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Crystal of benzoxazole derivative

A crystal and benzo technology, applied in the crystal field of benzoxazole derivatives, can solve the problems that have not yet been reported

Active Publication Date: 2021-02-09
MEIJI SEIKA KAISHA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, it has not been reported to provide a compound that has excellent PDE4 inhibitory activity and is also excellent in stability to temperature, humidity, and light

Method used

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  • Crystal of benzoxazole derivative
  • Crystal of benzoxazole derivative
  • Crystal of benzoxazole derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065]21.9 mL of a mixed solvent of ethyl acetate and 2-propanol (1:1, v / v) was added to the solid (219 mg) of the compound represented by formula (1) obtained in Reference Synthesis Example 1, and heated to 60 ℃ to make it dissolved. The solution was concentrated to dryness, and 4.38 mL of a mixed solvent of ethyl acetate and 2-propanol (1:1, v / v) was added to the obtained residue, and the mixture was stirred at 45°C for 1 hour. After the temperature was brought to room temperature, 21.9 mL of hexane was added and stirred for 1 hour. After filtration, it was washed with hexane and dried to obtain 194 mg of type I crystals. The obtained type I crystals have diffraction angles (2θ±0.2°) based on X-ray powder diffraction, 7.7°, 9.4°, 13.2°, 13.7°, 14.5°, 15.7°, 17.0°, 18.9°, 19.4° , 22.9°, 23.3°, 25.7°, 28.7°, 35.7° show characteristic peaks. The X-ray powder diffraction pattern of type I crystal is shown infigure 1 . A differential scanning calorimetry (DSC) analysis of the obtained ...

Embodiment 2

[0067]To 584 mg of type I crystals obtained in Example 1, 50 mL of methanol was added and dissolved. Concentration under reduced pressure was performed so that the weight became about 1 / 6, and the resulting homogeneous solution was cooled to 0°C and stirred for 10 minutes, thereby depositing a solid. After concentration and drying, 35 mL of a mixed solvent of hexane and ethyl acetate (2:1, v / v) was added to the residue, and the mixture was stirred at room temperature for 30 minutes. After filtration, it was washed with a mixed solvent of hexane and ethyl acetate (2:1, v / v) and dried to obtain 566 mg of type II crystals. The obtained type II crystals are the diffraction angles (2θ±0.2°) based on X-ray powder diffraction, 7.4°, 7.8°, 8.2°, 12.7°, 13.6°, 14.3°, 14.7°, 15.7°, 16.5° , 19.3°, 22.1°, 25.0°, 25.6° show characteristic peaks. The X-ray powder diffraction pattern of type II crystal is shown infigure 2 .

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Abstract

Provided is a crystal of 1-((2-(3, 6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluoro-2-methylpropane-2-ol represented by formula (1).

Description

Technical field[0001]The present invention relates to a kind of 1-((2-(3,6-diazabicyclo[3.1.1]heptan-3-yl)-7-(thiazole- 2-yl)benzo[d]oxazol-4-yl)oxy)-1,1-difluoro-2-methylpropan-2-ol crystals.Background technique[0002]For pharmaceuticals, in addition to effectiveness and safety against diseases, they are also required to have the same quality and storage stability. Therefore, raw materials of pharmaceuticals are required to have excellent stability to temperature, humidity, and light.[0003]So far, it has not been reported to provide a compound having excellent PDE4 inhibitory activity and excellent stability to temperature, humidity, and light.Summary of the invention[0004][The problem to be solved by the invention][0005]The object of the present invention is to provide a raw material suitable as a pharmaceutical for a compound having excellent PDE4 inhibitory activity.[0006][Technical means to solve the problem][0007]The inventors of the present invention conducted intensive resear...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/08A61K31/4995A61P1/04A61P3/04A61P3/10A61P11/00A61P11/06A61P17/06A61P17/10A61P17/14A61P25/00A61P25/16A61P25/18A61P25/24A61P25/28A61P27/02A61P29/00A61P35/00A61P37/02A61P37/08
CPCA61P1/04A61P3/04A61P3/10A61P11/00A61P11/06A61P17/06A61P17/10A61P25/00A61P17/14A61P25/28A61P27/02A61P29/00A61P25/16A61P25/18A61P25/24A61P35/00A61P37/02A61P37/08C07D487/08A61K31/4995C07B2200/13C07D471/08
Inventor 久村兴田村圭司渡边尚志高桥美知子
Owner MEIJI SEIKA KAISHA LTD
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