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.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1998年第9期1411-1415,共5页
Chemical Journal of Chinese Universities
关键词
头孢菌素
连三唑
半合成
抗菌活性
衍生物
Cephalosporins, Vicinal triazole, Semisynthesis, Antibacterial activity, Centrifugal TLC
