Palladium-catalyzed amino group arylation of 1,3-disubstituted 1H-pyrazol-5-amine based on Buchwald–Hartwig reaction
[Figure not available: see fulltext.] 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.
Kucharek, Mateusz,Danel, Andrzej
p. 633 - 639
(2021/07/02)
Synthesis and structural determination of 5-arylamino-1,3-dimethylpyrazoles
Treatment of 4-arylamino-4-thioxo-2-butanones with methylhydrazine in acetic acid gives 5-arylamino-1,3-dimethylpyrazoles which are readily halogenated in the 4 position. The thermal decomposition of 3-anilino-1,2,5- trimethyl-1H-pyrazolium chloride gives
Britsun,Bazavova,Bodnar,Chernega,Lozinskii
p. 105 - 110
(2007/10/03)
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