Alpha and beta poly (L asparamide) amino acid derivatives cisplatin macromolecule prodrug, preparation method and use thereof
A technology of asparagine and aspartic acid, applied in the field of alpha, can solve problems such as spacer structure not considered
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Embodiment 1
[0034] Embodiment 1: α, the synthesis of β-poly[L-asparagine] (PA)
[0035] Add 25 grams (0.19mol) of L-aspartic acid powder and 12.5 grams of 85% phosphoric acid in a 500ml round bottom flask, mix well, and react under reduced pressure at 185°C on a rotary evaporator for 3 hours until no more water vapor is produced. until. Add 100mL N, N-dimethylformamide and stir to dissolve the solid matter, then slowly add the obtained solution dropwise into a beaker filled with 500mL water under stirring to obtain a white precipitate, let it stand, pour the supernatant, filter, The solid was washed with water until it became neutral, and dried under vacuum at 60° C. for 24 hours to obtain 17 g of a powdery solid α, β-poly[L-asparagine] prepolymer. Dissolve the prepolymer in 150mL N,N-dimethylformamide, add 0.2g N,N-dicyclohexylcarbodiimide to condense at room temperature for 24 hours, filter, concentrate the filtrate, and precipitate the product with distilled water °C and vacuum dried...
Embodiment 2
[0036] Embodiment 2: α, β, the synthesis of L-asparagine and [α, β, L-(N-hydroxyethyl) asparagine] copolymer (PB)
[0037] Dissolve 8g (82.5mmol) of poly[L-asparagine] in 20mL of N, N-dimethylformamide, and add dropwise 2.5mL (41.3mmol) of ethanolamine in N,N-dimethylformamide under stirring , reacted at room temperature for 2 hours, the reaction mixture was concentrated to 10mL, and the product was precipitated with 40mL of ethanol / ether (volume ratio 1:1) mixed solvent and then vacuum-dried to obtain 8g of white polymer (PB), and the ring-opening rate was measured by NMR 30% (D 2 O is the solvent).
Embodiment 3
[0038] Example 3: α, β, the synthesis of poly(L-aspartic acid) (PI)
[0039] Add 4.5g of polymer PA to 500mL of 0.1mol / L sodium hydroxide aqueous solution, stir and react at room temperature for 1 hour, adjust the pH value of the solution to 5 with 0.1mol / L hydrochloric acid, filter, concentrate to 5mL, and dialyze with twice distilled water After 24 hours, the polymer was precipitated with 30 mL of ethanol / ether (volume ratio 1:1), and dried in vacuo to obtain 3 g of poly(L-aspartic acid) (PI).
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