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Method for preparing Tebipenem pivoxil

A technology of tipipenem ester and molar ratio, applied in the field of medicine, can solve the problems of high equipment requirements, high price, difficult recycling and the like

Active Publication Date: 2018-10-12
科兴生物制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the Pd / C catalyst used in the technical solution with the patent application number CN201710764108.1 is very expensive due to the Pd / C catalyst, and it has high requirements for the equipment used and is difficult to recycle. Its catalytic performance needs to be further improved

Method used

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  • Method for preparing Tebipenem pivoxil
  • Method for preparing Tebipenem pivoxil
  • Method for preparing Tebipenem pivoxil

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preparation example Construction

[0032] In order to solve the above problems, the present invention provides a preparation method of tipipenem pixil, at least comprising the following steps:

[0033] Step 1: Add the first raw material, the second raw material, the solvent, and the first acid-binding agent into the reaction kettle in sequence, control the reaction temperature -5~0°C, and the reaction time is 1~1.5h. After the reaction is completed, add water to the system Afterwards, carry out suction filtration under reduced pressure to obtain a filter cake; add isopropanol to the filter cake, stir at room temperature, and suction filtration under reduced pressure again, and dry to obtain a condensate;

[0034] Step 2: Add the condensate, n-butanol, water, sodium bicarbonate and catalyst in the reaction kettle in step 1, first replace the air in the reaction kettle with nitrogen, and then pass hydrogen into the reaction kettle to carry out the hydrogenation reaction , after the reaction is completed, perform ...

Embodiment 1

[0078] Embodiment 1 of the present application provides a preparation method of tipipenem pixil, at least including the following steps:

[0079] Step 1: Add 0.5 mol of the first raw material, 0.515 mol of the second raw material, 4L of solvent, and 0.3 mol of the first acid-binding agent into the reaction kettle in sequence, control the reaction temperature at -3°C, the reaction time is 1.5h, and the reaction ends Finally, after adding 5L of pure water to the system, vacuum filtration was carried out to obtain a filter cake; 2.5L of isopropanol was added to the filter cake, stirred at room temperature, vacuum suction filtration again, and drying to obtain a condensate;

[0080] Described solvent is acetonitrile;

[0081] The first acid-binding agent is triethylamine;

[0082] Step 2: the condensate in step 1, the n-butanol of 0.75L, the water of 1.5L, 6g sodium bicarbonate and 15g catalyzer are added in the reactor, first replace the air in the reactor with nitrogen 3 times,...

Embodiment 2

[0103] Embodiment 2 of the present application provides a preparation method of tipipenem pixil, at least including the following steps:

[0104] Step 1: Add 0.5 mol of the first raw material, 0.515 mol of the second raw material, 4L of solvent, and 0.3 mol of the first acid-binding agent into the reaction kettle in sequence, control the reaction temperature at -3°C, the reaction time is 1.5h, and the reaction ends Finally, after adding 5L of pure water to the system, vacuum filtration was carried out to obtain a filter cake; 2.5L of isopropanol was added to the filter cake, stirred at room temperature, vacuum suction filtration again, and drying to obtain a condensate;

[0105] Described solvent is acetonitrile;

[0106] The first acid-binding agent is selected from: a mixture of triethylamine, 1,8-diazabicyclo[5.4.0]-7-undecene, wherein triethylamine, 1,8-diaza The molar ratio between bicyclo[5.4.0]-7-undecene is 30:1;

[0107] Step 2: the condensate in step 1, the n-butan...

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Abstract

The invention relates to the technical field of medicines and particularly relates to a method for preparing Tebipenem pivoxil. The method for preparing the Tebipenem pivoxil, provided by the invention, at least comprises the following steps: (1) condensation reaction; (2) hydrogenation reaction; (3) esterification reaction; and (4) purification and refining.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to a preparation method of tipipenem axetil. Background technique [0002] Tipipenem is currently the only oral carbapenem antibiotic. Because it is obtained by converting the C2 acid into pivate, its oral absorption is greatly increased, and it is even better than most β-lactam antibiotics already on the market. In pediatric clinics in my country, Haemophilus influenzae and Streptococcus pneumoniae are the main pathogenic bacteria of bacterial ENT and upper respiratory tract infections in children, and their drug resistance has been greatly enhanced. Research on a new drug with stronger antibacterial properties It is very necessary, and tipipenem axetil came into being, which has a good curative effect on various inflammations, and its antibacterial activity is stronger than that of amoxicillin, levofloxacin, cefdinir, etc. on the market, so its market prosp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D477/20C07D477/06
CPCC07D477/06C07D477/20
Inventor 仇渡先郝志海张允王翠翠崔宁
Owner 科兴生物制药股份有限公司
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