- Preparation method of piperacillin
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The invention discloses a preparation method of piperacillin. According to the method, DBU with stronger alkalinity is used as an initiator to promote the reaction of N-ethyl-2, 3-dioxopiperazine andtriphosgene to obtain N-ethyl-2, 3-dioxopiperazine acyl chloride, so that the use of trimethylchlorosilane is avoided; In the condensation reaction, sodium acetate is used as an acid-binding agent, sothat the pollution of carbon dioxide to the environment is avoided. The alkalinity of sodium acetate is weaker than that of sodium bicarbonate, the hydrolysis degree in the reaction process is low, meanwhile, DBU is used as a catalyst, and the N-ethyl-2, 3-dioxopiperazine acyl chloride hydrolysate can also react with ampicillin to obtain piperacillin, so that the reaction yield is increased, andthe production cost is further reduced.
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Paragraph 0028-0030; 0032-0033; 0035-0036; 0038-0039; 0042
(2021/02/06)
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- DERIVATIZATION OF BETA-LACTAM ANTIBIOTICS AS CALIBRATORS/ISTD IN MASSSPEC MEASUREMENTS
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The invention relates to a complex comprising an antibiotic substance and a nucleophilic derivatization reagent, compositions comprising the complex, kits comprising complex or composition, as well as uses of the complex or composition.
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Page/Page column 30-32
(2021/05/21)
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- A method for preparing paipai pulls the xilin acid (by machine translation)
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The invention discloses a method for preparing paipai pulls the xilin acid. The invention is directed to preparation method in the prior existing "N - ethyl hydrogen peroxide piperazine conversion is relatively low, a condensation step the non-condensable gas carbon dioxide, solvent loss is relatively large" disadvantages, this invention adopts the pyridine in place of the triethylamine as acid, in the acylation reaction of adding triphosgene is added a catalytic amount of 4 - dimethyl amino pyridine as an initiator, can effectively improve the reaction activity of the triphosgene, so that the N - ethyl hydrogen peroxide piperazine acyl chloride conversion is improved by about 10%. The invention in the condensation reaction, binary weak alkali such as for calcium carbonate to replace the one dollar weak alkali sodium bicarbonate, help to reduce the degradation, condensation reaction yield is improved by about 5%, at the same time can reduce the generation of carbon dioxide gas causes non-condensable 50%. (by machine translation)
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Paragraph 0028-0029; 0031-0032; 0034-0035; 0037-0038; 0041
(2019/05/22)
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- Process for preparing 6-/D(-)-Alpha-(4-ethyl-2,3-dioxo-1-piperazine-carboxamido)-phenylacetamido/pennicillanic acid
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Disclosed is a process for preparing 6-[D(-)-alpha-(4-ethyl-2,3-dioxo--1-piperazinecarboxamido)-phenylacetamido] penicillanic acid as well as pharmaceutically acceptable alkali metal salts thereof of the formula (I) wherein A represents a hydrogen atom, a sodium atom or a potassium atom, wherein active thioesters of 4-ethyl-2,3-dioxo-1-piperazinecarboxylic acid of the formula (II) wherein R represents a 2-mercaptobenzimidazole radical, 2-mercaptobenzoxa-zole radical and preferably 2-mercaptobenzothiazole radical, is condensed with silylated form of 6-[D(-)-alpha-aminophenylacetatamido] penicillanic acid of the formula (III) The compound of the formula II is a novel compound.
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- Novel penicillins and cephalosporins and process for producing the same
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Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.
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- Novel penicillins and cephalosporins and process for producing the same
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Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
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