三光气在合成4-氯-6-碘喹唑啉中的应用研究  

Study on the Application of Triphosgene for the Synthesis of 4-chloro-6-idioquinazoline

作　　者：郑海清[1] 王欢欢[1] 黄云云[1] 张豪[1] 黄权[1] 刘骏[1] 

机构地区：[1]绍兴文理学院,浙江绍兴312000

出　　处：《广东化工》2012年第9期90-90,103,共2页Guangdong Chemical Industry

基　　金：绍兴市大学生科技创新项目

摘　　要：以2-氨基-5-碘苯甲酸与醋酸脒反应制得6-碘喹唑啉-4-酚,再以三光气(BTC)为氯化试剂,DMF为催化剂,BTC与6-碘喹唑啉-4-酚的投料比为1.1∶3,二氯甲烷为溶剂,于40℃下反应2.5 h,得到抗癌药拉帕替尼的关键中间体4-氯-6-碘喹唑啉,收率78%。工艺具有条件温和,后处理简单,对环境友好等特点。6-iodoquinazolin-4-ol was synthesized from 2-chloro-5-iodobenzoic acid and formamidine acetate,which was then followed by chlorination using triphosgene as chlorinating reagent catalyzed by DMF in dichloromethane at 40 ℃ for 2.5 h to obtain the key intermediate 4-chloro-6-idioquinazoline of antitumor agent lapatini.The overall yield was 78 %.The process was characterized by mild reaction conditions,simple operation and environmental benign.

关 键 词：三光气 4-氯-6-碘喹唑啉 氯化 

分 类 号：TQ[化学工程]