7β-杂环酰胺基头孢菌素新衍生物的半合成及抗菌活性研究  

Studies on Semisynthesis and Antimicrobial Activity of 7 β Heterocyclicamido Cephalosporins

作　　者：张自义[1] 粱宇翔 郝兰[1] 管作武[2] 

机构地区：[1]兰州大学化学系应用有机化学国家重点实验室 [2]北京医科大学应用药物研究所

出　　处：《高等学校化学学报》1998年第9期1411-1415,共5页Chemical Journal of Chinese Universities

摘　　要：利用１－芳基－５－甲基－１Ｈ－１，２，３－连三唑－４－甲酰氯、苯并三唑－１－乙酰氯以及５－甲基异唑－３－甲酰氯在低温、丙酮－水条件下，分别同７－ＡＣＡ、７－ＡＤＣＡ和７－ＡＤＣＴ反应，制得１３种头孢菌素衍生物３ａ—３ｉ、６ａ—６ｂ和９ａ—９ｂ，所有化合物经葡萄糖聚糖凝胶柱层析和离心薄层层析反复精制得纯品，新化合物结构经元素分析、ＩＲ、１ＨＮＭＲ和ＦＡＢ－ＭＳ确认．其中代表物显示出强的抗菌活性．Nine new 7 β (1 aryl 5 methyl 1H 1,2,3 triazolyl 4 formamido)cephalosporins 3a 3j were synthesized by acylation of 7 β amino group of 7 ACA, 7 ADCA and 7 ACT, with 1 aryl 5 methyl 1H 1,2,3 triazolyl 4 formyl chloride 2a 2c. Two new 7 β (1,2,3 benzotriazolyl 1 acetamido) cephalosporins 6a 6b and two new 7 β (5 methyl isoxazolyl 3 formamido) cephalosporins 9a 9b were obtained with the same acid choride. Isolation and purification of the new compounds were fulfilled with Sephadex LH 20 column chromatography and centrifugal TLC technique. The structure of the compounds were confirmed by elementary analysis, IR, 1H NMR and FAB MS, some of them showed a significant antibacterial activity.

关 键 词：头孢菌素 连三唑 半合成 抗菌活性 衍生物 

分 类 号：TQ465.1[化学工程—制药化工]