头孢特仑酸的合成研究

Synthesis of Cefteram Acid

以7-氨基头孢烷酸为原料,于绿色溶媒碳酸二甲酯反应溶剂中,以三氟化硼/碳酸二甲酯络合物为催化剂,与5-甲基四氮唑反应合成了中间体7-氨基-3-[2-(5-甲基-2H-四氮唑基)甲基]头孢烷酸,然后与2-(2-氨基-4-噻唑基)-2-(甲氧亚氨基)乙酸硫代苯并噻唑酯反应合成了头孢特仑酸。优化条件下头孢特仑酸纯度98.8%,总收率63.8%。该合成工艺具有反应周期短、收率和纯度高、操作简单等优点,适合工业化生产。

Cefteram acid was obtained from the reaction of 7-ACA and 5-methyl-lH-tetrazol with 2-（2-Amino- 4-thiazolyl）-2-methoxyiminoacetic thiobenzothiazole ester using boron trifluoride/dimethyl carbonate complex as the catalyst. Under the optimizing condition, the purity of cefteram acid reached 98.8% , and the overall yield was 63.8%. This synthetic process was proved to be with many advantages including high yield, high purity, and simple-processing; it was suitable for industrial production.