Methylpyrazine derivative biological arginine hydrate

A technology of methylpyrazine and its derivatives, which is applied in the field of methylpyrazine derivative arginine hydrate, can solve the problem of acipimus crystallographic characterization parameters that are not mentioned, less crystal eutectic structure, and production problems. Low rate and other issues

Active Publication Date: 2019-03-08
LUNAN PHARMA GROUP CORPORATION
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are many related reports about acipimox, but mainly about its preparation, preparation, physical and chemical properties and pharmacological properties. There are few reports about its crystalline eutectic structure, as reported in patents US2005239803A1, CN 103508963A, etc. The preparation method of acipimox was disclosed, and the patent CN86103304-2 obtained the acipimox precipitate in crystal form, which was hydrated acipimox, and the yield was low
In the previous reports, there were few reports on the co-crystal of acipimus, and the crystallographic characterization parameters of acipimus were not mentioned

Method used

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  • Methylpyrazine derivative biological arginine hydrate
  • Methylpyrazine derivative biological arginine hydrate
  • Methylpyrazine derivative biological arginine hydrate

Examples

Experimental program
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Effect test

Embodiment 1

[0067] Dissolve 5.0g (32.4mmol) of methylpyrazine derivatives and 5.6g (32.4mmol) of arginine in aqueous methanol (50ml of methanol + 0.5ml of water) and heat to 60°C to dissolve. After the solution is clear, cool down to 20 ℃, static crystallization for 52 hours, filtered and dried to obtain 10.9 g of arginine hydrate, a methylpyrazine derivative, with a yield of 97.1%, HPLC: 99.94%, and impurity I: 0.05%.

Embodiment 2

[0069] Dissolve 5.0g (32.4mmol) of methylpyrazine derivatives and 11.2g (48.6mmol) of arginine in 50ml of ethyl acetate aqueous solution (50ml of ethyl acetate + 2ml of water), heat to 75°C to dissolve, and the solution is clarified , cooled to 15° C., static crystallization for 48 hours, filtered and dried to obtain 11.0 g of arginine hydrate, a methylpyrazine derivative, with a yield of 98.0%, HPLC: 99.93%, and impurity I: 0.06%.

Embodiment 3

[0071] Dissolve 10.0g (64.8mmol) of methylpyrazine derivatives and 13.4g (77.8mmol) of arginine amine in aqueous tetrahydrofuran (50ml of tetrahydrofuran + 0.1ml of water), and heat to 65°C to dissolve. After the solution is clear, cool down to Static crystallization at 10°C for 36 hours, filtration and drying to obtain 21.6 g of arginine hydrate, a methylpyrazine derivative, with a yield of 96.3%, HPLC: 99.92%, and impurity I: 0.07%.

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Abstract

The invention belongs to the technical field of medicine and specifically provides methylpyrazine derivative biological arginine hydrate, a preparation method thereof and application thereof in preparing blood fat reducing medicine. The prepared methylpyrazine derivative biological arginine hydrate disclosed by the invention is radiated by Cu-K alpha, and an X ray diffraction spectrogram represented by 2 theta has the characteristic peaks at the 5.7+ / -0.2 degree, 9.1+ / -0.2 degree, 16.2+ / -0.2 degree, 24.5+ / -0.2 degree, 24.8+ / -0.2 degree and 27.8+ / -0.2 degree positions. The prepared methylpyrazine derivative biological arginine hydrate disclosed by the invention has high stability; the purity basically cannot change when the methylpyrazine derivative biological arginine hydrate is placed ina dissolved state and a solid state; the solubility of the methylpyrazine derivative biological arginine hydrate in different media is 2.5 times of an existing crystal form; furthermore, the methylpyrazine derivative biological arginine hydrate has the advantages of higher bioavailability and better industrial application prospect.

Description

technical field [0001] The invention belongs to the technical field of organic drug eutectics, in particular to a methylpyrazine derivative arginine hydrate. Background technique [0002] Drug co-crystals are based on the principle of supramolecular chemistry, that is, molecular recognition and supramolecular self-assembly through intermolecular synergy. The active pharmaceutical ingredient (API) self-assembles with a suitable cocrystal former (CCF) through hydrogen bonds, or non-covalent bonds with saturation and directionality (such as van der Waals forces of aromatic hydrocarbons or benzene rings, π- π conjugation and halogen bond) to form a new structure, that is, drug co-crystal. It is based on hydrogen bonds, and neither needs to form new covalent bonds nor destroy existing covalent bonds. While retaining the pharmacological effects of the drug itself, it can also modify the physical and chemical properties of the drug, such as improving the Stability, reducing its h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/24C07C279/14C07C277/08A61K31/4965A61P3/06
CPCA61P3/06C07B2200/13C07D241/24
Inventor 刘忠翟立海郭立红马庆文
Owner LUNAN PHARMA GROUP CORPORATION
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