首页> 外国专利> ALKYLOXIM DERIVATIVE OF NOVEL 77AMINOTHIAZOLYLACETAMIDE CEPHALOSPOLANATE PROCESS FOR PREPARING SAME AND MEDICAL COMPOSITION

ALKYLOXIM DERIVATIVE OF NOVEL 77AMINOTHIAZOLYLACETAMIDE CEPHALOSPOLANATE PROCESS FOR PREPARING SAME AND MEDICAL COMPOSITION

机译:新颖的77氨基噻唑基乙酰胺头孢菌酸酯的烷氧基肟酸酯衍生物的制备及其药物组合物

摘要

Novel alkyloximes of 7-amino-thiazolyl-acetamide-cephalosporanic acids of the formula IMAGE I wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and -CH2-SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, an organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR2 is in one or the other of the two possible syn or anti isomeric positions having a very good antibiotic activity and novel processes and intermediates for their preparation.
机译: I的7-氨基-噻唑基-乙酰胺-头孢烷酸的新型烷基肟,其中R选自1至5个碳原子的烷基,3至5个碳原子的环烷基和-CH 2 -SR' R 1选自由2-4个碳原子的链烷酸的酰基,1-甲基-四唑基和2-甲基-1,3,4-噻二唑基组成的组,R 1选自由氢和R 2是易于通过酸水解或氢解除去的基团,R 2选自由1至4个碳原子的烷基和2至4个碳原子的烯基和炔基组成的组,A选自由氢,碱金属阳离子组成的组,相当于碱土金属或镁,有机胺碱阳离子和可通过酸水解或氢解除去的酯基,当R 1为氢时,A不是可通过氢解或酸水解除去的酯基;波浪线表示t所述OR2处于两个可能的顺式或反式异构体位置中的一个或另一个中,具有非常好的抗生素活性以及用于制备它们的新方法和中间体。

著录项

  • 公开/公告号JPS6229436B2

    专利类型

  • 公开/公告日1987-06-25

    原文格式PDF

  • 申请/专利权人 ROUSSEL UCLAF;

    申请/专利号JP19770032329

  • 发明设计人 RUNE EEMU;ANDORE RYUTSU;

    申请日1977-03-25

  • 分类号C07D501/06;A61K31/545;A61K31/546;A61P31/04;C07D277/20;C07D277/38;C07D501/04;C07D501/20;C07D501/22;C07D501/36;

  • 国家 JP

  • 入库时间 2022-08-22 07:23:58

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