摘 要

本文主要研究了氨基咪唑衍生物酰胺合成 4-羧酸乙酯-5氟咪唑的反应。研究内容分为三部分：

第一部分用廉价易得的4-氨基-5-咪唑甲酰胺制备4-羧酸乙酯-5-氨基咪唑。

第二部对氨基咪唑甲酸乙酯进行重氮化反应，制备4-羧酸乙酯-5-重氮咪唑。

第三部分在紫外光催化下合成4-羧酸乙酯-5氟咪唑。

研究结果初步验证了策略是可行的，且此反应条件温和，步骤简短。

本文主要亮点是原料廉价易得，底物容易合成。

关键词 ：氨基咪唑甲酸乙酯；紫外光催化；4-羧酸乙酯-5-氟咪唑。

Abstract

The thesis mainly focuses on ethyl 4-carboxylic acid-5-fluorimidazole from amino-imidazole derivatives amides was studied. The research content is divided into there parts:

The first part is to prepare ethyl 4-carboxylic acid -5-aminnimidazolate from 4-amino-5-imidazolamide,which ischeap and easycto obtain.

In the second part, ethyl 4-carboxylic acid-5-diazimidazole was prepared by diazotization of ethyl aminimidazolate formate.

In the third part, _\.4-carboxylic acid-5-fluoroidazole was synthesized under the catalysis of ultraviolet light.

The results show that the strategy is feasible,and the reaction conditions are mild and the step are brief.The main highlight of this paper is that the raw materials are cheap and easy to obtain,and the substrate is easy to synthesize.

Key Words：Ethyl aminimidazolate; UV catalysis; Ethyl 4-carboxylic acid-5-fluorimizole;

目 录

第1章 绪论.....................................................................................................................................1

1.1 氟元素性质简介....................................................................................................................1

1.2 咪唑及其衍生物的性质简介................................................................................................2

1.3 氨基咪唑类药物的氟化研究现状........................................................................................4

1.4 研究目的、内容以及意义....................................................................................................6

1.5合成策略.................................................................................................................................6

第2章 酰胺的酯化.........................................................................................................................9

2.1主要实验试剂与仪器.............................................................................................................9

2.2 酰胺的酯化............................................................................................................................9

第3章 4-羧酸乙酯-5-氨基咪唑的重氮化....................................................................................11

3.1 主要实验试剂与仪器...........................................................................................................11

3.2 4-羧酸乙酯-5-重氮咪唑的合成............................................................................................11

第4章 4-羧酸乙酯-5-重氮咪唑的氟化........................................................................................13

4.1 主要实验试剂与仪器...........................................................................................................13

4.2 4-羧酸乙酯-5-氟咪唑的合成................................................................................................14

第5章 总结....................................................................................................................................18

参考文献..........................................................................................................................................19

附录..................................................................................................................................................21

致谢..................................................................................................................................................23