4-(3-氯-4-氟苯胺基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉的合成  

Synthesis of 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline(ZD1839)

作　　者：袁立[1] 郝金恒[1] 张勇[1] 王玉亚[1] 王晖[1] 陈皎月[1] 宫平[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2005年第1期39-41,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成 4 (3 氯 4 氟苯胺基 ) 7 甲氧基 6 [3 (4 吗啉基 )丙氧基 ]喹唑啉 (ZD1839)。方法以 3 羟基 4 甲氧基苯甲酸甲酯作为起始原料 ,经 7步反应得到目标化合物。结果与结论目标化合物的结构经IR、1H NMR和MS确证。本合成反应条件温和 ,原料易得 ,操作简便 ,反应步骤比文献方法 (9步 )减少两步 ,反应总收率为 34 81%。Aim To investigate a synthetic route of 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline(ZD1839).Methods The target compound was synthesized through a se- ven-step procedure starting from 3-hydroxy-4-methoxybenzoic acid methyl ester.Result and conclusion The procedure developed has several advantages such as mild reaction conditions,easily obtained materials and convenient operation.The reaction steps were reduced when comparing with the literature method(nine steps)and the total yield reached 34.81%.The structure of the ZD1839 was characterized by IR, 1H-NMR and MS.

关 键 词：药物化学 制备 化学合成 ZD1839 抗癌药 

分 类 号：R914.5[医药卫生—药物化学]