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

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.