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A Comparison Between Suzuki Cross-Coupling Reaction and Direct Arylation in the Synthesis of New Antibacterial Imidazo-Pyrazines/Pyridazines Publisher



Salek Soltani S1 ; F Farnia SM1 ; Foroumadi A2, 3
Authors

Source: Journal of Heterocyclic Chemistry Published:2020


Abstract

Two efficient synthetic routes to preparation of 2,3-diarylimidazo[1,2-a]pyrazines and 2,3-diarylimidazo[1,2-b]pyridazines are described. The procedures involve a Suzuki cross-coupling reaction and a palladium-catalyzed direct arylation at position 3 and finally a comparative study is achieved. The antibacterial activities of the synthesized compounds in vitro were measured and the results showed that most products presented moderate to good antibacterial activities. Compounds 3a, 3c, 3j, 3k, 3l, and 3n revealed obvious potency against Staphylococcus aureus, Bacillus subtilis, and Escherichia coli with minimum inhibitory concentration values of 32 μg/mL, which were better compared with the others. © 2020 Wiley Periodicals, Inc.
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