Synthesis of C(5)-(p-Toluoyl substituted)-3,4-dihydropyrimidinones (or -thiones) via Biginelli Reaction Promoted with Microwave Irradiation under Solvent-Free Conditions

被引：4
|
作者：
Li, Li [1 ]
Liu, Qingjian [1 ]
Sui, Xueyan [1 ]
机构：
[1] Shandong Normal Univ, Coll Chem Chem Engn & Mat Sci, Jinan 250014, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2014年 / 34卷 / 08期
关键词：
Biginelli reaction; 3,4-dihydropyrimidin-2(1H)-ones (or -thiones); beta-diketone; microwave irradittion; ADRENOCEPTOR-SELECTIVE ANTAGONISTS; ONE-POT SYNTHESIS; DESIGN; METABOLITES;
D O I：
10.6023/cjoc201402018
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
The Biginelli reaction, which involves the one-pot acid catalyzed cyclocondensation of ethyl acetoacetate, urea, and arylaldehyde, was first discovered by Italian chemist Pietro Biginelli about 120 years ago. A large number researchers have shown persistent attention to the study of Biginelli reaction on account of its significant biological and pharmaceutical activities and diversity of structural changes of dihydropyrimidines (DHPMs) and its derivatives. Herein, the synthesis of C(5)-(p-toluoyl)-3,4-dihydropyrimidin-2(1H)-ones (or -thiones) via Biginelli reaction has been accomplished from aldehydes, p-toluoylacetone, and urea or thiourea in the presence of TsOH promoted with microwave irradiation under solvent-free conditions in good yields and high purity without chromatographic separation.
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收藏
页码：1669 / 1672
页数：4
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