Tetravalent platinum complex with anticancer activity, preparation method and application
A technology of tetravalent platinum and complexes, which is applied in anti-cancer, new tetravalent platinum complexes and its preparation, and anti-tumor applications, which can solve the problem of less combined work
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Embodiment 1
[0019] The preparation of embodiment 1 hydroxyplatinum (IV) compound A
[0020] Compound A:
[0021] Starting materials:
[0022] Add 3.21g of starting materials (synthesized with reference to the method in the prior art) and 80mL of distilled water to the flask, stir to disperse them, slowly add 130mL of hydrogen peroxide with a concentration of 30% to the reaction system, raise the temperature to 75°C and stir Reaction 4h. Stop the reaction, place it under cooling condition for crystallization for 12 hours, filter and separate to obtain a yellow solid, add appropriate amount of water, heat to dissolve it, cool and stand for crystallization for 12 hours, and filter to obtain white crystals.
Embodiment 2
[0023] The preparation of the monohydroxy platinum (IV) compound B that embodiment 2 carboxylate replaces
[0024] Compound B:
[0025] Add 1.7 g of compound A prepared in Example 1 and 0.38 g of acetic anhydride to a round-bottomed flask, add 70 mL of anhydrous DMSO under nitrogen protection, stir and react at 40°C for 4 days, evaporate DMSO under reduced pressure, add acetone, A white solid powder was precipitated, filtered by suction, washed 3 times with acetone to obtain a white solid product (1.5 g).
Embodiment 3
[0026] The synthesis of embodiment 3 target product 1
[0027]
[0028] Add 0.01 mol of compound B prepared in Example 2 and 0.02 mol of benzyl-protected galloyl chloride to the flask, protect with nitrogen and add anhydrous acetone, stir at room temperature for 12-36 hours, and stop the reaction. Acetone was removed by concentration, and the product was obtained by column chromatography. Dissolve the product in an appropriate amount of anhydrous dichloromethane, stir at -78°C for 15 minutes, slowly add 1M boron trichloride / dichloromethane solution dropwise to the reaction solution, continue stirring for 2 hours, and stop the reaction. The solvent was distilled off under reduced pressure, and the residual solid was washed three times with petroleum ether, and separated by column chromatography to obtain the target product, which was designated as compound 1.
[0029] The product is a light yellow solid; 1 H NMR (400MHz, DMSO-d 6 )δ9.21(s,2H),8.85(s,1H),7.02(s,2H),5.26-5....
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