A One-pot Multi-component Synthesis of some New Dihydropyrimidine Derivatives via Biginelli Condensations

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引用次数: 0

Abstract

The Biginelli Reaction is a one-pot acid catalyzed cyclocondensation of -keto ester, urea and aromatic aldehyde which leads to the synthesis of functionalized 3,4-dihydro-2(H)-pyrimidinones (DHPMs). These DHPMs (synthetic and natural) possess a wide range of pharmacological activities. A simple, efficient, and cost-effective method for the synthesis of 3,4-dihydropyrimidin-2(1H)-one by a one-pot three-component cyclocondensation reaction of a 1,3-dicarbonyl compound, an aldehyde and urea using HCl as catalyst is reported. The three-component condensation of an aldehyde, a -keto ester and urea in the presence of a catalytic amount of HCl, 3,4-Dihydropyrimidin-2(1H)-ones were synthesized in high yields. Recently much attention has been devoted towards dihydropyrimidine derivatives due to their significant therapeutic and medicinal properties. All the products in reaction obtained in good to very good yields by proceeding through a simple and efficient procedure. All the synthesized compound’s structure has been established by advanced spectroscopic data (FTIR, 1HNMR, and 13CNMR) and evaluated for their antibacterial activity against two types of bacteria (S. aureus and E.coli).
Biginelli缩合一锅多组分合成一些新的二氢嘧啶衍生物
Biginelli反应是一锅酸催化-酮酯、尿素和芳香醛的环缩合反应,可合成功能化的3,4-二氢-2(H)-嘧啶酮(DHPMs)。这些dhpm(合成的和天然的)具有广泛的药理活性。报道了一种简单、高效、经济的方法,以1,3-二羰基化合物、醛和尿素为催化剂,通过一锅三组分环缩合反应合成3,4-二氢嘧啶-2(1H)- 1。在一定催化量的盐酸存在下,合成了醛、酮酯和尿素的三组分缩合反应,收率高。近年来,由于二氢嘧啶衍生物具有重要的治疗和药用特性,引起了人们的广泛关注。通过一个简单而有效的程序,所有的反应产物都得到了很好的收率。通过FTIR、1HNMR和13CNMR等先进的光谱数据确定了化合物的结构,并对金黄色葡萄球菌和大肠杆菌两种细菌进行了抑菌活性评价。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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