Pd-catalyzed direct arylation of phenylpyrazole: Synthesis of fipronil derivatives with aryl boronic acids promoted by a stoichiometric amount of NIS

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• 作者：Ting Lv^a ; Xiao-Hong Zhang^a ; ^{kamenzxh@163.com} ; Jiang-Sheng Han^a ; Ping Zhong^a ; ^b ; ^{zhongp0512@163.com}
• 关键词：Palladium-catalyzed ; Direct arylation ; Phenylpyrazole ; Fipronil derivatives ; Trifluoromethyl group
• 刊名：Journal of Fluorine Chemistry
• 出版年：2012
• 期刊代码：52_00221139
• 类别：ch
• 出版时间：May, 2012
• 卷：137
• 期：Complete
• 页码：44-49
• 文件大小：435 K

摘要

The palladium-catalyzed direct arylation of phenylpyrazole with aryl boronic acid promoted by a stoichiometric amount of NIS has been reported. Several phenyl pyrazoles, especially for those with trifluoromethyl groups, can participate in the reaction, providing a series of fipronil derivatives of 4-aryl-phenylpyrazole with potential bioactivity in moderate to good yields. All the compounds were characterized by ¹H NMR, ¹³C NMR and HRMS spectroscopic techniques.