A kind of pectin-doxorubicin conjugate and its preparation method and application
A technology of doxorubicin and conjugates, applied in the field of pectin-doxorubicin conjugates and their preparation, can solve the problems of only topical medication, poor anti-tumor effect, insoluble in water and the like
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Embodiment 1
[0033] 150g of Compound 1 (0.44mol) was dissolved in 1.5 LTHF, NHS (56g, 0.49mol) and DCC (137g, 0.66mol) were added successively, stirred overnight at room temperature, filtered, washed twice with solid dichloromethane, the filtrate was concentrated to dryness, and weighed After one crystallization, the pure product of compound 2 can be obtained.
Embodiment 2
[0035]
[0036] 147g of compound 2 (0.34mol) was dissolved in 1.5 LTHF, followed by adding L-alanine (32g, 0.35mol), NaHCO 3 (30g, 0.35mol), and then add 500mL of water. Adjust the ratio of THF and water to make the reaction solution into a single phase (difficult). Stir overnight at room temperature. After the reaction is complete, concentrate to remove THF, dilute with water, adjust the pH to 3-4 with HCl, and precipitate a solid. The solid is washed with water, dried in vacuo, and washed with ethyl acetate to obtain 130 g of product 3 (containing a little impurity), which is purified by crystallization.
Embodiment 3
[0038]
[0039] 30g of compound 3 (73mmol) was suspended in 500mL of dichloromethane, followed by adding 4-aminobenzyl alcohol (11g, 90mmol), EEDQ (27g, 113mmol), and finally methanol until the solution was clear, stirred at room temperature overnight, filtered, solid dichloromethane After washing, the filtrate was concentrated to dryness to obtain the crude compound 4, and then washed with methyl tert-butyl ether to obtain 20 g of the pure product.
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