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Isonicotinamide methylpyrazine derivative eutectic I

A technology of isonicotinamide methyl pyrazine and methyl pyrazine, which is applied in the field of isonicotinamide methyl pyrazine derivative co-crystal I, can solve the problem of less crystal eutectic structure, low yield, and unimproved characterization parameters. and other issues

Active Publication Date: 2019-03-22
LUNAN BETTER PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are many relevant reports about acipimox, but mainly about its preparation, preparation, physical and chemical properties and pharmacological properties. About its crystal eutectic The report of structure is less, and patent US2005239803A1, CN 103508963 A etc. have all reported the preparation method of acipimox, and patent CN86103304-2 obtains the acipimox precipitate of crystalline character, is acipimox hydrate, and productive rate is relatively high. Low
In the previous reports, there were few reports on the acipimus cocrystal cocrystal, and the crystallographic characterization parameters of the acipimus cocrystal were not mentioned

Method used

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  • Isonicotinamide methylpyrazine derivative eutectic I
  • Isonicotinamide methylpyrazine derivative eutectic I
  • Isonicotinamide methylpyrazine derivative eutectic I

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Experimental program
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Effect test

Embodiment 1

[0064] Dissolve 5.0g (32.4mmol) of methylpyrazine derivatives and 4.0g (32.4mmol) of isonicotinamide in 50ml of methanol, heat to 60°C to dissolve, after the solution is clear, cool down to 20°C, and statically crystallize for 48 hours. After filtration and drying, 8.6 g of eutectic form I of the isonicotinamide methylpyrazine derivative was obtained, with a yield of 96.5%, HPLC: 99.96%, and impurity I: 0.03%.

Embodiment 2

[0066] Dissolve 5.0g (32.4mmol) of methylpyrazine derivatives and 6.0g (48.6mmol) of isonicotinamide in 50ml of ethyl acetate, heat to 77°C to dissolve, after the solution is clear, cool down to 15°C, and statically crystallize for 52 hours, filtered and dried to obtain 8.8 g of co-crystal form I of isonicotinamide methylpyrazine derivative, yield 98.0%, HPLC: 99.93%, impurity I: 0.05%.

Embodiment 3

[0068] Dissolve 10.0g (64.8mmol) of methylpyrazine derivatives and 9.6g (77.8mmol) of isonicotinamide in 50ml of methanol, heat to 65°C to dissolve, after the solution is clear, cool down to 10°C, and statically crystallize for 36 hours. After filtration and drying, 17.2 g of the eutectic form I of the isonicotinamide methylpyrazine derivative was obtained, with a yield of 96.0%, HPLC: 99.91%, and impurity I: 0.07%.

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Abstract

The invention belongs to the technical field of the medicine, and specifically provides isonicotinamide methylpyrazine derivative eutectic I, a preparation method thereof, and use thereof for preparing antilipemic agent. The isonicotinamide methylpyrazine derivative eutectic I prepared by the invention uses Cu-Kalpha radiation, an X-ray diffraction spectrum represented by 2theta has characteristicpeaks at 7.2+ / -0.2 degrees, 8.1+ / -0.2 degrees, 14.5+ / -0.2 degrees, and 16.2+ / -0.2 degrees. The prepared isonicotinamide methylpyrazine derivative eutectic prepared is good in stability in the medium,and is high in product purity and good in stability after being placed in a solid state; an animal experimental verifies that the bioavailability is high. The isonicotinamide methylpyrazine derivative eutectic I disclosed by the invention is simple in preparation process and has good industrial application prospect.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, in particular to a co-crystal I of isonicotinamide methylpyrazine derivatives. 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 Stabili...

Claims

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Application Information

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IPC IPC(8): C07D213/81C07D241/24A61K31/4409A61K31/4965A61P3/06
CPCA61P3/06C07B2200/13C07D213/81C07D241/24
Inventor 翟立海郭立红夏祥来
Owner LUNAN BETTER PHARMA
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