发明名称 Synthesis of 5-aminolevulinic acid trimer using citric acid for photodynamic therapy
摘要 PURPOSE: A 5-aminolevulinic trimer using citric acid is provided to minimize side effect and to quickly treat patients. CONSTITUTION: A 5-aminolevulinic trimer using citric acid, which is used as a photosensitizer of photodynamic therapy(PDT) is formed by covalent bond of aminolebulinic acid to a carboxylic group of citric acid. A method for preparing the trimer comprises: a step of dissolving 1M citric acid in 5ml of distilled water to prepare a first solution; a step of dissolving 3M N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride(EDC), 3M N-hydroxysuccimide, and 3M 5-aminolevulinic acid in 95ml of tetrahydrofuran(THF)/H_20 to prepare a second solution; a step of mixing the first and second solutions in a same ratio; a step of removing solvent and freeze-drying; a step of precipitating and recrystallizing at room temperature; a step of purifying the recrystallized product flash chromatography(3/1=ethylacetate/hexane); and a step of recrystallizing with dichloromethane(DCM)/hexane.
申请公布号 KR101254752(B1) 申请公布日期 2013.04.15
申请号 KR20110018008 申请日期 2011.02.28
申请人 发明人
分类号 A61K31/185;A61K31/197;A61P35/00 主分类号 A61K31/185
代理机构 代理人
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