Aurora激酶抑制剂ZM-447439的合成  

Synthesis of Aurora Kinase Inhibitor ZM-447439

作　　者：王刚[1] 张帆[1] 张玉珠[2] 

机构地区：[1]辽宁医学院药学院,辽宁锦州121001 [2]辽宁中医药大学附属医院药剂科,辽宁沈阳110032

出　　处：《中国医药工业杂志》2014年第1期13-16,共4页Chinese Journal of Pharmaceuticals

摘　　要：以3-甲氧基-4-羟基苯甲酸为原料经酯化、O-烃化、硝化、还原、环合、氯代制得4-氯-6-甲氧基-7-(3-氯丙氧基)喹唑啉(8)。另用对硝基苯胺与苯甲酰氯经酰化、还原反应制得N-(4-氨基苯基)苯甲酰胺(11)。8与11经亲核取代和N-烃化制得Aurora激酶抑制剂ZM-447439,总收率约31%(以3-甲氧基-4-羟基苯甲酸计)。4-Chloro-7-（3-chloropropoxy）-6-methoxyquinazoline （8） was prepared from 4-hydroxy-3- methoxybenzoic acid via esterification, O-alkylation, nitration, reduction, cyclization and chlorination. Meanwhile, N- （4- aminophenyl） benzamide （11） was synthesized from p-nitroaniline via acylation and reduction. Finally, ZM-447439 was synthesized by nucleophilic substitution of 8 with 11, followed by N-alkylation. The overall yield was about 31% based on 4-hydroxy-3-methoxybenzoic acid.

关 键 词：ZM-447439 AURORA激酶抑制剂 合成 

分 类 号：R979.19[医药卫生—药品]