： C07D231/12 ,  Y02P20/55

    摘要： The process for preparing cephalosporanic acid derivatives ##STR1## and salts thereof with bases as well as solvates thereof, comprising reacting a compound of the formula II: ##STR2## wherein R.sub.3 represents hydrogen or an amino protecting group and R.sub.2 represents hydrogen, an easily removable ester group or other carboxyl protecting group, with a compound of formula IIIa, ##STR3## wherein R.sub.1 represents hydrogen, an easily removable ester group or other carboxyl protecting group, and R.sub.4 is a 2-benzothiazol group and salts thereof with bases, and if required removing any ester group or protecting group.

    摘要翻译： 包括使式II的化合物：其中R 3表示氢或氨基保护基和R 2（R 3）的化合物，其中R 1，R 2， 代表氢，易除去的酯基或其它羧基保护基，与式IIIa的化合物，其中R 1表示氢，易脱除的酯基或其它羧基保护基，R 4是2-苯并噻唑 基团和其盐与碱反应，如果需要，除去任何酯基或保护基。

    Cephalosporin derivatives and use as antimicrobial agents
    4.
    发明授权
    Cephalosporin derivatives and use as antimicrobial agents 失效
    头孢菌素衍生物并用作抗微生物剂

    公开(公告)号：US4477448A

    公开(公告)日：1984-10-16

    申请号：US390323

    申请日：1982-06-21

    申请人： Helmut Hamberger ,  Hans Fliri

    发明人： Helmut Hamberger ,  Hans Fliri

    IPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40 ,  C07D501/20 ,  A61K31/545 ,  C07D501/56

    CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40

    摘要： Novel compounds of formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl, phenylalkyl, carbalkoxyalkyl, acyl, carboxyalkyl, alkoxyalkyl, hydroxyalkyl, cyanoalkyl, or carbamoylalkyl,R.sub.2 is hydrogen, pivaloyloxymethyl or the residue of an easily splittable ester grouping,R.sub.3 is a pyrazolyl radical, unsubstituted or mono- or di-substituted by alkyl, phenyl, alkoxy, alkylthio, carboxy, carboxyalkyl, carbamoyl, carbamoylalkyl, alkylsulphonyl, azido, acylamino, hydrazino, acylhydrazino alkylidenehydrazino, phenylidenehydrazino, in which the phenyl nucleus is unsubstituted or substituted by NH.sub.2, lower alkoxy or lower alkyl, furylidenehydrazino, carbalkoxy or a group R.sub.5 R.sub.6 N--, in which R.sub.5 and R.sub.6 are the same or different and are hydrogen or alkyl, provided that the nitrogen atoms and the 4-position of the pyrazole nucleus are either unsubstituted or substituted by alkyl, phenyl, or carbalkoxy, andR.sub.4 is hydrogen, acetoxy, carbamoyloxy or --S--Rh, in which Rh is a heterocyclic radical.

    摘要翻译： 新的式I化合物，其中R 1是氢，烷基，苯基烷基，烷氧基烷基，酰基，羧基烷基，烷氧基烷基，羟烷基，氰基烷基或氨基甲酰基烷基，R2是氢，新戊酰氧基甲基或易裂解酯基 苯基，苯基，烷氧基，烷硫基，羧基，羧基烷基，氨基甲酰基，氨基甲酰基烷基，烷基磺酰基，叠氮基，酰氨基，肼基，酰肼基亚烷基肼基，苯基亚肼基，其中苯基核是未取代的 或被NH 2，低级烷氧基或低级烷基，亚芳基亚肼基，烷氧基或R5R6N-基团取代，其中R5和R6相同或不同，为氢或烷基，条件是吡唑核的氮原子和4-位 未取代或被烷基，苯基或烷氧基取代，R4是氢，乙酰氧基，氨基甲酰氧基或-S-Rh，其中Rh是杂环基。