艾拉莫德的合成研究  

Synthesis of iguratimod

作　　者：汪燕翔[1] 高红[1] 曹凤华[1] 宋丹青[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2006年第23期2042-2044,共3页Chinese Journal of New Drugs

摘　　要：目的:合成艾拉莫德。方法:以4-氯-3-硝基苯甲醚为起始原料,经亲核取代、还原、甲磺酰化、盖特曼-科赫反应、酰化、水解、环化等7步反应制得目标产物。结果:目标化合物经质谱、核磁共振氢谱、核磁共振碳谱、红外光谱等确证其化学结构,总收率为35．4％。结论:本路线操作简单,成本较低,适合工业化生产。Objective： To synthesize iguratimod. Methods： The target compound was synthesized from 4-chloro-3-nitroanisole as a starting material via seven steps including nucleophilic substitution, reduction, methanesulfonylization, classical Gattermann-Koch reaction, acylation, hydrolysis, and cyclization. Results： The structure of the target compound was confirmed by MS, ^1H-NMR, ^13C-NMR and IR analysis. The total yield of iguratimod was 35.4%. Conclusion： This cost-saving and simplified synthetic method is worthy of the further pilot manufacture.

关 键 词：艾拉莫德 类风湿性关节炎 骨关节炎 

分 类 号：R971.1[医药卫生—药品] R684.3[医药卫生—药学]