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Preparation method of polyamide-amine dendrimer/2-methoxy estradiol compound with terminal functional groups

A technology of polyamidoamine dendrimers and methoxyestradiol, which is applied in the field of preparation of polyamidoamine dendrimers/2-methoxyestradiol complexes

Inactive Publication Date: 2010-06-16
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Relevant literature and patents on the synthesis of dendrimers and 2-ME complexes with adjustable surface functional groups have been searched at home and abroad, but there is no relevant report on the synthesis of dendrimers with adjustable surface functional groups and 2-ME complexes

Method used

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  • Preparation method of polyamide-amine dendrimer/2-methoxy estradiol compound with terminal functional groups
  • Preparation method of polyamide-amine dendrimer/2-methoxy estradiol compound with terminal functional groups
  • Preparation method of polyamide-amine dendrimer/2-methoxy estradiol compound with terminal functional groups

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (1) 50 milligrams of terminal groups are the fifth generation dendrimers (G5.NH 2 ) was dissolved in 10 ml of dimethyl sulfoxide solution, succinic anhydride (with G5.NH 2 The molar ratio of peripheral amino groups is 2:1 or 3:1) dissolved in 10 ml of dimethyl sulfoxide solution (the dendrimers whose terminal groups are amino groups react with succinic anhydride to generate dendrimers whose terminal groups are carboxyl groups) Macromolecules), mixed two DMSO solutions under vigorous stirring, and reacted at room temperature for 24 hours, then dialyzed with water for 3 days (6 times 4 liters) to remove excess succinic anhydride and organic solvent. Then freeze-dry to obtain carboxylated dendrimer (G5.SAH) solid (yield: 53.6-75.2%);

[0044] (2) 10 milligrams of carboxylated dendrimers G5.SAH were dissolved in 1.5 milliliters of water, and 2-ME, which was 10 times the molar equivalent of G5.SAH dendrimers, was dissolved in 300 microliters of methanol, and then the two M...

Embodiment 2

[0046] (1) Add 0.5 ml of triethylamine to a solution of 100 mg of G5.NH 2 10 ml of methanol solution. Will work with G5.NH 2 Acetic anhydride with a molar ratio of 2.5:1 peripheral amino groups was dissolved in 10 ml of methanol solution, and the two methanol solutions were mixed under vigorous stirring. After reacting at room temperature for 24 hours, the methanol was removed with a rotary evaporator, and the resultant was dissolved in water. Dialyzed with water for 3 days (6 times 4 liters) to remove by-products and excess reactants, and then freeze-dried to obtain acetylated dendrimer (G5.Ac) solid (yield: 91.4-94.2%);

[0047] (2) Dissolve 10 mg of acetylated dendrimer G5.Ac in 1.5 milliliters of water, dissolve 2-ME 10 times the molar equivalent of G5.Ac dendrimer in 300 microliters of methanol, and then dissolve the two Mix them together and vigorously stir at room temperature, overnight, evaporate the methanol naturally, centrifuge the mixed solution (7000 rpm, 10 min...

Embodiment 3

[0049] (1) Add 0.305 grams of G5.NH 2 Dissolve in 20 milliliters of methanol, and add 0.418 grams of glycidol in 10 milliliters of methanol solution (glycidyl alcohol / -NH 2 Molar ratio=4.4:1), after reacting at room temperature for 24 hours, remove methanol with a rotary evaporator, dissolve the resultant in water and dialyze with water for 3 days (6 times 4 liters), remove by-products and excess reactants, and then freeze Dry to obtain 0.45 g of hydroxylated G5.NGlyOH dendrimer solid (yield: 93.9%);

[0050] (2) 10 mg of hydroxylated dendrimer G5.NGlyOH was dissolved in 1.5 milliliters of water, and 2-ME, which was 10 times the molar equivalent of G5.NGlyOH dendrimer, was dissolved in 300 microliters of methanol, and then the two Mix them and stir vigorously at room temperature, overnight, evaporate methanol naturally, centrifuge the mixed solution (7000 rpm, 10 minutes), obtain the supernatant containing G5.NGlyOH / 2-ME complex, and collect the uncoated 2-ME precipitate thi...

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Abstract

The invention relates to a preparation method of a polyamide-amine dendrimer / 2-methoxy estradiol compound with terminal functional groups. The method comprises the following steps of: dissolving polyamide-amine dendrimers G.5NH2 in an organic solvent, and adding a functionalized reactant to carry out the functionalized modification of terminal groups of the polyamide-amine dendrimers; after reacting, removing by-products and redundant reagents, and drying to obtain polyamide-amine dendrimers of different terminal functional groups; then adding an organic solvent containing 2-methoxy estradiol and mixing and stirring to package the 2-methoxy estradiol; and finally, centrifuging and drying to obtain the polyamide-amine dendrimer / 2-methoxy estradiol compound. The compound has modification groups of different functional terminals, is hopeful to be used for the packaging and transporting other medicines and has better application prospect in the aspect of medicinal preparations. The invention has simple preparation method, moderate reaction condition and easy operation and has industrialization application prospect.

Description

technical field [0001] The invention belongs to the field of preparation of polyamidoamine dendrimer complexes, in particular to a preparation method of polyamidoamine dendrimer / 2-methoxyestradiol complexes with terminal functional groups. Background technique [0002] Dendrimers are a new type of highly branched, monodisperse and synthetic macromolecules with precise structures. The customizable core, internal structure, surface functional groups, and algebra-related geometric properties make it a unique material with wide applications in catalysis, sensors, optics, electronics, environmental remediation, drug delivery, and more. The latest research progress in nanomedicine based on dendrimers shows that dendrimers have been used in drug delivery in two different ways: 1) using dendrimers as a platform to covalently bind drug molecules for cancer treatment; Dendrimers or functionalized dendrimers physically encapsulate or complex drug molecules inside them to improve the w...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/565C08G69/48A61P35/00A61K47/59
Inventor 史向阳沈明武
Owner DONGHUA UNIV
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