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

Authors

  • Mateusz Kucharek Department of Biotechnology and General Technology of Food, Faculty of Food Technology, University of Agriculture in Krakow, 122 Balicka St., Krakow 30-149, Poland
  • Andrzej Danel Faculty of Materials Engineering and Physics, Cracow University of Technology, 1 Podchorążych St., Krakow 30-048, Poland

DOI:

https://doi.org/10.1007/6059

Keywords:

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

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.

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Published

2021-06-19

Issue

Vol. 57 No. 6 (2021)

Section

Original Papers