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新型N-(2’-芳胺嘧啶-4’-基)-N,2,3-三甲基-2H-吲唑-6-胺衍生物的合成及其抗肿瘤活性
Synthesis and Antitumor Activities of N-(2′-arylaminepyrimidin4′-yl)-N,2,3-trimethyl-2H-indazol-6-amine Derivatives
【摘要】 以3-甲基-6-硝基-1H-吲唑为原料,经N-甲基化、催化还原、亲核取代及烷基化反应制得关键中间体N-(2’-氯嘧啶-4’-基)-N,2,3-三甲基-2H-吲唑-6-胺(5);5与芳胺经亲核取代反应合成了一系列新型的N-(2’-芳胺嘧啶-4’-基)-N,2,3-三甲基-2H-吲唑-6-胺衍生物,其结构经1H NMR和MS确证。初步生物活性测试结果表明,部分化合物具有明显的抗肿瘤活性。
【Abstract】 A key medicine intermedia,N-(2′-chloropyrimidin-4′-yl)-N,2,3-trimethyl-2H-indazol-6-amine(5),was obtained by N-methylation,catalytic reduction,nucleophilic substitution and alkylated reaction from 3-methyl-6-nitro-1H-indazole.Eleven novel N-(2′-arylaminepyrimidin-4′-yl)-N,2,3-trimethyl-2H-indazol-6-amine derivatives were synthesized by nucleophilic substitution of 5 with arylamine.The structures were characterized by 1H NMR and EI-MS.The preliminary bioassay test indicates that some of them exhibited obvious antitumor activities.
【Key words】 N-(2-chloropyrimidin-4-yl)-N,2,3-trimethyl-2H-indazol-6-amine； nuclephilic substitution； synthesis； antitumor activity；
- 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2011年06期
- 【分类号】R914;TQ460.1
- 【被引频次】5
- 【下载频次】208