| Cu（Ⅰ）催化的分子内氨基化反应合成吲哚并[1,2-b]吲哒唑类化合物 |
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| 引用本文： | 池建文,杭臣臣,朱永明.Cu（Ⅰ）催化的分子内氨基化反应合成吲哚并[1,2-b]吲哒唑类化合物[J].苏州大学学报(医学版),2009,25(4):84-87. |
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| 作者姓名： | 池建文 杭臣臣 朱永明 |
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| 作者单位： | 苏州大学药学院,江苏苏州215123 |
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| 基金项目： | 江苏省自然科学基金资助项目(BK2006048) |
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| 摘 要： | 以取代的邻溴苯乙酮和取代苯肼为原料,用费舍尔吲哚合成法合成吲哚化合物,经过一系列转化得到中间体乙酰胺基取代的吲哚啉化合物,再经Cu（I）催化下的分子内氨基化反应得到吲哚并1,2-b]吲哒唑结构的中间体,水解、空气中氧化后,最终得到具有潜在药理活性的吲哚并1,2-b]吲哒唑类目标物.
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| 关 键 词： | 吲哚并 吲哒唑 Cu(I)催化 分子内氨基化 抗肿瘤活性 |
Synthesis of indolo[1,2-b]indazole derivatives via copper(I)-catalyzed intramolecular amination reaction |
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| Chi Jianwen,Hang Chenchen,Zhu Yongming.Synthesis of indolo[1,2-b]indazole derivatives via copper(I)-catalyzed intramolecular amination reaction[J].Journal of Suzhou University(Natural Science),2009,25(4):84-87. |
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| Authors: | Chi Jianwen Hang Chenchen Zhu Yongming |
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| Institution: | College of Pharmacy;Suzhou University;Suzhou 215123;China |
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| Abstract: | 2'-Bromoacetophenone reacted with phenylhydrazine by the Fischer indole synthesis to give 2-(2-bromophenyl)indole,which followed undergo a four-step reaction to afford intermediate 1-acetylamino-2-(bromophenyl)indoline.The latter was cyclized via a copper(I)-catalyzed intramolecular amination reaction to obtain product 6-acetyl-10b,11-dihydro-6H-indoloindazole.Hydrolysis and subsequent air oxidation allowed the formation of title compound in good yield. |
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| Keywords: | indolo indazole Cu （ I ） -catalyzed intramolecular amination anticancer activity |
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