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Crystal form B and preparation method

A technology of crystal form and diffraction peak, applied in the field of medicinal chemistry, can solve the problems of poor stability and incompatibility, and achieve the effects of good controllability and reproducibility, stable storage and good stability

Inactive Publication Date: 2016-06-08
孙霖
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the compound has poor stability during storage and is hygroscopic, so it is not suitable for the inhaled dry powder preparation to be developed

Method used

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  • Crystal form B and preparation method

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Embodiment 1

[0014] 10gN-[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N'-{2-[(3-{2-[(2 -Hydroxyethyl)thio]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)thio]benzyl}urea was refluxed in 100ml ethyl acetate and heated To 40°C, add 100ml of solvent tert-butyl methyl ether, cool down to zero at a rate of 2°C / min, filter, and vacuum-dry to obtain crystal B. Using Cu-Kα radiation, X-ray powder diffraction expressed in 2θ angles as figure 1 As shown, the HPLC purity was 99.92%.

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Abstract

The invention discloses a crystal form B. The crystal form B is characterized in that Cu-K alpha radiation is used, X-RPD (X-ray powder diffraction) indicated by the 2 theta angle has diffraction peaks at 6.4+ / -0.2 degrees, 7.9+ / -0.2 degrees, 8.7+ / -0.2 degrees, 9.8+ / -0.2 degrees, 10.0+ / -0.2 degrees and 17.0+ / -0.2 degrees. The crystal form B can be prepared on a large scale safely and purified, can be stored stably, does not have moisture absorption, is very suitable for preparation of an inhalable preparation and has good compatibility with excipients such as lactose, starch and the like.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, specifically, the present invention relates to N-[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N'- {2-[(3-{2-[(2-Hydroxyethyl)thio]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)thio] A new crystal form B of benzyl}urea, as well as a preparation method and application of the crystal form. Background technique [0002] N-[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N'-{2-[(3-{2-[(2 -Hydroxyethyl)thio]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)thio]benzyl}urea is the latest development for the treatment of chronic New compounds for allergic and non-allergic airway diseases of obstructive pulmonary disease (COPD), a class of p38MAP kinase inhibitors. However, the compound has poor stability during storage and is hygroscopic, so it is not suitable for the inhaled dry powder preparation to be developed. Contents of the invention [0003] Aiming at the problems in...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P11/00A61P37/08
CPCC07D471/04C07B2200/13
Inventor 孙霖
Owner 孙霖
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