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单环β-内酰胺类抗生素,具有抗G~-菌活性高、耐酶性好的特点。因而在抗生素研究领域中相当活跃。单环类的母核——吖丁啶酮的合成,可从开链及双环化合物开始。由于6-APA具有来源方便、价格低廉、氨基构型符合单环类抗菌活性需要的特点,许多研究都以6-APA作为从双环裂解法合成单环β-内酰胺的原料。6-APA经酯化、三苯甲基化保护羧基及氨基后,进行裂解及氧化反应,得到吖丁啶酮。后者再经
Monocyclic β-lactam antibiotics, with anti-G ~ - bacteria activity, resistance to enzyme characteristics. It is quite active in the field of antibiotic research. Monocyclic nucleus-azetidinone synthesis, starting from open-chain and bicyclic compounds. Since 6-APA has the advantages of convenient source, low cost and the amino configuration conforms to the needs of monocyclic antibacterial activity, many studies have used 6-APA as a raw material for synthesis of monocyclic β-lactam from bicyclic cleavage. 6-APA by esterification, tritylation of carboxyl and amino protection, the cracking and oxidation reaction, azetidinone. The latter by