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1. (WO2018054300) CHOLIC ACID DERIVATIVE FREE ALKALI, CRYSTALLINE FORM, PREPARATION METHODS THEREFOR AND APPLICATIONS THEREOF

Pub. No.:    WO/2018/054300    International Application No.:    PCT/CN2017/102453
Publication Date: Fri Mar 30 01:59:59 CEST 2018 International Filing Date: Thu Sep 21 01:59:59 CEST 2017
IPC: C07J 9/00
C07J 43/00
C07J 51/00
A61P 9/00
A61K 31/58
Applicants: JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.
江苏豪森药业集团有限公司
SHANGHAI HANSOH BIOMEDICAL CO., LTD.
上海翰森生物医药科技有限公司
Inventors: SU, Yidong
苏熠东
GONG, Sujuan
龚素娟
BAO, Rudi
包如迪
Title: CHOLIC ACID DERIVATIVE FREE ALKALI, CRYSTALLINE FORM, PREPARATION METHODS THEREFOR AND APPLICATIONS THEREOF
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.