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Tazobactam ampicillin amide composite, its preparation method and application

A technology of zobactam ampicillin amide and ampicillin trihydrate, which is applied in the pharmaceutical field and achieves good application prospects

Inactive Publication Date: 2012-11-28
CHONGQING ACAD OF ANIMAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Effective against Gram-negative bacteria, but susceptible to drug resistance

Method used

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  • Tazobactam ampicillin amide composite, its preparation method and application
  • Tazobactam ampicillin amide composite, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Measure 100 mL of ethyl acetate, add 1 mmol of tazobactam, 3 mmol of N-hydroxysuccinimide (NHS), and 3 mmol of dicyclohexylcarbodiimide (DCC), fill with nitrogen, and stir Add 1mmol ampicillin trihydrate in batches, and stir for 24 hours at 5°C. After the reaction is completed, slowly pour the reactant into ice water under stirring, crystallize, filter with suction, and filter the cake with cold water and cold absolute ethanol in turn. washing. Pumping to dryness, and drying under reduced pressure, the crude product (I) was obtained as a white powdery solid. The crude product was added in batches to absolute ethanol at 50°C under stirring. After it was completely dissolved, it was cooled to room temperature in a water bath, and needle-like crystals were precipitated. Then cool it down to minus 15°C with an ice-salt bath and keep it warm for 3 hours. After suction filtration, the filter cake was washed twice with a small amount of cold absolute ethanol, and...

Embodiment 2

[0024] Example 2: Measure 150 mL of dioxane, add 2 mmol of tazobactam, 2 mmol of N-hydroxysuccinimide (NHS), and 2 mmol of dicyclohexylcarbodiimide (DCC), and fill with nitrogen to protect. Add 1mmol ampicillin trihydrate in batches under stirring, and stir for 5 hours at 30°C. After the reaction is completed, slowly pour the reactant into ice water under stirring, crystallize, and filter with suction. The filter cake is washed with cold water and cold anhydrous Ethanol wash. Pumping to dryness, and drying under reduced pressure, the crude product (I) was obtained as a white powdery solid. The crude product was added in batches to absolute ethanol at 60°C under stirring. After it was completely dissolved, it was cooled to room temperature in a water bath, and needle-like crystals were precipitated. Cool to 0°C with an ice-salt bath and keep warm for 1 hour. After suction filtration, the filter cake was washed twice with a small amount of cold absolute ethanol, and then drie...

Embodiment 3

[0025] Example 3: Measure 100mL of tetrahydrofuran and dioxane (1:1) mixed solvent, add 1.5mmol of tazobactam, 3mmol of N-hydroxysuccinimide (NHS), 5mmol of dicyclohexylcarbodiimide (DCC), under nitrogen protection, add 1mmol ampicillin trihydrate in batches under stirring, and stir for 12 hours at 20°C. After the reaction is completed, slowly pour the reactant into ice water while stirring, crystallize, suction filter, and filter The cake was washed successively with cold water and cold absolute ethanol. Pumping to dryness, and drying under reduced pressure, the crude product (I) was obtained as a white powdery solid. The crude product was added to absolute ethanol at 80°C in batches under stirring. After it was completely dissolved, it was cooled to room temperature in a water bath, and needle-like crystals were precipitated. Then cool it to minus 10°C with an ice-salt bath and keep it warm for 3 hours. After suction filtration, the filter cake was washed twice with a sma...

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PUM

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Abstract

The invention relates to a tazobactam ampicillin amide composite, its preparation method and application. The tazobactam ampicillin amide composite has a structural formula (I) as the following. The preparation method of the composite comprises: in the presence of dicyclohexycarbodiimide (DCC) and N-hydroxysuccinimide (NHS), carrying out an acylation reaction on tazobactam and ampicillin trihydrate, thus obtaining the tazobactam ampicillin amide composite (I). The tazobactam ampicillin amide composite can be used for treating swine acute bacterial infections.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a modified ampicillin complex, a preparation method and an application thereof. Background technique [0002] Ampicillin (Ampicillin, Ⅲ), the chemical name is D(-)6-(α-amino-phenylacetamide) penicillanic acid, white microcrystalline powder, the melting point of its anhydrous compound is 199-202°C (decomposition), Optical rotation +287.9° (water), slightly soluble in water, almost insoluble in ethanol, ether and chloroform. It is a broad-spectrum semi-synthetic penicillin with extremely low toxicity. The antimicrobial spectrum is similar to that of penicillin, and the bacteria that are sensitive to penicillin are less effective, and the antibacterial effect on Streptococcus viridans is similar to or slightly stronger than that of penicillin. Its efficacy against diphtheria bacillus, tetanus bacillus and actinomycetes is basically the same as that of penicillin. The effect on Enterococcu...

Claims

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Application Information

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IPC IPC(8): C07D519/06A61P31/04
Inventor 王建华王晓中林渝宁陈诚
Owner CHONGQING ACAD OF ANIMAL SCI
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