AIMS:
A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol-5(4H)-one
derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4-dihydro
isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as a
catalyst.
BACKGROUND:
Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-
yl)methyl)oxazol-5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity.
OBJECTIVE:
The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline.
METHOD:
The target molecules i.e. 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl)oxazol5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from
benzoic acid in few steps.
RESULT:
All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR &
LCMS) and the chemical structures of all compounds were determined by elemental analysis.
CONCLUSION:
Antibacterial activity of the derivatives was examined for the synthesized compounds and results
indicate that compound with bromine substitution has a good activity profile.
In this article, a zirconia-based nano-catalyst (Nano-ZrO2), with intermolecular C-N bond formation for the synthesis of various benzimidazole-fused heterocycles in a concise method is reported. The robustness of this reaction is demonstrated by the synthesis of a series of benzimidazole drugs in a one-pot method. All synthesized materials were characterized using 1HNMR, 13CNMR, and LC-MS spectroscopy as well as microanalysis data. Furthermore, the synthesis of nano-ZrO2 was processed using a standard hydrothermal technique in pure form. The crystal structure of nano-ZrO2 and phase purity were studied, and the crystallite size was calculated from XRD analysis using the Debye–Scherrer equation. Furthermore, the antimicrobial activity of the synthesized benzimidazole drugs was evaluated in terms of Gram-positive, Gram-negative, and antifungal activity, and the results were satisfactory.
ABSTRACT. An efficient and convenient procedure has been described for one-pot multi-component synthesis of tetrahydrobenzo [b]pyrans known as 2-amino-7,7-dimethyl-5-oxo-4-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile which can be obtained from the reaction of substituted aromatic aldehydes, dimedone, malonitrile, in the presence of base such as potassium tertiary butoxide and THF in methanol as solvent at RT condition. All the compounds were examined by advanced spectroscopic data ( 1 H NMR, 13 C NMR and LCMS) and the structural determination was evaluated by elemental analysis. In addition to this, all the newly synthesized compounds were examined for their antibacterial activities and antifungal activity by disc diffusion method against the organism of Aspergillus niger and Candida ablicans L.
Seven 4-arylbenzelidene-2-((5-fluoro-1H-indol-1-yl)methyl)oxazol-5(4H)-one derivatives were synthesized by the condensation of 2-(2-(5-fluoro-1H-indol-1-yl) acetoamide) acetic acid, substituted aromatic aldehydes with acetic anhydride and sodium acetate in the presence of MgO/Al2O3 under reflux using nickel ferrite nanoparticles. Seven of the compounds are new derivatives. 2-(2-(5-fluoro-1H-indol-1-yl)acetoamide) acetic acid was obtained from 2-(5-fluoro-1H-indol-1-yl)acetyl chloride with lysine in the presence of NaOH and HCl in the ice cold solution. 2-(5-fluoro-1H-indol-1-yl)acetyl chloride can be prepared from 5-fluoro indole with chloroacetyl chloride in triethylamine and dichloromethane. The structures of the compounds were evaluated based on 1 H-NMR, 13 C-NMR and LC-MS and by elemental analysis. These compounds were screened by antioxidant as well as anti-microbial activity.
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