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一氧化氮供体N-芳基-N′-羟基胍类化合物的合成

Synthesis of N-Aryl-N′-Hydroxyguanidines,a New Class of NO Donors

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【Author】 SHI Wei-bing~1, WANG Wei-dong~2, LAI Yi-sheng~1, ZHANG Yi-hua~1* (1.Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China; 2.Tasly Group R&D Institute, Tianjin 300402, China)

【机构】中国药科大学新药研究中心；天士力集团研究院；中国药科大学新药研究中心江苏南京210009；天津300402；江苏南京210009；江苏南京210009；

【摘要】目的:改进新型一氧化氮供体N-芳基-N′-羟基胍的合成工艺。方法:以取代苯胺为起始原料,通过缩合、水解、肟化反应获得目标化合物。结果:肟化收率由文献报道的20%提高至40%,目标化合物的结构经IR、1HNMR和MS确证。结论:本合成工艺具有原料易得、操作简便、收率较高等优点,适合工业化生产。更多还原

【Abstract】 Objective: To improve the synthetic procedure of N-Aryl-N′-Hydroxyguanidines, a new class of NO donors. Methods: The target compound was synthesized using substituted aniline as starting material by condensation, hydrolysis and oximation. Results: The yield of oximation was increased from 20% to 40%. The structure of target compound was confirmed by IR, ~1HNMR and MS. Conclusion: In comparison with the method reported, this method increases the yield and simplifies the procedure. It is suitable for industrial manufacture, in which the starting material is available more readily.更多还原

【关键词】 N-芳基-N′-羟基胍；一氧化氮供体；取代苯胺；合成；
【Key words】 N-Aryl-N′-Hydroxyguanidines； NO donor； Substituted aniline； Synthesis；

【文献出处】药学进展 ,Progress In Pharmaceutical Sciences , 编辑部邮箱 ,2005年11期

【分类号】R914.5
【被引频次】1
【下载频次】274

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