A kind of pyrazolopyrimidine derivative, its preparation method and its application in medicine preparation
A technology of azolopyrimidine and derivatives, which is applied in the field of pyrazolopyrimidine derivatives and their preparation, to achieve the effects of inhibiting proliferation and significant targeted therapy
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Embodiment 1
[0024] (1) Add 4-amino-2-fluorophenol (6.4g, 50mmol) and sodium hydroxide (0.80g, 50mmol) to 100mL of water, stir at room temperature for 30 minutes, then add potassium carbonate (7.2g, 52mmol), and The temperature was raised to 60°C, and the tetrahydrofuran solution of 4-chloro-6,7-dimethoxyquinazoline (13.5g, 60mmol) was slowly added to the above reaction solution, and the reaction was stopped after 2 hours, and the tetrahydrofuran solution of the reaction system was After evaporating to dryness, the remaining system was extracted twice with ethyl acetate and water, and the ethyl acetate layer was dried with anhydrous magnesium sulfate and then spin-dried to obtain 4-(6,7-dimethoxyquinazolin-4-oxyl) -3-fluoroaniline (8.9g, 28mmol);
[0025] (2) Dissolve 3-amino-5-tert-butylisoxazole (4.2g, 30mmol) in 150mL of tetrahydrofuran, slowly drop into the solution of triphosgene (9g, 30mmol) in tetrahydrofuran, and continue stirring for 2h after the drop is complete. Add 25g of pota...
Embodiment 2
[0028] (1) Add 4-amino-2-fluorophenol (6.5g, 51mmol) to 120mL of acetonitrile, stir and dissolve at room temperature, then add triethylamine (15.2g, 150mmol), while raising the temperature to 60°C, and 4- The acetonitrile solution of chloro-6,7-dimethoxyquinazoline (13.5g, 60mmol) was slowly added to the above reaction solution, and the reaction was stopped after 3 hours. After the acetonitrile in the reaction system was evaporated to dryness, the remaining system was washed with ethyl acetate Esters and water were extracted twice, and the ethyl acetate layer was dried with anhydrous magnesium sulfate and then spin-dried to give 4-(6,7-dimethoxyquinazolin-4-oxyl)-3-fluoroaniline (7.9g, 25mmol);
[0029] (2) Dissolve 3-amino-5-tert-butylisoxazole (4.2g, 30mmol) in 150mL of acetonitrile, slowly drop it into triphosgene (9g, 30mmol) in acetonitrile, and continue stirring for 2h after dropping. Add 19g of triethylamine to the reaction solution, then add 4-(6,7-dimethoxyquinazolin...
Embodiment 3
[0032] (1) Add 4-amino-2-fluorophenol (6.5g, 51mmol) into 100mL of ethyl acetate, stir and dissolve at room temperature, add diisopropylethylamine (19.4g, 150mmol), and raise the temperature to 60°C , and the ethyl acetate solution of 4-chloro-6,7-dimethoxyquinazoline (13.5g, 60mmol) was slowly added to the above reaction solution, the reaction was stopped after 2 hours, extracted twice with water, ethyl acetate The ester layer was dried with anhydrous magnesium sulfate and then spin-dried to give 4-(6,7-dimethoxyquinazolin-4-oxyl)-3-fluoroaniline (9.1g, 29mmol);
[0033](2) Dissolve 3-amino-5-tert-butylisoxazole (4.2g, 30mmol) in 150mL of dichloroethane, and slowly drop it into the dichloroethane of triphosgene (9g, 30mmol). Stirring was continued for 2h. Add 24g of diisopropylethylamine in the reaction solution, then add 4-(6,7-dimethoxyquinazoline-4-oxyl group)-3-fluoroaniline (9.1g, 29mmol), at 80 The reaction was stopped after 8 hours at reflux at °C. Spin-dry dichloro...
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