A simple and efficient solvent-free method was developed for the acetylation of alcohols, phenols and amines in excellent yields employing glycerol-based sulfonic acid (SO 3 H) functionalized carbon catalyst under environmentally benign reaction conditions. The salient features of this protocol are the short reaction time, ease of product isolation and reusability of the carbon catalyst.
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In continuation of our efforts to find new antimicrobials, herein we report the synthesis of various pyrazole, pyrazoline, and pyridine based novel bioactive heterocycles (3a-t). Newly synthesized compounds analysed for their antimicrobial activity. Compounds 3c, 3h, 3i, 3k, 3n, and 3q were showed significant antimicrobial activity. Molecular docking study for the most active analogues DNA gyrase subunit b (PDB ID: 1KZN) corroborated well with observed antimicrobial potency exhibiting significant binding affinity. For the interpretation of the chemical structures reported in this paper were based on IR, 1H NMR, 13C NMR, and mass spectral data.
A variety of aldehydes undergo smooth coupling with N-tosyltryptamine in the presence of carbon−SO3H in ethanol at 80 °C to furnish the corresponding tetrahydro-β-carbolines in excellent yields with high selectivity. The coupling of tryptamine with isatins affords the respective spiro-tetrahydro-β-carbolines in good yields. The use of a recyclable solid acid catalyst makes this method simple, convenient, and cost-effective.
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