32 results about "6-APA" patented technology

The present invention relates to the field of drug synthesis, in particular to a method for preparing amoxicillin sodium. The method of the present invention comprises the following steps: (1) preparation of acid anhydride; (2) preparation of 6-APA solution; (3) condensation: Move the 6-APA salt solution into the mixed acid anhydride reaction bottle, and time it for 3 hours; (4) Hydrolysis: add the condensation solution of step (3) to the hydrolyzed solution; (5) Crystallization: Leave the crystal to grow for 1 hour and then stir to grow the crystal for 1 hour (6) Suction drying: wash with water first, then wash with acetone, and dry in vacuum at 40° C. for 3 hours to obtain amoxicillin.

The invention discloses a penicillin antibiotic aptamer obtained by the screening technology for an improved aptamer without a fixed point target substance in the field of screening a penicillin antibiotic aptamer without a fixed point target substance, and an application thereof. The unfixed nucleic acid is eluted through a fixed oligonucleotide library; the parent nucleus 6-APA (6-aminopenicillanic acid) of the penicillin antibiotic is added in positive screening to act on the fixed nucleic acid; after eluting the nucleic acid molecules which can be combined with 6-APA, PCR (polymerase chain reaction) amplification is directly performed for next screening; and other antibiotics are added in negative screening, and the nucleic acid molecules in non-specific binding with the penicillin antibiotics are removed by elution. Through multiple rounds of positive and negative screening, 10 nucleic acid aptamers with high specificity and strong affinity with 6-APA are obtained; and the nucleic acid aptamer with a stable secondary structure is selected for developing a nucleic acid aptamer sensor for detecting 6-APA.

The present invention discloses isolation of Penicillin Acylase (PA) from Achromobacter sp CCM 4824 expressed in recombinant strain E. coli BL21 CCM 7394 bearing the recombinant plasmid pKXIP1 and processing of PA into biocatalyst useful for the industrial synthesis of antibiotics. More particularly the invention discloses a synthesis of semi-synthetic [beta]-lactam antibiotics in the reaction mixture consisting of activated acyl-donor (D-p-hydroxyphenylglycine methyl ester or amide for Amoxicillin and Cefadroxil; D-phenylglycine methyl ester or amide for Ampicillin and Cephalexin) and nucleophile (6-APA or 7-ADCA) catalyzed by PA obtained from recombinant E. coli BL21 CCM 7394 as the biocatalyst.

The invention relates to a method for recovering phenylacetic acid (PAA) in an enzymatic aqueous solution of 6-aminopenicillanic acid (6-APA). The method comprises the following steps: firstly, usinga mixed solvent to extract PAA from the enzymatic aqueous solution of 6-APA to a solvent phase, so as to enable 6-APA to be separated from PAA; then, performing lye stripping and evaporation concentration on the solvent phase to obtain an aqueous solution containing phenylacetate; and finally, recovering PAA in the aqueous solution in a manner of combining secondary nanofiltration with reverse osmosis. The method provided by the invention can directly separate and obtain high-quality aqueous solution of phenylacetate from the enzymatic aqueous solution of 6-APA in a manner of combining extraction, stripping, concentration and nanofiltration, can be directly used for fermentation to produce penicillin, further treats high-impurity nanofiltration concentrate in a manner of combining water dilution, nanofiltration and reverse osmosis, realize zero discharge of PAA, and minimizes discharged wastes by recycling of a solvent and water in the process.

A first compound is converted to a second compound enzymatically in a solvent mixture containing water and a fluorinated, non-chlorinated alkane, alkene, or alkyne having up to 4 carbon atoms. Lactams, for example 6-aminopenicillanic acid (6-APA), may be prepared by enzymatic conversion of a first compound, for example penicillin-G, in a solvent mixture comprising water and a non-aqueous organic solvent, for example 1,1,1, 2-tetrafluoroethane. The 6-APA can be caused to precipitate, isolated by filtration and optionally derivatized to produce a desired compound. A by-product of the enzymatic conversion, for example phenylacetic acid, can be isolated by solvent extraction, suitably using a solvent which also comprises 1, 1, 1, 2-tetrafluoroethane.

The invention relates the field of pharmacy, and specifically relates to an improved method for recycling phenylacetic acid waste liquid in 6-APA production. The method includes the following steps: (1) performing extraction; (2) performing degreasing; (3) performing heat preservation; (4) performing decolorization and impurity removal; (5) performing crystallization; and (6) processing sulfate radical in mother liquor. The method can perform decolorization under a water phase condition without using a solvent, so that costs can be obviously saved, and the recycling rate of phenylacetic acid can reach more than 90%; and the color of an obtained product is white, and the purity of the product can reach more than 99%. The processing and recycling of the sulfate radical in the mother liquor are also related, so that generated inorganic salt is less, and the pollution on environments is less, and therefore, the products obtained through the method can be applied to penicillin fermentation.

The invention provides a preparation method of D(-)-sulbenicillin sodium, which comprises the following steps: preparing D(-)-sulfophenylacetyl chloride from D(-)-sulfophenylacetic acid; preparing a D(-)-sulbenicillin sodium crude product from the D(-)-sulfophenylacetyl chloride and 6-APA; and purifying to obtain the final product D(-)-sulbenicillin sodium, wherein the 6-APA and the D(-)-sulfophenylacetyl chloride are added to a mixed solvent of water, ethanol and 2-methyltetrahydrofuran and react at the pH of 5.6-7.0 and the room temperature of 15-25 DEG C for 20-40 minutes. The preparation method has mild reaction condition, high yield and high purity of the obtained product.

The invention belongs to the technical field of medicines and in particular discloses a synthesis method of single-ring imipenem p-nitro benzyl ester. In the method, 6-APA is used as a raw material, and the single-ring imipenem p-nitro benzyl ester is prepared through reactions of nitration, bromination, oxidation, esterification, ring-opening, and the like. The method is characterized in that noval reagents and catalysts are adopted during synthesis, a single aromatic organic solvent is used as a reaction solvent, and an obtained product is easy to recover and convenient to apply. In the synthesis process, a one-pot synthesis method is adopted, thereby simplifying the process flow and shortening the production period.

Compositions and methods are provided, comprising at least one beta-lactam compound selected from the group consisting of cefuroxime, a penicillin, ceftriaxone, clavulanic acid, 6-aminopenicillanic acid (6-APA) and tazobactam, for enhancing T cell mediated immune responses in a subject, such as anti-tumor and anti-viral immune responses.

The invention relates to a method for comprehensively recovering effective ingredients in amoxicillin mother liquid prepared by an enzyme process. The method comprises the following steps: (1) concentrating the amoxicillin mother liquid, namely adjusting the pH value of the amoxicillin mother liquid prepared by the enzyme process to be 8.0-9.5, and performing nanofiltration and concentration to obtain concentrated mother liquid; (2) synthesizing amoxicillin under enzyme catalysis, namely adjusting the pH value of the concentrated mother liquid to be 5.8-7.0, and converting 6-APA (6-amino penicillanic acid) and D-methyl hydroxyphenyl glycinate into amoxicillin in the presence of immobilized penicillin acylase for synthesis; (3) preparing D-hydroxyphenyl glycine concentrated liquid by ultrafiltration and nanofiltration, namely separating after the enzyme catalysis reaction is ended to obtain amoxicillin crystals and secondary amoxicillin mother liquid, and performing ultrafiltration and nanofiltration on the secondary mother liquid to obtain the D-hydroxyphenyl glycine concentrated liquid; (4) crystallizing D-hydroxyphenyl glycine. According to the method, 6-APA and D-methyl hydroxyphenyl glycinate remained in the mother liquid are consumed through an indirect process of synthesizing amoxicillin under enzyme catalysis, the product quality of D-hydroxyphenyl glycine is improved, and the yield of D-hydroxyphenyl glycine is increased.

The invention relates to a 6-aminopenicillanic acid (6-APA) degrading bacterium and a screening method thereof. Particularly, the invention relates to a strain of 6-APA degrading bacterium Bordetella sp.L2, which is preserved in China General Microbiological Culture Collection Center (CGMCC) on October 18, 2012, with the preservation number of CGMCC No. 6691; and the GenBank registration number of the 16S rRNA gene sequence of the 6-APA degrading bacterium Bordetella sp.L2 is HQ840720. The 6-APA degrading bacterium Bordetella sp.L2 is an aerobic bacillus brevis; and when the pH value is 8.0, the 6-APA degradation rate of the 6-APA degrading bacterium Bordetella sp.L2 is 28%. The strain achieves higher 6-APA degradation capability and has a practical significance and an important engineering application value for treatment of waste water containing 6-APA cephalosporin.

The present invention discloses an improved process for the preparation of 6-amino penicillanic acid (6-APA) from a fermentatively produced N-substituted penicillin comprising the steps of extraction of the N-substituted penicillin compound as present in a fermentation broth or fluid to an organic solvent, back extraction of the N-substituted penicillin compound to water, treatment of the aqueous phase with a penicillin acylase and isolation of the 6-APA from the thus-obtained conversion solution by crystallization. Further improvements comprise extraction of the side chain to an organic solvent and isolation of 6-APA from the thus-obtained aqueous phase using a specific crystallization process.

The invention discloses a preparation method of a penicillin acylase immobilized carrier. In the invention, the surface active agent is used as the dispersant, the vinyl compound is used as the monomer, and the cross-linking polymerization is carried out by adopting the reverse phase suspension technology, so as to obtain the penicillin acylase immobilized carrier. The apparent enzymatic activity of carrier-immobilized penicillin acylase (IME) to hydrolyze penicillin G potassium salt to prepare 6-APA can reach more than 125IU / g. The epoxy group-containing polymer bead carrier obtained by the method of the invention has high apparent enzyme activity, simple process, convenient operation, cheap and easy-to-obtain raw materials, and is easy for industrial scale production.

The invention discloses a technology for preparing amoxicillin by a straight-through method. The technology takes a penicillin degreasing fluid as a starting raw material; 6-APA (6-amino penicillanic acid) crystallization, suction filtration, washing and drying steps are saved; the amoxicillin can be prepared without obtaining solid 6-APA via separation; and the prepared amoxicillin meets a requirement of a medicinal standard. The technology saves an operation procedure, reduces the labor intensity of production personnel, lowers the production cost, reduces environmental protection pressure, avoids contact between the production personnel and 6-APA dry powder, and reduces anaphylaxis.

A synthetic method for the general artificial antigen of a beta-lactam medicine belongs to the biochemical technical field. The invention adopts 6-amino penicillanic acid as hapten, couples the hapten with the carrier protein of bovine serum albumin BSA through an N-(m-maleimide group benzene methanoyl) succinimides MBS method, and determines the coupling ratio of the coupled matter through a gelelectrophoresis method. The method successfully synthesizes the 6-APA general artificial antigen with a simple and effective synthesis process. The method which can completely be used for immune analysis provides necessary artificial antigen for future study and meets the requirements of domestic study on the artificial antigen.