Using the inexpensive and readily available 4,5-dimethoxy-2-nitrobenzoic acid as the starting material,gefitinib was syn-thesized through demethylation,esterification,side-chain alkylation,reduction,cyclization,chlorination and ammoniation reaction. This route included seven steps,the total yield was more than 50％. The purity of product was 99. 8％. The route could reduce envi-ronmental pollution,simplify conventional processes,and had high yield. It was suitable for industrial production.%本合成工艺以价廉、易得的4,5-二甲氧基-2-硝基苯甲酸为起始原料,经脱甲基、酯化、侧链烷基化、还原、环合、氯代、氨代反应合成了吉非替尼.整个合成路线共七步,总收率达到50％以上,纯度可达99.8％,具有操作简单、收率高、环境污染小等优点,有良好的工业化前景.
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