头孢特仑新戊酯的合成

Synthesis of cefteram pivoxil

目的研究头孢特仑新戊酯的合成工艺。方法 7-ACA与5-甲基四氮唑反应制备7-氨基-3-[2-(5-甲基-2H-四氮唑基)甲基]头孢烷酸(7-MTCA),然后与2-(2-氨基-4-噻唑基)-2-甲氧亚胺乙酸苯并噻唑硫酯(AE活性酯)缩合得头孢特仑酸,再与特戊酸碘甲酯反应得产物。结果产品总收率40.8%,质量符合日本药典标准。结论本工艺简单可行,为中试生产提供了依据。

Objective To study the process for synthesis of cefteram pivoxil. Methods The 7-amino-3- [2-（5-methyl-2H-tetrazolyl）methyl]cephalosporanic acid（7-MTCA）, obtained by condensation of 7-ACA with 5-methyl-lH-tetrazol, reacted with 2-（2-aminothiazol-4-thiazolyl）-2-[[（z）-methoxy]imino]acetic acid s-mercapto benzothiazolylester（activated ester） to give cefteram. Then cefteram reacted with iodomethyl pivalate to give cefteram pivoxil. Results The overall yield was 40.8% and the product complied with Japanese Pharmacopoeia specification. Conclusion This process was simple and feasible, and it provided a basis for pilot scale production.