2-(2-氯乙基)-N1-(4-((6,7-二甲氧基-4-喹啉基))氧基)苯基)-N3-(4-氟苯基)丙二酰胺的合成  

Synthesis of 2-(2-Chloroethyl)-N^1-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N^3-(4-fluorophenyl)malonamide

作　　者：彭冠 宋皓 古亮 陈辉 付敏 PENG Guan;SONG Hao;GU Liang;CHEN Hui;FU Min(Jiangxi Qingfeng Pharmaceutical Co.,Ltd.Ganzhou,Jiangxi 341000,China;Jiangxi Kewei Collaborative Innovative Pharmaceutical Co.,Ltd.,Ganzhou,Jiangxi 341000,China)

机构地区：[1]江西青峰药业有限公司,江西赣州341000 [2]江西科维协同创新药物有限公司,江西赣州341000

出　　处：《浙江化工》2020年第11期13-15,25,共4页Zhejiang Chemical Industry

基　　金：江西省重点研发计划资助项目(20171ACG70014)。

摘　　要：以卡博替尼为原料,二氯亚砜为溶剂,在三氟化硼乙醚催化下开环得到2-(2-氯乙基)-N1-(4-((6,7-二甲氧基-4-喹啉基))氧基)苯基)-N3-(4-氟苯基)丙二酰胺。目标化合物经核磁确证,该反应易于控制,操作简便。Using thionyl chloride as solvent,and boron trifluoride ethyl ether as catalysis,2-(2-chloroethyl)-N^1-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N^3-(4-fluorophenyl)malonamide was obtained from cabozantinib by ring-opening reaction.The target compound is confirmed by NMR.The reaction is easy to control and operate.

关 键 词：卡博替尼 2-(2-氯乙基)-N1-(4-((6 7-二甲氧基-4-喹啉基))氧基)苯基)-N3-(4-氟苯基)丙二酰胺 合成 

分 类 号：TQ464.8[化学工程—制药化工]