6 results about "Aminopenicillanic acid" patented technology

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 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.

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.