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Title:
LIFITEGRAST MORPHOLINE SALT, METHOD FOR PREPARING SAME, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2024/001995
Kind Code:
A1
Abstract:
The present invention relates to the technical field of drug synthesis, in particular to a lifitegrast morpholine salt, a method for preparing same, and use thereof. The lifitegrast morpholine salt provided by the present invention can be used for dissociating and removing morpholine in trace acidic water to obtain high-purity lifitegrast; and the yield is high, operation is easy, and the generation of waste solvents and wastewater in a lifitegrast purification process can be greatly reduced. The method for preparing the lifitegrast morpholine salt provided by the present invention is easy to implement, and the prepared lifitegrast morpholine salt is high in yield and high in purity, and has a very good removal effect on chiral isomer impurities. In the lifitegrast purification process, a lifitegrast crude product is firstly prepared into the lifitegrast morpholine salt, and then simple acid hydrolysis and dissociation is carried out, so that the lifitegrast purification process can be greatly simplified, the generation of waste solvents and wastewater is reduced, the reaction coherence is strong, the process is safe and controllable, and the impurity content in the product is lower.

Inventors:
CHEN JINPING (CN)
ZHAO JUNXU (CN)
NIU GUOZHI (CN)
LIU YERAN (CN)
WANG SHA (CN)
Application Number:
PCT/CN2023/102344
Publication Date:
January 04, 2024
Filing Date:
June 26, 2023
Export Citation:
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Assignee:
ZHEJIANG HISOAR PHARMACEUTICAL CO LTD (CN)
HEBEI ZHIHENG MEDICAL TECH CO LTD (CN)
International Classes:
C07D405/06; C07D295/023; C07D295/027
Domestic Patent References:
WO2019053607A12019-03-21
WO2023040103A12023-03-23
Foreign References:
CN115010703A2022-09-06
US20200306242A12020-10-01
CN112300139A2021-02-02
US20110092707A12011-04-21
Attorney, Agent or Firm:
SINO-CREATIVITY INTELLECTUAL PROPERTY LAW FIRM (CN)
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