Title:
CHOLIC ACID DERIVATIVE FREE ALKALI, CRYSTALLINE FORM, PREPARATION METHODS THEREFOR AND APPLICATIONS THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/054300
Kind Code:
A1
Abstract:
Provided is a crystalline form cholic acid derivative free alkali, a preparation method therefor and an application. The chemical name of the cholic acid derivative free alkali is (5R)-5-((2R)-2-((3R,5S,6R,7R,10S,13R)-6-ethyl-3,7-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)propyl)thiazolidine-2,4-dione, and the power X-ray diffraction pattern thereof comprises peaks at diffraction angles (2θ) of 16.5±0.2°, 13.6±0.2°, 12.1±0.2°, and 20.4±0.2°. Also provided are an optically pure cholic acid derivative, a preparation method therefor and an application thereof. The purity of the obtained optical isomer reaches 90.0% or more, and the problem in the prior art of being difficult to obtain the optical purity by means of separation is resolved. In addition, also provided a method for preparing a cholic acid derivative and an application thereof. The preparation method overcomes the defect existing in the prior art; a multi-step reaction can be implemented at room temperature; the obtained product has good purity, high yield, and strong process operability; the process safety is greatly improved; the preparation method is suitable for industrial application.
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Inventors:
SU YIDONG (CN)
GONG SUJUAN (CN)
BAO RUDI (CN)
GONG SUJUAN (CN)
BAO RUDI (CN)
Application Number:
PCT/CN2017/102453
Publication Date:
March 29, 2018
Filing Date:
September 20, 2017
Export Citation:
Assignee:
JIANGSU HANSOH PHARMACEUTICAL GROUP CO LTD (CN)
SHANGHAI HANSOH BIOMEDICAL CO LTD (CN)
SHANGHAI HANSOH BIOMEDICAL CO LTD (CN)
International Classes:
C07J9/00; A61K31/58; A61P9/00; C07J43/00; C07J51/00
Domestic Patent References:
| WO2016086169A1 | 2016-06-02 | |||
| WO2016173397A1 | 2016-11-03 | |||
| WO2006122977A2 | 2006-11-23 |
Foreign References:
| CN102282157A | 2011-12-14 | |||
| CN104876995A | 2015-09-02 |
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (CN)
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