Abstract: A carotenoid oil suspension and preparation method thereof are provided. The method includes the following steps: a) mixing carotenoid with organic solvent, heating the mixture to dissolve the carotenoid sufficiently to obtain carotenoid solution; b) introducing the carotenoid solution obtained in step a) into a vegetable oil solution stirred in high speed by spraying, meanwhile recovering the organic solvent generated during spraying under vacuum condition, then, simultaneously completing recycling and spraying, thereafter, obtaining carotenoid oil suspension; wherein, the carotenoid oil suspension comprises a carotenoid crystal with an average particle size of less than 5 ?m. The method is applicable in industrial scale with continuous operation and increased efficiency without additional carotenoid crystal grinding processes, and decreases the degradation of carotenoid during the preparation process of carotenoid oil suspension.

Abstract: 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.

Abstract: The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability.

Abstract: The invention discloses a method for preparing high-content zeaxanthin. In the conventional preparation methods, some methods adopt certain toxic organic solvents; some methods require the multi-step crystallization process; and some methods are featured by long reaction time, high temperature and lower product yield, thus being not suitable for industrial production. The invention adopts lutein crystal or its fatty acid ester as the raw material and utilizes isomerization reaction to produce zeaxanthin, and is characterized in that a mixed catalyst consisting of an organic base catalyst and a cocatalyst is used in the isomerization reaction, wherein the cocatalyst is palladium carbon. The invention has the advantages of simple process route, low reaction temperature, short reaction time, good product purity and high yield, thus being suitable for industrial production, and no poisonous and harmful organic solvent residues in the product, thus being suitable for the use as a food additive or drug.

Abstract: The present invention provides a method for producing and purifying ?-carotene by Blakeslea trispora fermentation and use thereof. The method comprises the following steps: a) separately inoculating the Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) adjusting the fermentation liquid to be basic by using an organic or inorganic base, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure ss-carotene. The content of the ss-carotene in the present invention exceeds 96%, and the yield is above 85%.

Abstract: The invention discloses a D-biotin preparation method. In the prior art, with a synthesis method utilizing malonic acid diester as raw materials, impurities are also produced along with the obtained D-biotin. The D-biotin preparation method is characterized in that with the presence of dimethyl sulfoxide and inorganic base as catalysts, methane tricarboxylic acid trialkyl ester and (3aR, 8aS, 8bS)-1,3-dibenzyl-2-oxo-10H-iminazole [3,4-d] thiophene [1,2-a] sulfuryl halide are subjected to condensation reaction in methylbenzene solvent to obtain intermediate (3 aS,4S,6aR)-1,3-dibenzyl-4-(?,?,?-3-methoxycarbonylbutyl)-4H-1H-thiophene[3,4-d]iminazol e-2,4(1H)-ketone, and the D-biotin is obtained after the intermediate is treated by the aftertreatment method. By the D-biotin preparation method, production of the impurities is avoided, quality of the biotin is greatly improved on the existing basis, and side reaction is avoided too.

Abstract: Provided in the present invention is a method for synthesizing 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde.

Abstract: 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? 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.

Abstract: The invention discloses a method for preparing high-content zeaxanthin. In the conventional preparation methods, some methods adopt certain toxic organic solvents; some methods require the multi-step crystallization process; and some methods are featured by long reaction time, high temperature and lower product yield, thus being not suitable for industrial production. The invention adopts lutein crystal or its fatty acid ester as the raw material and utilizes isomerization reaction to produce zeaxanthin, and is characterized in that a mixed catalyst consisting of an organic base catalyst and a cocatalyst is used in the isomerization reaction, wherein the cocatalyst is palladium carbon. The invention has the advantages of simple process route, low reaction temperature, short reaction time, good product purity and high yield, thus being suitable for industrial production, and no poisonous and harmful organic solvent residues in the product, thus being suitable for the use as a food additive or drug.

Abstract: Disclosed is a preparation method of the lycopene intermediate 3-methyl-4,4-dialkoxy-1-butaldehyde. The preparation method comprises the following steps: (1) reacting 2-methyl-3,3-dialkoxy-1-halopropane with magnesium powder in the solvent of anhydrous tetrahydrofuran at a temperature of 45˜65° C. to generate a mixture of Grignard reagents under the protection of an inert gas; and (2) adding N,N-disubstituted carboxamide to the mixture of Grignard reagents and reacting at a temperature of 10° C.˜35° C. to obtain 3-methyl-4,4-dialkoxy-1-butaldehyde. The process route of the present invention is simple and direct, the operation is easy, the conditions are mild and the yield is good, and thus the invention has commercial value.

Abstract: 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)—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.

Abstract: The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer.

Abstract: 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.

Abstract: The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C1-C14 alkoxy, monosubstituted or bisubstituted or polysubstitued C1-C14 alkyl, monosubstituted or bisubstituted or polysubstitued C2-C14 alkenyl, monosubstituted or bisubstituted or polysubstitued C6-C14 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom; Y represents hydrogen, monosubstituted or bisubstituted or polysubstitued C1-C16 alkyl, monosubstituted or bisubstituted or polysubstitued C6-C12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom.

Abstract: The invention makes public a method for preparing xanthophyll crystals with higher content of zeaxanthin from plant oleoresin. The current methods generally are to get quite pure crystal forms of xanthophyll or zeaxanthin, and they refer to several separation steps.

Abstract: 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.

Abstract: 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.

Abstract: The present invention provides a method for producing and purifying ?-carotene by Blakeslea trispora fermentation and use thereof. The method comprises the following steps: a) separately inoculating the Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) adjusting the fermentation liquid to be basic by using an organic or inorganic base, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure ss-carotene. The content of the ss-carotene in the present invention exceeds 96%, and the yield is above 85%.

Abstract: The present invention relates to a method for preparing a carotenoid oil suspension with low viscosity and high fluidity. The method includes the steps of mixing carotenoid crystals with tetrahydrofuran, heating the resulting mixture to a reflux temperature of about 50˜70° C. under stirring, and filtering-the resulting solution to remove fat-soluble fibers. The resulting filtrate is then condensed to dryness, mixed with a ketone solvent, heated to a reflux temperature of about 60˜80° C., and filtered to remove non-soluble phospholipids. The filtrate obtained is condensed to a residue, and absolute alcohol is added to the residue, and then crystallized under stirring at room temperature. The resulting crystals are filtered and dried to-provide carotenoid crystals. The carotenoid crystals are ground and mixed with plant oils to provide a carotenoid oil suspension with low viscosity and high fluidity, which provides easy filling, for example, into capsules.

Abstract: The present invention provides caffeoylquinic acid derivatives and a method of preparing for the same, and also provides pharmaceutical compositions containing caffeoylquinic acid derivatives, and uses of caffeoylquinic acid derivatives in preparation of a medicament for the treatment or prophylaxis of virus diseases, in particular, uses of respiratory syncytial virus and hepatitis B virus, which has the characteristics of safety, high effectiveness and low toxicity.