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31.
Facile synthesis of α-iodo enaminones 2 was carried out by the use of iodine and triethylamine in methylene chloride in short time in excellent yields. 相似文献
32.
The NH- and α-CH-insertion reactions of tosyl isocyanate with N-monosubstituted and N,N-disubstituted trifluoromethyl-containing enaminones have been studied. The regioselectivity of N-tosylcarbomoylation of N-monosubstituted β-aminovinyl trifluoromethyl ketones depends on the structure of enaminones, the reaction temperature, the nature of solvent and catalyst. The Z configuration of fluorinated vinylogous sulphonylurea 3e was deduced from X-ray analysis. The reaction of N,N-disubstituted enaminone 5a with tosyl isocyanate gave the product mixture of electrophilic attack on either the α-CH- or the oxygen atom of COCF3 group—vinylog of sulfonylurea 6a and tosylamide 7a, correspondingly. 相似文献
33.
4-(p-methoxyphenyl)-β-carboline was prepared in four steps from indole. The key step involved palladium-catalyzed dehydrogenation of a dihydro-β-carboline dichlorophosphinic acid salt. The success of the dehydrogenation was found to depend on the catalyst support. 相似文献
34.
Mohamed Abdel‐Megid 《合成通讯》2013,43(18):3211-3218
Condensation of 4‐acetyl‐5,6‐diphenyl‐2,3‐dihydropyridzin‐3‐one (1) with dimethylformamide dimethylacctal (DMFDMA) afforded the enaminone 2. This could be converted into the pyrazolylpyridazine derivative 4 on reaction with hydrazine hydrate and into pyridazinylpyridazinone 7a,b via coupling with aromatic diazonium salts and subsequent treatment with active methylene compounds. The reaction of 6 with dimethyl acetylenedicarboxylate in the presence of triphenylphosphine afforded the pyridazinylpyridazine derivative 8. Compound 1 converted into 9 upon reflux in acetic acid in the presence of ammonium acetate and afforded 10 on reflux in acetic acid. 相似文献
35.
Herein we have reported a facile solvent-, catalyst-, and aldehyde-free, one-pot synthesis of 3,4-dihydropyridin-2-one from 1,3-diones using simple and mild reaction conditions. The substrate scope has been also extended to β-ketoesters. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource: Full experimental and spectral details.] 相似文献
36.
Zahira Kibou Nadia Aissaoui Ismail Daoud Julio A. Seijas María Pilar Vzquez-Tato Nihel Klouche Khelil Noureddine Choukchou-Braham 《Molecules (Basel, Switzerland)》2022,27(11)
A new and suitable multicomponent one-pot reaction was developed for the synthesis of 2-amino-3-cyanopyridine derivatives. Background: This synthesis was demonstrated by the efficient and easy access to a variety of substituted 2-aminopyridines using enaminones as key precursors under solvent-free conditions. Methods: A range of spectroscopic techniques was used to determine and confirm the chemical structures (FTIR, 1H NMR, 13C NMR). The antimicrobial potency of synthesized compounds (2a–d) was tested using disk diffusion assays, and the Minimum Inhibitory Concentration (MIC) for the active compounds was determined against a panel of microorganisms, including Gram-positive and Gram-negative bacteria and yeasts. Moreover, a docking analysis was conducted by Molecular Operating Environment (MOE) software to provide supplementary information about the potential, as well as an ADME-T prediction to describe the pharmacokinetic properties of the best compound and its toxicity. Results: The results of the antimicrobial activity indicated that compound 2c showed the highest activity against Gram-positive bacteria, particularly S. aureus and B. subtilis whose MIC values were 0.039 ± 0.000 µg·mL−1. The results of the theoretical study of compound 2c were in line with the experimental data and exhibited excellent antibacterial potential. Conclusions: On the basis of the obtained results, compound 2c can be used as an antibacterial agent model with high antibacterial potency. 相似文献