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Half 5-fluorocytosine salt, its preparation method and application

A technology of flucytosine salt and flucytosine, which is applied in the field of chemical pharmaceuticals to achieve the effects of high repeatability, simple preparation process and high crystal purity

Active Publication Date: 2016-06-15
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In fact, no pharmaceutically acceptable hemi-5-fluorocytosine salt with good moisture stability has been reported so far

Method used

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  • Half 5-fluorocytosine salt, its preparation method and application
  • Half 5-fluorocytosine salt, its preparation method and application
  • Half 5-fluorocytosine salt, its preparation method and application

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preparation example Construction

[0027] In some embodiments of the present invention, the preparation method of the salt may include the following steps:

[0028] (1) At a certain temperature, 5-fluorocytosine and acesulfame potassium are completely dissolved in the solvent according to a certain molar ratio to form a supersaturated, saturated or nearly saturated state;

[0029] (2) Lower the temperature of the above mixed solution, let it stand or volatilize the solvent, and precipitate salt crystals;

[0030] (3) Vacuum drying the obtained crystals to obtain colorless transparent crystals or white powder is the final product.

[0031] Further, the aforementioned solvent may be selected from, but not limited to, one of water, methanol, ethanol, acetic acid or a mixed solvent in any proportion thereof.

[0032] In a preferred embodiment, the dissolution temperature of the raw materials such as 5-fluorocytosine and acesulfame potassium is from room temperature to 80°C.

[0033] In a preferred embodiment, the...

Embodiment 1

[0038] Example 1 Preparation of salt (semi-5-fluorocytosine salt, the same below): Weigh 0.2mmol 5-fluorocytosine and 0.1mmol acesulfame potassium, dissolve in 20mL methanol at 40°C, and volatilize at 25°C after filtration to obtain crystals Salt, productive rate 95%, XRD pattern such as figure 2 shown.

Embodiment 2

[0039] Example 2 Preparation of salt: Weigh 1mmol 5-fluorocytosine and 0.5mmol acesulfame potassium, dissolve in 15mL water at room temperature, and volatilize at 60°C after filtration to obtain crystalline salt with a yield of 84%. Its solid NMR fingerprint spectrum is as follows: image 3 , as shown in 4.

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Abstract

The invention discloses a semi-5-fluorocytosine salt, its preparation method and application. The salt is acesulfame potassium salt, which is mainly composed of 5-fluorocytosine cation (FCH+), 5-fluorocytosine neutral molecule (FC) and acesulfame potassium anion (AH-) in a molar ratio of 1:1:1 Composition, and the unit cell of the salt belongs to the triclinic system, its axial length a=7.2613 (2)? , b=10.5289(3)? , c=11.6662(4)? , axis angle α=66.8180(11)°, β=82.0220(12)o, γ=78.5670(12)o. The semi-5-fluorocytosine salt prepared by the invention can effectively improve the problem of poor moisture stability of 5-fluorocytosine, has good effective drug content and thermal stability, and has simple preparation process, easy operation and low cost , there is no toxic solvent residue, and the guest molecular component is a sweetener, which can improve the taste of the drug and is suitable for the pharmaceutical industry.

Description

technical field [0001] The invention particularly relates to a 5-fluorocytosine salt and a preparation method thereof, belonging to the field of chemical pharmacy. Background technique [0002] More than 80% of pharmaceutical products are developed and applied in the form of solid oral dosage forms. The same drug substance can be developed into different solid state forms, such as: polymorphs, hydrates, solvates, salts and co-crystals. Different solid state forms have different physicochemical properties. Drug salt formation technology is widely used in the pharmaceutical industry to improve the physical and chemical properties of drugs. According to statistics, more than half of APIs are developed into their salt forms. [0003] The molecular formula for 5-fluorocytosine is C 4 h 4 FN 3 O, which is a widely used antibacterial drug, is mainly used in the treatment of infective endocarditis, urinary tract infection and lung infection. 5-fluorocytosine itself has no ant...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/47C07D291/06A61P31/10
CPCC07D239/47C07D291/06
Inventor 张海禄王林汪莲艳邓宗武
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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