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A kind of 5-fluorocytosine salt, its preparation method and application

A technology of flucytosine salt and flucytosine, which is applied in the field of chemical pharmacy, can solve the problems of reducing the absorption capacity of the small intestine, loss of appetite, causing stones, etc., and achieves the effects of wide boundary conditions of crystallization parameters, high repeatability and mild conditions.

Active Publication Date: 2016-04-27
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Among them, saccharin salt and oxalate are reported to improve hydration problems, but excessive oxalic acid intake has the risk of causing stones, and excessive saccharin intake will affect the normal secretion of gastrointestinal digestive enzymes, reduce the absorption capacity of the small intestine, and reduce appetite. And has a record of causing cancer in experimental animals

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  • A kind of 5-fluorocytosine salt, its preparation method and application
  • A kind of 5-fluorocytosine salt, its preparation method and application
  • A kind of 5-fluorocytosine salt, its preparation method and application

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preparation example Construction

[0031] Further, the preparation method may include: dissolving 5-fluorocytosine and acesulfame potassium in a solvent to form a solution, then filtering, and at least choosing any one of the methods of leaving the solution to stand and removing the solvent in the solution After processing the solution, the obtained colorless transparent crystal or white powder is the final product.

[0032] In the preparation method, the molar ratio of 5-fluorocytosine and acesulfame potassium is preferably 1:1-1:8, 1:3-1:8 or 1:1.

[0033] In this preparation method, the solvent is preferably water.

[0034] In a more specific embodiment, the preparation method of 5-fluorocytosine salt of the present invention may comprise the following steps:

[0035] 1) Under 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 unsaturated solution;

[0036] 2) After filtering, let...

Embodiment 1

[0050] Example 1: Preparation of salt (namely, 5-fluorocytosine salt, the same below): Weigh 0.2mmol 5-fluorocytosine and 0.2mmol acesulfame potassium, dissolve them in 10mL ultrapure water successively, filter them and put them into the liquid Freeze in nitrogen and freeze-dry for 72h to obtain 46.8mg of salt. Yield 80.1%. XRD patterns such as figure 2 shown.

Embodiment 2

[0051] Example 2: Preparation of salt: 0.4mmol 5-fluorocytosine and 0.4mmol acesulfame K were weighed, dissolved in 20mL ultrapure water successively, filtered and then frozen in liquid nitrogen, freeze-dried for 72 hours to obtain 94.0mg of salt. Yield 80.5%. Its solid-state NMR fingerprint image 3 , as shown in 4.

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Abstract

The invention discloses a 5-fluorocytosine salt, its preparation method and application. The 5-fluorocytosine salt is acesulfame potassium salt, which is mainly composed of 5-fluorocytosine cation (FCH+), acesulfame potassium anion (AH-) and water molecule (H2O) in a molar ratio of 1:1:0.5 , its unit cell belongs to the monoclinic system, its axial length a=26.3596(11)? , b=5.8523(3)? , c=32.3137(11)? , axis angle α=90.00°, β=105.987(4)o, γ=90.00o. The 5-fluorocytosine salt of the present invention can effectively improve the problem of poor moisture stability of 5-fluorocytosine, and has good thermal stability, and can be prepared by conventional methods such as freeze-drying method and solution crystallization method, with simple process and easy operation Yes, low cost, no toxic solvents involved, and at the same time, the guest molecule is a sweetener, which can improve the taste of medicines, and can be used in 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] Crystal engineering is to understand the interaction between molecules on the basis of molecular packing, and on this basis to design new solid-state forms to improve the physical and chemical properties of raw materials. In recent years, crystal engineering has been widely used in the pharmaceutical industry. Crystal engineering provides the possibility to prepare solid-state forms of various raw materials through the use of supramolecular synthons. The study of solid state forms of pharmaceuticals is of great significance to the pharmaceutical industry. The same raw drug can be prepared in different solid forms (polymorphs, hydrates, solvates, salts and co-crystals), and different solid forms have different physical and chemical properties, such as: solubility, stability, dissoluti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/47C07D291/06A61K31/513A61K47/22A61P31/00
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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