Twenty-two new 3,4,5-trisubstituted 1,2,4,5-oxadiazaboroles were prepared by the cyclocondensation reaction of
N-substituted thiophene, furan and pyridine carboxamidoximes with phenylboronic acid in ...refluxing toluene in good yields.The structures of the new oxadiazaboroles were elucidated by means of spectral measurements (IR,
1H,
13C,
11B NMR, MS, X-ray) and physical data (melting points, elemental compositions by HRMS).
Twenty-two new 3,4,5-trisubstituted 1,2,4,5-oxadiazaboroles were prepared by the cyclocondensation reaction of
N-substituted thiophene, furan and pyridine carboxamidoximes with phenylboronic acid in refluxing toluene in good yields. The structures of the new oxadiazaboroles were elucidated by means of spectral measurements (IR,
1H,
13C,
11B NMR, MS, X-ray) and physical data (melting points, elemental compositions by HRMS).
Some new pyrido3′,2′:4,5thieno2,3-
e
-1,2,4triazolo4,3-
a
pyrimidin-5(4
H
)-ones were prepared through heterocyclization of ethyl 3-aminothieno2,3-
b
pyridine-2-carboxylate with phenyl or ethyl ...isothiocyanate followed by nucleophilic displacement with hydrazine, and finally cyclocondensation with orthoesters.
A new procedure for the synthesis of known azo pyridone dyes is presented. A series of 5-(substituted arylazo)-6-hydroxy-4-methyl-3-cyano-2-pyridones were prepared from ethyl 3-oxo-2-(substituted ...phenylazo)buta-noates and cyanoacetamide in acetone using potassium hydroxide as a catalyst by simple refluxing the reaction mixture. The structure of these dyes was confirmed by FT-IR, NMR and UV--Vis spectroscopy.
A novel consecutive three-component synthesis of 3-(hetero)aryl-1H-pyrazoles via room temperature Sonogashira arylation of propynal diethylacetal used as a propargyl aldehyde synthetic equivalent has ...been disclosed. The final acetal cleavage-cyclocondensation with hydrazine hydrochloride at 80 °C rapidly furnishes the title compounds in a one-pot fashion.
This review describes the reactions of α/β-mercaptoalkanoic acids as building blocks for the synthesis of heterosteroids, polyfunctional heterocycles with pharmacological interest. Annelated ...heterocycles have been prepared by the cyclocondensation reaction of α- and β-mercaptoalkanoic acids with carbonyl compounds. This reaction takes place by nucleophilic addition, followed by cyclization with elimination of water. The main objective of this survey is to provide a comprehensive account of this reaction type in building various heterocycles, and examining their potential in developing better chemotherapeutic agents.
To synthesize new congeners by incorporating isoniazid with 1,2,3,4-tetrahydropyrimidinones moieties in a single molecular frame work and to evaluate their antimicrobial and antimycobacterial ...activity.
A new series of some novel isoniazid cyclocondensed 1,2,3,4-tetrahydropyrimidines was prepared by N′-acetoacetylisonicotinohydrazide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made benzenesulphonic acid. Confirmation of the chemical structure of the synthesized compounds (4a-n) was substantiated by melting point, TLC, different spectral data IR, 1H-NMR, and Mass spectra were done. The synthesized compounds were evaluated for in vitro antimicrobial and antimycobacterial activity against Bacillus subtilis (B. subtilis), Escherichia coli (E. coli), Mycobacterium tuberculosis (M. tuberculosis) CIP and H37Rv strain.
The titled compounds exhibited weak, moderate, or high antimicrobial and antimycobacterial activity. Compounds 4l, 4m, and 4n, exhibited potential antimicrobial and antimycobacterial action, when compare with the current therapeutic agent of Norfloxacin and Rifampicin.
Compound 4l, 4m, and 4n is arguably the most potent, our present study makes it an interesting compound when compared to the current therapeutic agents and are considered the candidates to investigate further for the same.
A convenient solvent less cyclocondensation from thiosemicarbazone of benzofuranone and chloroacetic acid using an ionic liquid, N-methylpyridinium tosylate for obtaining novel 4-thiazolidinones in ...excellent yields is reported. Also, the green expedient synthesis of new 2,4-disubstituted thiazoles under grinding condition from phenacyl bromides and thiosemicarbazide derivatives in quantitative yields is reported.
10-Amino-7,11-dicyano-9-aza-3-azoniaspiro5,5undeca-7,10-diene-8-selenolates have been obtained by the interaction of
N
-alkylpiperidin-4-ones with 2 equiv. cyanoselenoacetamide or with malononitrile ...and cyanoselenoacetamide. Aminomethylation of the obtained compounds proceeded under mild conditions and led to the formation of 8'-selenoxo-3',5',7',11'-tetraazaspiropiperidine-4,13'-tri-cyclo7.3.1.0
2,7
tridec2ene-1',9'-dicarbonitriles. The structure of 1-methyl-5',11'-di(4-methyl-phenyl)-8'-selenoxo-3',5',7',11'-tetraazaspiropiperidine-4,13'-tricyclo7.3.1.0
2,7
tridec2ene-1',9'-di-carbonitrile was determined by X-ray structural analysis.
Microwave irradiation was used to accelerate the cyclocondensation of isoflavones with 2-aminoimidazole to synthesize 5,6-diphenylimidazo1,2-apyrimidines. A series of 17 new compounds were ...characterized by Fourier transform infrared, NMR, and elemental analysis. 5-(2-Hydroxyl-4-isopropoxyphenyl)-6-phenylimidazo-1,2-apyrimidine was determined by x-ray diffraction. A variety of substrates can participate in the process with good yields and purities, making this methodology suitable for library synthesis in drug discovery.
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