Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory

Shaoxing University

Other

Zhe Jiang Medicine Co., Ltd

Shanghai Jiao Tong University

University of Shaoxing

Zhanggui Wu

Xinchang Pharmaceutical Factory

Zhejiang Medicine Co., Ltd. Xinchang Pharaceutical Factory

Wu, Zhanggui

Weidong Ye

Runpu Shen

Xuejun Lao

Xiaohua Song

Chunlei Wu

Luo Liu

Xiaoyue Jiang

Chunlei Lv

Jianyong Yuan

Shiqing Pi

Guofeng Wu

Gang Chen

Xianjin Luo

Siping Hu

Chaotian Chen

Guoqi Yu

Wei Mao

Kui Wang

Huan Yu

Haisong Xie

Bingxiang Xu

Zhigang Wu

Xiongsheng Sun

Liujiang Hu

Yibin Wu

Duanjun Xu

Jingjing Nie

Zhike Tian

Deping Yi

The present invention relates to a pharmaceutical composition for treating hepatitis B virus infection comprising crystalline entecavir as the pharmaceutically active ingredient and one or more pharmaceutically acceptable excipients. The tablet and capsule of the pharmaceutical composition have improved stability compared to that of amorphous entecavir under the conditions of light, high temperature and high humidity.

Crystal entecavir, crystal entecavir formulation and methods for the preparation thereof

The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R' and R&#x2033; are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety. 

Oxadiazole compound and preparation method thereof, pharmaceutical composition and use thereof

Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)&#x2014;N-(3-chloro-2-hydroxy-1-propyl) acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high. 

Linezolid intermediate and method for synthesizing linezolid

The present invention relates to a crystalline form of entecavir and its process for preparation, and provides a pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of entecavir. Furthermore, the present invention also provides a use of the crystalline form of entecavir in preparation for a medicament for the treatment of hepatitis B viral infections. The present invention is beneficial toe preparations for pharmaceutical formulations and enhancements of its bioavailability.

Crystalline form of entecavir, its preparation and the pharmaceutical composition and uses thereof

The present invention relates to an intermediate (12) of lycopene of 2,6,10-trimethyl-1,1-dialkoxyl-3,5,9-undecantriene of formula, (12) and its intermediate of 4-methyl-5,5-dialkoxyl-1-pentenyl-1-phosphonic acid dialkyl ester of formula (10), and their preparation methods. The process route is simple, the starting materials are available easily, the cost is low, and it is valuable in industry.

Intermediate of lycopene and preparation method of intermediate thereof

The invention relates to a novel important lycopene intermediate 3,7,11-trimethyl-1,3,6,10-tetraene-dodecyl diethyl phosphonate. A current lycopene intermediate 2,4,6,10-tetra-double bond pentadec-carbon phosphonate is difficult to synthesize. The invention provides a novel intermediate, which has the following synthesis steps of: preparing 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde from pseudoionone; preparing 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde from the 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde; and subjecting the 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde and tetraethyl methylenediphosphonate to condensation reaction to obtain target product. The invention can generate novel intermediate from raw material pseudoionone only by four reactions, thus the reactions are easy to control and great industrial value are achieved.

Lycopene intermediate 1, 3, 6, 10-tetra-double bond pentadec-carbon phosphonate as well as preparation method and use thereof

The invention discloses an intermediate 1-methoxyl-2,6,10-trimethyl-1,3,5, 9-undec-tetraene, and a preparation method and uses thereof. In the synthesis method for the current lycopene intermediate 2-pos double bond C-14 aldehyde (2,6,10-trimethyl-2,5,9-undecatriene-1-aldehyde), expensive methyl iodide, polluting dimethyl sulphide and dangerous strong base are needed, so that the method is hardly applied to industrial production. The invention provides a new compound 1-methoxyl-2,6,10-trimethyl-1,3,5,9-undec-tetraene, and pure 2-pos double bond C-14 aldehyde can be prepared by hydrolyzing and refining the compound. The synthetic route is simplified and the great suitability for industrial production is achieved.

1-methoxyl-2, 6, 10-trimethyl-1, 3, 5, 9-undec-tetraene, and preparation method and uses thereof

The present invention relates to 2,6,10-trimethyl-3,5,9-undecatrienyl-1-aldehyde represented by formula (3), and a method for preparing this intermediate. The process route of the present invention is simple, the starting materials are available easily, and the cost is low.

Intermediate of lycopene and preparation method of intermediate

The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds. 

2, 6-dinitrogen-containing substituted purine derivatives, the preparation and uses thereof

1,4,6,10-tetra-double bond pentadec-carbon phosphonate of formula (4), and preparation method thereof are provided. The preparation method comprises: reacting a pseudo ionone of formula (2) with sulfonium salt to prepare a epoxide of formula (9), and then reacting the epoxide of formula (9) with magnesium bromide to prepare a C-14 aldehyde of formula (3); condensing the C-14 aldehyde of formula (3) with tetra-alkyl methylene diphosphonate to obtain 1,4,6,10-tetra-double bond pentadec-carbon phosphonate of formula (4). Furthermore, the preparation method of lycopene via 1,4,6,10-tetra-double bond pentadec-carbon phosphonate of formula (4) is also provided. The present method has the advantages of short route, easily obtained raw materials, and low cost.

1,4,6,10-tetra-double bond pentadec-carbon phosphonate, preparation method thereof, and preparation method of lycopene using the same

The present invention provides a deshydroxy vancomycin compound,a method of its preparation and a pharmaceutical composition comprising a pharmaceutically effective amount of the deshydroxy vancomycin and the use of the said composition in the preparation of drugs for the treatment of susceptible bacteria infections. The method includes the following steps: (1) preparing a concentrated vancomycin solution containing the deshydroxy vancomycin by fermentations ofwith Deposit No. CGMCCNO.1183; (2) separating and purifing the concentrated vancomycin solution to obtain a refined filtrate of vancomycin hydrochloride containing the deshydroxy vancomycin by column chromatography; and (3) further separating and purifing the refined filtrate to obtain the deshydroxy vancomycin by chromatography. Wherein, separation and purification is processed by column chromatography in a gel chromatography column containing a salt-water mobile phase, separation and purification is processed by chromatography in a macroporous adsorption resin chromatography column containing a buffer-methanol mobile phase.

Dehydroxy vancomycin, the preparation, pharmaceutical composition and the use

1-Chloro-2-methyl-4-acyloxy-2-butene derivatives can be synthesized in good yields and high purity starting from isoprene and employing a chlorohydrin formation reaction in a system made of N-chloroisocyanuric acid derivatives and water, followed by esterification and rearrangement of the crude product mixture.

Method of manufacturing 1-chloro-2-methyl-4-acyloxy-2-butene derivatives

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Xinchang County, China

Weidong Ye