盐酸埃洛替尼的合成  

Synthesis of Erlotinib Hydrochloride

作　　者：李铭东[1] 曹萌[1] 吉民[1] 

机构地区：[1]东南大学化学化工学院,江苏南京210096

出　　处：《中国医药工业杂志》2007年第4期257-259,共3页Chinese Journal of Pharmaceuticals

摘　　要：3,4-二羟基苯甲酸甲酯经烷基化、硝化、还原、闭环、氯代反应制得4-氯-6,7-二-(2-甲氧基乙氧基)-喹唑啉,再经间乙炔基苯胺氨解、成盐得到抗肿瘤药盐酸埃洛替尼,总收率约49%。Erlotinib hydrochloride was synthesized from methyl 3,4-dihydroxybenzoate by alkylation, nitration, reduction, cyclization, chlorination to give 4-chloro-6,7-bis-（2-methoxyethoxy）-quinazoline, which was subjected to amination with m-ethynylaniline and HCl salt formation with an overall yield of about 49%.

关 键 词：埃洛替尼 抗肿瘤药 酪氨酸激酶抑制剂 合成 

分 类 号：R979.19[医药卫生—药品]