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Acrivastine novel crystal A and preparation method and application thereof

A crystal form and crystal technology, applied in the field of medicinal chemistry, can solve the problems of low chemical stability and achieve the effects of high chemical stability, high bioavailability, and easy process production

Inactive Publication Date: 2019-03-08
CHONGQING HUABANGSHENGKAI PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The molecular structure of Avastatin contains two double bonds, and it is easy to degrade under light conditions to generate multiple cis-trans isomers, and its chemical stability is low. Since the drug was launched in 1988, no crystal structure and corresponding data reporting

Method used

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  • Acrivastine novel crystal A and preparation method and application thereof
  • Acrivastine novel crystal A and preparation method and application thereof
  • Acrivastine novel crystal A and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Take 2g of a sample of formula I and add it to 20ml of methanol, raise the temperature and reflux for 20 minutes, the system gradually dissolves, stir for 10 minutes, cool down to 10-15°C, a large amount of solids precipitate, stir for 30 minutes, filter, the filter cake is at 75-85°C, The vacuum pressure was -0.09Mpa~-0.10MPa and dried under reduced pressure for 5 hours to obtain 1.2g solid with a yield of 60%. It was confirmed to be crystal form A by X-ray powder diffraction. effect.

Embodiment 2

[0058] Take 2g of the sample of formula I and add it to 20ml of isopropanol, heat up and reflux for 20 minutes, if it is not dissolved, add 20ml of isopropanol, stir for 20 minutes, part of the solid dissolves, add 20ml of isopropanol, stir for 10 minutes, the system dissolves Clear, continue to stir for 10 minutes, cool down to 0-10°C and stir for 30 minutes, there is no solid precipitation, continue to cool to -15°C, there is solid precipitation, continue to stir for 30 minutes, filter, filter cake at 75-85°C, vacuum pressure Dry under reduced pressure at -0.09Mpa~-0.10MPa for 5 hours to obtain 1.6g of solid with a yield of 80%. It was confirmed to be crystal form A by X-ray powder diffraction. The preparation made of this material is equivalent to Xinminle Bio.

Embodiment 3

[0060] Take 200g of a sample of formula I and add it to 2800ml of ethanol, heat up to 75°C and stir, the system gradually dissolves, stir for 10 minutes, naturally cool down to 35-40°C, the system gradually becomes turbid, continue to cool down to 10-15°C, a large amount of solids precipitate , continue to cool down to -5~-15°C and stir for 1.5 hours, filter, filter cake at 75~85°C, vacuum pressure is -0.09Mpa~-0.10MPa and dry under reduced pressure for 8 hours to obtain 170g solid, yield 85%, after X -ray powder diffraction confirmed that it is crystal form A, and the preparation made of this raw material is equivalent to Xinminle Bio.

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Abstract

The invention discloses acrivastine novel crystal A and a preparation method and application thereof. The acrivastine novel crystal A is subjected to X-ray powder diffraction; diffraction peak positions 2 theta (+ / -20 degrees) are used as spectrogram characteristic parameters; the diffraction peak positions 2 theta include 8.49 degrees, 9.21 degrees, 10.04 degrees, 12.52 degrees, 16.99 degrees, 17.55 degrees, 18.41 degrees, 19.33 degrees, 19.96 degrees, 21.34 degrees, and 23.30 degrees. The preparation method includes: adding acrivastine into a solvent, heating, clarifying to obtain acrivastine solution, crystalizing by a temperature differential method, carrying out solid-liquid separation, and drying the solid to obtain acrivastine novel crystal A. The acrivastine novel crystal A provided herein fills the gap of this research field, has high chemical stability and bioavailability, matches for bulk acrivastine of Semprex, and is important to the further domestic development of its dosage forms or industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a new crystal form A of arvastatin and its preparation method and application. Background technique [0002] The chemical structure of Avastin is shown in the following formula, and the chemical name is: (E,E)-3-[6-[1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1- Acryl]-2-pyridyl]-2-acrylic acid Avastin is white or off-white powder, dissolved in chloroform, slightly soluble in 0.1mol / L hydrochloric acid, slightly soluble in ethanol, very soluble in water Slightly soluble, almost insoluble in ethyl acetate. [0003] [0004] Avastin is a second-generation antihistamine drug with a pyrrolamine structure and a competitive histamine H1 receptor antagonist. It was developed by Glaxo-Wellcome in the UK. Its capsule formulation was first listed in the UK in August 1988. , the product name is Semprex, and its Chinese product name is Xinminle. This product has no obvious antic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/55A61P37/08
CPCA61P37/08C07B2200/13C07D213/55
Inventor 倪尉杨玉金王绍辉
Owner CHONGQING HUABANGSHENGKAI PHARM
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