| 新型2-取代嘧啶酮-5-甲酰苄胺的合成及抗肿瘤生物活性试验 |
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| 引用本文： | 陈卫民,冯金,涂洪谊.新型2-取代嘧啶酮-5-甲酰苄胺的合成及抗肿瘤生物活性试验[J].化学通报,2006,69(8):623-626. |
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| 作者姓名： | 陈卫民 冯金 涂洪谊 |
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| 作者单位： | 暨南大学药学院药物化学教研室，第一军医大学药物研究所广州510515，暨南大学药学院药物化学教研室，第一军医大学药物研究所 广州510632，广州510632，广州510515 |
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| 基金项目： | 广东省自然科学基金;暨南大学校科研和教改项目 |
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| 摘 要： | 以丙二酸单甲酯单甲酰氯、苄胺为起始原料,经与DMF-DMA反应后形成的关键中间体分别与胍或脒缩合关环,合成了2-取代嘧啶酮-5-甲酰苄胺化合物6和7。产物经1HNMR、13CNMR、MS、HRMS进行了结构表征。初步的生物活性试验显示化合物6和7具有抗肿瘤活性。
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| 关 键 词： | 嘧啶酮 合成 抗肿瘤 |
| 收稿时间： | 2006-01-04 |
| 修稿时间： | 2006-01-042006-03-29 |
Synthesis and Antitumor Activities of Novel 2-Substituted Pyrimidinone-5-carboxylic Acid Benzylamides |
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| Chen Weimin,Feng Jin,Tu Hongyi.Synthesis and Antitumor Activities of Novel 2-Substituted Pyrimidinone-5-carboxylic Acid Benzylamides[J].Chemistry,2006,69(8):623-626. |
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| Authors: | Chen Weimin Feng Jin Tu Hongyi |
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| Institution: | 1.Department of Medicinal Chemistry, School of Pharmacy, Jinan University, Guangzhou 510632; 2 .Institute of Pharmaceutical Sciences, The First Military Medical University, Guangzhou 510515 |
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| Abstract: | Title compounds were synthesized via N-benzyl-malonamic acid methyl ester (3) as key intermediate, which was prepared starting from methyl malonyl chloride and benzylamine. Then 3 reacted with dimethylformamide dimethyl acetal yielded vinylogue amides 4 and 5. While isomers 4 and 5 reacted with amidine and guanidine respectively, target 2-substituted pyrimidinone-5-carboxylic acid benzylamides 6 and 7 were obtained. All the compounds were identified by 1H NMR, 13 C NMR, MS and HRMS. The results of the test of anticamcer activities indicated that both compoands 6 and 7 show some antitumor activities. |
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| Keywords: | Pyrimidinone Synthesis Antitumor |
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