Abstract

An efficient and facile approach for the synthesis of 5-aminopyrazoles from ketene S,N -acetal and hydrazine hydrate via catalytic reaction under solvent free condition has been described. V 2 O 5 /SiO 2 as a heterogeneous catalyst was prepared and characterized using X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). KEY WORDS : One-pot synthesis, 5-Amino-1 H -pyrazole, Hydrazine hydrate, Vanadium oxide, Silica Bull. Chem. Soc. Ethiop. 2019 , 33(1), 135-142 DOI: https://dx.doi.org/10.4314/bcse.v33i1.13

Highlights

  • Pyrazoles and their derivatives have attracted considerable interest during the last two decades due to their biological activities

  • We reported in this paper the synthesis of 5-aminopyrazole derivatives from the ketene acetal with hydrazine hydrate in solvent free condition by using catalysis for simple procedure optimum results than previous methods

  • The reaction was started by mixing ketene S,N-acetals (10 mmol) and hydrazine hydrate (20 mmol), the V2O5/SiO2 (0.2 g, 20 mol %) was added and the mixture was allowed to stir at 70-80 oC

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Summary

INTRODUCTION

Pyrazoles and their derivatives have attracted considerable interest during the last two decades due to their biological activities. Compound A, has been shown to exhibit antifungal activity [1]. Compound B is a potent inhibitors of neutrophil chemotactic responsiveness [2]. Compound C showed antitumor activity by inhibition of cyclindependent kinases (CDK) [3] (Figure 1). Pyrazole compounds used as intermediates in the synthesis of various bioactive compounds such as pyrazolopyrimidines, pyrazolotriazines, pyrazoloquinazolines and Schiff bases [4,5,6,7,8,9]

C PHA-533533 antitumor activity
RESULTS AND DISCUSSION
70 Catalyst
CONCLUSION
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