吉非替尼的合成工艺改进

Process Improvement on the Synthesis of Gefitinib

以3-羟基-4-甲氧基苯甲醛为原料,先与N-(3-氯丙基)吗啉缩合,后依次经过醛基转化为氰基、硝化、还原、与3-氯-4-氟苯胺环合等反应合成了抗肿瘤药物吉非替尼,总收率约50%。其结构经1H NMR,MS和元素分析表征。

Geftinib was synthesized by the condensation reaction of 3-hydroxy-4-methoxybenzaldehyde with N-（3-chloropropyl）morpholine,and then conversion of aldehyde to nitrile,nitration,reduction,and cyclization in total yield about 50%.The structure was characterized by 1H NMR,MS and elemental analysis.