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自六十年代初分离鉴定出了头孢菌素C结构以来,已对其结构改造进行了广泛的工作,但对具有7位腙(肼)的头孢菌素衍生物研究甚少,特别是在此基础上引入7α位甲(烷)氧基的工作至今未见报道。 我们实验室在合成6α-甲氧基-6β-取代腙基青霉素酯的工作过程中,开发了一个在6β-腙青霉素6α位引入一至三个碳的烷氧基的新方法,本文报道将此方法运用到合成7α-甲氧基-7β-取代腙基头孢菌素衍生物取得了成功。
Since the cephalosporin C structure was isolated and identified from the early 1960s, extensive work has been done on its structural modification, but little is known about cephalosporin derivatives with a 7-hydrazone (hydrazine), especially here Based on the introduction of 7α methionine (oxygen) work has not been reported. In our work in the synthesis of 6α-methoxy-6β-substituted hydrazone penicillin ester, we developed a new method to introduce one to three carbon alkoxy groups at the 6α-position of 6β-hydrazone penicillin. The method was successfully applied to the synthesis of 7α-methoxy-7β-substituted hydrazone cephalosporin derivatives.