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Preparation method of azlocillin sodium and azlocillin sodium used for injection

A technology of azlocillin sodium and azlocillin acid, which is applied in the direction of organic chemistry, can solve the problems of low reaction efficiency, and achieve the effects of improving reaction efficiency, increasing yield, and being easy to dissolve

Active Publication Date: 2011-08-24
SUZHOU ERYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this method reacts in pure water, and the reaction efficiency is not high

Method used

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  • Preparation method of azlocillin sodium and azlocillin sodium used for injection
  • Preparation method of azlocillin sodium and azlocillin sodium used for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1 - the preparation of azlocillinic acid.

[0045] 1. Feeding formula:

[0046] Ampicillin Trihydrate 30 Kg

[0047]Acetone 50~55 Kg

[0048] Triethylamine 7.5 Kg

[0049] 1-Chloroformyl-2-imidazolidinone 10.92Kg

[0050] Purified water 240 Kg.

[0051] 2. crafting process:

[0052] Weigh the raw materials according to the above feeding formula, put acetone, purified water, and ampicillin trihydrate into the synthesis tank at about 25°C, and stir evenly. Cool the feed liquid in the synthesis tank. When the temperature is below 15°C, add triethylamine dropwise and stir to make the solution completely clear. Control the temperature of the feed liquid at 6~9°C and slowly add 1-chloroformyl-2-imidazolidinone at a uniform speed, and complete the addition within 25~30 minutes. After feeding, stir for 1 hour, and add 150L (150 Kg). Keep the temperature between 6~9℃, and stir for 2~3 hours. The reaction solution was concentrated, and hydrochloric acid was ...

Embodiment 2

[0053] Embodiment 2---the preparation of azlocillin sodium.

[0054] 1. Feeding formula:

[0055] Azlocillin acid: water for injection 1:3.0~3.5

[0056] Activated carbon for needles: 2.0~4.0% by weight of azlocillinic acid.

[0057] 2. Process:

[0058] Add the azlocillin acid prepared according to Example 1 into water for injection, and cool the feed solution to 0-5°C. Add 2M NaOH dropwise to adjust the pH to 7.0~7.5. Add activated carbon for needles, stir for 20 minutes, press filter, and decarbonize through a plate and frame filter. The decarbonized filtrate is sterilized and filtered through 0.45 μm and 0.22 μm filters to a 10,000-class clean area, and placed on a plate under a 100-class laminar flow to a freeze-drying box. The liquid thickness of each plate is about 10mm. When the temperature of the board layer drops below -30°C, the products are packed into boxes. Continue to cool down. After the product temperature reaches -40°C (about 1.5~2h), turn on the vacuu...

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Abstract

The invention provides a preparation method of azlocillin sodium and azlocillin sodium used for injection, and the azlocillin sodium and the azlocillin sodium used for injection which can be prepared by the method. The method comprises the steps of: in a new solution system, leading ampicillin trihydrate to have a reaction with 1- chloroformyl-2-imidazolone under the optimized temperature condition, and producing high-quality azlocillin acid with higher reaction efficiency and yield; and directly salifying, sterilizing and freeze-drying the prepared azlocillin acid, and obtaining the azlocillin sodium product used for injection.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a preparation method of azlocillin sodium and azlocillin sodium for injection, and azlocillin sodium and azlocillin sodium products for injection prepared by the method. Background technique [0002] Azlocillin sodium is a semi-synthetic penicillin with the chemical name (2S,5R,6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidine Formamido-2-phenylacetylamino)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt. The chemical formula is shown in the following formula I: [0003] . [0004] Azlocillin sodium is not destroyed by penicillinase produced by Staphylococcus aureus and is effective against enzyme-producing Staphylococcus aureus, mainly used for surrounding infections of penicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis, including internal organs, skin and soft tissues Infection of other parts. When combined with amikaci...

Claims

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Application Information

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IPC IPC(8): C07D499/04C07D499/16
Inventor 陈学文陆夕明顾丰陆文娟
Owner SUZHOU ERYE PHARMA CO LTD
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