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Siponimod crystal form and preparation method thereof

A crystal form and X-ray technology, applied in the field of siponimod crystal form and its preparation, can solve the problems of poor stability or solubility of siponimod free base

Active Publication Date: 2020-02-11
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The existing crystalline form of siponimod free base has poor stability or solubility; therefore, it is of great significance to carry out research on its crystalline form

Method used

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  • Siponimod crystal form and preparation method thereof
  • Siponimod crystal form and preparation method thereof
  • Siponimod crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation method of embodiment 1 crystal form C

[0046] Take 0.80g of the raw material and add it to 40mL of pure water at 25°C, stir for 12h, the material is dispersed, filtered and dried at 50°C for 12h to obtain the crystal form C, see Figure 1-3 .

Embodiment 2

[0047] The preparation method of embodiment 2 crystal form C

[0048] Dissolve 50 mg of raw material in 0.5 mL of methanol at room temperature, add 1.0 mL of pure water after dissolving, continue stirring for 12 hours to obtain a dispersed solid, filter and dry to obtain crystal form C, detect, and Figure 1-3 unanimous.

Embodiment 3

[0049] The preparation method of embodiment 3 crystal form C

[0050] Take 50mg of raw material and dissolve it in 0.5mL ethanol at room temperature. If it cannot be completely dissolved at room temperature, heat it to 40°C to dissolve it. After dissolving, add 0.5mL pure water to become an oily substance. Add 0.5mL pure water and continue stirring for 12 hours to obtain Solid, filtered and dried to obtain crystal form C, detected, and Figure 1-3 unanimous.

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Abstract

The invention provides a siponimod crystal form and a preparation method thereof, and belongs to the field of medicinal chemistry, wherein the crystal form has good solubility and good stability. Thepreparation method comprises: mixing siponimod and a solvent, optionally adding an anti-solvent, stirring, and filtering to obtain the siponimod crystal form. According to the invention, the preparation method is simple to operate, mild in condition and beneficial to implementation in production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular, the invention relates to a siponimod crystal form and a preparation method thereof. Background technique [0002] BAF-312 (SiponiMod) Siponimod is a second-generation S1P receptor modulator that selectively acts on S1P1 and S1P5 receptors, and is more selective than S1P2, S1P3 and S1P4 receptors. Studies have shown that siponimod can effectively delay the progression of disability in secondary multiple sclerosis. [0003] The structure of siponimod is shown in formula (I): [0004] [0005] At present, there have been reports disclosing the crystal form A of siponimod free base and providing solubility data, but the solubility of crystal form A is average. [0006] The crystal form of a drug is an important factor affecting the quality of a drug. Different crystal forms of the same drug molecule will have significant differences in appearance, solubility, melting point, diss...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D205/04
CPCC07D205/04C07B2200/13
Inventor 谷慧科陈勇罗忠华黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD