Crystal form I of alkynyl-containing compound as well as preparation method and application thereof

A crystal form, ethynyl technology, applied in organic chemical methods, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as compound polycrystals, and achieve good stability

Active Publication Date: 2020-08-07
SHANGHAI YASHENG MEDICAL TECH +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Known compounds generally have polymorphism, and general drugs may have two or more different crystalline states

Method used

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  • Crystal form I of alkynyl-containing compound as well as preparation method and application thereof
  • Crystal form I of alkynyl-containing compound as well as preparation method and application thereof
  • Crystal form I of alkynyl-containing compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1: the preparation of crystal form I

[0077] 40mg 3-((1H-pyrazol[3,4-b]pyridine-5-substituted)ethynyl)-4-methyl-N-(4-((4-methylpiperazine-1-substituted) Methyl)-3-(trifluoromethyl)phenyl)benzamide was added to 0.1 mL of methanol, stirred at room temperature for 1-3 h, filtered and the solid was collected to obtain Form I.

[0078] The XPRD diagram of crystal form I is shown in figure 1 Shown; In its X-ray powder diffraction figure represented by 2θ angle, 2θ value is as shown in Table 1;

[0079] Table 1

[0080] .

[0081] The TGA diagram of the crystal form I is as follows: figure 2 As shown, the weight loss gradient at 200°C is 0.15%, and the "%" is the weight percentage. The DSC diagram of the crystal form I is shown in image 3 As shown, there is a heat absorption peak at 235°C; the DVS diagram of crystal form I is shown in Figure 4 Shown; Microscopic picture of crystal form I is shown in Figure 5 As shown, the crystal form presents a sheet...

Embodiment 2

[0082]Embodiment 2: the preparation of crystal form I

[0083] 40mg 3-((1H-pyrazol[3,4-b]pyridine-5-substituted)ethynyl)-4-methyl-N-(4-((4-methylpiperazine-1-substituted) Methyl)-3-(trifluoromethyl)phenyl)benzamide was added to 0.1 mL of ethanol, stirred at room temperature for 1-3 h, filtered and the solid was collected to obtain Form I.

Embodiment 3

[0084] Embodiment 3: the preparation of crystal form I

[0085] 40mg of 3-((1H-pyrazol[3,4-b]pyridine-5-substituted)ethynyl)-4-methyl-N-(4-((4-methylpiperazine-1-substituted)methyl Base)-3-(trifluoromethyl)phenyl)benzamide was added into 0.1mL isopropanol, stirred at room temperature for 1-3h, filtered and collected solid to obtain Form I.

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PUM

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Abstract

The invention discloses a crystal form I of an alkynyl-containing compound as well as a preparation method and application thereof. The invention particularly discloses a crystal form I of 3-((1H-pyrazole [3, 4-b] pyridine-5-substituted) ethynyl)-4-methyl-N-(4-((4-methylpiperazine-1-substituted) methyl)-3-(trifluoromethyl) phenyl) benzamide. The crystal form provided by the invention has good stability, and has important value for optimization and development of drugs.

Description

technical field [0001] The invention belongs to the field of chemistry and medicine, and in particular relates to a crystal form I of an alkyne group-containing compound, a preparation method and application thereof. Background technique [0002] The application relates to an alkynyl-containing compound, the chemical name is 3-((1H-pyrazol[3,4-b]pyridine-5-substituted)ethynyl)-4-methyl-N-(4-(( 4-Methylpiperazine-1-substituted)methyl)-3-(trifluoromethyl)phenyl)benzamide, the report on this compound in the patent is very limited and does not involve the crystal form of the above compound. [0003] It is known that polymorphism commonly exists in compounds, and general drugs may exist in two or more different crystal forms. The existing form and quantity of polymorphic compounds are unpredictable. Different crystal forms of the same drug have significant differences in solubility, melting point, density, stability, etc., which affect the temperature profile, uniformity, and bi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61P35/00A61P35/02A61K31/496
CPCA61P35/00A61P35/02C07B2200/13C07D471/04
Inventor 温剑锋林艳琼冯建鹏吴天助邵振中李卫东
Owner SHANGHAI YASHENG MEDICAL TECH
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