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Title:
PREPARATION AND POST-TREATMENT METHOD FOR 5-AMINOLEVULINATE
Document Type and Number:
WIPO Patent Application WO/2023/019839
Kind Code:
A1
Abstract:
Provided in the present invention is a preparation and post-treatment method for 5-aminolevulinate. The method comprises: under a low temperature condition, adding a mixed solvent of a liquid saturated chain hydrocarbon and dimethylformamide to a reaction container, stirring and cooling same, then adding 5-aminolevulinic acid and a corresponding glycerol derivative, stirring and dissolving same, then adding 4-dimethylaminopyridine, dropwise adding dicyclohexylcarbodiimide, maintaining same at room temperature, and then reacting same to obtain 5-aminolevulinate; and then dissolving a hydrochloride salt of the above prepared 5-aminolevulinate with a solvent to obtain a mixed liquid, stirring and refluxing same, and when the temperature of the mixed liquid is 35-45ºC, dropwise adding an aqueous sodium bicarbonate solution while the mixed liquid is still hot, followed by stirring and crystallization, drying, and crushing to obtain the product. In the present invention, the unconventional crystallization method of dropwise adding an aqueous sodium bicarbonate solution is used, such that a compound A with a high yield and a low impurity content can be obtained. The compound A obtained by means of crystallization according to the method has small product particles and is easy to crush, relevant substances can be effectively removed, and the problems in the prior art are effectively solved.

Inventors:
LU GUANGYING (CN)
Application Number:
PCT/CN2021/139309
Publication Date:
February 23, 2023
Filing Date:
December 17, 2021
Export Citation:
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Assignee:
HUNAN FURUI BIOPHARMA TECH CO LTD (CN)
International Classes:
C07C227/18; C07C227/40; C07C227/42; C07C229/22
Foreign References:
CN113651708A2021-11-16
US20100273725A12010-10-28
CN1178521A1998-04-08
Other References:
BATTAH S H, ET AL.: "SYNTHESIS AND BIOLOGICAL STUDIES OF 5-AMINOLEVULINIC ACID-CONTAINING DENDRIMERS FOR PHOTODYNAMIC THERAPY", BIOCONJUGATE CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 12, no. 06, 1 November 2001 (2001-11-01), US , pages 980 - 988, XP001092540, ISSN: 1043-1802, DOI: 10.1021/bc010027n
Attorney, Agent or Firm:
SUZHOU GUOCHENG PATENT AGENCY CO., LTD (CN)
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