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Trifluridine compound and medicine composition thereof

A compound and composition technology, applied in the field of new Trifluridine crystal form and its preparation method and pharmaceutical composition, can solve the problems of no literature reports

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

AI Technical Summary

Problems solved by technology

[0006] Trifluridine, which is an effective drug component of TAS-102, has the chemical structure shown in formula I, but there is no literature report about its pharmaceutical crystal form with high crystallinity, high purity and good stability, so a stable Good, high-purity, high-crystallinity trifluridine in crystalline form suitable for pharmaceutical applications has important practical significance

Method used

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  • Trifluridine compound and medicine composition thereof
  • Trifluridine compound and medicine composition thereof
  • Trifluridine compound and medicine composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]Add 1.5g (5.07mmol) Trifluridine primary product into 10mL methyl acetate, beat at 20°C for 20min, filter, add the filtered solid into 3mL mixed solvent of water and methanol (1:1 V / V), heat to 60°C The solid was fully dissolved until clear, then cooled to 10° C., left to stand for crystallization for 3 hours, filtered, collected and dried to obtain 1.06 g of white solid, yield: 70.7%.

Embodiment 2

[0036] Add 1.5g (5.07mmol) Trifluridine primary product into a mixed solvent composed of 7.5mL ethyl acetate and 7.5mL n-heptane, beat at 25°C for 30min, filter, add the filtered solid to water and ethanol (2:1V / V ) in 3mL mixed solvent, heated to 65°C to fully dissolve the solid until clear, then cooled to 16°C, stood for crystallization for 3.5h, filtered, collected the solid, and dried to obtain 1.13g of white solid, yield: 75.3%.

Embodiment 3

[0038] Add 1.5g (5.07mmol) Trifluridine primary product into a mixed solvent composed of 5.7mL butyl acetate and 14.3mL n-hexane, beat at 30°C for 45min, filter, add the filtered solid to water and n-butanol (3:1V / V ) in 3mL mixed solvent, heated to 75°C to fully dissolve the solid until clear, then cooled to 20°C, stood for crystallization for 3.5h, filtered, collected the solid, and dried to obtain 1.1g of white solid, yield: 73.3%.

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical chemical engineering, and particularly discloses a novel crystal form Trifluridine compound, a preparation method and medicine composition thereof. The Trifluridine novel crystal form is good in stability and solubility; the preparation method is relatively good in reproducibility, the operation is simple and convenient, the period is short, the cost is low, damage to the environment and staff is little, and the preparation method is suitable for industrial large-scale production, and has quite important application value in medicine preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and specifically relates to a new crystal form of Trifluridine, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Trifluridine (Trifluorothymidine, referred to as FTD or TFT) is also known as trifluorothymidine, trifluorothymidine, 5-trifluoro-2'-deoxythymidine (5-trifluoro-2'-deoxythymidine), 5-trifluoromethyl -2′-Deoxyuridine (5-trifluromethyl-2′-deoxyuridine), α,α,α-trifluorouridine (α,α,α-trifluoro-Uridine), its molecular formula is C 10 h 11 f 3 N 2 o 5 , the chemical structural formula is as follows: [0003] [0004] People have paid attention to the thymidine structural analog Trifluridine for many years, because of its antitumor and antiviral activities, people have done a lot of research on it in the field of medicine. Trifluridine is a thymidylate synthase (TS) inhibitor that interferes with the production of th...

Claims

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Application Information

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IPC IPC(8): C07H19/073C07H1/06A61K31/7072A61P35/00A61P31/12
Inventor 陈庆财赵俊赵小伟赵骞杨瑞峰李淦
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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