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以4,7-二取代香豆素-3-乙酸为侧链酸,用酰氯法与7-ACA,7-ADCA,7-ACT及一系列的3-取代苯甲基头孢母核<5c-5f)进行缩合,合成了一系列7β-(4,7-二取代香豆素-S-乙酰胺基)头孢菌素衍生物(2a-2m)。并且研究了7-ACA的3位乙酰氧基被取代酚取代及2a的3位乙酰氧基被取代吡啶取代的亲核取代反应,分别合成了一系列3-取代苯甲基头孢母核(5c-5f)及3-取代吡啶离子甲基头孢菌素衍生物(2n,20)。体外抑菌活性试验结果表明,所合成的14个新的头孢菌素衍生物对包括青霉素耐药菌株在内的革兰氏阳性菌都有较强的抑菌作用。
With 4,7-disubstituted coumarin-3-acetic acid as the side chain acid, with the acid chloride method and 7-ACA, 7-ADCA, 7-ACT and a series of 3-substituted benzyl cephalosporin nuclear <5c- 5f), a series of 7β- (4,7-disubstituted coumarin-S-acetamido) cephalosporin derivatives (2a-2m) were synthesized. In addition, a series of 3-substituted phenylmethyl cephalosporin nuclei (5c and 5c) were synthesized by the nucleophilic substitution reaction of substituted acetoxy at position 3 of 7-ACA and substituted acetoxy at position 3 of 2a by substituted pyridine. -5f) and 3-substituted pyridine ion methylcephalosporin derivatives (2n, 20). In vitro antibacterial activity test results show that the synthesis of 14 new cephalosporin derivatives, including penicillin-resistant strains of Gram-positive bacteria have a strong antibacterial effect.