抗肿瘤药物吉非替尼的合成方法研究  

Study on synthetic method of antineoplastic gefitinib

作　　者：孙键[1] 李娇毅 张喜全[1] 顾红梅[1] 杨玲[1] 李宝林[2] 

机构地区：[1]江苏正大天晴药业股份有限公司,江苏南京210042 [2]教育部药用资源与天然药物化学重点实验室,陕西师范大学化学化工学院,陕西西安710062

出　　处：《化学研究与应用》2013年第8期1180-1184,共5页Chemical Research and Application

基　　金：国家自然科学基金项目(No.21272144)资助

摘　　要：以异香兰素为原料,通过氰基化、氯烷基化、硝化、还原、Dimroth重排和吗啉基的引入六步反应,高收率地合成了抗肿瘤药物吉非替尼。所得各种中间体化合物及吉非替尼均经波谱学方法鉴定,六步反应总收率为49.8%。该合成方法高效、简捷,适用于工业化生产。Gefitinib was synthesized from isovanillin as the starting material by six-step reactions including cyanidation,chloroalkylation,nitration,reduction,Dimroth rearrangement and amination with morpholine.The structures of synthesized intermediates and gefitinib were identified by spectroscopy.The total yield of six-steps was 49.8%.This method was suitable for industrial production with the advantages of efficient and simple.

关 键 词：吉非替尼 异香兰素 4-甲氧基-3-(3-氯丙氧基)苯甲腈 2-硝基-4-甲氧基-5-(3-氯丙氧基)苯甲腈 2-氨基-4-甲氧基-5-(3-氯丙氧基)苯甲腈 

分 类 号：O629.171[理学—有机化学]