Taxol prodrug using polyethylene glycol as carrier as well as preparation method and chemical modifier thereof
A technology of polyethylene glycol and paclitaxel, which is applied in the field of chemical modifiers, can solve problems such as limited drug loading, and achieve the effects of improving performance, increasing stability, and improving solubility
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Embodiment 1
[0033] 1. Preparation of mPEG5000 carboxylate
[0034] Dissolve 10g of vacuum-dried mPEG5000 in 100ml of sodium-metal-dried 1,4-dioxane, add sodium metal cut into filaments, and stir magnetically for about 24 hours until no bubbles are released. After standing for 24 hours, use G 4 Filter under reduced pressure on a sand core funnel, and concentrate the filtrate to 20-30ml. Add 0.2g KI as a catalyst, add 6ml of tert-butyl bromoacetate drop by drop under stirring at room temperature, continue stirring for 24 hours after completion, extract with treated anhydrous ether, filter again, and dry in a vacuum oven to obtain a yellowish precipitate .
[0035] 2. Synthesis of Carboxyl mPEG5000
[0036] The resulting solid dry product was dissolved in 125ml of 0.1mol L -1 NaOH solution, hydrolysis reaction at 55℃ for 24h, with 3mol L -1 Adjust the pH value to 2.8 to 3 with hydrochloric acid, the color of the solution gradually becomes lighter from brownish-yellow, evaporate the water ...
Embodiment 2
[0046] 1. Preparation of PEG6000 carboxylate
[0047] As in Example 1, 12 g of PEG6000 was used to replace mPEG5000.
[0048] 2. Synthesis of Carboxyl PEG6000
[0049] On the basis of Example 1, carboxy PEG6000 was prepared using the same experimental method as Step 2 of Example 1.
[0050] 3. Activation of Carboxyl PEG6000
[0051] On the basis of Example 1, use the same experimental method as Example 1 step 3 to prepare carboxyl PEG6000 active ester.
[0052] 4. Synthesis of branched PEG6000 modifier
[0053] On the basis of Example 1, using the same experimental method as in Step 4 of Example 1, a branched PEG6000 modifier was prepared, except that the dosage of malic acid was doubled, and the dosage of other reagents was the same as in Example 4.
[0054] 5. Preparation of branched PEG6000 active ester
[0055] On the basis of Example 1, using the same experimental method as Step 5 of Example 1, the branched PEG6000 active ester was prepared.
[0056] 6. Synthesis of...
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