Method for preparing novel crystal form of bilastine

A bilastine and crystal form technology, applied in the field of medicinal chemistry, can solve problems such as instability of crystal form II and crystal form III

Inactive Publication Date: 2014-11-19
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the Chinese patent CN1628112A, the crystal form of bilastine was first proposed. Crystal forms I, II, III, crystal form II and crystal form III are unstable and can be converted into crystal form I. The patent only gives the unit cell data and infrared data

Method used

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  • Method for preparing novel crystal form of bilastine
  • Method for preparing novel crystal form of bilastine

Examples

Experimental program
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Effect test

Embodiment 1

[0014] Add 3g of bilastine to the reaction flask, add 18ml of acetone and water mixed solvent (90:10), heat until bilastine dissolves, cool to room temperature to crystallize, filter and dry to obtain the new crystal form of bilastine , yield 80.1%.

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Abstract

The invention relates to a method for preparing a novel crystal form of bilastine. The method comprises the following steps: dissolving bilastine in a mixed solvent of an organic solvent and water, heating until all bilastine is dissolved, and cooling and crystallizing to obtain the novel crystal form of bilastine.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl]-piperidin-1-yl }Ethyl)-phenyl]-2-methyl-propionic acid (bilastine) new crystal preparation. Background technique [0002] Bilastine, the 2nd generation histamine H developed for Spanish FAES pharmaceutical company 1 Receptor antagonist, approved by the European Union for the treatment of allergic rhinitis and chronic idiopathic urticaria in 2010, and launched in Ireland in 2011. This product is safe, without the sedative effect and cardiotoxicity of commonly used antihistamines. [0003] [0004] In the Chinese patent CN1628112A, the crystal form of bilastine was first proposed. Crystal forms I, II, III, crystal form II and crystal form III are unstable and can be converted into crystal form I. The patent only gives the unit cell data and infrared data. In the patent CN201310107513.8, a new crystal form of bilastine is men...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/454A61P11/02A61P37/08A61P17/00
CPCC07D401/04C07B2200/13
Inventor 赵月楠闫起强马苏峰
Owner BEIJING VENTUREPHARM BIOTECH
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