Abstract: The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.
Type:
Grant
Filed:
December 11, 2018
Date of Patent:
September 13, 2022
Assignee:
Yabao Pharmaceutical Group Co., Ltd.
Inventors:
Fanghui Tang, Jiyu Bao, Junfeng Gao, Zhouhong Tan
Abstract: A pyranoglucose-substituted pyrazole compound, used as a pharmaceutical intermediate, having the structural formula represented by formula (9c). The present invention further relates to an intermediate compound represented by formula (10c) or a salt thereof. The present invention further relates to a preparation method of the aforementioned intermediate compound and a method of using the same to prepare an SGLT inhibitor. By means of the novel key intermediate, the preparation technique of an SGLT inhibitor is greatly simplified. In addition, because the intermediate can be precipitated in the form of a salt and is easy to purify, the purity of the SGLT inhibitor is significantly increased, compared with the original preparation pathway (crude product purity can reach 99% or more).
Abstract: The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.
Type:
Application
Filed:
December 11, 2018
Publication date:
December 2, 2021
Applicant:
Yabao Pharmaceutical Group Co., Ltd.
Inventors:
Fanghui TANG, Jiyu BAO, Junfeng GAO, Zhouhong TAN
Abstract: The present application relates to a salt of a pyranose-substituted heterocyclic compound, a preparation method therefor, and use thereof, and in particular, to an acid addition salt of a compound of formula (I) or a prodrug thereof, and further relates to D-glucuronate of a crystalline compound of formula (I) or a prodrug thereof. D-glucuronate of a crystalline compound of formula (II) has particular advantages in terms of crystallizability, subsequent purification, stability, formulation medicinal properties or quality control, and is most applicable for improving the formulation pharmaceutical properties, purity and quality control, as well as large-scale process development of such drugs.