Beilstein J. Org. Chem.2011,7, 179–197, doi:10.3762/bjoc.7.25
herein report a detailed account of the synthetic methods available for 5-aminopyrazoles.
As pyrazolederivatives do not exist in nature, probably, due to the difficulty in the construction of N–N bond by living organisms, their availability depends on the synthetic methods. A large number of synthetic
chloride, which affords, again after Fmoc removal, the diglycylpyrazole 142 (Scheme 38) [80].
A new synthetic route [81] to 5-amino-1-aryl-4-benzoyl pyrazolederivatives 144 involves the reaction of β-ketonitriles with N,N’-diphenylformamidine to give initially the cyclocondensation precursors 143 which is
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Graphical Abstract
Figure 1:
Pharmacologically active 5-aminopyrazoles.
Beilstein J. Org. Chem.2011,7, 173–178, doi:10.3762/bjoc.7.24
, no corresponding regioisomers were obtained.
Keywords: imidazole derivatives; methyl acrylate; Michael-type addition; pyrazolederivatives; 1,2,4-triazole derivatives; Introduction
Derivatives of azoles are important biologically active compounds. Many, especially those containing imidazole
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Graphical Abstract
Figure 1:
Examples of azole derivatives as important therapeutic agents.