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Pomalidomide crystal form and preparation method thereof

A technology of pomalidomide and crystal form, which is applied in the field of medicinal chemistry and achieves the effects of simple operation, stable storage and good thermal stability

Inactive Publication Date: 2015-03-25
SHANGHAI ACEBRIGHT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

WO9803502 discloses pomalidomide compound, but there is no literature report about its crystal form

Method used

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  • Pomalidomide crystal form and preparation method thereof
  • Pomalidomide crystal form and preparation method thereof
  • Pomalidomide crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Add DMF (80ml) to pomalidomide raw material (10.0g), stir at room temperature until clear. The resulting solution was slowly added dropwise to hot water (800 ml) at 90°C. After the dropwise addition, keep stirring for 1 hour. Filter and dry under reduced pressure at 50°C for 16 hours to obtain 9.2 g of light yellow crystals with an HPLC purity of 99.86%. Its powder X-ray diffraction (XRD) spectrum is as follows figure 1 As shown, the differential scanning calorimetry (DSC) diagram is shown in figure 2 shown.

Embodiment 2

[0059] Add DMSO (20ml) to pomalidomide raw material (2.0g), stir at room temperature until clear. The resulting solution was slowly added dropwise to hot water (250 ml) at 80°C. After the dropwise addition, keep stirring for 1 hour. Filter and dry under reduced pressure at 60°C for 15 hours to obtain 1.8 g of light yellow crystals with an HPLC purity of 99.80%. Its XRD spectrogram and DSC spectrogram are basically consistent with Example 1.

Embodiment 3

[0061] Add N-methylpyrrolidone (15ml) to pomalidomide raw material (2.0g), stir at room temperature until clear. The resulting solution was slowly added dropwise to hot water (120 ml) at 100°C. After the dropwise addition, keep stirring for 30 minutes. Filter and dry under reduced pressure at 50°C for 16 hours to obtain 1.8 g of light yellow crystals with an HPLC purity of 99.81%. Its powder XRD spectrogram, DSC spectrogram are basically consistent with embodiment 1.

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Abstract

The invention relates to a pomalidomide crystal form and a preparation method thereof. Specifically, the invention discloses a pomalidomide anhydrous crystal form and a preparation method thereof. The pomalidomide anhydrous crystal form of the invention has the advantages of good thermal stability, good light stability, strong antioxidant capacity and storage stability, and is suitable for application to pharmaceutical preparation.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry. Specifically, the present invention relates to a pomalidomide anhydrate crystal form and a preparation method thereof. Background technique [0002] The chemical name of pomalidomide is 3-amino-N-(2,6-dioxo-3-piperidinyl)phthalimide, and its structural formula is: [0003] [0004] Pomalidomide is a thalidomide analogue, which has antitumor activity, can inhibit the proliferation of hematopoietic tumor cells and induce cell apoptosis. In addition, pomalidomide can inhibit the proliferation of lenalidomide-resistant multiple myeloma cell lines, and can synergistically induce tumor cell apoptosis with dexamethasone. Pomalidomide can also enhance the immune response mediated by T cells and natural killer cells, while inhibiting the production of pro-inflammatory cytokines (such as TNF-α, IL-6) by monocytes. [0005] Pomalidomide was developed by Celgene Pharmaceuticals of the Unite...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/454A61P35/00
CPCC07D401/04C07B2200/13
Inventor 安晓霞吕峰胡猛陈小林邓义
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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