Synthesis and antitumor activities of novel 2-substituted pyrimidinone-5-carboxylic acid benzylamides

• 来源期刊: 中国高等学校学术文摘·化学
• 关键词: pyrimidinone synthesis antitumor
• 年，卷（期）: 2007,（2）
• 页码范围: 127-130
• 页数: 4页
• 语种: 英文

摘要

The title compounds were synthesized via Nbenzylmalonamic acid methyl ester (3).As the key intermediate,3 was prepared from methyl malonyl chloride and benzylamine.Then,compound 3 was reacted with dimethylformamide dimethyl acetal yielding vinylogue amides 4 and 5.Isomers 4 and 5 were respectively treated with amidine and guanidine to afford the title compounds 2-substituted pyrimidinone-5-carboxylic acid benzylamides 6 and 7.All of the new compounds were characterized by 1H-NMR(nuclear magnetic resonance),13C-NMR,MS and High Resolution Mass Spectrometer (HRMS).The antitumor activities of the compounds were tested in vitro against LoVo cells and Hep3B cells.Both compounds 6 and 7 show activity against these two cell lines.