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Macitentan crystal form and preparation method thereof

A technology of macitentan and its crystal form, which is applied in the field of drug synthesis, can solve problems such as unreported information on the crystal form of macitentan, and achieve the effects of easy production and storage, good stability of the crystal form, and simple operation

Inactive Publication Date: 2016-04-06
天津市医药集团技术发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] J.Med.Chem.2012,55(17):7849-7861. Reported the synthesis method of the compound macitentan (melting point is 135°C), and did not report the crystal form information of macitentan

Method used

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  • Macitentan crystal form and preparation method thereof
  • Macitentan crystal form and preparation method thereof
  • Macitentan crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0060] Dissolve 1 g of macitentan crude product in 10 ml of methanol, heat until dissolved, slowly cool down to 20-25°C, keep warm for 2 hours, then slowly cool down to 0-5°C, keep warm for 2 hours, filter, and dry to obtain the present invention The crystal form sample of macitentan is 0.82g.

Embodiment 2

[0062] Dissolve 1 g of macitentan crude product in 50 ml of ethanol, heat until dissolved, slowly cool down to 20-25°C, keep warm for 3 hours, then slowly cool down to 0-5°C, keep warm for 3 hours, filter, and dry to obtain the present invention The crystal form sample of macitentan is 0.78g.

Embodiment 3

[0064] Dissolve 1 g of macitentan crude product in 70 ml of isopropanol, heat until dissolved, slowly cool down to 20-25°C, keep warm for 2 hours, then slowly cool down to 0-5°C, keep warm for 3 hours, filter, and dry to obtain The crystalline form sample of macitentan described in the present invention is 0.82g.

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Abstract

The present invention relates to a macitentan crystal form and a preparation method thereof, wherein the characteristic absorption peaks exist when the diffraction angle (2[theta]) is 11.32+ / -0.2, 12.94+ / -0.2, 15.98+ / -0.2, 18.05+ / -0.2, 18.46+ / -0.2, 21.94+ / -0.2, 23.32+ / -0.2, 25.28+ / -0.2, 26.50+ / -0.2, 28.42+ / -0.2, and 31.06+ / -0.2 in the X-ray powder diffraction pattern of the crystal form. The macitentan crystal form prepared by using the method of the present invention has characteristics of good stability, simple operation, easy production, and easy storage.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and relates to a preparation method of a crystal form of macitentan. Background technique [0002] Macitentan is a new generation of high-efficiency endothelin receptor antagonist, which can strongly antagonize endothelin-induced vasoconstriction and inhibit the increase of pulmonary artery pressure. It is clinically used to treat cardiovascular diseases—pulmonary arterial hypertension (PAH). Compared with bosentan (Bosentan), macitentan has the advantages of strong effect, small dose and high safety. [0003] The chemical structural formula of macitentan: [0004] [0005] Patent WO0253557 discloses the synthesis of sulfonamide derivatives, and the compound macitentan is disclosed for the first time, but the crystal form information is not disclosed. [0006] Patents WO2004050640, WO2006051502, WO2009024906, etc. disclose the synthesis of sulfonamide derivatives, including the c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/47A61K31/506A61P9/12A61P11/00
Inventor 周永健程玉红边颖孟红赵平
Owner 天津市医药集团技术发展有限公司
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