铁螯合剂去铁斯若衍生物的合成

Synthesis of Deferasirox Derivatives

目的合成铁螯合剂去铁斯若衍生物。方法以水杨酸、水杨酰胺、对肼基苯甲酸为原料,经酰胺化-缩合、加成-消除、提纯等步骤合成系列铁螯合剂去铁斯若衍生物。结果目标产物采用质谱(MS)、核磁共振氢谱(^(1)H NMR)进行结构确证,最终产品纯度可达99.5%以上。结论该工艺简单、合理、可操作性强,产品纯度高,可作为药物去铁斯若的杂质对照品。

Objective To synthesize derivatives of deferasirox.Methods Using salicylic acid,salicylamide and p-hydrazine benzoic acid as starting materials,a series of deferasirox derivatives were synthesized by amidation and condensation,addition and elimination,and purification,etc.Results The structure of target products was verified by ^(1)H NMR and MS.The purity of the end products was above 99.5%.Conclusion The process is simple,reasonable and easy to operate,and the product has high purity,which can be used as the impurity reference substance of deferasirox.