Abstract

A facile and highly efficient one-pot three-component synthesis of chromene pyrimidine-2,4-dione derivatives from available substrates catalyzed by heteropoly acid (H₃PW₁₂O₄₀) is described. In this protocol, the reaction of diverse aldehydes, 4-hydroxycoumarin, and 4-amino-1,3-dimethyluracil in the mixture of EtOH / H₂O (1:2) at room temperature in the presence of heteropoly acid (H₃PW₁₂O₄₀) as a highly efficient catalyst affords the corresponding chromene pyrimidine-2,4-dione in good to excellent yields. Operational simplicity, low cost, eco-friendly with the environment, easy workup and purification, short reaction time, high yield of products, green media of the reaction and mild conditions are the advantages of this method. The in vitro antibacterial activities of title compounds were obtained against Escherichia coli (ATTC 35218) and Staphylococcus aureus (ATCC 6538) as Gram-negative and Gram-positive bacteria, respectively, and their activities were compared to gentamycin and penicillin as reference drugs.

Graphic abstract

中文翻译：

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一锅三组分反应可轻松，高效地绿色合成亚甲基嘧啶-2,4-二酮衍生物及其抗菌活性

摘要

描述了一种由杂多酸（H ₃ PW ₁₂ O ₄₀）催化的可利用的底物容易且高效的一锅三组分合成亚甲基嘧啶-2，4-二酮衍生物的方法。在此方案中，在杂多酸（H _3）存在下，室温下EtOH / H ₂ O（1：2）混合物中的各种醛，4-羟基香豆素和4-氨基-1,3-二甲基尿嘧啶的反应PW ₁₂ O ₄₀）作为高效催化剂以良好至优异的产率提供相应的色烯嘧啶-2,4-二酮。该方法的优点是操作简单，成本低，对环境友好，后处理和纯化容易，反应时间短，产物产率高，反应的绿色介质和温和的条件。获得了标题化合物对革兰氏阴性和革兰氏阳性菌分别对大肠杆菌（ATTC 35218）和金黄色葡萄球菌（ATCC 6538）的体外抗菌活性，并将它们的活性与庆大霉素和青霉素作参比药物进行了比较。

图形摘要