Check patentability & draft patents in minutes with Patsnap Eureka AI!

Method for preparing pantoprazole sodium sesquihydrate

A technology of sesquihydrate and pantoprazole sodium, which is applied in the field of providing the preparation of pantoprazole sodium sesquihydrate, can solve the problems of being unsuitable for commercial production, the quality of raw materials, and complicated operations, and achieves The effect of increasing market competitiveness, easy control of drying methods, and simplified preparation process

Pending Publication Date: 2021-10-01
BEIJING XINLINGXIAN MEDICAL TECH DEV CO LTD
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage is also the relatively cumbersome operation. In addition, it potentially brings the risk of negative quality of raw materials. Acetone and dichloromethane are used in the process.
The European Agency for Drug Quality Supervision (EDQM) clearly stipulates that acetone has a very high risk of being polluted by the Class I solvent benzene (limit ≤ 2ppm), and dichloromethane (limit ≤ 600ppm) is also not recommended as a Class II solvent Therefore, this method is not suitable for commercial production in order to ensure the quality of raw materials and avoid the waste of research and development resources caused by the minimum solvent in the research and development process

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
  • Method for preparing pantoprazole sodium sesquihydrate
  • Method for preparing pantoprazole sodium sesquihydrate
  • Method for preparing pantoprazole sodium sesquihydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Add 300ml of ethyl acetate, 2.8g of purified water and 50.00g of pantoprazole into a 500ml reaction bottle, slowly add sodium hydroxide in batches under stirring, after the addition is complete, raise the temperature to 40°C and stir for 10 minutes, then add 1.5g after dissolving Activated carbon, heat preservation and stirring for 30min, suction filtration, cooling the filtrate to -10~0°C to crystallize for 6 hours, suction filtration, vacuum drying at 30°C for 12 hours to obtain 51.27g of white crystalline powder, moisture 6.226%, yield 90.92g, HPLC Purity: 99.97%;

Embodiment 2

[0041] Add 400ml of methyl isobutyl ketone, 3.2g of water, and 50.00g of pantoprazole into a 500ml reaction bottle, slowly add 20.67g of sodium carbonate in batches under stirring, after the addition is complete, heat up to 60°C and stir for 30min, then add 1.2g of activated carbon , heat preservation and stirring for 30 minutes, hot filtration, cooling the filtrate to 5-10°C, heat preservation and crystallization for 12 hours, suction filtration, vacuum drying at 45°C to obtain 50.87g of off-white crystalline powder, moisture 6.432%, yield 90.21%, HPLC purity: 99.93%.

Embodiment 3

[0043] Add 800ml of methyl tert-butyl ether, 28.17g of water, and 120.00g of pantoprazole into a 1L reaction bottle, slowly add 25.04g of sodium hydroxide in batches under stirring, after the addition is complete, heat up to 50°C, stir for 30min, and add activated carbon , 4.8g, heat preservation and stirring for 30min, hot filtration, cooling the filtrate to 20-30°C, heat preservation and crystallization for 8 hours, suction filtration, vacuum drying at 45°C to obtain 129.06g of off-white crystalline powder, moisture 6.375%, yield 95.36%, HPLC Purity: 99.90%.

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 invention relates to the field of medicinal chemistry, and provides a method for preparing pantoprazole sodium sesquihydrate. The method for preparing the pantoprazole sesquihydrate comprises the following steps: adding pantoprazole, an organic solvent, purified water and an aqueous inorganic alkali solution into a reaction container, adding 0.3-5.0% by weight of activated carbon, stirring for 30 minutes, filtering out the activated carbon, cooling obtained filtrate to a certain temperature, stirring for crystallizing, performing suction filtration to obtain a pantoprazole sesquihydrate wet product, and drying at a certain temperature to obtain white-like crystalline powder. The operation is simple and convenient, the condition is mild, and the product can be obtained with high yield and high purity.

Description

technical field [0001] The invention provides a preparation method of pantoprazole sodium sesquihydrate (Pantoprazole Sodium sesquihydrate). This method prepares 5-difluoromethoxy-2-[[(3,4-dimethoxy 2-pyridyl)methanol by reacting pantoprazole and inorganic base in a mixed solvent of organic solvent and purified water Base]sulfinyl]-1H-benzimidazole sodium sesquihydrate (pantoprazole sodium sesquihydrate). Background technique [0002] Pantoprazole Sodium Sesquihydrate (Pantoprazole Sodium Sesquihydrate), the chemical name is 5-difluoromethoxy-2-[[(3,4-dimethoxy 2-pyridyl)methyl]sulfinyl] -1H-benzimidazole sodium sesquihydrate, its chemical structural formula is: [0003] [0004] Pantoprazole sodium is a kind of medicine that is used for the treatment of gastrointestinal ulcer developed by German Becton pharmaceutical company, is the third proton pump inhibitor after omeprazole and lansoprazole. The bulk drug of pantoprazole sodium included in European, American and In...

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): C07D401/12
CPCC07D401/12
Inventor 何杰王辉高世静陶新华
Owner BEIJING XINLINGXIAN MEDICAL TECH DEV CO LTD
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com