抗癌药雷替曲塞中间体的合成  

Synthesis of Intermediates of Raltitrexed

作　　者：温新民[1] 张波[1] 王惠云[1] 虞心红[2] 

机构地区：[1]济宁医学院药物化学教研室 [2]华东理工大学化学与制药学院

出　　处：《济宁医学院学报》2006年第2期22-23,共2页Journal of Jining Medical University

摘　　要：目的合成了抗结直肠癌药雷替曲塞的重要中间体5-硝基-2-噻吩甲酸。方法以噻吩-2-甲酸为原料,经乙酸酐中硝化制得5-硝基-2-噻吩甲酸和4-硝基-2-噻吩甲酸,直接过滤出此混合物沉淀,按每克沉淀约加18mL水溶解。结果根据两种物质的钡盐在水中溶解度的不同分离得纯品5-硝基-2-噻吩甲酸,收率73%。结论收率得到提高,适合工业化生产。Objective To synthesize 5 - nitro - 2 - thiphenecarboxylic acid, an important intermediate of raltitrexed. Methods Starting from 2 - thiphenecarboxylic acid,which was nitrated in acetic anhydride to give 5 - nitro - 2 - thiphenecarboxylic acid and 4 - nitro - 2 - thiphenecarboxylic acid. The precipitate is filtered, dissolved in water（18mL/g）. Results The yield was 73 % after separation of 5 - and 4 - nitro- 2 - thiphenecarboxylic acid owing to the different solubility in water of their barium salts. Conclusion The yield was increased and is suitable for industrial production.

关 键 词：5-硝基-2-噻吩甲酸 雷替曲塞 

分 类 号：R979.1[医药卫生—药品] R914.5[医药卫生—药学]