Novel trifluridine crystal form and preparation method thereof

A technology of trifluridine crystal and crystal form, which is applied in the field of drug preparation, can solve the problems of no crystal form patent report of trifluridine, and achieve the effect of stable crystal form properties

Inactive Publication Date: 2015-12-30
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Trifluridine has no

Method used

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  • Novel trifluridine crystal form and preparation method thereof
  • Novel trifluridine crystal form and preparation method thereof
  • Novel trifluridine crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 10g of crude trifluridine, add it to 90ml of methanol, dissolve at 10°C, slowly add 2700ml of dichloromethane dropwise, stir at 10°C for 12h, filter to obtain 7.1g of white solid, which is determined to be crystal form II by X-ray diffractometer , whose spectrum is as figure 1 shown.

Embodiment 2

[0030] Weigh 10g of crude trifluridine, add it to 100ml of ethanol, dissolve at 10°C, slowly add 3000ml of dichloromethane dropwise, stir at 10°C for 12h, filter to obtain 7.7g of white solid, which is determined to be crystal form II by X-ray diffractometer .

Embodiment 3

[0032] Weigh 10g of crude trifluridine, add it to 70ml of methanol, heat to reflux to dissolve, turn off the heating, cool down to 10°C and stir for 12h, filter to obtain 5.3g of white solid, which is determined to be crystal form II by X-ray diffractometer.

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PUM

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Abstract

The invention relates to a novel trifluridine crystal form and a preparation method thereof. The trifluridine crystal form II shown in the formula (I) is characterized in that a CuKa ray is used as the feature X-ray for powder determination, and characteristic peaks are shown when the 2Q diffraction angle is located at the following positions such as 7.405, 9.933, 10.602, 14.865, 17.428, 18.675, 19.027, 20.274 and 23.911. The preparation method of the trifluridine crystal form II shown in the formula (II) comprises the step that trifluridine is crystallized in a supersaturated solution with protic solvent or aprotic solvent at the temperature of 0-30 DEG C, so that the crystal form II is obtained. The property of the crystal form is stable, and the crystal form meets the development requirement for pharmaceutical preparations (please see the specification for the formula).

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a new crystal form of trifluridine and a preparation method thereof. Background technique [0002] Trifluridine, molecular formula: C 10 h 11 f 3 N 2 o 5 , molecular weight: 296.2, full name: 1-(2-deoxy-β-D-erythrofuranose)-5-trifluoromethyl-2,4-dihydroxypyrimidine, English name: Trifluridine, its chemical structure is as follows: [0003] [0004] Trifluridine has the strongest effect on herpes simplex virus (HSV-1 and HSV-2), and also has a certain effect on adenovirus, vaccinia virus, cytomegalovirus, and herpes zoster virus, and has a certain effect on acyclovir-resistant herpes Viruses work. Its triphosphate derivatives can be incorporated into DNA and compete with thymidine triphosphate to inhibit DNA polymerase. No selectivity for viral DNA and host cell DNA. It is suitable for herpes simplex keratitis, conjunctivitis and other herpetic ...

Claims

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Application Information

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IPC IPC(8): C07H19/073C07H1/06
Inventor 王永恒武华周李孝壁赵军军
Owner JIANGSU HANSOH PHARMA CO LTD
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