- Temperature-dependent product selectivity in the Vilsmeier-Haack reaction on bis(phenylhydrazones) of bis(aroylmethyl) sulfides (=1,1'-[thiobis(methylene) ]bis[arylmethanone] bis(2-phenylhydrazones)): Synthesis of 3-aroylindoles (=aryl(1H-indol-3-yl)methanones)
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The bis(phenylhydrazone) of substituted diphenacyl sulfides (=1,1'-[thiobis(methylene)]bis[arylmethanone] bis(2-phenylhydrazones)) 1 underwent a tandem sequence of reactions upon treatment with Vilsmeier reagent, ultimately yielding 3-aroylindoles (=aryl(1H-indol-3-yl)methanones) 3 (Scheme 1 and Table 1). The reaction seems to be product selective depending upon the reaction temperature. Copyright
- Paul, Nidhin,Muthusubramanian, Shanmugam
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- Phenyl pyrazole compound, pharmaceutical composition and preparation method and application of phenyl pyrazole compound
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The invention discloses a phenyl pyrazole compound, a pharmaceutical composition and a preparation method and application of the phenyl pyrazole compound. The phenyl pyrazole compound shown in a formula I or a formula II can be used for preparing drugs fo
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Paragraph 0252-0255
(2020/02/19)
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- Pyrazole-4-carboxylic Acids from Vanadium-catalyzed Chemical Transformation of Pyrazole-4-carbaldehydes
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The conversion of aldehydes into carboxylic acids using oxidizing agents is a common protocol in transformation chemistry. An efficient oxidation strategy of transformation of pyrazole-4-aldehydes to the corresponding acids using vanadium catalysts in the presence of 30% H2O2 as an oxidant is described. The catalytic technology was successfully applied to a range of various 4-formylpyrazoles, and plausible mechanism is also discussed.
- Bala, Renu,Kumari, Poonam,Sood, Sumit,Phougat, Harshita,Kumar, Anil,Singh, Karan
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p. 1787 - 1793
(2019/04/30)
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- Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
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This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
- Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
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p. 753 - 768
(2015/10/29)
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- Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
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This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
- Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
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p. 753 - 768
(2016/01/09)
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- Synthesis of pyrrol-2-yl- and pyrazol-4-ylmethylidene derivatives of betulin and allobetulin
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Aldol-crotonic condensation of allobetulone and betulonic aldehyde with N-substituted pyrrole-2- and pyrazole-4-carbaldehydes afforded a series of new α,β-unsaturated ketones of lupane series. Their reduction provided 2-ylidene derivatives of allobetulin
- Babak,Semenenko,Gella,Musatov,Shishkina,Novikova,Sofronov,Morina,Lipson
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p. 715 - 726
(2015/07/02)
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- Synthesis and antimicrobial activity of substituted [(pyrazol-4-yl) methylene]hydrazono-2,3-dihydrothiazoles and their sugar derivatives
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A number of new [(pyrazol-4-yl)methylene]hydrazono-2,3-dihydrothiazole derivatives, their sugar hydrazones and N-glycosides were synthesized. Furthermore, N-substituted oxygenated alkyl and hydroxyl derivatives and 1,3,4,-oxadiazoline acyclic nucleoside analogs were prepared. The newly synthesized compounds were tested for their antimicrobial activities and showed moderate to high inhibition activities.
- Abdel-Rahman, Adel A.-H.,El-Sayed, Wael A.,Zaki, El-Sayed G.,Mohamed, Asem A.,Fadda, Ahmed A.
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experimental part
p. 93 - 101
(2012/05/05)
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- Azoles. 17. Beta-(4-pyrazol)acrylic and propionic acids and their anti-inflammatory activity
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beta-(4-Pyrazole)acrylic acids 22-28 were prepared by the Knoevenagel reaction of malonic acid and 4-formylpyrazoles 8-14. 4-Pyrazolemethylenemalonic acids 15-21 were isolated as intermediates. The latter compounds were also synthesized by treating the 4-formylpyrazoles 8-14 with diethyl malonate followed by hydrolysis of the obtained diethyl esters 15a-21a. The effect of piperidine and pyridine on the Knoevenagel condensation was investigated. The beta-(4-pyrazole)acrylic acids 22-27, on catalytic reduction, gave the corresponding beta-(4-pyrazole)propionic acids 29-34. Compounds 23, 24, 27, 29-31 and 34 appeared to be less active than phenylbutazone in carrageenin-induced oedema test, but they were less toxic than the reference drug.
- Bernard,Hulley,Molenda,Stochla,Wrzeciono
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p. 560 - 562
(2007/10/02)
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