Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of mitiglinide calcium

A technology of mitiglinide calcium and benzyl succinic acid, which is applied in the field of pharmacy, can solve the problems of long steps, lack of purity, and short steps, and achieve the effects of reducing related substances, saving reagents, and shortening reaction steps

Inactive Publication Date: 2018-04-27
JIANGXI JIMINKEXIN PHARMA +1
View PDF7 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The commonly used process route is as follows: use dimethyl succinate and benzaldehyde as raw materials, undergo Stobble condensation, hydrolysis, and dehydration to form an acid anhydride, condense with cis-perhydroisoindole, reduce to obtain racemic acid, and bromide Benzyl reaction, salt formation, the current problems: some steps are short, the purity cannot be achieved, and some processes reach the purity, but the steps are long, and there are 10 steps to complete the reaction

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
  • Preparation method of mitiglinide calcium
  • Preparation method of mitiglinide calcium
  • Preparation method of mitiglinide calcium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0066] Step 1: Synthesis of benzylidene succinic acid: Add 480 grams of anhydrous methanol and 65 grams of sodium methylate into the reaction tank to stir and dissolve, add 450 grams of diethyl succinate, heat to reflux, and drop 100 grams of benzene Formaldehyde, reflux for not less than 1 hour, then distill methanol, slowly add 480 grams of 40% sodium hydroxide solution, add drinking water, dichloromethane, stir for 30-60 minutes, add concentrated hydrochloric acid dropwise to adjust the pH value to 2- 3. Precipitate the product and dry it.

[0067] The molar ratio of diethyl succinate and benzaldehyde to the above reaction is 5.0.

[0068] Step 2: Synthesis of benzyl succinic acid: dissolve benzylidene succinic acid with 4.8 times the absolute ethanol of benzylidene succinic acid, add 3% activated carbon for decolorization for 2 hours, filter the activated carbon, add to the reaction tank and stir, pass through Nitrogen, exhaust the air, add 25 grams of 10% palladium carbo...

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 a preparation method of mitiglinide calcium, which includes steps of step 1, synthesis of benzal butanedioic acid; step 2, synthesis of benzylsuccinic acid; step 3, synthesisof (S)-benzylsuccinic acid (R)-alpha- phenylethylamine; step 4, synthesis of (S)-benzylsuccinic acid; step 5, synthesis of 2S-dihydro-isoindole indolebutyric acid; step 6, synthesis of crude product of mitiglinide calcium; step 7, refining of mitiglinide calcium.

Description

technical field [0001] The invention belongs to the field of pharmacy, and the invention relates to a preparation method of mitiglinide calcium. Background technique [0002] Miglinide calcium dihydrate, the chemical name is: bis[(2s)-2-benzyl-3-(cis-hexahydroisoindole-2-carbonyl)propionic acid] monocalcium dihydrate, the structural formula is as follows : [0003] [0004] Molecular formula: C38H48CaN2O6 2H2O [0005] Molecular weight: 704.91 [0006] Miglinide Calcium is a hypoglycemic drug developed by Japan Tachibana Co., Ltd., and it is a new type of benzylsuccinic acid insulin secretion accelerator. Miglinide closes the ATP-dependent K+ channel on the pancreatic β-cell membrane, causing Ca2+ influx, increasing the intracellular Ca2+ concentration and degranulating the extracellular insulin-containing vesicles, thereby stimulating insulin secretion. Miglinide Calcium Tablets (the original research company Tachibana Pharmaceutical Industry Co., Ltd.) was launched ...

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): C07D209/44
CPCC07D209/44
Inventor 李义保文万江彭常春何平清马利雄赵有红彭启华余宣
Owner JIANGXI JIMINKEXIN PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com