Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Zhiqing Yang

Liang Zhang

Xiangyang Zhang

Hua Bai

Jian Chai

Hongying Luo

Jian Zhang

Xuyang Zhao

Qifeng Zhu

Yuncai Zhang

Xiaojie Xu

Yong Zhang

Xufei Li

Li Zhang

Xiaoming Wang

Zehua Zhong

Dezhou Xu

Zhenjuan Shi

Jinyi Xu

Fuli Zhang

Wei Zhang

Xiaohe Zheng

Zhezhou Yang

Hairong Luo

Chunbo Yang

Daoxin Chen

Rentong Sun

Tianmin Zhu

Di Su

Dejin Fu

Xufeng Yu

Guo Wei

Chuan Liu

Zhaozhao Zhang

Haibo Wang

Zhi Chen

Hongfu Kuang

Zhengjiang Cai

Min Zhao

Zhongwei Wu

Xinzeng Wang

Guan Wang

Provided are a new crystal form of fludarabine phosphate, a preparation method therefor, a pharmaceutical composition containing same, and an application thereof in preparing medicine. Crystal forms I and II of the fludarabine phosphate have excellent properties in terms of solubleness, dissolution rate, chemical stability, and processing adaptability.

Crystal form of fludarabine phosphate, preparation method therefor, and application thereof

The present invention relates to technical fields of organic chemistry and pharmaceutical chemistry, specifically to water-soluble rapamycin derivatives modified with glutathione. More specifically, the present invention discloses a compound of formula I and the preparation method thereof, wherein Rand Rare as defined in the description. The compound of formula I can be used in inducing immunosuppression and in the treatment of diseases such as transplant rejection and solid tumor, etc. 

Water-soluble rapamycin derivatives

Provided are crystal forms I, II, III and IV of a pyrroloquinoline quinone sodium salt and a preparation method thereof. Also provided are a pharmaceutical composition, a cosmetic composition, a functional food or a nutritional agent containing the above-mentioned crystal forms. The crystal forms have excellent properties in terms of solubility, crystal stability, hygroscopicity and the like.

Crystal form of pyrroloquinoline quinone sodium salt and preparation method and use thereof

Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production. 

Method for preparing azetidinone compound and intermediate of azetidinone compound

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

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

The present invention provides a preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate, preparation methods for intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, as well as a method for using (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium to prepare rivastigmine which can be used for the treatment of Alzheimer's disease.

Preparation method for rivastigmine, intermediates thereof, and preparation method for said intermediates

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Taizhou, China

Zhiqing Yang