抗溃疡剂佐利米定及其含氟衍生物的合成研究  

Study on the synthesis of antiulcer agent Zolimidine and its fluorinated derivatives

作　　者：朱雪 付鑫磊 余树琴 陈才博 李镇霖 郭小华 杨凯 ZHU Xue;FU Xin-ei;YU Shu-qin;CHEN Cai-bo;LI Zhen-in;GUO Xiao-hua;YANG Kai(School of Pharmacy,Gannan Medical University,Ganzhou,Jiangxi 341000)

机构地区：[1]赣南医科大学药学院,江西赣州341000

出　　处：《赣南医科大学学报》2024年第11期1126-1131,共6页JOURNAL OF GANNAN MEDICAL UNIVERSITY

基　　金：江西省高等学校大学生创新创业训练计划项目(S202310413008);江西省科技厅自然科学基金面上项目(20224BAB203010)。

摘　　要：目的:探究抗溃疡剂佐利米定及其含氟衍生物的合成方法。方法:以2-氨基吡啶和2-溴-1-(4-甲磺酰基)苯乙酮为原料合成佐利米定,再分别与三氟乙醛水合物、三氟丙酮酸酯和二氟乙醛缩半乙醇反应,合成相应的含氟衍生物。结果:设计合成了佐利米定及其含氟衍生物,目标化合物经^(1)H NMR、^(13)C NMR、^(19)F NMR和高分辨质谱确证。结论:佐利米定及其含氟衍生物的合成方法具有工艺简单、产率高和操作方便等优点。Objective:To explore the synthesis of the antiulcer agent Zolimidine and its fluorinated derivative.Methods:Zolimidine was synthesized from 2-aminopyridine and 2-bromo-1-(4-methanesulfonyl)acetophenone,and then reacted with trifluoroacetaldehyde hydrate,trifluoromethylacetone esters,and difluoroacetaldehyde ethyl hemiacetal to synthesize corresponding fluorinated derivatives.Results:Zolimidine and its fluorinated derivatives were synthesized.The chemical structures of the target compounds were confirmed by ^(1)H NMR,^(13)C NMR,^(19)F NMR and HR-MS.Conclusion:The synthesis methods of Zolimidine and its fluorinated derivatives has the advantages of simple process,high yield,and convenient operation.

关 键 词：佐利米定 有机合成 含氟化合物 

分 类 号：R284.3[医药卫生—中药学]