Palladium-catalyzed amino group arylation of 1,3-disubstituted 1H-pyrazol-5-amine based on Buchwald–Hartwig reaction

被引:0
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作者
Mateusz Kucharek
Andrzej Danel
机构
[1] University of Agriculture in Krakow,Department of Biotechnology and General Technology of Food, Faculty of Food Technology
[2] Cracow University of Technology,Faculty of Materials Engineering and Physics
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关键词
5-; -arylaminopyrazoles; palladium catalyst; arylation; cross coupling;
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摘要
An efficient Pd-catalyzed C–N bond formation for the synthesis of different pyrazole derivatives using XPhos as a ligand and KOH as a base is presented. The developed procedure can be successfully applied for the synthesis of 5-N-aryl-1,3-disubstituted 1H-pyrazol-5-amines. Contrary to previously described procedures, this one proceeds in one step utilizing commercially available aminopyrazoles and aryl halides. Thus, a series of 5-N-aryl-1,3-disubstituted 1H-pyrazol-5-amines were obtained with satisfactory yields under optimized reaction conditions.
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页码:633 / 639
页数:6
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