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。
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.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第1期51-53,共3页
Chinese Journal of Medicinal Chemistry
关键词
药物化学
工艺改进
化学合成
呋布西林钠
medicinal chemistry
process improvement
chemical synthesis
furbenicillin sodium
