极光激酶小分子抑制剂AT9283的合成  

Synthesis of AT9283,an inhibitor of small molecular Aurora kinase

作　　者：张曙光[1] 郑友广[1] 冯成亮[1] 吉民[1] 

机构地区：[1]东南大学化学化工学院,南京211189

出　　处：《中国新药杂志》2013年第19期2292-2295,共4页Chinese Journal of New Drugs

基　　金：国家"973"计划项目(2011CB933500)

摘　　要：目的:合成极光激酶抑制剂AT-9283。方法:以3,4-二硝基苯甲酸为原料,经酰胺化,还原,关环,得到关键中间体5-吗啉基-4-甲基-2-(4-硝基-1H-3-吡唑基)-1H-苯并咪唑(4),4经还原后再与环丙胺成脲制得AT-9283。结果和结论:目标产物结构经IR,1H-NMR,13C-NMR和ESI-MS确证。本合成路线条件温和,操作简单,总收率较高,而且整个过程不需要柱色谱纯化。Objective： To synthesize AT-9283, an Aurora kinase inhibitor. Methods： The intermediate 5- morpholin-4-ylmethyl-2-（4-nitro-1H-pyrazol-3-yl） -1H-benzimidazole （ 4 ） was prepared by amidation, reduction and cyclization with 3,4-dinitrobenzoic acid as the starting compound. AT-9283 was produced by urea formation. Results and Conclusion： The structure of AT9283 was verified by IR, 1H-NMR, 13C-NMR and ESI-MS. The pragmatic synthesis method with mild reactive conditions is simple and highly productive, and the preparation has no need of column chromatography.

关 键 词：极光激酶抑制剂 AT9283 合成 温和 简单 

分 类 号：R914.5[医药卫生—药物化学]