Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF7 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Trifluridine has no crystal form patent report

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com