Green Proess For The Preparation Of Drugs Of Guanidines

Guanidines R₁HNC(=NR₂)NHR3 (R₁,R₂,R₃=H,Alkyl or Aryl) areparts of arginine residues which play an important part in biologicallyactive proteins and peptides. Many of them have biological activities,such as effects on the nervous system, with anti-virus, anti-tumor, anti-AIDS effect. But the proesses for the preparation of drugs of guanidineshave been reported still exist some problems such as high polluton toenvironment or complex routes. Thus the preparation of guanidines withhigh yield and low-pollution to environment under mild conditions haveimportant meaning .This dissertation consisted of four chapters. In the first chapter, wesimply outlined the progress of applications of guanidines. The rest ofthree chapters have studyed three guanidine drugs including Agmatinesulfate, Hydroxyguanidine sulfate and Creatine ethyl ester hydrochloride. We designed three green routes to prepare these guanidines.The main place of innovation of this paper is that we choose O-Methylisourea hemisulfate as an agent of guanidination. And compared toother methods , the advantages of our present procedures are mildreaction condition, simple operation, so they can be considered of goodprospect for industrial application.