新型3-氨基吲唑环衍生物的合成  

Synthesis of New Indazol-3-ylamine Derivatives

作　　者：曹瑞霞 Cao Ruixia(College of Chemistry and Chemical Engineering,Qilu Normal University,Jinan,Shandong 250200,China)

机构地区：[1]齐鲁师范学院化学与化工学院,山东济南250200

出　　处：《化学世界》2021年第6期354-357,共4页Chemical World

基　　金：齐鲁师范学院教师科研基金(No.2015L0604);山东省高等学校科技计划(No.J16LC52)资助项目。

摘　　要：4-溴-2-氟苯腈(1)与盐酸肼关环得到3-氨基-6-溴-^(1)H-吲唑(2);化合物2的3位氨基与烷基酮通过还原胺化反应,得到(6-溴-1 H-吲唑-3-基)-环己基-胺(3)和(6-溴-^(1)H-吲唑-3-基)-异丙基-胺(4);然后化合物3和化合物4分别与不同的卤代烃发生取代反应,1位氮原子被不同的烷基修饰,得到一系列新型的(6-溴-1-烷基-1 H-吲唑3-基)-烷基-胺(5~10),其结构经^(1)H NMR和MS表征。A key intermediate,6-bromo-^(1)H-indazol-3-ylamine(2),was prepared by the ring-closure reaction from 4-bromo-2-fluoro-benzonitrile with hydrazine hydrochloride;Compounds of(6-bromo-1 Hindazol-3-yl)-cyclohexyl-amine(3)and(6-bromo-^(1)H-indazol-3-yl)-isopropyl-amine(4)were prepared by the reductive amination reaction from compound 2 with alkyl ketones.Six new(6-bromo-1-substituted-1 Hindazol-3-yl)-substituted-amine were synthesized by nucleophilic substitution of compound 3,4 with alkyl halides.The structures were characterized by ^(1)H NMR and MS.

关 键 词：吲唑 帕唑帕尼 盐酸格拉司琼 还原胺化反应 

分 类 号：O626[理学—有机化学]