Magnesium Powder-Catalyzed, Highly Efficient, Solvent-Free Synthesis of Amides through N-Acetylation of Amines and their Antibacterial Activity

Q4 Chemistry Asian Journal of Chemistry Pub Date : 2024-03-30 DOI:10.14233/ajchem.2024.31196
Najma Bajracharya, Sunita Shrestha, G. B. Bajracharya
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Abstract

Magnesium powder was found to be an efficient catalyst for the acetylation of amines (1) with Ac2O affording corresponding amides (2) in excellent yields (> 99%). This green synthetic protocol has utilized 2.5 mol% of magnesium powder and a stoichiometric amount of Ac2O (1.2 equiv.). Amides 2a-k were synthesized within a short reaction time (2-3 min) at an ambient temperature under solvent free condition. The products were screened against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus epidermidis bacterial strains. N-(2-Hydroxyphenyl)acetamide (2f) was found most active against Gram-positive S. aureus and S. epidermidis indicating its efficacy in treating skin diseases.
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镁粉催化下通过胺的 N-乙酰化无溶剂高效合成酰胺及其抗菌活性
研究发现,镁粉是用 Ac2O 对胺(1)进行乙酰化的高效催化剂,能以极高的产率(> 99%)生成相应的酰胺(2)。这一绿色合成方案使用了 2.5 摩尔% 的镁粉和等量的 Ac2O(1.2 等量)。酰胺 2a-k 是在无溶剂的环境温度下,在很短的反应时间(2-3 分钟)内合成的。针对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和表皮葡萄球菌等细菌菌株对产品进行了筛选。结果发现,N-(2-羟基苯基)乙酰胺(2f)对革兰氏阳性的金黄色葡萄球菌和表皮葡萄球菌最有效,这表明它在治疗皮肤病方面的功效。
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来源期刊
Asian Journal of Chemistry
Asian Journal of Chemistry 化学-化学综合
CiteScore
0.80
自引率
0.00%
发文量
229
审稿时长
4 months
期刊介绍: Information not localized
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