(R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, and preparation method and use thereof

A pyrrolidineacetamide, -4- technology, applied in the direction of organic chemical methods, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problem of less research on preparation methods and crystal forms, and no crystal form of pyrrolidineacetamide , disclosure and other issues

Inactive Publication Date: 2018-07-20
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the preparation method and crystal form of (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide are less, and there is no (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide Crystal Form Disclosure

Method used

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  • (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, and preparation method and use thereof
  • (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, and preparation method and use thereof
  • (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Add 50 mg of (R)-4-hydroxy-2-oxo-1-pyrrolidine acetamide to 2 mL of sec-butanol, stir continuously, heat to 40°C, and filter to obtain a supersaturated solution, which is sealed and placed at -19 Cool and crystallize at ℃ for 24 hours to obtain colorless sand-like crystals.

Embodiment 2

[0056]The (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide colorless sand granular crystal obtained in Example 1 is subjected to crystal parameter measurement, including powder diffraction measurement, infrared spectrum measurement, differential calorimetry measurement, Thermogravimetric assay. Test instrument conditions: The test uses a DX2500 X-ray diffractometer (Danfang Yuan Instrument, Liaoning) to analyze the pre-oxidized body and carbonized particles in each stage of the thermal stabilization process. Ni filter, CuKα as radiation source, X-ray wavelength λ=0.1541nm, acceleration voltage and current intensity are 40kV and 50mA respectively. Set the scanning interval to 0.02°, the scanning speed to 3° / min, and the scanning range to 5° to 45°. The crystals prepared in Example 1 have diffraction angles 2θ of 12.423, 14.928, 16.285, 16.465, 17.344, 19.198, 20.459, 20.707, 21.548, 21.889, 23.203, 25.054, 26.117, 29.913, 30.49, 35.1369, 37° peak, powder diffraction results as fi...

Embodiment 3

[0072] In 2mL of isopropanol, add 20mg of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, stir continuously, heat to 50°C, and filter to obtain a supersaturated solution, which is sealed and placed in- Cool and crystallize at 17°C for 3 hours to obtain colorless sand-like crystals. Identified by the method of Example 2, it is (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form I.

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Abstract

The invention provides an (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form has diffraction peaks at 2theta of 12.423 + / - 0.2 DEG, 16.465 + / - 0.2 DEG, 17.344 + / - 0.2 DEG, 21.889 + / - 0.2 DEG and 25.054 + / - 0.2 DEG. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form can promote the synthesis of phosphorylcholine and o-acylethanolamine, promote brain metabolism, has a stimulation effect on the specific central nervous pathway through blood brain barrier, and has special bioactivity in calming and anti-epilepsy fields. Thepeak melting temperature of the (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form is 133.1 + / - 2 DEG C, and the (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form has a fast dissolution rate in water, has a solubility in water of 100 mg / mL or more, has a high bioavailability, a good stability and a good particle fluidity, and is suitable for being applied to the production of medicinalpreparations, storage and transportation; and the (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form is suitable for preparing various medicinal compositions, and also can be processed to prepare various preparations, such as a tablet, a capsule, a dripping pill, a sustained release and controlled release preparation and a lyophilized powder injection. The preparation method is simple, and is suitable for industrial production.

Description

technical field [0001] The present invention relates to (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide, in particular to a crystal form and preparation method of (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide and uses. Background technique [0002] (R)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide (CAS No. 68252-28-8), the dextrorotatory version of the nootropic drug 4-hydroxy-2-oxo-1-pyrrolidineacetamide body. The latest research shows that this compound has special biological activities in the fields of sedation and anti-epileptic, and it has low toxicity and wide range of drug safety. It is expected to become a substitute for the existing highly toxic anti-epileptic drugs. The specific structure of (R)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide is as follows: [0003] [0004] (R)-4-Hydroxy-2-oxo-1-pyrrolidineacetamide [0005] To effectively develop (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide into pharmaceuticals, a solid state form with ease of manufacture and acceptable chemical...

Claims

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Application Information

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IPC IPC(8): C07D207/273A61K31/4015A61P25/08
CPCC07D207/273C07B2200/13A61K31/4015A61P25/08A61K9/2095A61K9/4858C07D207/46
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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