α-(7-取代香豆素-3-甲酰胺)苯乙酰胺头孢菌素及7-取代香豆素-3-甲酰胺头孢菌素的合成

Sythesis of 7-[α-(7-Substituted-Coumarin-3-Formamido) Phenylacetamido-Cephalosporic Acids and 7-(7-Substituted-Coumarin-3-Formamido)-Cephalosporic Acids

采用酰氯法和活化酯法合成了14个未见文献报道的α-(7-取代香豆素-3-甲酰胺)苯乙酰胺头孢菌素。通过葡聚糖凝胶(Scphadcx LH-20)柱层析、离心薄层层析纯化精制。由红外光谱、元素分析和核磁共振谱确证其化学结构。初步抗菌试验表明,对某些革兰氏阳性菌有不同程度的抑制作用,但对革兰氏阴性菌无效。

14 new 7-[α-(7-substituted-coumarin-3-formamido)phenylacctamido-cephalosporic acids and 7-(7-sub-stituted-coumarin-3-formamido)-cephalosporic acids were prepared by acyl chloride and active ester methods. Isolation and purification were fulfiled in combination with method of Sephadex LH-20 column chromatography and centrifugal-TLC technique. Their chemical structures were comfirmed by IR, elemental analysis and ~1HNMR. Antibacterial tests showed that most of these compounds possessed some activities against Gram-positive bacteria, but no activity against Gram-negative bacteria.