New crystal form of trifluridine, and preparation method thereof

A crystal form and compound technology, applied in the field of medicinal chemistry, can solve the problems such as no crystal form patent report of trifluridine

Active Publication Date: 2015-12-23
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Trifluridine has no

Method used

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  • New crystal form of trifluridine, and preparation method thereof
  • New crystal form of trifluridine, and preparation method thereof
  • New crystal form of trifluridine, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Preparation of Trifluridine Form I Using Acetone / Isopropyl Ether

[0021] Compound 1 (29.6g, 0.1mol) was added to acetone (300ml), heated to reflux, isopropyl ether (1L) was added dropwise, and then stirred at 50°C for 12h for crystallization. After filtration, the resulting solid was dried under reduced pressure at 50°C to constant weight. The target product (10.2 g, off-white solid) was obtained with a yield of 34.4%.

[0022] figure 1 It is the X-ray diffraction figure of the crystal form I obtained in Example 1.

experiment example 1

[0023] Experimental Example 1 Stability Experiment

[0024] The accelerated stability study was carried out on the crystal form prepared in Example 1, and the X-ray diffraction data comparison between 0M and 6M in the accelerated stability test is shown in Table 1.

[0025] Table 1 X-ray diffraction data comparison table of accelerated stability test samples

[0026]

[0027] Experimental conclusion: after 6 months of accelerated experimentation, the X-ray diffraction spectrum is consistent with the initial data, and no crystal transformation occurs, indicating that the crystal form provided by the present invention has good stability.

experiment example 2

[0028] Experimental Example 2 Stability Experiment

[0029] Table 2 Stability test comparison table

[0030]

[0031] Experimental conclusion: the crystal form provided by the present invention has good stability.

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PUM

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Abstract

The present invention discloses a new crystal form of trifluridine, and a preparation method thereof, and particularly relates to a new 5-trifluoromethyl-2'-deoxyuridine crystal form represented by a formula (I), and a preparation method thereof, wherein the characteristic peaks of the crystal form in the X-ray powder diffraction spectrum are positioned at (a) 7.3 DEG, (b) 10.0 DEG, (c) 14.5 DEG and (d) 23.4 DEG C by adopting 2[theta] (2[theta]+/-0.2 DEG) to represent. According to the present invention, the crystal form has characteristics of stable characteristics and good repeatability, and is suitable for drug development. The formula I is defined in the specification.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a crystal form of 5-trifluoromethyl-2'-deoxyuridine and a preparation method thereof. Background technique [0002] Trifluridine is a nucleoside analogue. Foreign name: Trifluridine, Viroptic. The structure of this product is similar to iodine glucoside. It has the strongest effect on herpes simplex virus (HSV-1 and HSV-2), has certain effect on adenovirus, vaccinia virus, cytomegalovirus, and herpes zoster virus, and is effective on acyclovir-resistant herpes virus. 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 eye diseases. The curative effect is similar to vidarabine but better than that of iodine. Those who are ineffective or allergic to iodine can try this product....

Claims

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Application Information

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IPC IPC(8): C07H19/073C07H1/06
Inventor 武华周杜祖银李孝壁李辉
Owner JIANGSU HANSOH PHARMA CO LTD
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