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6-取代香豆素-3-甲酰胺头孢菌素的合成

SYNTHESIS OF 6-SUBSTITUTED-COUMARIN-3-FORMAMIDO CEPHALOSPORINS

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【作者】 郭红段廷汉李明华

【Author】 Guo Hong, Duan Tinghan and Li Minghua (Department of Pharmaceutical Chemistry)

【机构】 中国药科大学中国药科大学制药化学教研室中国药科大学制药化学教研室 1986届研究生

【摘要】 本文以6-取代香豆素-3-羧酸与头孢菌素母核缩合,合成了15个未见文献报道的6取代香豆素-3-甲酰胺头孢菌素化合物。其合成方法采用了Vilsmeier试剂法,改进了溶媒及摩尔配比,并进一步探索了分离纯化的过程,以元素分析、IR及NMR确证结构。抑菌试验表明,对某些革兰氏阳性菌具有不同程度的抑菌作用,而某些革兰氏阴性菌的效果则不明显。

【Abstract】 Fifteen novel derivatives of the 6-substituted-coumarin-3-formamido cephalosporins were obtained by reacting 6-substituted coumarin-3-carboxylic acids with four cephalosporin-nuclears. Vilsmeier reagent method was mainly employed in the procedure of the condensation. Some improvements were made on the solvent system used in the reactions and the mole ratio of the starting materials. In addition, the seperation and purification of the final products were studied. The antibacterial sensitivity test showed that most of these novel derivatives exhibited gram-positive bacteriostatic activities, but there was no action aganist gram-negative bacteria observed.

  • 【文献出处】 中国药科大学学报 ,Journal of China Pharmaceutical University , 编辑部邮箱 ,1987年03期
  • 【被引频次】5
  • 【下载频次】81
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