吉非替尼的合成研究

Study on Synthesis of Gefitinib

以3-羟基-4-甲氧基苯甲醛为起始原料合成了抗肿瘤药吉非替尼。先将3-羟基-4-甲氧基苯甲醛的醛基转化成氰基,再与N-(3-氯丙基)吗啉缩合,依次经硝化、还原、与DMF-DMA反应、与3-氯-4-氟苯胺反应合成得到吉非替尼,总收率约33%。

With 3-hydroxy-4-methoxybenzaldehyde as raw materials,gefitinib was synthesized via conversion of aldehyde to nitrile,condensation with N-（3-chloropropyl）morpholine,nitration,reduction,reaction with DMF-DMA,reaction with 3-chloro-4-fluoroaniline,sequently.The total yield was about 33%.