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Isoquinoline drug, its preparation and application

A technology of isoquinolines and derivatives, applied in the field of medicine, can solve the problems of berbamine hydrochloride crystalline hydrate that have not been published in the literature, and achieve the effects of improving operability, facilitating storage and transportation, and preventing adhesion

Inactive Publication Date: 2013-04-03
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently published literature has only reported berbamine hydrochloride [C 37 h 40 N 2 o 6 2HCl, molecular weight: 681.65], and the pharmacology and clinical application of berbamine, such as literature: Analysis of the pharmacological effects of berbamine [Chinese Tropical Medicine 2005, 5(1):109-110)], Berbamine Cardiovascular pharmacological action research progress [Chinese Journal of Integrated Traditional Chinese and Western Medicine, 2005, 25 (8): 765-768)] etc., but so far, there is no published literature at home and abroad to report the hydration of berbamine hydrochloride crystals of the present invention thing[C 37 h 40 N 2 o 6 2HCl n H 2 O, wherein n=3.0, 3.5] and its preparation method and use

Method used

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  • Isoquinoline drug, its preparation and application
  • Isoquinoline drug, its preparation and application
  • Isoquinoline drug, its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0065] Embodiment 2 (attached Figure 4 ), at the positions of the following 2θ values ​​of about 6.37, 7.30, 9.28, 10.32, 11.15, 11.67, 12.71, 13.36, 13.80, 14.40, 15.04, 15.64, 16.66, 17.16, 18.30, 19.26, 19.92, 20.71, 21.20, 243.62 , 25.46, 26.64, 27.14, 27.86, 29.04, 29.97, 30.53, 31.90, 33.45 etc. have characteristic peaks,

[0066] attached Figure 4 Where the above data is unclear, the following data can be seen, and the details are as follows:

[0067] PEAK: 21-pts / Parabolic Filter, Threshold=3.0, Cutoff=1.0%, BG=3 / 1.0, Peak-Top=Centroid Fit

[0068]

[0069]

[0070] In another embodiment (Example 3), measured by powder X-ray diffraction method, within the measurement range of diffraction angle 2θ (3-60°), berbamine hydrochloride 3.5 hydrate of the present invention can include the following 2θ values The positions have corresponding eigenvalues, about 6.31, 6.84, 7.24, 11.05, 11.61, 12.67, 13.77, 14.31, 14.83, 15.59, 16.56, 17.13, 18.20, 19.02, 19.62, 20.69,...

Embodiment 1

[0071] Example 1 Preparation of berbamine hydrochloride trihydrate In a 250ml flask, add 60ml of water, 10g of berbamine hydrate, add 6M hydrochloric acid solution, stir to dissolve, control the pH of the solution to about 1.5-3.5, and continue stirring for 30 minutes Add an appropriate amount of activated carbon, stir, filter, concentrate the filtrate, add an appropriate amount of isopropanol, cool, leave to precipitate solid crystals, filter, and dilute the obtained solid at about 30°C for about 2 days, then place it in a container with a color-changing silica gel desiccant Dry in a glass desiccator at room temperature of about 20°C, and dry in vacuum at about 45°C (the reading of the vacuum gauge in the vacuum drying oven is about 0.08MPa) for 6 hours to obtain 8.3g of off-white to light yellow crystalline powder. Identification: (1) Take about 10 mg of the product of the present invention, add 5 ml of water to dissolve it, put it in two test tubes, add 1 drop of bismuth pot...

Embodiment 3

[0073] Example 3 Preparation of berbamine hydrochloride 3.5 hydrate Take 12.6g of berbamine, add 50ml of ethanol and 5ml of water in a 250ml flask, add hydrochloric acid solution with a concentration of about 6M, stir to make the solution pH=1.0-3.5 after dissolution , continue stirring for about 30 minutes, after concentration, add an appropriate amount of isopropanol, place it, cool it to about 0°C, place it, wait until the precipitate is fully separated, filter, and recrystallize the obtained solid twice with an appropriate amount of water, isopropanol, and acetone , cooled, placed, until the solid is fully separated, filtered, the obtained solid is diluted and dried at about 30°C for about 1 day, and then placed in a glass desiccator with a color-changing silica gel desiccant and dried at room temperature at about 20°C, the obtained solid The product was dried at about 42°C for 6 hours to obtain 6.1 grams of off-white solid; identification: (1) Take about 10 mg of the produ...

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PUM

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Abstract

The invention relates to an isoquinoline drug, and its preparation method and application. The molecular formula of the drug is C37H40N2O6.2HCl.nH2O, wherein n is 3 or 3.5. With good storage stability, the isoquinoline drug is suitable for application in preparation of medicines promoting proliferation of white blood cells, preventing white blood cell decrease after cancer radiotherapy and chemotherapy, resisting inflammation, resisting tuberculosis, resisting silicosis, resisting tumor, reducing blood pressure, resisting myocardial anoxia and ischemia, resisting arrhythmia, and treating or preventing other diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, and specifically provides bisbenzyl isocyanate, which has the functions of promoting leukocyte proliferation, anti-inflammation, anti-hypertension, anti-myocardial hypoxia-ischemia, anti-arrhythmia, anti-tuberculosis, anti-tumor, and anti-silicosis. Quinoline alkaloid berbamine derivatives and their preparation and use. Background technique [0002] Berbamine is an isoquinoline alkaloid, which has the effects of promoting leukocyte proliferation, anti-inflammation, anti-hypertension, anti-myocardial hypoxia-ischemia, anti-arrhythmia, anti-tuberculosis, anti-tumor, and anti-silicosis. Currently published literature has only reported berbamine hydrochloride [C 37 h 40 N 2 o 6 2HCl, molecular weight: 681.65], and the pharmacology and clinical application of berbamine, such as literature: Analysis of the pharmacological effects of berbamine [Chinese Tropical Medicine 2005, 5(1):109-110)]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/18A61K31/4748A61P35/00A61P7/06A61P29/00A61P31/06A61P11/00A61P9/12A61P9/10A61P9/06
Inventor 刘力
Owner 刘力
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