Synthesis Of Polyethylene Glycol And Its Derivatives

Polyethylene glycol is a class of compounds derived from ethylene glycol.It has the advantages of innocuity,without immunogenicity and antigenicity,good biocompatibility and low price,Polyethylene glycol can be coupled with a variety of drugs through covalent or noncovalent bonds,PEG-modified drugs can greatly increase the water solubility of drugs and increase the stability in the body,and extend the drug half-life.At present,there are few reports on the synthesis of polyethylene glycol,this dissertation aims to explore the new monodisperse polyethylene glycol and polyethylene glycol derivatives of synthetic methods,and design of polyethylene glycol as the hydrophilic side of the new material.The first part of the dissertation work on the synthesis of monodisperse polyethylene glycol method,to explore a new route and can be a real production process,and the route has a certain degree of universality.In addition,the synthesis of monodisperse polyethylene glycol amide derivatives has been explored,and a simple process has been developed to simplify the synthesis process and reduce the production cost of monodisperse polyethylene glycol amino derivatives.In the end,we also optimized the synthesis method of mPEG-NH2,and proposed a new mPEG-NH2 synthesis method based on Mitsunobu reaction.The method is simpler than that of traditional method,and the product quality has been greatly improved.In the second part of the dissertation,We designed two polyethylene glycol modified self-cleavable materials,all with mPEG-NH2 as hydrophilic side,with a number of carbonate and carbamate as the skeleton,and boron Acid ester and nitro as the trigger point.First,we studied the specific synthetic method of the lipophilic end of the compund,and explored the self-assembly of the two compounds in the water after the synthesis of the compound.In addition,we hope to explore its stability in the hydrogen peroxide environment and the reduction environment.