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PALLADIUM-CATALYZED AMINO GROUP ARYLATION OF 1,3-DISUBSTITUTED 1H-PYRAZOL-5-AMINE BASED ON BUCHWALD–HARTWIG REACTION

Mateusz Kucharek, Andrzej Danel
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Abstract


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.


Keywords


5-N-arylaminopyrazoles; palladium catalyst; arylation; cross coupling.

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