Novel photosensitizer monomer completely soluble in water, and preparation method and application thereof

A technology of monomer and water-soluble salt, applied in the field of completely water-soluble photosensitizer monomer and its preparation, which can solve problems such as complicated process

Active Publication Date: 2014-10-08
GUILIN HUIANG BIOCHEMISTRY PHARMA CO LTD
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  • Novel photosensitizer monomer completely soluble in water, and preparation method and application thereof
  • Novel photosensitizer monomer completely soluble in water, and preparation method and application thereof
  • Novel photosensitizer monomer completely soluble in water, and preparation method and application thereof

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Embodiment Construction

[0060] One, the preparation of pheophorbide-a methyl ester (MPPB)

[0061] Chlorophyll-a extract (100g) is dissolved in pre-prepared volume ratio concentration of H 2 SO 4 5% H 2 SO 4 / methanol mixed solution, the reaction mixture was stirred at room temperature for 4h, and after the raw materials and intermediate products were completely reacted, it was poured into water and washed with CH 2 Cl 2 After extraction, the organic layer was washed with water, and the residue after distilling off the solvent under reduced pressure was crystallized with ethyl acetate / vegetable oil extraction solvent (volume ratio: 1 / 1).

[0062] 2. Preparation and crude production of 3-desvinyl-3-(1'-hexylhydroxy)ethyl-pheophorbide-a methyl ester

[0063] Dissolve 50 g of pheophorbide-a methyl ester in CH 2 Cl 2 (350ml), add 30% hydrogen bromide / acetic acid solution (300ml), the reaction mixture is stirred at about 20°C for 3-5h, then the solvent is evaporated in vacuo (water bath temperature...

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Abstract

The invention relates to a novel photosensitizer monomer completely soluble in water. Chlorophyll a is taken as a raw material for preparing pheophorbide a, 3-devinyl-3-(1'- hexahydro)ethyl-methyl pheophorbide-a is directly synthesized from pheophorbide a, and a water-soluble salt shown as the structural formula is obtained by processing with an alkali metal hydroxide. In the structural formula, R1, R2 and R3 are H or M, R1, R2 and R3 are not H simultaneously, and M is selected from Na, K or NH4<+>. The above water-soluble salts do not change the large ring structure with photosensitivity, are convenient to apply because of good water solubility, are applicable to prepare medicines for treating or diagnosing malignant tumor (especially superficial malignant tumor in all lumens), precancerous lesions and benign lesion during photodynamic therapy.

Description

technical field [0001] The invention relates to a drug for photodynamic therapy—photosensitizer, in particular to a novel completely water-soluble photosensitizer monomer and its preparation method and application. Background technique [0002] As new drugs for photodynamic therapy, second-generation photosensitizers have received widespread attention. There are also many methods for preparing second-generation photosensitizers using chlorophyll as raw materials and the resulting products. ZL01823093.8 relates to extracting spirulina biomass to produce a mixture photosensitizer of chlorin e6, rhodopsin 5 and rhodopsin 18. [0003] U.S. Patent No. 5,198,460 and its cited references, through low-temperature crushing of Spirulina cells, extraction, chromatographic purification and recrystallization separation to obtain pheophorbide-a methyl ester, and then at reflux temperature in trimethyl Thermal decarboxylation separation in pyridine. The pyropheophorbide-a methyl ester t...

Claims

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Application Information

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IPC IPC(8): C07D487/22A61K41/00A61P35/00
CPCA61K41/0071A61K49/00C07D487/22
Inventor 丁志坚韩臻周春秋陈双文苏文祖梁玉杰刘海明
Owner GUILIN HUIANG BIOCHEMISTRY PHARMA CO LTD
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