Process for preparing sodium azlocillin

A technology of azlocillin sodium and ampicillin, which is applied in the field of drug preparation, can solve the problems of long method steps, harsh reaction conditions, and high operating conditions, and achieve the effect of solving the problem of "three wastes" treatment, mild reaction conditions, and good product quality

Inactive Publication Date: 2005-10-19
黄春荣
View PDF4 Cites 11 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] The method of route 2 has long steps and high operating conditions, so it is not suitable for use
[0018] The method yield of route 3 is low (42%), and activator preparation is difficult, and operation requirement is higher, should not adopt
[0019] Although the method yield of route 4

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Process for preparing sodium azlocillin
  • Process for preparing sodium azlocillin
  • Process for preparing sodium azlocillin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (1) Raw material

[0043] raw material name

Feeding amount

molar weight

The molar ratio of

Remark

Ampicillin

1400g

3.47

1.05

Deionized water

14L

2-Imidazolidinone chloride

490g

3.3

1

Triethylamine

506mL

3.47

1.05

ethyl acetate

17L

Anhydrous Sodium Carbonate

368g

Methanol

2.3L

3N hydrochloric acid

1.47L

ethyl acetate

6L

Sodium isooctanoate

608.5g

3.64

1.1

ethyl acetate

5L

Washed products

[0044] (2) Process steps

[0045] Add 14 liters of water into a 50-liter reaction tank, cool to 4°C, add 1400g of ampicillin while stirring, slowly add 506ml of triethylamine dropwise at 4°C, and finish the dropwise addition in about half an hour, continue to stir for half an ho...

Embodiment 2

[0049] (1) Raw material

[0050] raw material name

Feeding amount

molar weight

The molar ratio of

Remark

Ampicillin

1467g

3.64

1.10

Deionized water

14L

2-Imidazolidinone chloride

490g

3.3

1

Triethylamine

530mL

3.64

1.10

ethyl acetate

17L

Anhydrous Sodium Carbonate

368g

Methanol

2.3L

3N hydrochloric acid

1.47L

ethyl acetate

6L

Sodium isooctanoate

636.2g

3.83

1.15

ethyl acetate

5L

Washed products

[0051] (2) Process steps

[0052] Add 14 liters of water into a 50-liter reaction tank, cool to 0°C, add 1467g of ampicillin while stirring, slowly add 530ml of triethylamine dropwise at 0°C, continue stirring for half an hour, and then the reaction solution becomes cle...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The preparation process of sodium azlocillin includes the following steps: 1. adding triethylamine slowly into water solution of ampicillin at 0-4 deg.c and stirring to clarify the reaction liquid; 2. adding 2-imidazolidinyl ketacyl chloride into the solution at 0-4 deg.c while dropping water solution of Na2CO3 or NaHCO3 to control pH 7.5-8.5 and performing condensation; 3. adding ethyl acetate into the reaction mixture at 0-5 deg.c and regulating pH value to 1.7-1.9; 4. separating to obtain organic phase, and eliminating heat source and impurity to obtain crystallization liquid; and 5. adding ethyl acetate solution of sodium isocaprylate to crystallize, separating and drying to obtain powdered white sodium azlocillin. The process has convenient operation, mild reaction condition, high yield and high product quality.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and more specifically, the invention provides a preparation method of azlocillin sodium. Background technique [0002] The chemical name of azlocillin sodium (benmidazole penicillin) is (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidine carboxamide Base-2-phenylacetamido)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt, its chemical formula is shown in formula (I). 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 Infections in other parts, such as amikacin, gentamicin, and netilmicin, can produce synergistic effects. [0003] [0004] Molecular formula: C 20 h 22 N 5 NaO 6 S molecular weight:...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07D499/46
Inventor 杨立志
Owner 黄春荣
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap