Method for crystal system conversion of zopiclone

A technology of zopiclone and conversion method, which is applied in the field of crystal form conversion of compounds, can solve the problems of low yield, difficulty in ensuring safety, difficulty in producing zopiclone, etc., and achieve high yield, safe and reliable production, large The effect of implementing value

Active Publication Date: 2008-06-11
QILU PHARMA HAINAN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is difficult to produce zopiclone that meets the requirements, and the isopropyl ether used in the method is an inflammable and explosive article, and large-scale production is difficult to guarantee safety, and the yield is low

Method used

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  • Method for crystal system conversion of zopiclone
  • Method for crystal system conversion of zopiclone
  • Method for crystal system conversion of zopiclone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Put 20g of zopiclone of crystal form C and 80g of isopropanol into a 500ml three-necked flask, raise the temperature to 55°C, keep it for 1.0 hour, then lower the temperature to 0°C, filter, and dry to obtain 18.5g of crystal form A Zopiclone, the yield is 92.5%, the melting point is about 177°C (decomposes at the same time when melting).

[0051] The obtained crystal form A Zopiclone has the following properties:

[0052] (1) X-ray powder diffraction (XRPD) (see Figure 5) curve is consistent with the curve of crystal form A in Figure 1.

[0053] (2) The thermogravimetric analysis (TGA) curve (see Figure 6) is a straight line with no weight change (before 130°C).

[0054] (3) The differential scanning calorimetry (DSC) curve (see Figure 7) has only one endothermic peak, and its maximum endothermic peak is about 177°C.

Embodiment 2

[0056] 20g of zopiclone of crystal form C and 120g of isopropanol were put into a 500ml three-necked flask, the temperature was raised to reflux, after holding for 0.5 hours, the temperature was lowered to 0°C, filtered, and dried to obtain 18.2g of zopiclone of crystal form A. Picclonal, the yield is 91.0%, the melting point is about 177°C (decomposes while melting). The properties of the crystal form C zopiclone raw material and the obtained crystal form A zopiclone are the same as in Example 1.

Embodiment 3

[0058] 20g of zopiclone of crystal form C and 160g of isopropanol were put into a 500ml three-necked flask, heated to reflux, after holding for 0.5 hours, cooled to 0°C, filtered and dried to obtain 18.4g of zopiclone of crystal form A Picclonal, the yield is 92.0%, the melting point is about 177°C (decomposes at the same time when melting). The properties of the crystal form C zopiclone raw material and the obtained crystal form A zopiclone are the same as in Example 1.

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Abstract

The invention relates to a method for converting crystal form of zopiclone. The invention uses zopiclone of crystal form C as material, to process crystal form conversion in dimethyl carbinol, while the reaction temperature is from 20DEG C to the boiling point of solvent system, and cools temperature to 0DEG C after the reaction, filters and dries to obtain zopiclone of crystal form A. The inventive method is characterized in safe and reliable production, high yield and high product quality.

Description

Technical field [0001] The invention relates to a crystal form conversion of a compound, in particular to a method for the crystal form conversion of zopiclone. Background technique [0002] Zopiclone, chemical name (5RS)6-(5-chloro-2-pyridyl)-7-oxo-6.7-dihydro-5H pyrrolo[3,4-b]pyrazine-5 -Yl 4-methylpiperazine-1-carboxylate. , Is developed by the French Rhone-Poulent Rorer company. It belongs to the pyrrolidone compound, as a new type of non-benzodiazepine sedative and hypnotic that has been used clinically, and is used to treat insomnia, especially for patients who cannot tolerate residual effects in the next morning. [0003] As the third-generation non-benzodiazepine hypnotics, it can selectively act on BZI receptors, and the residual effect is relatively small. The phenomenon of "sleeping" is rarely produced in the next morning, and it does not affect the mental activity and movement of the next morning. It is alert, and the dose is small, and repeated applications rarely ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 陈中南魏蒲仁李保勇任保钢
Owner QILU PHARMA HAINAN
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