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    3-Methylene cephalosporanic acid derivatives and process for preparation thereof
    1.
    发明授权
    3-Methylene cephalosporanic acid derivatives and process for preparation thereof 失效
    3-亚甲基头孢菌酸衍生物及其制备方法

    公开(公告)号：US4138553A

    公开(公告)日：1979-02-06

    申请号：US841321

    申请日：1977-10-11

    申请人： Sachio Ishimoto ,  Hisao Yamaguchi ,  Yoshinori Kato ,  Takeo Oba ,  Kenji Ozawa ,  Yataro Ichikawa ,  Koji Nakagawa ,  Hideki Tsuruta

    发明人： Sachio Ishimoto ,  Hisao Yamaguchi ,  Yoshinori Kato ,  Takeo Oba ,  Kenji Ozawa ,  Yataro Ichikawa ,  Koji Nakagawa ,  Hideki Tsuruta

    IPC分类号： C07D499/00 ,  C07D501/10 ,  C07D501/02

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： Novel substituted hydrazide derivatives of 7-(substituted)amino-3-methylene-cepham-4-carboxylic acids expressed by the formula ##STR1## wherein R.sub.1 represents alkyl containing at least 3 carbon atoms, cycloalkyl, or optionally substituted aryl, and one of R.sub.2 and R.sub.3 represents hydrogen with the other being hydrogen or the same as R.sub.1 ; or R.sub.1 and R.sub.2 form a heterocyclic ring optionally through a hetero atom together with the attached nitrogen and R.sub.3 represents hydrogen atom; and Z.sub.1 represents amino or protected amino; and acid addition salts thereof, which are useful as intermediates for synthesizing cephalosporin antibiotics. These compounds can be prepared in high yields from the corresponding substituted hydrazide derivatives of 6-substituted amino-1-oxide-2, 2-dimethyl-penam-3-carboxylic acids, which are readily available at low costs, by heating them in the presence of a thermal rearrangement promotor such as organic sulfonic acids and optionally in the further presence of a tertiary nitrogen-containing cyclic compound, followed if desired by splitting off the amino-protecting group and converting the product to acid addition salts.

    摘要翻译： 由式“IMAGE”表示的7-（取代的）氨基-3-亚甲基 - 头孢烯-4-羧酸的新型取代的酰肼衍生物，其中R 1表示含有至少3个碳原子的烷基，环烷基或任选取代的芳基， R2和R3代表氢，另一个是氢或与R1相同; 或R 1和R 2与所连接的氮一起任选地通过杂原子形成杂环，并且R 3表示氢原子; Z1表示氨基或被保护的氨基; 其酸加成盐，其可用作合成头孢菌素抗生素的中间体。 这些化合物可以以相当于6-取代的氨基-1-氧化物-2,2-二甲基 - 对甲苯磺酸的取代的酰肼衍生物的高收率制备，它们以低成本容易获得，通过在 存在热重排促进剂如有机磺酸，并且任选地在另外存在叔氮气环状化合物的情况下，如果需要的话，分解氨基保护基并将产物转化成酸加成盐。

    Process for preparing amino alcohols
    9.
    发明授权
    Process for preparing amino alcohols 失效
    制备氨基醇的方法

    公开(公告)号：US4151204A

    公开(公告)日：1979-04-24

    申请号：US771674

    申请日：1977-02-24

    申请人： Yataro Ichikawa ,  Eishin Yoshisato ,  Koji Nakagawa

    发明人： Yataro Ichikawa ,  Eishin Yoshisato ,  Koji Nakagawa

    IPC分类号： C07C215/08 ,  C07C89/00 ,  B01J23/40 ,  C07C85/06

    CPC分类号： C07C215/08

    摘要： A process for preparing amino alcohols, which comprises reacting a polyhydric alcohol containing at least one primary alcoholic hydroxyl group and at least one secondary alcoholic hydroxyl group and expressed by the following general formula ##STR1## wherein R.sup.1 is an alkyl group, R.sup.2 and R.sup.3 are identical or different and represent a hydrogen atom or a lower alkyl group an n is an integer of 0 to 3,With ammonia in the presence of specified hydrogenation catalyst thereby to aminate the secondary alcoholic hydroxyl group of the polyhydric alcohol selectively.

    摘要翻译： 一种制备氨基醇的方法，其包括使含有至少一个伯醇羟基的多元醇与至少一种仲醇羟基反应，并由以下通式表示：其中R 1为烷基，R 2和R 3为 相同或不同，代表氢原子或低级烷基，n为0至3的整数，在规定的氢化催化剂存在下氨基酸可选择性地选择多官能醇的二级醇基羟基。