【摘要】 以呋喃甲醛为起始原料,经肟化、贝克曼重排、异氰脲酸化、氨基化、缩合和成盐6步反应,合成了酰脲类青霉素抗生素呋布西林钠。该工艺路线使用甲酸钠代替异辛酸钠,减少了关键中间体6-氨基青霉烷酸(6-APA)的耗用量,收率从文献的70%提高到76%。中间体和最终产物的结构经1H-NMR确证。更多还原

【Abstract】 Furbenicillin sodium,a known semi-synthetic ureide type of antibiotic firstly marketed in China,was synthesized from starting material 2-furaldehyde via six steps including oximation reaction,Beckmann rearrangement,isocyannuration,amination,condensation and salification etc.The synthetic process was improved by using sodium formate instead of sodium 2-ethylhexanoate and yield of the modified method was also raised to 76% with low consumption of 6-APA comparing with the 70% in the literature.The structures of all the intermediate and target compound were determined by ()~1H-NMR.更多还原