Preparation method of 5-aminolevulinic acid glucan ester
A technology of aminolevulinic acid dextran ester and aminolevulinic acid hydrochloride, applied in the direction of medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problem of low skin permeability , phototoxicity, side effects and other issues, to achieve the effect of high yield and purity, uniform molecular weight distribution
Active Publication Date: 2020-09-08
上海易全化学有限公司
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Problems solved by technology
[0003] Since 5-aminolevulinic acid is a polar compound, the skin permeability is low, making it generally difficult to reach the target site of skin tissue, and higher concentrations of 5-aminolevulinic acid can produce phototoxic side effects
Method used
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[0026] The present invention will be further described in detail below in conjunction with examples, but the embodiments of the present invention are not limited thereto.
[0027] A preparation method of 5-aminolevulinic acid dextran ester comprises the following five steps, which correspond to abbreviated as acid chloride reaction, condensation esterification, alcohol analysis of crude product, membrane filtration and freezing treatment.
[0028] Step 1: Add 5-aminolevulinic acid hydrochloride to thionyl chloride and heat to reflux, distill under reduced pressure to remove excess thionyl chloride to obtain 5-aminolevulinyl chloride, and add to 5-aminolevulinyl chloride Tetrahydrofuran;
[0029] Step 2: Suspend and dissolve dextran in tetrahydrofuran, add the catalyst, add dropwise the tetrahydrofuran solution of 5-aminolevulinyl chloride in step 1, after the dropwise addition, remove excess tetrahydrofuran by distillation under reduced pressure, add water to dissolve and add ...
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The invention discloses a preparation method of 5-aminolevulinic acid glucan ester. The invention relates to the technical field of photosensitizer drug synthesis. The method comprises the following steps of: 1, reacting 5-aminolevulinic acid with thionyl chloride to obtain 5-aminoketone valeryl chloride, performing condensation with glucan in an anhydrous organic solvent to obtain ester, evaporating the obtained reaction liquid to remove the solvent, adding water for dissolution and filtration, adding alcohol for crystallization to obtain a crude product, dissolving the crude product in purewater, and performing membrane separation twice, conducting decolorization and freeze-drying to obtain the 5-aminolevulinic acid glucan ester. The obtained product is high in yield and purity, uniformin molecular weight distribution, and suitable for pharmacological research, and has extremely high industrial application value.
Description
technical field [0001] The invention relates to the technical field of photosensitizer drug synthesis, more specifically, it relates to a preparation method of 5-aminolevulinic acid dextran ester. Background technique [0002] Photodynamic therapy is a clinical treatment method that combines the application of photosensitizers and corresponding light sources to destroy diseased tissues through photodynamics. 5-Aminolevulinic acid is one of the most commonly used photosensitizers in clinical practice. It belongs to the second generation of photosensitizers and is an endogenous substance of organisms. Under the irradiation of a certain wavelength of light, 5-aminolevulinic acid undergoes a chemical reaction to generate new ecological oxygen, which causes damage to cell membranes, mitochondria and nucleic acids, and causes necrosis and apoptosis of tumor cells or other actively proliferating cells, thereby playing a therapeutic role. effect of disease. The characteristics of ...
Claims
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Patent Timeline
Login to View More IPC IPC(8): C08B37/02A61K41/00A61K47/61A61P35/00
CPCC08B37/0009A61K41/0061A61K47/61A61P35/00
Inventor 韩小兵
Owner 上海易全化学有限公司