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Veirofenib camphor sulfonate and preparation method thereof

A technology of camphorsulfonate and vemurafenib, which is applied in the field of medicinal chemistry, can solve the problems of low solubility and oral bioavailability of vemurafenib, serious adverse reactions and the like, and achieves easy control of the crystallization process and good reproducibility. , the effect of simple process

Pending Publication Date: 2021-11-05
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solubility and oral bioavailability of vemurafenib are low, so it is marketed in the form of an amorphous solid dispersion. The clinical recommended oral dose is 960mg once a day, twice a day, and the total amount per day is as high as 1920mg. The adverse reactions are also relatively serious
In addition, there are problems with hygroscopicity and stability of amorphous

Method used

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  • Veirofenib camphor sulfonate and preparation method thereof
  • Veirofenib camphor sulfonate and preparation method thereof
  • Veirofenib camphor sulfonate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Weigh 42.5 mg of vemurafenib and 20.2 mg of DL-camphorsulfonic acid, add 1 mL of n-heptane and 10 μL of methanol to obtain a suspension, stir the suspension at room temperature for 48 h, filter, and obtain a white solid at room temperature Vacuum-dried for 12 hours to obtain vemurafenib DL-camphorsulfonate.

[0041] Carry out X-ray powder diffraction analysis to the vemurafenib DL-camsylate that embodiment 1 makes, its analysis result sees attached figure 1 The X-ray powder diffraction pattern, X-ray powder diffraction data are shown in table 1.

[0042] The X-ray powder diffraction data of the vemurafenib DL-camsylate of table 1 embodiment 1

[0043]

[0044]

[0045] Differential scanning calorimetry chart as figure 2 As shown, the product presents an endothermic peak at 232.0°C.

[0046] Thermogravimetric analysis chart such as image 3 shown.

[0047]The positions of the Fourier transform infrared characteristic peaks are: 3432, 3130, 3020, 1742, 1640, 1...

Embodiment 2

[0050] Weigh 45.2 mg of vemurafenib and 20.2 mg of DL-camphorsulfonic acid, add 1 mL of n-heptane and 10 μL of ethanol to obtain a suspension, stir the suspension at room temperature for 48 h, filter, and obtain a white solid at room temperature Vacuum-dried for 12 hours to obtain vemurafenib DL-camphorsulfonate.

[0051] The X-ray powder diffraction data of vemurafenib DL-camsylate prepared in Example 2 are shown in Table 2.

[0052] The X-ray powder diffraction data of the vemurafenib DL-camsylate of table 2 embodiment 2

[0053]

[0054]

Embodiment 3

[0056] Weigh 45.2 mg of vemurafenib and 20.2 mg of DL-camphorsulfonic acid, add 1 mL of n-heptane and 10 μL of acetonitrile to obtain a suspension, stir the suspension at room temperature for 48 h, filter, and obtain a white solid at room temperature Vacuum-dried for 12 hours to obtain vemurafenib DL-camphorsulfonate.

[0057] The X-ray powder diffraction data of vemurafenib DL-camphorsulfonate prepared in Example 3 are shown in Table 3.

[0058] The X-ray powder diffraction data of the vemurafenib DL-camsylate of table 3 embodiment 3

[0059]

[0060]

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Abstract

The invention discloses a verofenib camphor sulfonate and a preparation method thereof. The salt comprises verofenib and camphorsulfonic acid in a molar ratio of 1:1. The salt has characteristic peaks at the diffraction angle 2[theta] values of 6.8+ / -0.2 degrees, 15.2+ / -0.2 degrees, 18.0+ / -0.2 degrees, 19.8+ / -0.2 degrees, 20.6+ / -0.2 degrees and 21.2+ / -0.2 degrees in an X-ray powder diffraction pattern measured by Cu K alpha rays. The velofenib camphor sulfonate provided by the invention has remarkable advantages in the aspects of hygroscopicity, stability and oral bioavailability. The salt preparation method provided by the invention is simple in process, easy to control the crystallization process, good in reproducibility and suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to vemurafenib camphorsulfonate and a preparation method thereof. Background technique [0002] Pharmaceutical active ingredients usually exist in crystalline forms, such as polymorphs, hydrates, solvates, salts, and co-crystals. For the same pharmaceutical active ingredient, different crystalline forms have different physical and chemical properties. Therefore, obtaining a suitable crystalline form of a drug is of great importance in the pharmaceutical industry. The drug exists in salt form, which can improve the stability, solubility and oral bioavailability of the active ingredient of the drug, which has significant advantages. Therefore, the drug salt form is an effective means to improve the physical and chemical properties of the active ingredients of the drug. [0003] The chemical name of Vemurafenib is N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61P35/00
CPCC07D471/04A61P35/00C07B2200/13
Inventor 陈嘉媚杨玲戴霞林
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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