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Crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2

A technology of o-chlorobenzyl pyrrolidone and crystal form, applied in the field of crystal form of trans-4-phenyl-5-o-chlorobenzyl pyrrolidone-2, achieves good reproducibility, improves bioavailability, and enhances learning effect of memory

Active Publication Date: 2020-06-02
北京优和康生物医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no report about the crystal form of this compound

Method used

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  • Crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2
  • Crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2
  • Crystal form of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Take 100 mg trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 sample, prepare acetone / ethyl acetate (1:1) mixed solvent 50 ℃ nearly saturated solution, drop to 0 at a rate of 0.5 ℃ / min Crystallize at °C, collect the crystals, and dry to prepare a trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A sample.

[0030] The single crystal diffraction data of the crystal were measured, and the diffraction pre-experiment and diffraction data collection were carried out using a Bruker D8VENTURE single crystal diffractometer (Mo / Kα, ) in a temperature environment of 175K. Diffraction data were processed using the APEX3 software package. Based on the 9943 diffraction points collected within the angle range of 2.383°figure 2 .

Embodiment 2

[0032] Take 200mg trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 sample, prepare methyl isobutyl ketone / 2-methyltetrahydrofuran (1:1) mixed solvent 50 ℃ nearly saturated solution, at 0.3 ℃ / min rate was reduced to 2°C for crystallization, and the crystals were collected and dried to obtain a trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A sample.

Embodiment 3

[0034] Take 200 mg trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 sample, prepare tetrahydrofuran / n-heptane (1:1) mixed solvent 50 ℃ nearly saturated solution, drop to 5 at a rate of 0.1 ℃ / min Crystallize at °C, collect the crystals, and dry to prepare a trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A sample.

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Abstract

The invention relates to a new crystal form A of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, as well as a medicine composition comprising the crystal form and application thereof. The crystal form Acan be used for preparing medicines such as high-selective calcium antagonists and medicines for improving disordered brain function, resisting Alzheimer's disease and depression, and enhancing learning and memory capability. The preparation method of the trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 crystal form A is simple in operation and is controllable in crystallization process. The producthas high crystallization degree and good repeatability, and can be absorbed and utilized by body better.

Description

technical field [0001] The invention relates to a new crystal form A of trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2, a pharmaceutical composition containing the crystal form and applications 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 preparing anti-senile dementia and enhancing learning and memory drugs. The chemical structural formula of the compound is as follows: [0003] [0004] trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 [0005] It has highly selective calcium antagonistic activity on nerve cells, and has the effects of improving brain dysfunction, treating senile dementia, and enhancing learning and memory. Chinese patent 94104879.9 discloses its synthesis method and its application in the preparation of drugs for anti-senile demen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/26A61P25/00A61P25/28A61P25/24A61K31/4015
CPCA61P25/00A61P25/24A61P25/28C07B2200/09C07B2200/13C07D207/26
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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