摘要
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。
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.
出处
《化学研究与应用》
CSCD
北大核心
2017年第9期1398-1401,共4页
Chemical Research and Application
基金
重庆市教委科技项目(KJ1504403)资助
关键词
吉非替尼
抗肿瘤药
新合成线路
gefitinib
antitumor drug
new synthesis technology
