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A new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2

A technology of o-chlorobenzylpyrrolidone and its crystal form, applied in medical preparations containing active ingredients, drug combinations, organic chemistry, etc.

Active Publication Date: 2021-04-27
北京优和康生物医药科技有限公司
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  • 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

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  • A new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2
  • A new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2
  • A new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2

Examples

Experimental program
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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 a mixed solvent of dichloromethane and n-heptane with a volume ratio of 1:5 to it, and fully dissolve it. Stand still in a fume hood for crystallization, collect the crystals, and dry them in vacuum to obtain the crystalline form B of fencrotone.

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 a mixed solvent of dichloromethane and n-heptane with a volume ratio of 3:1 therein, and fully dissolve it. Place in a refrigerator to cool down and crystallize, collect the crystals, and dry them in vacuum to obtain the crystalline form B of fencrotone.

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Abstract

The present invention relates to a new crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, and a pharmaceutical composition containing the crystal form, a preparation method and an application. Compared with the prototype compound, this crystal form has a significantly enhanced effect on improving memory acquisition impairment caused by transient cerebral ischemia-reperfusion, and can be used to prepare calcium antagonists, anti-Alzheimer's disease, anti-depression, enhance learning and memory, etc. drug. The crystal form of fencrotone provided by the invention has simple preparation method, easy control of crystallization process, high crystallinity, good reproducibility of crystal form, 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 "Fencrotone". 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

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Application Information

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Patent Type & Authority Patents(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
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