[关键词]
[摘要]
目的 合成地拉罗司并对工艺进行优化研究。方法 以水杨酸为原料,经与二氯亚砜氯化、水杨酰胺脱水环合和对羧基苯肼开环重排3步得到口服铁螯合剂地拉罗司。结果 地拉罗司合成总收率为59.36%。结论 对工艺进行了改进,提高了地拉罗司合成收率。
[Key word]
[Abstract]
Objective To synthesize deferasirox and optimize its synthetic technology. Methods Deferasirox, an orally available iron chelator, was synthesized by cyclization of salicylaldehyde chloride with salicylamide and 4-hydrazinobenzoic acid, in which salicylaldehyde chloride was prepared with salicylic acid and thionyl chloride under normal temperature. Results Deferasirox was prepared with an overall yield of 59.36%. Conclusion The improved technology could increase the yield of deferasirox.
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[基金项目]
2012年度大学生科技创新项目(2012DKC14)