铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成

doi:10.6023/A15040263

化学学报 ›› 2015, Vol. 73 ›› Issue (12): 1302-1306.DOI: 10.6023/A15040263 上一篇下一篇

所属专题：碳氢键官能团化

研究通讯

铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成

丁正伟^a, 谭启涛^a, 刘秉新^a, 张可^a, 许斌^a,b,c

a 上海大学化学系上海 200444;
b 中国科学院上海有机化学研究所金属有机化学国家重点实验室上海 200032;
c 华东师范大学化学系上海市绿色化学与化工过程绿色化重点实验室上海 200062

投稿日期:2015-04-16 发布日期:2015-06-15
通讯作者: 许斌, 谭启涛 E-mail:xubin@shu.edu.cn;qttan@shu.edu.cn
基金资助:
项目受国家自然科学基金(Nos.21272149,21302123),上海市教委科研创新重点项目(No.14ZZ094)以及上海市自然科学基金(No.13ZR1416400)资助.

Copper-Promoted Oxidative C-H Bond Amination of Hydrazones:Synthesis of 1H-Indazoles and 1H-Pyrazoles

Ding Zhengwei^a, Tan Qitao^a, Liu Bingxin^a, Zhang Kea^a, Xu Bin^a,b,c

a Department of Chemistry, Shanghai University, Shanghai 200444;
b State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032;
c Shanghai Key Laboratory of Green Chemistry and Chemical Processes, Department of Chemistry, East China Normal University, Shanghai 200062

Received:2015-04-16 Published:2015-06-15
Supported by:
Project supported by the National Natural Science Foundation of China(Nos. 21272149, 21302123), Innovation Program of Shanghai Municipal Education Commission(No. 14ZZ094) and Science and Technology Commission of Shanghai Municipality(No. 13ZR1416400).

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1. 铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成.PDF(4365KB)

摘要/Abstract

吲唑和吡唑是两类重要的含氮杂环化合物,具有广泛的生物活性.发展了一类铜促进下腙的C(sp²)-H键氧化胺化反应,简便、高效地构建了一系列1H-吲唑和1H-吡唑衍生物.该反应条件温和,具有广泛的底物适用范围和较好的官能团兼容性.

关键词: 碳-氢键活化, 胺化, 吲唑, 含氮杂环, 吡唑

An efficient copper-promoted C(sp²)-H bond amination was developed to afford 1H-indazoles and 1H-pyrazoles in moderate to excellent yields from easily accessible hydrazones. This process tolerated a variety of functional groups and afforded the corresponding 1H-indazoles and 1H-pyrazoles under mild conditions.

Key words: C-H activation, amination, indazole, nitrogen heterocycles, pyrazole

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丁正伟, 谭启涛, 刘秉新, 张可, 许斌. 铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成[J]. 化学学报, 2015, 73(12): 1302-1306.

Ding Zhengwei, Tan Qitao, Liu Bingxin, Zhang Kea, Xu Bin. Copper-Promoted Oxidative C-H Bond Amination of Hydrazones:Synthesis of 1H-Indazoles and 1H-Pyrazoles[J]. Acta Chim. Sinica, 2015, 73(12): 1302-1306.

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铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成

Copper-Promoted Oxidative C-H Bond Amination of Hydrazones:Synthesis of 1H-Indazoles and 1H-Pyrazoles

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