5-flucytosine salt as well as preparation method and application thereof

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

Active Publication Date: 2014-08-06
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

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  • 5-flucytosine salt as well as preparation method and application thereof
  • 5-flucytosine salt as well as preparation method and application thereof
  • 5-flucytosine salt as well as preparation method and application thereof

Examples

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preparation example Construction

[0032] 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 or removing the solvent in the solution After processing the solution, the obtained colorless transparent crystal or white powder is the final product.

[0033] 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.

[0034] In this preparation method, the solvent is preferably water.

[0035] In a more specific embodiment, the preparation method of 5-fluorocytosine salt of the present invention may comprise the following steps:

[0036] 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 unsaturated solution;

[0037] 2) After filtering, let the...

Embodiment 1

[0051] Example 1: Preparation of salt (that is, 5-fluorocytosine salt, the same below): Weigh 0.2 mmol 5-fluorocytosine and 0.2 mmol acesulfame potassium, dissolve them in 10 mL ultrapure water successively, filter them and put them in liquid nitrogen Freeze and freeze-dry for 72h to obtain 46.8mg of salt. Yield 80.1%. XRD patterns such as figure 2 shown.

Embodiment 2

[0052] Example 2: Salt preparation: Weigh 0.4 mmol 5-fluorocytosine and 0.4 mmol acesulfame K, dissolve them in 20 mL ultrapure water successively, filter them, freeze them in liquid nitrogen, freeze-dry for 72 hours, and obtain 94.0 mg 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-flucytosine salt as well as a preparation method and application thereof. The 5-flucytosine salt is an acesulfame salt, and mainly comprises 5-flucytosine cation (FCH+), acesulfame anion (AH-) and hydrone (H2O) according to the molar ratio of 1:1:0.5, wherein the structure cell belongs to a monoclinic system; the axial length a is equal to 26.3596 (11) angstroms; b is equal to 5.8523 (3) angstroms; c is equal to 32.3137 (11) angstroms; the axial angle alpha is equal to 90.00 degrees; beta is equal to 105.987 (4) degrees; gamma is equal to 90.00 degrees. The 5-flucytosine salt disclosed by the invention can effectively solve the problem that 5-flucytosine is low in humidity stability; the 5-flucytosine salt is of high heat stability, and can be prepared by conventional methods such as a lyophilization method and a solution crystallization process; the preparation method is simple in process, easy in operation, low in cost and free of poisonous solvents; in the meantime, as a sweetening agent, the guest molecule can improve the taste of a drug, and can be applied to 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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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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