Osalmid crystal form II, and preparation method and application thereof

A technology of salivamol and crystal form, which is applied in the field of medicinal chemistry, can solve the problems such as the report of undiscovered salivamol crystal form, and achieve the effects of improving drug performance, crystal form with low hygroscopicity, and process improvement

Inactive Publication Date: 2018-09-07
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] No report on the crystal form of salaminol has been found so far

Method used

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  • Osalmid crystal form II, and preparation method and application thereof
  • Osalmid crystal form II, and preparation method and application thereof
  • Osalmid crystal form II, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation of sulfanol crystal form II

Embodiment 1-1

[0060] Take about 3 g of sulfanol solid, add 400 ml of ethanol, mix and dissolve. Slowly volatilize to dryness at 25°C, and then collect the solid to obtain saliaminophen crystal form II, which is off-white crystals.

Embodiment 1-2

[0062] Take about 3 g of sulfanol solid, add 400 ml of ethanol and 400 ml of toluene, mix and dissolve. Slowly volatilize to dryness at 25°C, and then collect the solid to obtain saliaminophen crystal form II, which is off-white crystals.

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Abstract

The invention disclose an osalmid crystal form II, and a preparation method and application thereof. In the XRPD pattern of the crystal form expressed by 2theta angles, characteristic peaks occur whendiffraction angles are 7.527+ / -0.2 DEG, 13.653+ / -0.2 DEG, 14.644+ / -0.2 DEG, 15.037+ / -0.2 DEG, 19.62+ / -0.2 DEG, 20.092+ / -0.2 DEG, 20.454+ / -0.2 DEG, 22.618+ / -0.2 DEG, 24.45+ / -0.2 DEG, 25.226+ / -0.2 DEG,26.288+ / -0.2 DEG, 26.638+ / -0.2 DEG, 28.516+ / -0.2 DEG, 29.373+ / -0.2 DEG, 29.723+ / -0.2 DEG, 31.605+ / -0.2 DEG, 35.794+ / -0.2 DEG and 38.104+ / -0.2 DEG. The crystal form has excellent physical and chemicalproperties and drug-forming properties, is simple to prepare and low in hygroscopicity, and shows good stability and reproducibility.

Description

Technical field [0001] The invention belongs to the technical field of medicinal chemistry, and specifically relates to sulfanol crystal form II, and a preparation method and application thereof. Background technique [0002] Drug polymorphism refers to the existence of two or more different crystal forms of the active ingredient (API) of the drug. About 90% of small molecule drugs currently on the market are administered in the form of crystals. This is because the crystal form has obvious physical and chemical properties and processing advantages compared to other states, such as amorphous or liquid, has excellent physical and chemical stability, can effectively eliminate impurities, and has excellent processing properties. These advantages have a positive impact on the quality of the drug and the process. Therefore, crystal form research and control have become an important research content in the drug development process. [0003] Crystal form research includes two stages: c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/64C07C231/24
CPCC07B2200/13C07C231/24C07C235/64C07C231/08
Inventor 朱维良徐志建李波张勇
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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