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| 含1,3,4-噻二唑二氢嘧啶类衍生物的合成 |
| Synthesis of Dihydropyrimidine Derivatives Containing 1,3,4-Thiadiazole |
| 投稿时间：2024-04-11 修订日期：2024-05-05 |
| DOI： |
| 中文关键词: 1,3,4-噻二唑 二氢嘧啶 硫代卡巴肼 合成 |
| 英文关键词: 1,3,4-Thiadiazole, Dihydropyrimidine, thiocarbohydrazide, Synthesis |
| 基金项目:湖南省自然科学基金(2024JJ7176); 湖南省教育厅重点项目(22A0348) |
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| 中文摘要: |
| 二氢嘧啶类衍生物具有广泛的生物活性，因此对其新型衍生物的合成进行研究具有重要意义。本文以芳香醛、乙酰丙酮、硫脲为原料，通过Biginelli反应，合成中间产物4-甲基-6-芳基-5-乙酰基-2-巯基-1,6-二氢嘧啶1。以浓盐酸为催化剂，将中间体1与硫代卡巴肼反应得到化合物1-(4-甲基-6-芳基-2-巯基-1,6-二氢嘧啶-5-基)乙酮硫代卡巴腙2。以冰乙酸为催化剂，将化合物2与原甲酸三乙酯进行缩合反应合成了一系列新型含134-噻二唑二氢嘧啶衍生物。产物结构经 IR, 1H NMR, 13C NMR 和ESI-MS进行表征. |
| 英文摘要: |
| Abstract: Abstract: Dihydropyrimidine derivatives have a wide range of biological activities, so it is of great significance to study the synthesis of their new derivatives. Using aromatic aldehydes, acetylacetone,
and thiourea as raw materials, the intermediate product 1 4-methyl-6-aryl-5-acetyl-2-mercapto-1,6-
dihydropyrimidine was synthesized through the Biginelli reaction. The intermediate product 21- (4-methyl-6-aryl-2-mercapto-1,6-dihydropyrimidin-5-yl) ethanone thiocarbazone was achieved via the reaction of compound 1 with thiocarbohydrazide in the presence of catalyst concentrated hydrochloric acid. A series of novel dihydropyrimidine derivatives containing 1,3,4-thiadiazole were synthesized by condensation reaction of compound 2 with triethyl orthoformate using acetic acid as a catalyst. The structures of the products were characterized by IR, ESI-MS, 1H NMR, 13C NMR, HSQC, and HMBC. |
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