丙二醇头孢曲嗪的合成

Synthesis of cefatrizine propylene glycol

目的合成丙二醇头孢曲嗪。方法 7-ACA与5-巯基-1,2,3-三唑钾盐反应制备得到头孢曲嗪中间体7-TACA,再与D-(-)-对羟基苯甘氨酸邓钾盐缩合,得到甲醇头孢曲嗪,纯化后制得丙二醇头孢曲嗪。结果产品总收率32.4%,质量符合日本药典标准。结论本工艺简单易行,为中试生产提供了依据。

Objective To synthesize cefatrizine propylene glycol. Methods The intermediate of cefatrizine, 7-TACA, obtained by condensation of 7-ACA with potassium 1,2,3-triazole-5-thiolate, reacted with D-（-）- p-hydroxyphenylglycine dane potassium salt to give cefatrzine metholate. Then, cefatrzine metholate was purified and converted into cefatrizine propylene glycol. Results The overall yield was 32.4% and the product complied with Japanese Pharmacopoeia specification. Conclusion This process was simple and feasible, and it provided a basis for pilot scale production.