Overview[1][2]
Methoxy polyethylene glycol amine is an important type of modified polyethylene glycol. Modified PEG, also called modified polyethylene glycol, is a PEG modified with chemical modification groups or biologically active groups. In drug development research, in order to increase the half-life of protein or peptide drugs in the body, reduce immunogenicity, and increase the water solubility of the drug, activated polyethylene glycol is chemically coupled to proteins, peptides, small molecule organic drugs, and on liposomes.
Preparation[1]
Preparation of methoxypolyethylene glycolamine 2000
Dissolve 2g of monomethoxy polyethylene glycol azide 2000 in 20 mL of dry tetrahydrofuran, then add 0.2g of 10% palladium on carbon, replace the air in the reaction bottle with hydrogen, and react at 25°C for 24 hours. The reaction is complete. The palladium carbon was removed by suction filtration, the solvent was evaporated to dryness under reduced pressure, and purified by beating with anhydrous ether to obtain 1.8 g of product with a yield of 90.14%.
1H-NMR(M)δ＝3.65(3H,s),3.38(93H,J＝8Hz,d)
MS(EI):m/e＝2016.5
Preparation of methoxy polyethylene glycol azide 1000
Under the protection of nitrogen, mix 1.0g of monomethoxy polyethylene glycol 1000 and 0.53g of triphenylphosphorus. Dissolve 0.56g diphenyl phosphate azide in 10 mL of dry methylene chloride. Place the reaction bottle in a low temperature environment of 0°C and stir for a certain time until the temperature in the reaction bottle is lower than 5°C. Then slowly add azo 0.4g of diisopropyl diformate, keeping the temperature below 15°C during the dropwise addition. After the dropwise addition, the reaction system gradually changed from turbid to clear, and the color changed from light yellow to golden yellow. After 3 hours of reaction, the reaction was complete, and the volume was evaporated to dryness under reduced pressure to obtain a yellow oil, which was purified by beating with anhydrous ether to obtain 0.86 g of the product with a yield of 83.25%.
1H-NMR(CDCl3,M)δ＝3.62(3H,s),3.25(47H,J＝8Hz,d)
MS(EI):m/e＝1021.8
Apply[2-3]
CN201810706156 discloses a corrosion-resistant coating material for military sensors and a preparation method thereof. It solves the problem that waterproof coating materials for military components in the existing technology generally have poor corrosion resistance and are not suitable for acid and alkali corrosion. To solve the problem of short service life when used in the environment, the military sensors use corrosion-resistant coating materials, including the following raw materials: epoxy resin, polyester resin, vanadium pentoxide, methoxypolyethylene glycolamine, polyethylene glycol Alcohol 200, ceramic fiber, nano silicon carbide, lubricant. The invention has a scientific formula and rigorous proportions. The corrosion-resistant coating material for military sensors obtained has a wide temperature resistance range, can withstand temperatures of 75 to 150°C, has good moisture resistance, good corrosion resistance, long service life, and its preparation method is simple. , the preparation conditions are mild, easy for industrial production, and can be widely used.
CN201210384370.0 discloses a prodrug of oridonin A with polyethylene glycol as a carrier, and its preparation method is as follows: (1) Preparation of carboxylated oridonin A: oridonin A React with succinic anhydride to obtain carboxylated oridonin A; (2) Synthesis of oridonin A prodrug modified with methoxy polyethylene glycol amine: monomethoxy polyethylene glycol amine and carboxylation Rubescensine A reacts to obtain oridonin A prodrug in the form of a white solid. The prodrug of oridonin A with polyethylene glycol as a carrier uses succinic acid as a connecting arm to combine oridonin A with a hydrophilic polyethylene glycol derivative, thereby improving the effectiveness of oridonin A. The solubility of Rubescensine A enhances and improves the performance of the drug, increases the stability of Rubescensine A, and can decompose and fall off in an appropriate environment to release Rubescensine A, thereby improving its stability in the body. action time, thereby achieving the purpose of long circulation.
Main reference materials
[1][Chinese invention] CN201611055547.7 Preparation method of monomethoxy polyethylene glycol amine
[2]CN201810706156.X A corrosion-resistant coating material for military sensors and its preparation method
[3]CN201210384370.0 A prodrug of oridonin A with polyethylene glycol as a carrier and its preparation method
