Facile Regioselective On-Water Synthesis of 4,7-Dihydropyrazolo[1,5-a]Pyrimidines and 4,7-Dihydro[1,2,4]Triazolo[1,5-a]Pyrimidines
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DOI: 10.1007/s10593-019-02449-x
Abstract: Efficient and regioselective on-water synthesis of variously substituted 5-amino-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-carbonitriles and 5-amino-4,7-dihydro[1,2,4]triazolo[1,5-a]pyrimidine-6-carbonitriles using 1,8-diazabicyclo[5.4.0]undec-7-ene as catalyst has been demonstrated. The reaction of 2-benzylidenemalononitriles and 3-aryl-1H-pyrazol-5-amines or 1H-1,2,4-triazol-5-amine allows to obtain the respective pyrazolo[1,5-a]pyrimidines and [1,2,4]triazolo[1,5-a]pyrimidines in… read more here.
Keywords: water synthesis; regioselective water; water; dihydro triazolo ... See more keywords
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A3 adenosine receptor subtype.
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DOI: 10.1016/j.ejmech.2018.08.042
Abstract: [1,2,4]Triazolo[1,5-c]pyrimidine is a promising platform to develop adenosine receptor antagonists. Here, we tried to investigate the effect of the substituent at the 8 position of [1,2,4]triazolo[1,5-c]pyrimidine derivatives on affinity and selectivity at the human A3… read more here.
Keywords: position; adenosine receptor; receptor subtype; receptor antagonists ... See more keywords
Discovery of [1,2,4]triazolo[1,5-a]pyrimidines derivatives as potential anticancer agents.
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DOI: 10.1016/j.ejmech.2020.113108
Abstract: In this work, we reported the discovery of compound 6i with potent antiproliferative activity against MGC-803. Among these compounds, the most potent compound 6i could effectively inhibit MGC-803 (IC50 = 0.96 μM), being around 38-fold selectivity over GES-1.… read more here.
Keywords: mgc 803; discovery triazolo; triazolo pyrimidines; derivatives potential ... See more keywords
Direct (het)arylation of [1,2,4]triazolo[1,5-a]pyrimidines: Both eliminative and oxidative pathways
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DOI: 10.1016/j.tet.2017.07.042
Abstract: (Hetero)arylation of [1,2,4]triazolo[1,5-a]pyrimidine through the direct nucleophilic CH functionalization of the C-7 and C-5 positions has been implemented. The regioselective addition of a (het)aryl magnesium bromide to C-7 of 6-bromo-[1,2,4]triazolo[1,5-a]pyrimidine, followed by eliminative aromatization of… read more here.
Keywords: arylation triazolo; triazolo; direct het; het arylation ... See more keywords
Synthesis of New 3,7,9-Trisubstituted Pyrazolo[4,3-e][1,2,4]Triazolo[4,3-c] Pyrimidines Acyclo C-Nucleosides via Oxidative Cyclisation
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DOI: 10.3184/174751918x15414291150879
Abstract: Condensation of 4-hydrazino-1,3-diphenylpyrazolo[3,4-d]-pyrimidine with the aldohexoses, namely, D-glucose, D-galactose, D-mannose and the aldopentoses, D-arabinose, D-xylose and D-ribose, by heating in an aqueous ethanol in the presence of a catalytic amount of HCl, gave the respective… read more here.
Keywords: triazolo pyrimidines; acyclo nucleosides; synthesis new; oxidative cyclisation ... See more keywords