Acta Scientiarum Naturalium Universitatis Pekinensis

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Synthesis of Some Esters of Acids Containing Nitrogen with Metronidazole

ZHAO Xianrui,LI Chongxi   

  1. College of the Chemistry and Molecular Engineering, Peking University, Beijing, 100871
  • Received:2001-05-23 Online:2002-03-20 Published:2002-03-20

含氮羧酸的羟乙基甲硝唑酯的合成

赵宪瑞,李崇熙   

  1. 北京大学化学与分子工程学院,北京,100871

Abstract: In order to find replacer for Metronidazole and drug selection. Some diesters or esters of acids containing nitrogen with Metronidazole were designed and synthesized, which have difference in water-solubility. Metronidazole was reacted with the corresponding amino or imino multi-carboxylic acid compounds in the presence of acetic anhydride or thionyl chloride or DCC. The intermediate of nitrilotriacetic acid with Ac2O was identified by Mass Spectrum. Out of three diesters two are novel.

Key words: Metronidazole, amino carboxylic acid, amino acid, diester

摘要: 为寻找羟乙基甲硝唑的替代物,分别采用酸酐法、酰氯法或DCC法,将氨基羧酸与羟乙基甲硝唑反应,得到5个亲水性不同的单酯或二酯,用MS谱确证了次氨基三乙酸与乙酸酐反应的中间物,并对得到的酯的1H-NMR谱进行了初步研究。3个二酯中,有2个未见文献报道。

关键词: 羟乙基甲硝唑, α-氨基羧酸, 氨基酸, 二酯

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