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    4-Substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives
    3.
    发明授权
    4-Substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives 失效
    4-取代的氨基 - {6-氨基甲基苄醇衍生物

    公开(公告)号：US4063025A

    公开(公告)日：1977-12-13

    申请号：US651738

    申请日：1976-01-23

    申请人： Masuo Murakami ,  Kozo Takahashi ,  Kiyoshi Murase ,  Toshiyasu Mase ,  Hisashi Ida ,  Toichi Takenaka

    发明人： Masuo Murakami ,  Kozo Takahashi ,  Kiyoshi Murase ,  Toshiyasu Mase ,  Hisashi Ida ,  Toichi Takenaka

    IPC分类号： C07C275/40 ,  C07C125/06

    CPC分类号： C07C275/40 ,  Y10S514/826

    摘要： There are disclosed novel 4-substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives represented by the formula: ##STR1## wherein X represents a halogen atom; Y represents a hydrogen atom or a halogen atom; R.sub.1 represents a lower alkyl group, a carbamoyl group, a mono- or di-lower alkyl-substituted carbamoyl group, a phenyl-substituted carbamoyl group, a lower alkoxycarbonyl group, a lower alkoxy-substituted lower alkoxycarbonyl group, a phenyl-substituted lower alkoxycarbonyl group, or a cycloalkyloxycarbonyl group; and R.sub.2 represents a lower alkyl group, a cycloalkyl group, or the group shown by the formula ##STR2## wherein R.sub.3 represents a hydrogen atom or a lower alkyl group and R.sub.4 represents a hydrogen atom, a hydroxy group, or a lower alkoxy group and the pharmaceutically acceptable nontoxic salts thereof.These compounds are antiasthmatic agents useful for the prophylaxis and treatment of asthma.

    摘要翻译： 公开了由下式表示的新型4-取代氨基-α-氨基甲基苄醇衍生物：其中X表示卤素原子; Y表示氢原子或卤素原子; R 1表示低级烷基，氨基甲酰基，一或二低级烷基取代的氨基甲酰基，苯基取代的氨基甲酰基，低级烷氧基羰基，低级烷氧基取代的低级烷氧基羰基，苯基取代的低级 烷氧基羰基或环烷氧基羰基; 和R 2表示低级烷基，环烷基或下式所示的基团，其中R 3表示氢原子或低级烷基，R 4表示氢原子，羟基或低级烷氧基， 其药学上可接受的无毒盐。

    Process for the preparation of the cephalosporanic acid derivative
    4.
    发明授权
    Process for the preparation of the cephalosporanic acid derivative 失效
    制备头孢菌酸衍生物的方法

    公开(公告)号：US3935198A

    公开(公告)日：1976-01-27

    申请号：US426108

    申请日：1973-12-19

    申请人： Masuo Murakami ,  Kozo Takahashi ,  Ichiro Isaka ,  Teruaki Ozasa ,  Teruya Kashiwagi

    发明人： Masuo Murakami ,  Kozo Takahashi ,  Ichiro Isaka ,  Teruaki Ozasa ,  Teruya Kashiwagi

    IPC分类号： C07D20060101 ,  C07D499/04 ,  C07D501/10

    CPC分类号： C07D501/10

    摘要： A process for the preparation of cephalosporanic acid derivatives represented by the formula ##SPC1##Wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a univalent group other than a hydrogen atom, said R.sub.1 and R.sub.2 may be combined to form a divalent group and A represents a divalent group represented by the formulae ##SPC2##Wherein R.sub.3 represents a hydrogen atom or a group which does not contribute to the reaction, which comprises heating a penicillin sulfoxide derivative represented by the formula ##SPC3##Wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.The cephalosporanic acid derivatives prepared by the process of this invention are useful as a starting material for the preparation of antibacterials.

    摘要翻译： 制备由式WHEREIN R1和R2表示的头孢烷酸衍生物的方法可以相同或不同，分别表示氢原子以外的一价基团，所述R 1和R 2可以组合形成二价基团， A表示由下式表示的二价基团，其中R 3表示氢原子或对反应无贡献的基团，其包括加热由式WHEREIN R1表示的青霉素亚砜衍生物，R2和R3如上所定义。

    Process of preparing cephalosporanic acid ester derivatives
    6.
    发明授权
    Process of preparing cephalosporanic acid ester derivatives 失效
    制备头孢菌酸酯衍生物的方法

    公开(公告)号：US4137407A

    公开(公告)日：1979-01-30

    申请号：US775841

    申请日：1977-03-09

    申请人： Masuo Murakami ,  Kozo Takahashi ,  Teruaki Ozasa

    发明人： Masuo Murakami ,  Kozo Takahashi ,  Teruaki Ozasa

    IPC分类号： C07D501/04

    CPC分类号： C07D501/22 ,  C07D501/04

    摘要： A process of preparing a .DELTA..sup.3 -cephalosporanic acid ester derivative which comprises reacting a cephalosporanic acid sulfoxide ester derivative with thionyl halide or a phosphorous halide.The compounds prepared by the process of this invention are useful as intermediate compounds for preparing cephalosporin antibiotics and the compounds themselves are also potential antibacterials.

    摘要翻译： 一种制备DELTA 3-头孢菌酸酯衍生物的方法，其包括使头孢菌酸亚砜酯衍生物与亚硫酰卤或卤化磷反应。