Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Hualing Xiao

Shuhui Chen

Haiying He

Peng Li

Xiaolin Li

Zhi Luo

Chunyan Du

Weidong Li

Fei Hao

The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases. 

Steroid derivative FXR agonist

Disclosed are a crystalline or amorphous form of steroid derivative FXR agonist (formula I), and a preparation method therefor, and a crystalline composition and pharmaceutical composition comprising the crystalline or amorphous form, and the use of same in the preparation of a drug for treating or preventing various conditions associated with FXR. 

Crystalline or amorphous form of steroid derivative FXR agonist, preparation method therefor and use thereof

The present invention falls within the field of pharmaceutical chemistry, and relates to a method for preparing a steroid derivative FXR agonist and relevant intermediates. In particular, the present invention relates to a method for preparing a compound of formula I, comprising reacting a compound of formula 8 with a compound of formula 9 to obtain a compound of formula 10, obtaining a compound of formula 11 from a reaction of the compound of formula 10, and obtaining the compound of formula I from a reaction of the compound of formula 11, as well as the intermediates used, the methods for preparing the intermediates and the use of the intermediates. The reaction conditions of the preparation method are mild, and some of the steps can convert multiple groups simultaneously, thereby effectively shortening the sequence of steps. The preparation method is suitable for industrialized production. 

Method for preparing steroid derivative FXR agonist

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Shanghai, China

Hualing Xiao