一锅法合成5-氨基咪唑类衍生物  

Synthesis of 5-Aminoimidazole Derivatives by One-Pot Method

作　　者：章潮军 陈彩萍 王小平 徐作武 吴春雷[3,4] ZHANG Chaojun;CHEN Caiping;WANG Xiaoping;XU Zuowu;WU Chunlei(Zhejiang Changhai Medicine Co.,Ltd.,Shaoxing,Zhejiang 312000,China;Zhejiang Keming Biomedicine Co.,Ltd.,Shaoxing,Zhejiang 312000,China;College of Chemeal Engineering,Shaoxing University,Shaoxing Zhejiang 312000,China;Zhejiang Engineering Research Center of Fat-soluble Vitamin,Shaoxing,Zhejiang 312000,China)

机构地区：[1]浙江昌海制药有限公司,浙江绍兴312000 [2]浙江可明生物医药有限公司,浙江绍兴312000 [3]浙江绍兴文理学院化学化工学院,浙江绍兴312000 [4]脂溶性维生素浙江省工程研究中心,浙江绍兴312000

出　　处：《浙江化工》2023年第8期23-27,共5页Zhejiang Chemical Industry

摘　　要：目的:合成多取代的5-氨基咪唑类衍生物。方法:以对甲苯磺酰基甲基异腈、取代苯胺与二硫化碳为原料,三分子“一锅法”反应制备5-氨基咪唑类衍生物;以单因子法对反应条件进行筛选。结果:对甲苯磺酰基甲基异腈、取代苯胺与二硫化碳三者以1:1.2:1.5(摩尔比)投料,NaOH为催化剂,乙醇为溶剂,80℃下搅拌反应得到5-氨基咪唑类衍生物,收率为63%~82%,产物经1H NMR和13C NMR表征。结论:该“一锅法”合成方法具有原料廉价易得、反应操作简便等优点。Objective:Synthesis of polysubstituted 5-aminoimidazole derivatives.Methods:5-aminoimidazole derivatives were prepared by three-molecule"one-pot method"reaction using p-toluenesulfonylmethyl isonitrile,substituted aniline and carbon disulfide as raw materials;The reaction conditions were screened by a one-factor method.Results:p-Toluenesulfonylmethyl isocyanide,substituted aniline and carbon disulfide were fed at 1:1.2:1.5(molar ratio),NaOH was used as catalyst,ethanol was used as solvent,and 5-aminoimidazole derivatives were obtained by stirring reaction at 80°C,with a yield of 63%~82%,and the products were characterized by 1H NMR and 13C NMR.Conclusion:The"one-pot method"synthesis method has the advantages of cheap and easy availability of raw materials and simple reaction operation.

关 键 词：5-氨基咪唑 一锅法合成 氢氧化钠 对甲苯磺酰基甲基异腈 二硫化碳 

分 类 号：O626.23[理学—有机化学] TQ460.1[理学—化学]