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。
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.
出处
《合成化学》
CAS
CSCD
北大核心
2011年第6期723-726,共4页
Chinese Journal of Synthetic Chemistry
基金
国家重大新药创制大平台子课题(2009ZX09301-008-P-05)
