161715-24-8Relevant articles and documents
Preparation method of medicinal tebipenem pivoxil
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, (2021/05/19)
The invention discloses a preparation method of medicinal tebipenem pivoxil, which comprises the following steps: taking MAP and YKTP-1 as raw materials, sequentially carrying out condensation, reduction and substitution reaction, and purifying the material after the substitution reaction twice to obtain the medicinal tebipenem pivoxil. A primary purification process comprises the following steps: adding ethyl acetate into the material after the substitution reaction, conducting filtering, adding water into the filtrate, adjusting the pH value, carrying out liquid separation to obtain a water layer, adjusting the pH value of the water layer, conducting extracting with ethyl acetate to obtain an organic layer, washing the organic layer, conducting drying, decolorizing and filtering, carrying out vacuum concentration on the filtrate, conducting crystallizing and centrifuging, leaching a filter cake with ethyl acetate, and conducting drying in vacuum to obtain YKTP-4; and a secondary purification process comprises the following steps: mixing YKTP-4 with ethyl acetate, adding activated carbon, conducting stirring, conducting filtering to obtain filtrate, concentrating the filtrate to YKTP-4 under reduced pressure, conducting crystallizing and centrifuging, leaching a filter cake with ethyl acetate, and performing vacuum drying to obtain the medicinal tebipenem pivoxil.
Tebipenem pivoxil and synthetic method thereof
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Paragraph 0084-0098, (2019/07/04)
The invention provides tebipenem pivoxil and a synthetic method thereof. The invention relates to the technical field of drug synthesis. The synthetic method comprises the three-step synthetic reactions of condensation of a main ring and a tebipenem side chain, a TB-1 hydrogenation reduction reaction, and a reaction of a TB-2 intermediate and iodomethyl pivalate. The preparation method of tebipenem pivoxil provided by the invention is simple and convenient in preparation process, suitable for industrial production, and relatively high in yield; processing operations, such as column chromatography, which are required to be adopted by traditional synthesis are eliminated; a reasonable synthetic route is designed; the reaction time is effectively shortened; the post-processing process is simplified.
Industrial preparation process more than the [...] method
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Paragraph 0028; 0029; 0033; 0035; 0037; 0039, (2018/04/01)
The invention relates to the field of medical chemistry, and specifically relates to a tebipenem pivoxil industrial preparation method. The method comprises the following steps: tebipenem, a solvent I, salt, and a phase-transfer catalyst are mixed, and a salt-forming reaction is carried out under normal temperature; chloromethylpivalate is added under a same temperature, and an esterification reaction is carried out; when the reaction is finished, extraction and concentration are carried out; a solvent II is dropped for crystallization; and filtering is carried out, such that tebipenem pivoxil is obtained. With the method, operation is simple, and complicated operations of pH regulation and repeated extraction are avoided. Post-treatment solvent dose is low, such that resource is saved, and environment pollution is reduced. Chloromethylpivalate property is stable, and normal-temperature reaction requirement is low. Product yield is high, and a maximal yield can be higher than 88%. The purity of synthesized tebipenem pivoxil can be higher than 99.7%. Without refining, the obtained tebipenem pivoxil can be used for preparing medicine preparations as a raw material medicine satisfying medical requirements, and the medicine preparation can be safely used by patients. The method is suitable for industrial productions.
