摘要
目的通过合成新的金刚烷甲酰肼衍生物,发现新型抗流感病毒药物。方法以金刚烷甲酸为原料,与甲醇反应得到金刚烷甲酸甲酯(1),再与水合肼经酰化反应合成金刚烷甲酰肼(2)。金刚烷甲酰肼与氯乙酰氯酰化反应得到N-(氯乙酰基)-金刚烷甲酰肼(3),最后将N-(氯乙酰基)-金刚烷甲酰肼(3)与芳胺或1-苯乙胺通过亲核取代反应生成金刚烷甲酰肼衍生物(Ⅰ~Ⅴ)。结果合成了5个未见文献报道的金刚烷甲酰肼衍生物,其结构经ESI-MS谱图确证。结论该研究为抗流感病毒药物开发提供基础。
OBJECTIVE To search for novel anti-influenza virus drugs by the synthesis of adamantane formylhydrazine derivatives. METHODS Adamantane formic acid was treated with methanol to obtain adamantane methyl formate（ 1）,then 1 reacted with hydrazine hydrate to gain adamantane formylhydrazine（ 2）. N-（ chloride-acetyl）-adamantane formylhydrazine（ 3） was synthesized from 2 and chloroacetyl chloride. Finally,the target compounds,namely derivatives of adamantane formylhydrazine（ Ⅰ ~ Ⅴ） were obtained by using 3 and anilines or 1-phenethylamine through nucleophilic substitution. RESULTS Five novel target compounds were synthesized and their structures were confirmed by ESI-MS spectra. CONCLUSION The study provides the foundation for the development of anti-influenza virus drugs.
作者
刘丹
关月月
孙卓
张淑曼
王然
LIU Dan;GUAN Yueyue;SUN Zhuo;ZHANG Shuman;WANG Ran(Faculty of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang , Liaoning 110142, China)
出处
《今日药学》
CAS
2018年第3期148-149,158,共3页
Pharmacy Today
基金
辽宁省大学生创新创业训练计划(201610149010)
关键词
金刚烷甲酸
金刚烷甲酰肼衍生物
抗流感病毒
adamantane formic acid
derivatives of adamantane formylhydrazine
anti-influenza virus
