Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Jian Chai

Zhiqing Yang

Liang Zhang

Fuli Zhang

Xiangyang Zhang

Hairong Luo

Qingfeng Cai

Pengcheng Qiu

Jinyi Xu

Hua Bai

Jiang Li

Bin Liang

Yingqiu Wu

Hongying Luo

Chunbo Yang

Yanghui Guo

Yili Ding

Mingxing Yin

Chonghao Liu

Lifeng Cai

Xuan Yang

Xufeng Yu

Guo Wei

Jianchao Wu

Chuan Liu

Zhaozhao Zhang

Zhi Chen

Xinzeng Wang

Qingyan Yan

Kenneth Smith

Guan Wang

Provided are crystal forms I, II, and III of bedaquiline fumarate, and preparation methods thereof. The crystal forms have high purity, excellent physicochemical properties, and good stability. The preparation methods can effectively improve the quality of products, and are applicable to preparation and mass production of medicines.

Crystal forms of bedaquiline fumarate and preparation methods therefor

The present invention relates to a preparation method of 4-(4-amino-3-fluorophenoxy)-N-methylpyridine-2-formamide capable of enabling 4-chlorine-N-methylpyridine-2-formamide to react with 4-amino-3-fluorophenol in the presence of an inorganic base. The present invention employs the inorganic base to replace potassium t-butoxide in the prior art, thus effectively solving the problem of a potential safety hazard of the potassium t-butoxide in industrial production. In addition, after the reaction is completed, the present invention employs a crystallization method for separation to obtain a reaction product; thus compared with the methods of extraction, concentration and column isolation and purification employed in the prior art, the present invention has a simpler operation and a lower cost, results in less environment pollution and a higher yield, and is very suitable for industrial production.

Preparation method of 4-(4-amino-3-fluorophenoxy)-N-methylpyridine-2-formamide

Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.

Synthesis process of antiparasitic drug selamectin

The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2&#x3b8; diffraction angles: 5.7&#xb1;0.2&#xb0;, 6.2&#xb1;0.2&#xb0;, 11.2&#xb1;0.2&#xb0;, 12.4&#xb1;0.2&#xb0;, 18.2&#xb1;0.2&#xb0;, 21.4&#xb1;0.2&#xb0;, 21.8&#xb1;0.2&#xb0; and 23.6&#xb1;0.2&#xb0;; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2&#x3b8; diffraction angles: 6.0&#xb1;0.2&#xb0;, 11.8&#xb1;0.2&#xb0;, 18.2&#xb1;0.2&#xb0;, 21.6&#xb1;0.2&#xb0;, 24.4&#xb1;0.2&#xb0;, 27.7&#xb1;0.2&#xb0; and 29.7&#xb1;0.2&#xb0;. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.

Crystal form of dabigatran etexilate mesylate and preparation method and use thereof

A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. 

4-substituent-2-hydroxylmorpholine-3-one and preparation method thereof

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. 

Method for preparing linezolid intermediate

Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.

4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine derivatives having activity of inhibiting protein kinase and use thereof

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Taizhou, China

Jian Chai