铁鳌合剂去铁斯若的合成

Synthesis of deferasirox,an iron chelator

目的:合成铁离子鳌合剂去铁斯若。方法:以水杨酸和水杨酰胺为起始原料,先制得中间体4,再与对羧基苯肼环合制得去铁斯若1。结果:以总收率59.2%合成了铁离子鳌合剂去铁斯若,结构经核磁氢谱(1HNMR)、质谱(MS)确证。结论:本合成路线反应条件温和,原料价廉易得,收率较文献有所提高。

Objective： To synthesize deferasirox, an iron chelator. Methods： The intermediate product （4） was prepared from salicylic acid and salicylanlide as the starting material, and it was then converted to deferasirox （1） by cyclization with 4-hydrazino-benzoic acid. Results： The structure was verified by ^1HNMR and MS; the yield was 59.2%. Conclusion： A pragmatic synthesis method with mild reactive condition and cheaper reagents for deferasirox is achieved. The yield of deferasirox is much higher than those have been reported.