Synthesis of pyrazoles from sulfonyl hydrazone and benzyl acrylate under transition-metal-free conditions

被引:4
|
作者
Hao, Liqiang [1 ]
Wang, Zhichao [1 ]
Wang, Yangyang [1 ]
Yang, Zhaoziyuan [1 ]
Liu, Xian [1 ]
Xu, Xiaobo [1 ]
Ji, Yafei [1 ]
机构
[1] East China Univ Sci & Technol, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, 130 Meilong Rd, Shanghai 200237, Peoples R China
基金
中国国家自然科学基金;
关键词
POTENT; CYCLOADDITION; TOSYLHYDRAZONES; AROMATIZATION; 1H-PYRAZOLES; INHIBITORS; DISCOVERY; DESIGN; ARYNES;
D O I
10.1039/d3ob01172k
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Pyrazoles as an important class of heterocyclic compounds, are widely found in pharmaceuticals and bioactive natural products. Herein we report a [3 + 2] cycloaddition reaction for the synthesis of a series of pyrazoles, with the yield up to 77%. This approach exhibits many notable features, such as convenient operating conditions, excellent functional group compatibility and readily accessible raw materials, providing an alternative route for the construction of pyrazole derivatives. DBU-mediated [3 + 2] cycloaddition reaction for the synthesis of pyrazoles. It is noteworthy that this reaction constructed two new C-N bonds and a new C-C bond at the same time, providing a new door for the construction and functionalization of pyrazole scaffolds.
引用
收藏
页码:7611 / 7615
页数:5
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