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    Processes for the preparation of carbapenem-type antibacterial agents
    1.
    发明授权
    Processes for the preparation of carbapenem-type antibacterial agents 失效
    制备碳青霉烯类抗菌剂的方法

    公开(公告)号：US07034150B2

    公开(公告)日：2006-04-25

    申请号：US10438649

    申请日：2003-05-14

    申请人： Katsuhiko Fujimoto ,  Takashi Kasai

    发明人： Katsuhiko Fujimoto ,  Takashi Kasai

    IPC分类号： C07D477/20 ,  C07D495/08

    CPC分类号： C07D477/20 ,  C07D477/04 ,  C07D477/06 ,  C07D495/08

    摘要： A process for the preparation of a carbapenem antibacterial compound of the following formula (4) having a 1-alkylpyrrolidine structure or a salt thereof, a useful synthetic intermediate of the following formula (1) or a salt thereof, and a process for the preparation thereof: wherein R1 represents a C1–C3 alkyl group, R2 and R3 each independently represents a hydrogen atom or an organic residue or R2 and R3 together with the nitrogen atom they are attached to form a ring.

    摘要翻译： 一种制备具有1-烷基吡咯烷结构的下式（4）的碳青霉烯类抗菌化合物或其盐，下式（1）的有用的合成中间体或其盐的方法及其制备方法 其中R 1表示C 1 -C 3烷基，R 2和R 2各自独立地选自氢， 3个独立地表示氢原子或有机残基或R 2和R 3以及它们所连接的氮原子一起形成环。

    Process for carbapenem intermediates
    4.
    发明授权
    Process for carbapenem intermediates 失效
    碳青霉烯中间体的方法

    公开(公告)号：US4960879A

    公开(公告)日：1990-10-02

    申请号：US318717

    申请日：1989-03-03

    申请人： Shoichiro Uyeo

    发明人： Shoichiro Uyeo

    IPC分类号： C07D205/08 ,  C07D477/04 ,  C07F7/18

    CPC分类号： C07D477/04 ,  C07D205/08 ,  C07F7/186 ,  Y02P20/55

    摘要： A novel intermediate for synthesizing 1 .beta.-alkyl-1-carbapenem, i.e., 4 .beta.-(1 .beta.-alkyl-2-carboxyprop-2-enyl)azetidin-2-one (II), is prepared stereoselectively by treating 4-(leaving group substituted)azetidin-2-one (I) with trans-2-(leaving group substituted)-methyl-3-alkylacrylic acid (III) and a reducing metal. ##STR1## wherein R.sup.1 is hydrogen, alkyl, or substituted alkyl;R.sup.2 is optionally substituted alkyl;R.sup.3 is hydrogen or a carboxy-protecting group; andR.sup.4 and R.sup.5 each is a leaving group.

    Synthesis of carbapenems using n-substituted azetidinones
    7.
    发明授权
    Synthesis of carbapenems using n-substituted azetidinones 失效
    用n-取代的氮杂环丁酮合成碳青霉烯

    公开(公告)号：US4769451A

    公开(公告)日：1988-09-06

    申请号：US765767

    申请日：1985-08-15

    申请人： Pierre Dextraze

    发明人： Pierre Dextraze

    IPC分类号： C07D205/09 ,  C07D477/04 ,  C07F7/18 ,  C07D487/04

    CPC分类号： C07D477/04 ,  C07D205/09 ,  C07F7/186

    摘要： A novel process is disclosed for converting known 3,4-disubstituted azetidinones to carbapenems. The process proceeds through novel N-substituted intermediates and then cyclizes to the 4-position of the azetidinone to form the carbapenem.

    摘要翻译： 公开了一种将已知的3,4-二取代的氮杂环丁酮转化为碳青霉烯的新方法。 该方法通过新的N-取代的中间体进行，然后环化至氮杂环丁酮的4-位以形成碳青霉烯。

    Chiral synthesis of thienamycin from D-glucose
    10.
    发明授权
    Chiral synthesis of thienamycin from D-glucose 失效
    从D-葡萄糖手性合成噻吩霉素

    公开(公告)号：US4544502A

    公开(公告)日：1985-10-01

    申请号：US573742

    申请日：1984-01-25

    申请人： Philippe L. Durette

    发明人： Philippe L. Durette

    IPC分类号： C07D205/08 ,  C07D477/04 ,  C07H9/00 ,  C07H19/04 ,  C07C117/00 ,  C07C121/86

    CPC分类号： C07H19/04 ,  C07D205/08 ,  C07D477/04 ,  C07H9/00 ,  Y02P20/55

    摘要： Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.

    摘要翻译： 公开了从D-葡萄糖的手性全合成，其通过中间体I，II和III进行已知的醛IV，其已知可用于噻吗化合物（V）的全合成： 其中：R是具有1-6个碳原子的低级烷基或连接两个硫原子的具有2-6个碳原子的二价烷基; R1是低级烷基或芳烷基，例如苄基等; 并且R 2是氢或可除去的保护基团，例如三有机甲硅烷基，其中有机基团独立地选自低级烷基，苯基和苯基低级烷基。