11 results about "Aminopenicillanic acid" patented technology

The present invention relates to a method for determining the methicillin-resistance properties of a Staphylococcus aureus strain present in a biological sample, the method comprising the following steps: •a) incubating the biological sample containing the Staphylococcus aureus strain for at least 15 minutes in the presence of an antibiotic from the class of beta-lactams selected from the following group: cefoxitin and 6-APA (6-aminopenicillanic acid); •b) isolating the bacteria present in the biological sample; •c) lysing the bacteria and hydrolysing the bacterial proteins in order to obtain a mixture of peptides; and •d) analysing this mixture of peptides by targeted mass spectrometry, the detection of at least one peptide originating from the protein PBP2a (SEQ ID NO. 1) or PBP2c (SEQ ID NO. 2) during this analysis step being indicative of the methicillin resistance of the Staphylococcus aureus strain present in the biological sample.

The invention belongs to the technical field of synthesis of organic compounds, and relates to a synthesis method of ticarcillin sodium. The synthesis method comprises the following steps: a condensation reaction step: in a nitrogen atmosphere, in an organic solvent and in the presence of N, N-bis (trimethylsilyl) urea, carrying out a reaction on 6-aminopenicillanic acid and 2, 2-dimethyl-5-(3-thienyl)-1, 3-dioxane-4, 6-diketone to generate ticarcillin, and filtering to obtain a solution containing ticarcillin; and a salt forming reaction step: carrying out a one-step salt forming reaction on the obtained solution containing ticarcillin and a sodium isooctanoate solution to obtain ticarcillin sodium. In the synthesis process, no acid or alkali is used for adjusting the pH value, so that open-loop degradation of a lactam ring in a ticarcillin structure is avoided; no water is added in the synthesis process, an organic solvent is used in the whole process, and other impurities generated by hydrolysis reaction are avoided; meanwhile, tedious steps such as extraction or reduced pressure distillation are not needed, the preparation process is easy and convenient to operate, the yield is high, the purity is high, and large-scale production is easy.

The invention belongs to the technical field of medicine separation, and discloses a coupling crystallization method for preparing a dicloxacillin sodium premium-grade product, which comprises the following steps: taking 6-aminopenicillanic acid (6-APA) as an initial raw material, carrying out acylation reaction and salt forming reaction, and finally carrying out evaporation-elution coupling crystallization to obtain the dicloxacillin sodium premium-grade product. The dicloxacillin sodium premium-grade product with regular crystal morphology, large particle size (greater than 200 [mu] m), high crystallinity, high purity (up to 99.4%), process yield greater than or equal to 80% and good stability can be obtained. The method is simple in required equipment, large in treatment scale, simple and convenient to operate and easy for industrial production, and has better technical economy and higher industrial application value.

The present invention belongs to the field of drug synthesis, and in particular to a method for synthesizing oxacillin sodium. The method is based on 6-aminopenicillanic acid (6-APA) and 5-methyl-3-phenyl-4-isoxazolecarbonyl chloride (MPCC) as raw materials, including a synthesis process of a condensation stage, an extraction salt formation stage, and a refined crystallization stage. The method of the present invention adopts a low-temperature phase-splitting process, introduces a phase-transfer catalyst, shortens the reaction time, suppresses the degradation of raw materials, and improves product quality; the refined crystallization stage adopts an inorganic salt-forming agent for refined salt formation, which has lower cost and further reduces the level of impurities. The crystal scale of the product is larger, the product particle size uniformity is better, and the fluidity is better. At the same time, the product does not need to be crushed and can be directly packaged.

The invention discloses a preparation method of high-purity cloxacillin sodium, which comprises the following steps: carrying out condensation reaction on 6-aminopenicillanic acid and 3-o-chlorophenyl-5-methyl-4-isoxazole acyl chloride to obtain a cloxacillin sodium aqueous solution; the cloxacillin sodium aqueous solution passes through macroporous strong-basicity anion exchange resin, cloxacillin sodium is adsorbed on the resin, and is resolved by absolute ethyl alcohol to obtain high-purity cloxacillin sodium resolved solution, so that the high-purity cloxacillin sodium is obtained. According to the method, the condensation reaction of the 6-aminopenicillanic acid and the 3-o-chlorophenyl-5-methyl-4-isoxazole acyl chloride does not need to dissolve the 6-aminopenicillanic acid and ensures that the reaction is performed under an alkaline condition, so that the materials are subjected to a solid-liquid mixed system reaction, the dissolution and clarification processes are reduced, the reaction time is shortened, and the reaction efficiency is improved. The generation of impurities caused by decomposition of the 6-aminopenicillanic acid in the dissolving process is prevented; a high-purity cloxacillin sodium product is obtained by using macroporous strong-basicity anion exchange resin, the content of the cloxacillin sodium product is 96.0% or above, and the purity of the cloxacillin sodium product can reach 99.7% or above.

The invention relates to the technical field of analysis and testing, and discloses a quality detection method for 6-aminopenicillanic acid, which can effectively detect coporphyrin I which is generated in a penicillin fermentation-enzyme method process and causes the 6-aminopenicillanic acid to become powder, and can be used for detecting the content of porphyrin in each main step of the process. The generation reasons and the effective removal steps are known, so that the technical process control is better guided; meanwhile, the chromatographic conditions can also be used for detecting the content of porphyrin in each main step of the process for producing 6-aminopenicillanic acid so as to understand the generation reasons and effective removal steps of the porphyrin, so that the process control is better guided.

The present invention relates to a method for determining the methicillin resistance properties of a strain of Staphylococcus aureus present in a biological sample, comprising the following steps: a) incubation of the biological sample containing said strain of Staphylococcus aureus for at least 15 minutes, in the presence of a beta-lactam antibiotic selected from the following group: cefoxitin and 6-APA (6-aminopenicillanic acid), b) isolation of the bacteria present in said biological sample, c) lysis of the bacteria and hydrolysis of the bacterial proteins, in order to obtain a mixture of peptides, d) analysis of this mixture of peptides by targeted mass spectrometry, the detection of at least one peptide from the PBP2a protein (SEQ ID NO. 1) or PBP2c protein (SEQ ID NO. 2) during this analysis step being indicative of the methicillin resistance of the strain of Staphylococcus aureus present in said biological sample.

The invention discloses a preparation method of a high-purity pimezlocillin hydrochloride crystal form, and relates to the field of preparation of pimezlocillin hydrochloride. The method comprises the following steps: dissolving 6-APA serving as an initial raw material in an organic solvent under an alkaline condition, carrying out nucleophilic substitution reaction on the 6-APA and chloromethyl pivalate, and generating 6-aminopenicillanic acid methyl pivalate salt from the 6-aminopenicillanic acid methyl pivalate salt and organic acid; then dissolving in an organic solvent under an alkaline condition, and carrying out an addition elimination reaction with N-dimethoxy methyl azacycloheptane to obtain pimemecillin; and salifying and crystallizing the obtained pimecillin to obtain the stable crystal form pimecillin hydrochloride. The pimemecillin hydrochloride crystal form reaches the medicinal purity, the effective component is greater than 99.0%, the impurity content is less than 0.1%, and the pimemecillin hydrochloride crystal form is suitable for industrial production.

A one-step method for synthesizing amoxicillin from penicillin or a salt thereof through an enzyme catalysis is provided. Conventional amoxicillin production requires sequential use of distinct penicillin acylases for hydrolysis and synthesis steps, necessitating isolation of the intermediate 6-aminopenicillanic acid (6-APA) and resulting in elevated manufacturing costs and suboptimal process efficiency. To address these limitations, the inventive method utilizes a mutant of penicillin acylase derived from Kluyvera citrophila as the exclusive biocatalyst in an aqueous reaction system. By reacting penicillin G potassium salt with D-p-hydroxyphenylglycine methyl ester, the process achieves direct amoxicillin synthesis in a single enzymatic step, attaining a product yield of 99%. This method exhibits advantages including fast catalytic rate, high product yield, environmentally friendly pure aqueous reaction system, low cost, and excellent economic benefits.

The invention discloses a sulbactam acid preparation method, which comprises: S1, bromination reaction: dissolving 6-aminopenicillanic acid in a hydrobromic acid aqueous solution, adding a sodium nitrite aqueous solution, and carrying out a reaction to generate dibromo-penicillin alkanoic acid; s2, oxidation reaction: dissolving the brominated product in water, and adding an oxidation system composed of potassium hydrogen persulfate composite salt, sodium tungstate and a phosphate buffer solution for reaction; s3, reduction purification: adding a sodium hydrogen sulfite aqueous solution to terminate the reaction, extracting with a mixed solvent, and treating an organic phase with a composite adsorbent; s4, filtering and purifying: adding the extracting solution into a filtering and purifying device for filtering and purifying treatment; and S5, crystallization and purification: concentrating the filtered and purified extract liquor, adding a cosolvent and an anti-solvent, introducing carbon dioxide for crystallization, growing crystals, and then filtering, washing and drying to obtain the high-purity sulbactam acid. According to the invention, the preparation of sulbactam acid with high yield and high purity is realized by improving bromination, oxidation and purification processes.

The invention relates to the synthesis of novel penicillin β-lactam antibiotics with synthetic peptide structures containing C-C and C-N multiple bonds, and the synthesis of their pharmaceutically acceptable salts, via four-component reactions using 6-aminopenicillanic acid (6-APA) as the aldehyde, amine, isonitrile, and carboxylic acid, or 6-aminopenicillanic acid (6-APA) as the aldehyde carboxylic acid and amine.