- Synthesis of 3-Pyrazolyl-1,2,4-Triazoles via One-Pot Multicomponent Reaction in Phosphoric Acid
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A high-yielding synthetic route towards pyrazolyl-[1,2,4]triazole derivatives has been developed via one-pot multicomponent reaction of polyfunctionalized triazoles, DMF-DMA, acetophenone, ethyl cyanoacetate, and/or 3-oxo-3-phenylpropanenitrile in ortho-phosphoric acid (85%). In the same manner, a new series of 2-triazolyl-tetrahydro-indazol-4-ones and pyrazolo[3,4-d]pyrimidines has been synthesized by reaction of triazoles, DMF-DMA and 1,3-cyclohexanediones and/or barbituric acid, respectively. The same products were prepared a classical manner via reaction of triazoles with the corresponding enaminones in ortho-phosphoric acid (85%).
- Amer, Amer Anwar,Moustafa, Amr Hassan
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- An efficient one-pot expeditious synthesis of 3-phenyl-1-(6-phenyl-7H-[1,2,4] triazolo[3,4-b] [1,3,4] thiadiazin-3-yl)-1H-pyrazol-5-amines via multicomponent approach
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An efficient synthesis of 3-phenyl-1-(6-phenyl-7H-[1,2,4] triazolo[3,4-b][1,3,4]thiadiazin-3-yl)-1H-pyrazol-5-amines was accomplished by a simple, atom-economical, and multicomponent approach. Reaction of 4-amino-5-hydrazinyl-4H-1,2,4-triazole-3-thiol with various phenacyl bromides and benzoylacetonitriles in ethanol and catalytic amount of acetic acid afforded the titled compounds. The structures of newly synthesized compounds were confirmed by their analytical and spectral (IR, 1H-NMR, 13C-NMR, and Mass) data.
- Sujatha, Kodam,Deshpande, Ravindra Pramod,Kesharwani, Rajesh Kumar,Babu, Phanithi Prakash,Rao Vedula, Rajeswar
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- One-pot, Multicomponent Cascade Reaction for the Synthesis of Various Aralkyl/alkylthio-3,5-dimethyl-1H-pyrazolyl-4H-1,2,4-triazol-4-amine and Their Docking Studies
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A facile and simple one-pot procedure for the synthesis of various aralkyl/alkylthio-3,5-dimethyl-1H-pyrazolyl-4H-1,2,4-triazol-4-amines has been described via a multicomponent reaction of 4-amino-5-hydrazinyl-4H-1,2,4-triazole-3-thiol, acetylacetone, and various aryl/alkyl halides in good yields. All the newly synthesized compounds were characterized by using analytical and spectral studies. Our in silico studies confirmed that 4e, 4f, 4g, and 4j have the best inhibition activity among the synthesized compounds with a high selective index against the Tubulin protein and showed best interactions with receptor structure. The present study provides a novel series of compounds with a promising inhibitor to prevent on Tubulin protein.
- Jilloju, Parameshwara Chary,Vinaykumar, Allam,Shyam, Perugu,Vedula, Rajeswar Rao
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- A regioselective and convenient one-pot multicomponent synthesis of 9-amino-3,5-diaryl-4,9-dihydro-5H-[1,2,4]triazolo[5,1-c][1,2,4]triazepine-8-thiol
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An efficient and environment-friendly procedure for the synthesis of a new series of nitrogen bridge-head [1,2,4]triazolo[5,1-c][1,2,4]triazepine derivatives through one-pot three-component reaction of polyfunctional triazole with aromatic aldehydes and acetophenone derivatives using alcoholic sodium hydroxide solution. The same new products were prepared in classical route through reaction of triazole with the corresponding chalcones under the same conditions.
- Moustafa, Amr Hassan,Amer, Amer Anwar
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supporting information
p. 1102 - 1109
(2017/05/25)
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- Addition-Cyclisations of Ethoxycarbonyl Isothiocyanate with Hydrazine Derivatives as a Source of Thiadiazoles and Triazoles
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Ethoxycarbonyl isothiocyanate reacts additively with hydrazine, ethoxycarbonylhydrazine, as well as amino- and 1,2-diaminoguanidine.Simultaneous or subsequent cyclisation of the resulting 1:1- or 2:1-adducts in acidic or alkaline media yields substituted 1,3,4-thiadiazoles or 1,2,4-triazoles, respectively.
- Kurzer, Frederick,Secker, Jane L.
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p. 355 - 360
(2007/10/02)
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