- A chloroflurocarbon synthesis method for carbenicillindisodium (by machine translation)
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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)
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Paragraph 0052-0099
(2019/03/24)
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- Flucloxacillin sodium monohydrate synthetic method
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The invention discloses a method for compounding flucloxacillin sodium-hydrate, which belongs to the technical field of drug synthesis, and comprises the steps: 6-aminopenicillanic acid (6-APA) is salified, then 3-(2-chloro-6-fluorophenyl)-5- methyl isoxazole-4-formyl chloride or equivalents thereof are added to do an acylation reaction, and then acids are added drop by drop to adjust a potential of hydrogen (pH) value to obtain flucloxacillin acid aqueous solutions. Organic solution is used to extract, and organic phases are washed, dried and filtered to obtain flucloxacillin acid solutions through saturated salt water, then white solids are dissolved out in the flucloxacillin acid solutions which are added with sodium iso-octoate solutions, and products are obtained by controlling temperature and crystallizing. The method for compounding the flucloxacillin sodium-hydrate does not separate intermediate flucloxacillin acids, obtained flucloxacillin acids are directly salified with sodium iso-octoate after being extracted trough the organic solution, reduces separation steps and operation process, also reduces usage amount and times of organic solution simultaneously, greatly reduces discharge amount of organic solution relative to patent documentation CN 102964356A, reduces production cost above 20%, and obviously improves economic and environmental values.
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Paragraph 0032-0036; 0038-0042; 0043-0047; 0048-0051
(2017/09/01)
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- A method of preparing sodium Flucloxacillin
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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.
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Paragraph 0026; 0029
(2017/04/07)
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- IMPROVED PROCESS FOR PREPARING PENICILLINS AND INTERMEDIATE COMPOUNDS
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Disclosed is an improved process for the preparation of isoxazolyl penicillins of formula (I), wherein X1 and X2 can be independently selected from the group comprising hydrogen, chlorine or fluorine, and its pharmaceutically suitable salts. The process is economic in -situ synthetic method without isolation of any intermediate. (I).
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Page/Page column 11
(2013/02/27)
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- Pharmaceutical formulations
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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.
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