Les Laboratoires Servier

Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

China State Institute of Pharmaceutical Industry

Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd.

Xueyan Zhu

Peng Zhang

Zhedong Yuan

Hanbin Shan

Xiong Yu

Hubo Wang

Yu Huang

Meng Guo

Mingtong Hu

Hongjuan Pan

Xiquan Zhang

Hongjiang Xu

Aiming Zhang

Wei Song

Xiaomin Zhang

Zhou Zhou

Huadong Yao

Yajun Guo

Leilei Yang

Ling Tong

Hui Fu

Jiude Sun

Duzheng Wang

Jiasong Zhang

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production. 

Synthesis process of ruxolitinib

The present invention relates to a nintedanib diethanesulfonate salt A-type crystal represented by formula (II), and also relates to a crystalline composition and pharmaceutical composition comprising the crystal, and preparation method and use thereof. An X-ray powder diffraction spectrum of the nintedanib diethanesulfonate salt A-type crystal of the present invention has a diffraction peak at about 14.64, 18.79, 19.31, 20.11, 21.20, 22.45 and 26.71&#xb0; when represented via a 2&#x3b8; value. The nintedanib diethanesulfonate salt A-type crystal of the present invention has a stable property, is non-hygroscopic and difficult to degrade, and is particularly suitable for medicine production. 

Nintedanib diethanesulfonate salt crystal and preparation method and use thereof

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C-Calkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production. 

Method for preparing dabigatran etexilate intermediate, and intermediate compound

The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.

Crystal form VII of agomelatine, preparation method and use thereof and pharmaceutical composition containing same

Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Dihydroindolinone derivatives

The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.

Agomelatine hydrobromide hydrate and preparation thereof

The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

Agomelatine hydrochloride hydrate and preparation thereof

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Shanghai, China

Xueyan Zhu