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Medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol and preparation method thereof

A technology of medicinal salts and succinates, applied in organic chemistry methods, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as changes in physical and chemical properties, unfavorable drug development or production, etc., and achieve suitable melting point and excellent thermal stability Sex, TGA weight loss small effect

Pending Publication Date: 2022-06-07
北京拓领博泰生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the prior art, it is rare to directly use the drug itself to prepare a drug with corresponding efficacy. Generally, the drug is prepared as its salt form, and then the performance of the salt drug drug is developed or produced. However, the drug is prepared as its After the salt form, its physical and chemical properties are very likely to change. Some of these changes are beneficial to the research and development or production of pharmaceuticals, and some are not conducive to the research and development or production of pharmaceuticals. Therefore, finding a suitable salt form is conducive to the practical use of pharmaceuticals. development or production of

Method used

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  • Medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol and preparation method thereof
  • Medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol and preparation method thereof
  • Medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol and preparation method thereof

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Embodiment 1

[0066] An embodiment of the present invention provides a method for preparing a pharmaceutically acceptable salt of a compound represented by formula I, wherein the pharmaceutically acceptable salt is succinate, include:

[0067] 1: Weigh about 100 mg of the compound represented by formula I (for the preparation process, see: WO2019089648) into a 20.0 mL glass vial;

[0068] 2: add 52.5 mg of succinic acid;

[0069] 3: Add 2.5 mL of acetonitrile to dissolve the sample (using ultrasound), and record the dissolution. A stirring bar was added, and the suspension was stirred at room temperature on a magnetic stirrer.

[0070] 4: After stirring at room temperature for about 4 days, the obtained solid was centrifuged and dried in a vacuum drying oven at 50° C. for 4 hours to obtain a pharmaceutically acceptable salt.

[0071] Structure confirmation:

[0072] The structure of the compound shown in the formula I of Example 1 is confirmed, and the results are detailed in Figure ...

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Abstract

The invention relates to the technical field of salt formation of compounds, in particular to medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol and a preparation method of the medicinal salt of 4-(7-methoxyquinoline-4-yl)-2-methylphenol. The pharmaceutical salt in the pharmaceutical salt of the compound shown in the formula I is succinate, has excellent physicochemical properties such as small TGA weight loss, high crystallinity and appropriate melting point, especially has excellent thermal stability, high humidity stability, solid stability and equilibrium solubility, and is beneficial to research and development or production of the medicament.

Description

technical field [0001] The present invention relates to the technical field of compound salt formation, in particular, to a pharmaceutically acceptable salt of 4-(7-methoxyquinolin-4-yl)-2-methylphenol and a preparation method thereof. Background technique [0002] In the specific process of drug production or research and development, the physical and chemical properties of the drug have an extraordinary impact on its research and development or production, such as drug solubility, stability, hygroscopicity and melting point, etc. Therefore, it is necessary to study the physicochemical properties of drugs in particular. In the prior art, it is less direct to use the medicine itself to prepare the medicament with the corresponding effect. Generally, the medicine is prepared as its salt form, and then the performance of the medicament of the salt type medicine is carried out for research and development or production, but the medicine is prepared as its salt form. After the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/20A61K31/47
CPCC07D215/20A61K31/47C07B2200/13
Inventor 高萌丁东
Owner 北京拓领博泰生物科技有限公司
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