申请人:Uclaf; Roussel
公开号:US04396618A1
公开(公告)日:1983-08-02
Novel alkyloximes of 7-amino-thiazolyl-acetamide-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --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, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 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 R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.sub.2 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.
7-氨基噻唑基乙酰胺头孢菌素酸的新型烷氧基肟化合物,化学式如下:其中R选自由1到5个碳原子的烷基、3到5个碳原子的环烷基和--CH.sub.2 --SR',R'选自由2到4个碳原子的脂肪酸酰基、1-甲基四唑基和2-甲基-1,3,4-噻二唑基,R.sub.1选自氢和易于通过酸水解或氢解去除的基团,R.sub.2选自由1到4个碳原子的烷基和2到4个碳原子的烯基和炔基,A选自氢、碱金属阳离子、碱土金属或镁的等价物、有机胺碱基阳离子和易于通过酸水解或氢解去除的酯基团,但当R.sub.1为氢时,A不是易于通过氢解或酸水解去除的酯基团。其中波浪线表示OR.sub.2在两种可能的同构或反异构位置之一。该化合物具有很好的抗生素活性,并且提供了其制备的新方法和中间体。