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    6-Substituted-2-carbamimidoyl-pen-2-em-3-carboxylic acids, process for preparing them and antibiotic compositions comprising them
    8.
    发明公开
    6-Substituted-2-carbamimidoyl-pen-2-em-3-carboxylic acids, process for preparing them and antibiotic compositions comprising them 失效
    6-取代的-2-甲脒基笔-2-青霉-2-烯-3-羧酸，其制备方法和组合物含有它们的抗生素的组合物。

    公开(公告)号：EP0087792A1

    公开(公告)日：1983-09-07

    申请号：EP83101923.7

    申请日：1983-02-28

    申请人： Merck & Co., Inc.

    发明人： Leanza, William J. ,  Christensen, Burton G. ,  Dininno, Frank P. ,  Ratcliffe, Ronald W.

    IPC分类号： C07D499/00 ,  A61K31/43

    CPC分类号： C07D499/88

    摘要： Disclosed are 6-substituted-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure:
    wherein R 6 , and R 7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkoxyl, halo, OH, COOH, alkenyl, aryl and aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryi, heteroaryl, heteroalkyl: R' and R 2 . which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of one of the nitrogen atoms of said carbamimidoyl.
    Such compounds are useful as antibiotics. Also disclosed are processes for the preparation of such compounds.

    摘要翻译： 公开的是具有代表性的结构6- substituiertem -2-甲脒基笔-2-青霉-2-烯-3-羧酸（I）： worin - [R <6>和R <7>除其他外，unabhängig选自 选自由氢，烷基，烷氧基，卤素，OH，COOH，烯基，芳基和芳烷基的; A是一个直接的，单键连接所指示的S和C原子，或A为选择的环状或非环状的连接基团，特别是选自烷基，环烷基，芳基，杂芳基，杂烷基; [R <1>和R <2>，它定义了脒功能，是除其他外，unabhängig选自氢，烷基，芳基; 此外，所述甲脒基是通过经由它们的取代基和由它们的连接到连接基团A上的两个氮原子的该接合取得的环状结构为特征的; 另外，“carbamimidiums”是盘由所述脒的氮原子中的一个的quarternization游离缺失。 搜索化合物可用作抗生素。 所以圆盘游离缺失是用于测试的化合物的制备方法。