Study On Synthesis Of Amphiphilic Polymers Containing Methoxypolyethylene Glycols And This Amphiphilic Polymers For Delivery Of Poorly Water-soluble Drugs

The content of my research is divided into the following three parts:1. Synthesis and Characterization of Amphiphilic Polymers Containing Methoxypolyethylene GlycolsNowadays research focus in the pharmaceutical workers is to find the dosage form for delivery of poorly water-soluble drugs. Solid dispersion method is one of the most development space and prospects among solubilization methods, and the principle of this method is suppressing drug crystallization and using surfactant system to form of inclusion compound to improve the drug dissolution rate and water soluble. But all kinds of carrier dispersion are each have advantages and disadvantages. Amphiphilic polymers has been used in many disciplines,such as chemical, petroleum, medicine, materials and life science, etc. In the field of biomedical,amphiphilic polymers containing polyethylene glycol (PEG) has a great application in drug solubilization, sustained release and drug targeting carrier direction. This subject adopts esterification method for macromolecular monomer containing carboxyl in advance, and then the polymerization of this macromolecular monomer in Re-Dox system gets a series of functional amphoteric polymer.2. Study on Amphiphilic Polymers Containing mPEG 5000 for Delivery of Poorly Water-Soluble DrugsAbout 40% of works in new drug research and development at present stage is to try to improve the drug solubility. Amphoteric molecules as solid dispersion carrier is trendy in recent years of research. Mirabegron and topiroxostat are new type of first choice in treatment of bladder activities and gout drug respectively, The two drugs have good treatment effect and less adverse reaction, but at the same time, the solubility of the two drugs are very poor. This topic screens experiment to obtain the corresponding appropriate proportion of the two kinds of solid dispersions with homemade amphiphilic polymer containing polyethylene glycol monomethyl ether as dispersing carrier and mirabegron and topiroxostat as drug model, and results the solvent limit of Mirabegron increased from 55% to 55%, the dissolution limit of topiroxostat increased from 32% to 85%.3. Study on Copper-Promoted Direct C-H Amination of 1, 3-thiazolesThe construction of carbon-nitrogen bond of heteroaromatic compounds is a highly important transformation in the chemical synthesis. This kind of skeleton unit has great application prospect in biology, medicine and material sciences and so on, constituting the basic framework of many natural medicines and advanced materials. The traditional coupling method is difficult to overcome the disadvantages of organic waste, poor atomic economy, environmental pollution and so on. Transition metals, especially palladium, copper, iron, etc., high chemical selectively catalyzed C-H bond directly functional groups of constructing C-N bond to synthesis of amino-heteroaromatic compounds has been developed gradually in organic synthesis and has been applied more and more. In this study, copper-promoted direct C-H amination of benzothiazoles for synthesis of 2-aminothiazoles using formamides as nitrogen sources. Studies on the coupling reaction of heteroaromatic compounds and amide compounds provide a more novel, highly selective and efficient catalytic system.