1847-24-1Relevant articles and documents
A chloroflurocarbon synthesis method for carbenicillindisodium (by machine translation)
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Paragraph 0052-0099, (2019/03/24)
The invention discloses a chloroflurocarbon synthesis method for carbenicillindisodium, comprises the following steps: (I) in triethylamine and under the action of the triethyl phosphate, 3 - (2 - chloro - 6 - fluorophenyl) - 5 - methyl-isoxazole - 4 - carboxylic acid and dibenzothiazyl disulfide occurred in dichloromethane in the condensation reaction, to obtain the active ester reaction solution; (II) to the step (I) of the active ester in the reaction solution by adding water and 6 - amino penicillanic acid, then drop adds the triethylamine carries out amidation reaction, after the reaction is finished after treatment to obtain the flucloxacillin sodium. The synthetic method avoids the use of acyl chloride intermediate, at the same time intermediate without purification, directly through the one-pot synthesis follow-up step, the operation is simple, and the yield of the product and high purity, convenient for industrialization. (by machine translation)
A method of preparing sodium Flucloxacillin
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Paragraph 0026; 0029, (2017/04/07)
The invention discloses a preparation method for flucloxacillin sodium. The method comprises: (1) adding an initial raw material 1 into dichloromethane, dropwise adding triethylamine, and then dropwise adding pivaloyl chloride for reaction, so as to obtain a mixed anhydride; (2) adding 6-APA into dichloromethane, then adding triethylamine, reacting until the material solution is clear, so as to obtain a 6-APA triethylamine salt solution; dropwise adding the mixed anhydride into the 6-APA triethylamine salt solution for reaction, then distilling at a reduced pressure to remove dichloromethane, so as to obtain an oily substance, then adding acetone into the oily substance, stirring, and filtering off triethylamine hydrochloride, so as to obtain an acetone solution of flucloxacillin triethylamine salt; and (4) adding water and an ethyl acetate solution of sodium 2-ethylhexanoate into the acetone solution of flucloxacillin triethylamine salt, controlling the temperature to be 0-40 DEG C after adding is finished, and crystallizing, so as to obtain flucloxacillin sodium monohydrate. The preparation method has the advantages of mild reaction conditions, high yield, good purity, simple operation, friendliness to environment, and the like.
Pharmaceutical formulations
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, (2008/06/13)
Microcapsules which have an average diameter of from 100μ to 300μ and which comprise 94% to 99.9% of a medicament coated by 0.1% to 6% of a coating agent may be formed into a powder with 0% to 95% excipients or a tablet or capsule with a carrier.