摘要
目的优化头孢克肟的合成工艺。方法以7-氨基-3-乙烯基-3-头孢环-4-羧酸(简称7-AVCA)与2-(2-氨基噻唑-4-基)-2-[(Z)-甲氧羰基甲氧亚氨基]乙酸-2-苯骈噻唑硫酯(简称MICA活性酯)为起始原料经缩合、水解反应得到目标产物。结果目标产物的纯度达到99.5%,二步反应的总收率达90%。结论该制备过程操作简单,环境污染小,适合工业化大生产。中间体头孢克肟甲酯不需经过烘烤直接用于水解反应,简便高收率地制备头孢克肟。
Objective To improve the manufacturing process ofcefixime. Methods Cefixime was synthesized by reaction of 7-amino-3-vinyl-3-cephem-4-carboxylic acid（Abbreviation 7-AVCA） with 2-（2-aminothiazol-4-yl）- 2-[（Z）-methoxycarbonylmethoxyimino]acetic acid-2-S-mercapto benzo thiazole ester （abbreviation MICA ester） via amidation and hydrolysis. Results The purity was 99.5% and the total yield was more than 90%. Conclusion With simplified operational process and less pollution, this synthesis method of cefixime can be used for industrial production. Since the intermediate cefixime methyl ester can be hydrolyzed without the drying process, cefixime can be synthesized more simply and efficiently.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2012年第9期687-690,共4页
Chinese Journal of Antibiotics
基金
黄岩区重大科技计划项目(No.2004016)
