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Xanthiphenylketamine crystal and its preparation method and medical use

A technology of piperphentonamine and crystals, which is applied in the fields of piperphentonamine crystals and its preparation and medicinal uses, and can solve problems such as piperphentonamine crystals not specified, preparation methods of piperphentonamine crystals not specified, and medicinal uses, etc. problems, to achieve the effect of good storage stability, high purity and high biological activity

Active Publication Date: 2008-08-06
江西国能医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The Chinese patent with application number 02125318.8 discloses the preparation method of piperphentonamine compound, but it does not specify the existence of the crystal form of piperphentonamine crystals, nor does it explain the preparation method and pharmaceutical use of piperphentonamine crystals

Method used

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  • Xanthiphenylketamine crystal and its preparation method and medical use
  • Xanthiphenylketamine crystal and its preparation method and medical use
  • Xanthiphenylketamine crystal and its preparation method and medical use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 1.56g of piperphentonamine hydrochloride (see Chinese patent 02125318.8 for the preparation method of piperphentonamine hydrochloride) and put it into a 500ml eggplant-shaped bottle, add 100ml of ethyl acetate, and slowly add saturated aqueous sodium bicarbonate solution under cooling in an ice-water bath 80ml, the solution gradually changed from a suspension to a clear solution with the addition of saturated aqueous sodium bicarbonate solution, and after one hour, the solution turned into a cloudy solution again, and was stirred for 5 hours under ice-water bath cooling, the organic layer was separated, and the water layer was re- Extracted with ethyl acetate, the combined organic layers were washed with NaCl saturated aqueous solution, washed with anhydrous NaCl 2 SO 4 Dry, filter, and when the filtrate is concentrated to a small amount of liquid, off-white flaky crystals are precipitated, filtered, off-white flaky crystals are washed with absolute ethanol, dried ...

Embodiment 2

[0039] Take 720 mg of piperphentonamine-like white flaky crystals described in Example 1, heat and dissolve them with 90 ml of ethyl acetate to obtain a colorless and clear solution, filter, and place the filtrate in an incubator at 8° C. for 10 days to slowly precipitate out the like White flaky crystals are piperphentonamine crystal grains. When the grains gradually become larger and thicker and grow into single crystals, they can be used as single crystal X-diffraction samples for X-ray diffraction of piperphentonamine single crystals. test.

[0040] Instrument model: Japan MAC DIP-2030K single crystal X-ray surface detector. Test conditions: moka radiation, graphite monochromator, distance between crystal and IP plate d=100mm, tube pressure 50Kv, tube current 90mA, ω scan, maximum 20 angle is 50.0°, scan range is 0-180°, swing angle is 5°, the interval is 5°, the scanning speed is 1.5° / min, each frame is scanned twice, and a total of 3 images are taken, with 3870 independ...

Embodiment 3

[0046] Analyze the crystal structure with the direct method on the microcomputer, directly obtain 24 non-hydrogen atom positions from the E map, use the least square method and the difference Fourier method to obtain the remaining non-hydrogen atom positions, and use the least square method to correct the structural parameters and discrimination Atomic types, use the geometric calculation method and difference Fourier method to obtain all hydrogen atom positions, the final reliability factor Rf=0.069, Rw=0.063 (w=1 / σ|F| 2 ). Finalize the stoichiometric formula as C 21 h 23 o 4 N 1 , the calculated molecular weight is 353.42, and the calculated crystal density is 1.261g / cm 3 . The molecular structure diagram of the compound is shown in the description, figure 2 is the projection diagram of the three-dimensional structure of the molecule shown, image 3 Shown is the unit cell packing diagram of the molecules along the b-axis. Table 2 shows the atomic coordinate paramete...

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Abstract

The invention relates to a peperphentonamine crystal represented as (E)-5-{(3, 4-methylenedioxy phenylethyl) dimethylamino}-1-p-hydroxybenzene-1-amylene-3-ketone, which formula is represented as above, wherein the crystal powder X diffraction has characteristic peaks under the diffraction angles as 2-theta of 12.06, 15.28, 17.16 and 21.88, the single crystal is colorless, transparent and sheet belonging to monoclinic system, the space group is P21 / a, the molecule number Z in lattice is 4, and the fusion point is 148 to 151 DEG C. The invention further provides a single crystal preparation method, an agent prepared from the crystal and a relative drug application. The inventive peperphentonamine crystal has the advantages of high purity, activity and stable storage or the like, with better agent shape, solubility and clarity.

Description

technical field [0001] The invention relates to a piperphentonamine crystal, a preparation method thereof and an application as a medicine. Background technique [0002] Heart failure is the terminal stage of cardiovascular disease, with a high mortality rate. Myocardial infarction and myocardial reperfusion injury are important causes of heart failure. Experimental studies at home and abroad have shown that calcium antagonists and free radical scavenger can treat myocardial infarction and resist reperfusion injury. However, most calcium antagonists inhibit myocardial contraction and reduce cardiac function, and their clinical effects are limited. Free radical scavengers have no direct impact on cardiac function, and their clinical effects have not yet been confirmed. [0003] The treatment principle of heart failure is to strengthen the heart, dilate blood vessels and diuresis. Cardiotonic drugs enhance cardiac contractility, increase cardiac output, and maintain blood su...

Claims

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Application Information

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IPC IPC(8): C07D317/58A61K31/36A61K9/19A61P9/04
Inventor 万华印李茹冰朱莉亚李永贺周力践刘铁球
Owner 江西国能医药科技有限公司
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