A preparation method for a biapenem active ingredient, comprising: 1) dissolving crude biapenem in water to prepare an aqueous solution; 2) adding activated carbon, stirring for decolorization, filtering, and cooling the filtrate for use; 3) adding the filtrate dropwise in a pre-cooled mixed solvent of acetone and ethanol, and crystallizing; 4) growing crystals; and 5) separating, washing, and drying the precipitated crystals to obtain a biapenem active ingredient.
C07D 519/06 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or containing at least one condensed beta-lactam ring system, provided for by groups , or , e.g. a penem or a cepham system
2.
PREPARATION METHOD FOR MEROPENEM KEY INTERMEDIATE N-TRIMETHYLSILYLIMIDAZOLE
Provided is a preparation method for N-trimethylsilylimidazole, said method comprising the following steps: 1) under the protection of inert gas, heating imidazole and hexamethyldisilazane to T1, and allowing to react for 1-4 hours; 2) after completing step 1, cooling the reaction system to 30-50°C, evacuating until the vacuum degree is V1, heating to T2, performing distillation at reduced pressure, and collecting a front fraction D1 below 90°C; 3) after completing step 2, heating the reaction system to T3, and collecting a fraction D2 at 95-105°C; after completing step 3, the residual in the reaction system is imidazole.
The present invention relates to a method for preparing an imipenem active pharmaceutical ingredient, the method comprising the following steps: 1) dissolving crude imipenem in water at 5-25°C to obtain an aqueous solution of imipenem; 2) concentrating the aqueous solution of imipenem obtained in step 1) by passing through nanofiltration so as to obtain a concentrated aqueous solution of imipenem; 3) decolorizing the concentrated aqueous solution of imipenem obtained in step 2) by means of activated carbon, filtering out the activated carbon, and then crystallizing; and 4) separating, washing, and drying the crystal precipitated in step 3) so as to obtain an imipenem active pharmaceutical ingredient. Said method has a simple, compact and controllable process, and at the same time has high product yield, high purity and low costs, and has huge economic advantages.
Disclosed in the present invention is a bulk drug of meropenem, characterized in that the meropenem content in the bulk drug is 98.5%~101.0% based on the anhydrous substances; the impurities A and B in the related substances of the bulk drug are both no more than 0.25%; any single unknown impurity is no more than 0.05%; the sum of the other impurities in addition to A and B is no more than 0.2%; the residue of acetone is no more than 400ppm, preferably no more than 100ppm. Also disclosed in the present invention is a meropenem pharmaceutical composition with very good stability for injection using the meropenem bulk drug provided by the present invention as the active ingredient. The meropenem bulk drug provided by the present invention has high purity, well-defined impurity levels, low residual solvent content, good solubility, and good stability for long-term storage, so it ensures that the drug is effective and safe. The present invention has a simple process, a very low cost, a compact process, and is easy to control, so it is suitable for the production of sterile meropenem bulk drug and pharmaceutical preparations on an industrial scale.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
Provided is a method for preparing ertapenem sodium. In the method provided by the invention, ertapenem sodium is prepared by directly catalytic hydrogenation of an undried ertapenem intermediate or by catalytic hydrogenation of the ertapenem intermediate being dried at 20~30℃ to a water content of 5~65%。The method provided by the invention is advantageous to getting ertapenem sodium with a high quality simply and efficiently.
C07D 477/06 - Preparation from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
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