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Iodine-Mediated Synthesis of Novel Pyrazole Derivatives Publisher



Mahdavi M1 ; Khoshbakht M2 ; Saeedi M3, 4 ; Asadi M1 ; Bayat M2 ; Foroumadi A1 ; Shafiee A1
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Department of Chemistry, Imam Khomeini International University, Qazvin, Iran
  3. 3. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran

Source: Synthesis (Germany) Published:2016


Abstract

The reaction between N,2-diarylhydrazinecarbothioamide (generated from arylhydrazines and aryl isothiocyanates) and malononitrile in the presence of iodine/triethylamine in N,N-dimethylformamide at 80 °C afforded novel pyrazoles, 5-amino-1-aryl-3-(arylamino)-1H-pyrazole-4-carbonitriles, in good yields. In this strategy, iodine served as a versatile desulfurizing agent, efficiently promoting the cyclization reaction. © 2016 Georg Thieme Verlag Stuttgart · New York.