Biphenyl ammonia acetate butantriol salt and preparation method thereof

A technology of felbinac tromethamine and phenylacetic acid tromethamine salt, which is applied in the field of felbinac tromethamine salt compound and its preparation, and can solve the problems that it can only be used as an external drug and affects the popularization and use of drugs. , to achieve the effect of simple and feasible synthesis process, reasonable design and easy access to raw materials

Active Publication Date: 2008-04-30
SHIJIAZHUANG YILING PHARMA
View PDF0 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, felbinac is insoluble in water and can only be used as an external drug, which has seriously affected the popularization and use of this drug. We screened through a large number of tests, and the screening results believe that the salt of felbinac tromethamine is the best form, so the combination Phenylacetic acid is made into the form of tromethamine salt, which solves the problems of felbinac well, which cannot be solved by ordinary technicians without creative work, nor is it obvious

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
  • Biphenyl ammonia acetate butantriol salt and preparation method thereof
  • Biphenyl ammonia acetate butantriol salt and preparation method thereof
  • Biphenyl ammonia acetate butantriol salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of felbinac tromethamine salt

[0022] In a dry and clean 250ml three-neck round bottom flask, add 21.2g (0.1mol) of felbinac and 210ml of methanol, heat to 60°C and stir until completely dissolved, then add 12.1g (0.1mol) of tromethamine at 60°C, and mix The solution was clear and transparent, stirred and reacted under this condition for 1 hour, and TLC detected that the reaction was complete. After cooling below 0°C for 5 hours, a large amount of white crystals precipitated, which were filtered by suction and vacuum-dried at 80°C to obtain 30.5 g of white crystalline felbinac tromethamine salt. Measured: mp: 162-163°C, yield 91.6%. The product is analyzed by elements (theoretical value: C64.9% H6.9% N4.2% O24%;

[0023] Measured value: C64.1% H7.3% N3.6% O25%), NMR, MS, UV, IR and HPLC analysis, the product is felbinac tromethamine salt, the purity is 99.5%.

[0024] Determination of felbinac tromethamine sample solubility:

[0025] A...

Embodiment 2

[0031] Embodiment 2: the preparation of felbinac tromethamine salt

[0032] In a dry and clean 250ml single-necked round bottom flask, add 21.2g (0.1mol) felbinac and 12.1g (0.1mol) tromethamine, add 150ml absolute ethanol to it, shake and heat to completely dissolve until clear , keep the temperature (50° C.) for 30 min, and concentrate to dryness under reduced pressure with a rotary evaporator to obtain a white powder. Dry in vacuum at 80°C to obtain 32.0 g of felbinac tromethamine salt. mp: 163-164°C, yield: 96.0%, the product is analyzed by elemental analysis, NMR, MS, IR, UV and high performance liquid chromatography, and the product is felbinac tromethamine salt with a purity of 99.2%.

Embodiment 3

[0033] Embodiment 3: the preparation of felbinac tromethamine

[0034] In a dry and clean 250ml three-necked round-bottomed flask, add 21.2g (0.1mol) felbinac and 200ml benzene, heat and stir until dissolved, then add 12.1g (0.1mol) tromethamine, mix until clear, The reaction was stirred at 70°C for 2 hours, and the end point of the reaction was identified by TLC. After the reaction was completed, a large amount of crystalline solid was precipitated by sufficient cooling, filtered by suction, washed with a small amount of anhydrous ether, and dried in a vacuum oven at 80°C to obtain 28.5 g of bismuth Tromethamine phenylacetate. mp: 163-164, yield 85.6%. The product is analyzed by elemental analysis, NMR, MS, IR, UV and HPLC. The product is felbinac tromethamine salt with a purity of 99.8%.

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

A felbinac tromethamine salt, the chemical formula is C18H23NO5. The invention has reasonable synthesis route design, simple and feasible synthesis process, easy-to-obtain raw materials, stable reaction conditions, high reaction yield, good product purity and no serious "three wastes" pollution in the reaction. Pharmacological experiments have proved that the compound has few side effects, no irritation, is easily soluble in water, and has low toxicity to ensure the safety of medication. The preparation is simpler, easier to implement, and easier to control. Analgesic effect, it may be further developed as antipyretic and analgesic new drugs.

Description

Technical field: [0001] The invention relates to a felbinac tromethamine salt compound, a preparation method and application thereof. Background technique: [0002] Antipyretic and analgesic drugs have been used by humans for more than 150 years. Now, antipyretic and analgesic drugs have become an indispensable and important drug in people's daily life. They are one of the most widely used and most widely used medicines in the world. The global annual output of antipyretic and analgesic drugs has reached more than 200,000 tons, and the preparations are hundreds of billions of tablets. Paracetamol, aspirin, ibuprofen, naproxen, and diclofenac are the five pillar products, with a combined annual sales of over US$5 billion. [0003] As an anti-inflammatory and analgesic drug, felbinac was launched in Japan, Italy and other countries in 1993 for the treatment of osteoarthritis, periarthritis of the shoulder, tenosynovitis, peritendinitis, muscle pain, swelling pain after trauma...

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): C07C57/38C07C215/10C07C215/40A61K31/133A61K31/192A61P29/00
Inventor 陈文展王伟
Owner SHIJIAZHUANG YILING PHARMA
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