Compound containing tauzaserti structure and its preparation method and use
A technology of tauzaserti and compounds, which is applied in the fields of compounds containing tauzaseri structures and their preparation and application, can solve problems such as loss of vision function and poor effect, and achieve easy dissolution, excellent effect, and drug treatment effect Good results
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Embodiment 1
[0031] 1) The mixture of 50 g of sebacic acid in 500 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;
[0032] 2) 6.5g of methoxypolyethylene glycol amine, 68mg of citric acid, 160mg of dicyclohexylcarbodiimide and 8.2mg of pyridine were mixed and added into 32ml of dichloromethane, stirred at room temperature overnight; then washed with ether, and Drying at lower temperature, obtains polymkeric substance;
[0033] 3) Mix the products of step 1) and step 2) into a flask, and conduct a solution polymerization reaction under reduced pressure at 180°C for 1 hour; when the polymer is cooled to room temperature, it is dissolved in chloroform, washed with petroleum ether and dried;
[0034] 4) Put 200mg of Tauzarasete and 800mg of the polymer in step 3 into 10ml of dimethyl sulfoxide and 10ml of dichloromethane solution for 48 hours; ultrasonic for 5 minutes; then put it in an oven for 1 hour; Stir in a homogenizer at 20°C for 3 minutes at ultra-high speed, then put ...
Embodiment 2
[0036] 1) Mix 3 g of methoxypolyethylene glycol amine, 45 mg of citric acid, 200 mg of dicyclohexylcarbodiimide and 6 mg of pyridine, add 20 ml of methylene chloride, stir overnight at room temperature; then wash with ether and dry under vacuum ;
[0037] 2) Mix 20 g of acetyl-sebacic acid (commercially available) and the product of step 1 into a flask, and react at 170°C for 1.5 hours; the polymer is cooled to room temperature and dissolved in chloroform, washed with petroleum ether and dried to obtain Polymer (the structure may be slightly different from the self-made one, and the molecular weight may be different due to commercial quality);
[0038] 3) Put 30mg of Tauzatase and 150mg of the polymer into a solution mixed with 1ml of methanol and 1ml of dichloromethane; ultrasonic for 2 minutes; then put in an oven for 24 hours; at minus 10-20 degrees, homogeneous The product was stirred at high speed for 2 minutes, and the product was put into 3% cholic acid solution and st...
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