A kind of 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: 2022-03-25
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
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[0026] The present invention will be further described in detail below with reference to the 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, and the five steps are correspondingly referred to as acid chloride reaction, condensation esterification, alcohol precipitation of crude product, membrane filtration and freezing treatment.
[0028] Step 1: add 5-aminoketovalerate hydrochloride into thionyl chloride and heat to reflux, remove excess thionyl chloride by distillation under reduced pressure to obtain 5-aminoketovaleryl chloride, add to 5-aminoketovaleryl chloride tetrahydrofuran;
[0029] Step 2: suspend and dissolve the dextran in tetrahydrofuran, add a catalyst, dropwise add the tetrahydrofuran solution of 5-aminoketovaleryl chloride in step 1, after the dropwise addition, remove excess tetrahydrofuran by vacuum distillation, add water t...
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Abstract
The invention discloses a preparation method of 5-aminolevulinic acid dextran ester, relates to the technical field of photosensitizer drug synthesis, comprising the following steps: reacting 5-aminolevulinic acid and thionyl chloride to form 5-aminolevulinic acid Acyl chloride, condensed with dextran in an anhydrous organic solvent to form an ester, the resulting reaction solution was evaporated to remove the solvent, dissolved in water and filtered, added alcohol to crystallize to obtain a crude product, dissolved in pure water, and then separated by membrane twice, decolorized, frozen dry to obtain 5-aminolevulinic acid dextran ester, the product obtained in the present invention has high yield and purity, uniform molecular weight distribution, is 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, in particular to a preparation method of 5-aminolevulinic acid dextran. Background technique [0002] Photodynamic therapy is a clinical treatment method that combines photosensitizers and corresponding light sources to destroy diseased tissue through photodynamics. 5-Aminolevulinic acid is one of the most commonly used photosensitizers in clinic, belongs to the second generation photosensitizer, and is an endogenous substance of the organism. Under light irradiation of a certain wavelength, 5-aminolevulinic acid undergoes a chemical reaction to generate new ecological oxygen, causing damage to cell membranes, mitochondria and nucleic acids, and necrosis and apoptosis of tumor cells or other actively proliferating cells. role of disease. The functions of 5-aminolevulinic acid as a photosensitizer include: 1. Small side effects and short light-avoiding time. Since it is a...
Claims
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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