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|1. (WO2018054300) CHOLIC ACID DERIVATIVE FREE ALKALI, CRYSTALLINE FORM, PREPARATION METHODS THEREFOR AND APPLICATIONS THEREOF|
|Applicants:||JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.
SHANGHAI HANSOH BIOMEDICAL CO., LTD.
|Title:||CHOLIC ACID DERIVATIVE FREE ALKALI, CRYSTALLINE FORM, PREPARATION METHODS THEREFOR AND APPLICATIONS THEREOF|
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.