4-氯-7-甲氧基-6-(3-氯丙氧基)喹唑啉的合成  

Research on Synthesis of 4-Chloro-7-Methoxy-6-(3-Chloropropyloxy) Quinazoline

作　　者：杨绍娟[1] 孟令强[2] 李志军[1] 张爱琴[3] 曹黎华[1] 

机构地区：[1]南昌航空大学科技学院,南昌330034 [2]国防科技大学理学院,长沙410000 [3]南昌航空大学环境与化学工程学院,南昌330034

出　　处：《化工生产与技术》2012年第3期14-16,70,共3页Chemical Production and Technology

摘　　要：以3-羟基-4-甲氧基苯甲酸为初始原料,经过6步反应,合成了喹唑啉类酪氨酸激酶抑制剂Gefitinib及一系列衍生物的关键中间体4-氯-7-甲氧基-6-(3-氯丙氧基)喹唑啉,其中涉及到喹唑啉环的合成、羟基的合理保护等,反应总收率为44.56%;产物结构经H NMR确证。该方法反应条件温和,原料易得操作简便,适合于工业化生产。4-chloro-7-methoxy-6-(3-chloropropyloxy)quinazoline is a key intermediate for quinazoline tyrosine kinase inhibitor Gefitinib and there derivatives synthesis which was realized and reacted starting from 3-hydroxy-4-methoxy-benzoic acid via six steps,including the synthesis of the quinazoline,reasonable protection of hydroxyl and so on.The total yield was 44.56%.Its structure was confirmed by HNMR.The method has mild reaction conditions,easily available raw materials,and simple operation,suitable for industrialized production.

关 键 词：4-氯-7-甲氧基-6-(3-氯丙氧基)喹唑啉 酪氨酸激酶抑制剂 合成 

分 类 号：TQ252[化学工程—有机化工]