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Title:
EPRISTERIDE IMPURITY, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/184789
Kind Code:
A1
Abstract:
Disclosed in the present invention are an epristeride impurity, and a preparation method therefor and the use thereof, which fall within the field of medicinal chemistry. The chemical name of the epristeride impurity is 17β-(N-tert-butyl-amino-formyl)androst-4-en-3-one-5-hydroxy. The preparation method therefor comprises the following steps: 1) taking epristeride as a raw material and stirring and mixing uniformly with an oxidant in an organic solvent I to undergo a reaction; after the reaction is finished, obtaining a crude product reaction solution of the epristeride impurity; and after processing the crude product reaction solution of the epristeride impurity, concentrating to obtain an oily substance; and 2) recrystallizing the oily substance by means of using an organic solvent II to obtain the epristeride impurity. The present invention is simple and efficient in operation, moderate in reaction conditions, high in safety, and is easy to control. The epristeride impurity prepared by the preparation method has a high yield and a purity reaching 96% or above, and is suitable for being used as a reference substance for researching the quality of epristeride crude drugs and preparations thereof, thus laying a solid foundation for effective control of the quality of epristeride-related drugs.

Inventors:
HE QIU (CN)
YU BO (CN)
HUANG KUN (CN)
ZHAO JIE (CN)
Application Number:
PCT/CN2020/128606
Publication Date:
September 23, 2021
Filing Date:
November 13, 2020
Export Citation:
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Assignee:
JIANGSU LIANHUAN PHARMACEUTICAL CO LTD (CN)
International Classes:
C07J41/00; G01N30/02; G01N30/06
Domestic Patent References:
WO2003029268A12003-04-10
Foreign References:
CN111362999A2020-07-03
CN111624291A2020-09-04
US4910226A1990-03-20
Other References:
YAN DONGMEI, TU LINGLAN, SONG ZHONGYING, PENG XIAOYING, LI WENJUN: "HPLC Determination of the Content and Dissolution of Epristeride Tablets", CHINESE JOURNAL OF PHARMACEUTICAL ANALYSIS, vol. 27, no. 8, 31 December 2007 (2007-12-31), pages 1264 - 1266, XP055851390, DOI: 10.16155/j.0254-1793.2007.08.039
MACEK, J.: "Separation of finasteride and analogues", JOURNAL OF CHROMATOGRAPHY B, ELSEVIER, AMSTERDAM., NL, vol. 764, no. 1-2, 25 November 2001 (2001-11-25), NL, pages 207 - 215, XP004322154, ISSN: 1570-0232, DOI: 10.1016/S0378-4347(01)00317-6
Attorney, Agent or Firm:
NANJING TIANHUA PATENT AGENT CO., LTD. (CN)
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