Novel crystal of paliperidone and preparation method thereof

A kind of technology of paliperidone and crystal form, which is applied in the field of crystal crystal form control, and can solve the problems of reported crystal form research and preparation method, etc.

Active Publication Date: 2012-05-16
SHANGHAI CHENPON PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The crystal form patent of paliperidone has not yet entered China, and there is c...

Method used

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  • Novel crystal of paliperidone and preparation method thereof
  • Novel crystal of paliperidone and preparation method thereof
  • Novel crystal of paliperidone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of the new crystal form VII of paliperidone:

[0030] Add 5.0g paliperidone into a 500mL round bottom flask, then add 250mL isopropanol, start stirring and heat to reflux, keep for two hours after dissolving, naturally cool to 60°C and keep for 2 hours, then naturally cool to 40°C °C and maintained for 2 hours, and finally cooled to 20 °C and maintained for 16 hours. The precipitated crystals were collected by filtration and dried at 60° C. for 3 hours. 4.3 g of crystal samples of the new crystal form VII were obtained. 99.67% purity.

Embodiment 2

[0031] Example 2 Preparation of the new crystal form VII of paliperidone:

[0032] Add 5.0g paliperidone into a 500mL round bottom flask, then add 250mL isopropanol, start stirring and heat to reflux, keep for two hours after dissolving, naturally cool to 60°C and keep for 2 hours, then naturally cool to 40°C °C and maintained for 2 hours, and finally cooled to 20 °C and maintained for 16 hours. The precipitated crystals were collected by filtration and dried at 60° C. for 3 hours. 4.2 g of crystal samples of the new crystal form VII were obtained. 99.62% purity.

Embodiment 3

[0033] Embodiment 3 Preparation of the crystal of the new crystal form VII of paliperidone:

[0034] Add 5.0g paliperidone into a 500mL round bottom flask, then add 250mL isopropanol, start stirring and heat to reflux, keep for two hours after dissolving, naturally cool to 60°C and keep for 2 hours, then naturally cool to 40°C °C and maintained for 2 hours, and finally cooled to 20 °C and maintained for 16 hours. The precipitated crystals were collected by filtration and dried at 60° C. for 3 hours. 4.1 g of a crystal sample of the new crystal form VII was obtained. 99.61% pure.

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Abstract

The invention relates to a novel crystal (defined as the crystal form VII) of paliperidone and a preparation method thereof. The reflection angle 2Theta in the X-ray powder diffraction pattern of the novel crystal has characteristic peaks at the following values: 8.14 degrees, 10.24 degrees, 12.40 degrees, 12.84 degrees, 13.02 degrees, 13.75 degrees, 14.56 degrees, 14.92 degrees, 16.18 degrees, 18.60 degrees, 19.14 degrees, 20.46 degrees, 21.42 degrees, 21.94 degrees, 24.58 degrees, 24.98 degrees, 27.98 degrees, 28.54 degrees and 31.19 degrees; the melting point in the DSC thermograms is 185.0 degrees centigrade. The crystal of the novel crystal form VII disclosed by the invention has a good stability under normal storage conditions. The solvent used during the preparation process has a high safety. The paliperidone can produce crystals in isopropanol easily. The obtained crystal has a high purity and is more helpful for the product development.

Description

technical field [0001] The present invention relates to crystal form control technology, more specifically, relates to a novel crystal of Paliperidone (defined as crystal form VII) and a preparation method thereof. Background technique [0002] As described in the international patent application US5198952, it is known that Paliperidone represented by the following formula has the utility of treating mental diseases. Paliperidone was launched in the U.S. in 2007, produced by ALZA Company, and its commercial name is Invega. The chemical structural formula is as follows: [0003] [0004] There are several crystalline forms of paliperidone. US Patent US20080177067 describes I, II, III, IV, V, VI and amorphous powder of the compound and its preparation method. Among them, crystal I is obtained by recrystallization from acetonitrile; crystal II is obtained by refluxing with ethanol (acetonitrile, isopropanol), cooling to room temperature, stirring for 5 hours, cooling to 0...

Claims

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Application Information

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IPC IPC(8): C07D471/04
Inventor 严宏营齐创宇刘文华杜狄峥
Owner SHANGHAI CHENPON PHARM TECH CO LTD
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