摘要:
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.
摘要:
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.
摘要:
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 of Amycolatopsis Orientalis with 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.
摘要:
The invention relates to the field of microbial technology. It discloses a method to apply the cloud point system (CPS) in biotransformation by selecting one or more types of nonionic surfactant to form a aqueous system with a cloud point below the microbial transformation temperature, which serves as transformation medium. The method disclosed is suitable in particular for microbial transformation of hydrophobic compounds, for the system where substrate or product inhibits microbial growth or where product is further degraded by microbes. The CPS in the present invention forms a microemulsion of water-in-oil and oil-in-water, where the drops of surfactant is able to solubilize, serving as substrate reservoir and product extractant. This enhances bioavailability of substrates and elimination of product inhibition. The large water vesicles existing in the continuous surfactant phase provide aqueous environment to the cells where they can be sheltered from detrimental effects of surfactants, resulting in improvement of biocompatibililty.
摘要:
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.
摘要:
The present invention relates to a pharmaceutical composition for treating hepatitis B virus infection, comprising the crystal entecavir as pharmaceutically active ingredients and pharmaceutically acceptable excipients. The tablet and capsule of the pharmaceutical composition have more stronger stabilization than that of amorphous entecavir under conditions of lighting, high temperature and high humidity.
摘要:
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.
摘要:
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.
摘要:
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.