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.
Preparation method of tebipenem pivoxil and intermediate thereof
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Paragraph 0074-0076; 0077-0079; 0080-0082; 0083-0088, (2018/01/13)
The invention provides a preparation method of tebipenem pivoxil. A three-step method synthesis route taking MAP (compound 2) and TAT (compound 3) as starting raw materials is adopted. The preparation method is characterized in that in the first step, the temperature of reaction for preparing an intermediate compound 4 of the tebipenem pivoxil from the MPA and the TAT is -4 to 5 DEG C. Compared with the preparation method using the three-step method synthesis route in the prior art, the preparation method has the following advantages: the step avoids ultralow reaction temperature, so that the method is mild in reaction condition, easy to implement and suitable for industrialized production; furthermore, the reaction yield in each step is increased and the purify of reactants is improved.