The Synthesis Of Basic Violet5, Landiololhydrochloride, Trihaloisocyanuric Acids, And The Process Design Of Lamivudine

This paper is made up of the synthesis of basic Violet5, landiololhydrochloride,trihaloisocyanuric acids,and the process design of lamivudine.The first part is on the synthesis of Basic Violet 5,whose chemical name is 3-amino-7-dimethylamino-5-phenylphenazinium chloride.It mainly used for the dyeing cotton,silk,leather in early days,now drives extensive conduct and actions on electroplating.Considering the synthesis method of Basic Violet 5,we designed a simple and new one,which employed N,N-dimethyl-p-phenylenediamin dihydrochloride and aniline as raw materials,potassium dichromate and hydrochloric acid as oxidizing agent and afforded a higher yield. The craft is favorable for industrialization.The structure of the product was characterized by IR.The second part is on the synthesis of landiololhydrochloride,whose chemical name is benzenepropanoic acid,4-(2-hydroxy-3-((2-((4-morpholinylcarbonyl)amino)ethyl)amino)propoxy)-, (2,2-dimethyl-1,3-dioxolan-4-y1)methyl ester,(S-(R^*,R^*))-hydrochloride. Landiolol is a newly developed blockage for ultra-short-acting,high cardioselective adrenergicβ₁ antagonists(β₁ antagonists).It is mainly used to treat intra-operative tachyarrhythmias(atrial fibrillation,flutter or supraventricular tachycardia).We firstly design a new way which employed morpholine and bis(trichloromethyl)carbonate as raw materials,through Friedel-Crafts reaction, ammonolysis reaction to synthesize 4-[N-(2-Amino ethyl)carbamoyl]morpholine. Compared with literature,there were many merits in our method,such as simple craft,easy operation and high yield.In addition,we designed a new one,which employed(2S)-(+)-Glycidyl tosylate and 3-(4-Hydroxyphenyl)propionic acid ethyl ester as raw materials,through ring-opening reaction,ammonolysis,hydrolyzation, transesterification reaction to synthesize landiololhydrochloride,which needn't under an atmosphere of argon.The craft is favorable for industrialization.The third part is on the synthesis of trihaloisocyanuric acids,which comprise trichloroisocyanuric acid,tribromoisocyanuric acid and triiodoisocyanuric acid. Trihaloisocyanuric acids are efficient halogenating agents,due to their capability of halenium('X+')atoms transfer to unsaturated substrates.These trihaloisocyanuric acids are also very interesting from the green chemistry point of view,as they can introduce halogen atoms in organic compounds without using toxic and corrosive X₂ and also present good atom economy.In the thesis,we make sure a better craft condition,which employed cyanuric acid and halogen to synthesis trihaloisocyanuric acids.The craft is favorable for industrialization.The structures of the products were characterized by IR.The forth part is on the process design of lamivudine,whose chemical name is 2-deoxy-3-thiacytidine(2R-cis)-4-Amino- 1-[2-(hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidinone.Lamivudine is a synthetic nucleoside analogue for oral administration,which first form ally come to use for the clinical treatment of HBV.In this thesis,following the fundament of advanced technology, reliable craft,rational economy and optimal system,the design aimed at the resolution of the problem of production technology.The optimal condition of the influencing factors(material mixture ratio,reaction temperature and reaction time)in technological process was determined according to the experiment data in laboratory.