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Novel crystal form compound of leflunomide and preparation method of novel crystal form compound

A leflunomide and compound technology, applied in the field of pharmaceutical compound preparation, can solve the problem of not giving a spectrum, and achieve the effects of good reproducibility and high purity

Inactive Publication Date: 2019-01-11
SHENZHEN NYCRIST TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Crystal form III is reported in patent CN1411373, which is a solvate of N-methyl-2-pyrrolidone, which is not suitable for drug use. Crystal form IV is reported in patent CN107311954A, with a melting point of 142.07°C, lower than that of crystal form I, and influencing factors One-month test and three-month accelerated test, the patent claims that the X-ray powder diffraction pattern of Form IV has no change, but no pattern is given

Method used

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  • Novel crystal form compound of leflunomide and preparation method of novel crystal form compound
  • Novel crystal form compound of leflunomide and preparation method of novel crystal form compound
  • Novel crystal form compound of leflunomide and preparation method of novel crystal form compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Preparation of Leflunomide Form I (refer to CN107311954A).

Embodiment 2

[0041] Example 2: Preparation of leflunomide crystal form II (refer to CN107311954).

Embodiment 3

[0042] Example 3: Preparation of Leflunomide Form V.

[0043] A preparation method for new crystal form V of leflunomide, comprising the following steps:

[0044] A. Heating leflunomide at a uniform speed until the raw material of leflunomide is completely melted and then vaporized (180-200°C);

[0045] B, cooled to room temperature;

[0046] C. Collect the sample after desublimation of the upper layer of glass.

[0047] Leflunomide Form V has the following characteristics:

[0048] 1. Powder X-ray Diffraction

[0049] Instrument: Sharp Shadow X-ray Diffractometer (PANalytical, Netherlands)

[0050] Target: Cu-Kα radiation

[0051] wavelength:

[0052]X-ray light tube voltage: 45kV

[0053] X-ray tube electric current: 40mA

[0054] Step size: 0.01313°

[0055] Scanning speed: 0.041683° / s

[0056] Scanning range: 2°-40°

[0057] The results show that: at 2θ7.8255°, 8.7099°, 9.1789°, 9.6017°, 11.1488°, 14.9436°, 15.6434°, 18.6293°, 19.3055°, 20.2744°, 23.3166°, 23....

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Abstract

The invention discloses a crystal form compound of leflunomide V. The crystal form is different from X-ray powder diffraction and differential scanning patterns of the leflunomide, which are publishedin the existing document, and is a novel crystal form; and the X-ray powder diffraction pattern has characteristic diffraction peaks different from a reported crystal form at 2theta of 7.8255 degrees, 8.7099 degrees, 9.1789 degrees, 9.6017 degrees, 11.1488 degrees, 14.9436 degrees, 15.6434 degrees, 18.6293 degrees, 19.3055 degrees, 20.2744 degrees, 23.3166 degrees, 23.5235 degrees, 30.1244 degrees, 30.6877 degrees, 31.5469 degrees and 37.2453 degrees. The solubility of the crystal form is better than that of other all crystal forms in existing reports, the purity is high and the repeatabilityis good; and the invention further discloses a preparation method of the crystal form.

Description

technical field [0001] The invention relates to the field of preparation of pharmaceutical compounds, in particular to a new crystal form compound of leflunomide and a preparation method thereof. Background technique [0002] Leflunomide (Leflunomide), chemical formula: C12H9F3N2O2, molecular weight: 270.2, chemical name: N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide, structural formula I is as follows: [0003] [0004] Leflunomide is an isoxazole immunomodulator with antiproliferative activity, used for the treatment of rheumatoid arthritis, systemic lupus erythematosus, etc., and has been approved in the United States for the treatment of rheumatoid arthritis. [0005] The present invention relates to polymorphs of leflunomide. Polymorphism is the property of certain molecules to assume more than one crystal form in the solid state. Different crystal forms show different weight loss within 110° C. on the X-ray powder diffraction pattern, differential sc...

Claims

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Application Information

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IPC IPC(8): C07D261/18
Inventor 田芳安妮·齐默尔曼
Owner SHENZHEN NYCRIST TECH CO LTD
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