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

New crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2

A technology of o-chlorobenzylpyrrolidone and its crystal form, which is applied to medical preparations containing active ingredients, organic active ingredients, nervous system diseases, etc., to achieve good reproducibility, good stability, and the effect of improving learning and memory

Active Publication Date: 2020-05-08
北京优和康生物医药科技有限公司
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no reports about other crystal forms of fencrotone compound

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
  • New crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2
  • New crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2
  • New crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation example of embodiment 1 fencrotone crystal form B

[0021] Weigh an appropriate amount of fencrotone and place it in a 3ml glass bottle, to which a mixed solvent of dichloromethane and n-heptane is added at a volume ratio of 1:1. Fully dissolve, then filter the solution into a 4ml single crystal bottle through a PTFE filter head with a pore size of 0.45 μm, seal it with a single crystal bottle stopper and make a small hole on it, and place it in a fume hood for slow volatilization and crystallization at room temperature. The crystals were collected and dried in vacuum to obtain the crystalline form B of fencrotone.

Embodiment 2

[0022] The preparation example of embodiment 2 fencrotone crystal form B

[0023] Weigh an appropriate amount of fencrotone and place it in a 3ml glass bottle, add dichloromethane and n-heptane mixed solvent with a volume ratio of 1:5 to it, and fully dissolve it. Stand still in a fume hood for crystallization, collect crystals, and vacuum-dry to obtain the fencrotone crystal form B.

Embodiment 3

[0024] The preparation example of embodiment 3 fencrotone crystal form B

[0025] Weigh an appropriate amount of fencrotone and place it in a 3ml glass bottle, add dichloromethane and n-heptane mixed solvent with a volume ratio of 3:1 to it, and fully dissolve it. Place in the refrigerator to cool down and crystallize, collect the crystals, and dry them in vacuum to obtain the crystalline form B of fencrotone.

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 novel crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2, a pharmaceutical composition containing the crystal form, and a preparation method and applications of the crystal form. Compared with the prototype compound, the crystal form of the invention has the advantages that the improvement effect on memory acquisition impairment caused by transient cerebral ischemia reperfusion is obviously enhanced, and the crystal form can be used for preparing calcium antagonists, anti-senile dementia drugs, anti-depression drugs, learning and memory enhancing drugs andthe like. The phenchlobenpyrrone crystal form provided by the invention has characteristics of simple operation of preparation method, easy crystallization process control, high crystallinity, good crystal form reproducibility and good stability, and is suitable for preparation process application and long-term storage.

Description

technical field [0001] The invention relates to a new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, a pharmaceutical composition containing the crystal form, a preparation method and application thereof. Background technique [0002] Chinese patent ZL94104879.9 discloses the compound trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, and the common name of this compound is "fenkelone". The literature discloses the synthesis method of the compound and its application in the preparation of anti-senile dementia, anti-depression, and enhancing learning and memory drugs. The structural formula of the compound is as follows: [0003] [0004] It has highly selective calcium antagonistic activity on nerve cells, and has the functions of improving brain cell metabolism, treating senile dementia, anti-depression, and improving learning and memory. Chinese patent 94104879.9 discloses its synthesis method and its application in the preparation of drugs for anti-senile d...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/267A61K31/4015A61P25/00A61P25/28A61P25/24
CPCA61P25/00A61P25/24A61P25/28C07B2200/13C07D207/267
Inventor 李七一郝小江赵如胜龙祥
Owner 北京优和康生物医药科技有限公司
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