氨噻肟乙酸苯并噻唑硫酯的合成

Synthesis of 2-(2-Amino-4-thiazolyl)-2-(Z)-methoxyiminoacetic Acid 2-Benzthiazolyl Thioester

改进第三代头孢菌素类抗生素中间体氨噻肟乙酸苯并噻唑硫酯的合成方法。采用二氯甲烷和甲苯 (体积比 1∶ 1 )的混合溶剂代替单一溶剂二氯甲烷 ,反应可在室温下进行 ,不需要进一步的精制 ,提高了产品品质 ,收率达到 85 %。中试结果证明 :产品品质稳定 ,重现性好 。

Synthesis of 2-(2-amino-4-thiazolyl)-2-(Z)-methoxyiminoacetic acid 2-benzthiazolyl thioester, one of the most important intermediates of the third generation cephalosporins, was improved. Used a mixture of 1,2-dichloromethane and toluene instead of the single 1,2-dichloromethane, the reaction can be carried out successfully at room temperature. Products with high quality were obtained without further purification and the yield was over 85 percent. The reproducibility of the method in large scale is good.