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Composition and application of composition to medicine for increasing white blood cells

A technology for increasing white blood cells and compositions, which is applied in the field of preparation and compositions, and can solve problems such as low safety and high toxicity of white blood cells

Inactive Publication Date: 2016-02-03
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of leukopenia have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

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  • Composition and application of composition to medicine for increasing white blood cells
  • Composition and application of composition to medicine for increasing white blood cells
  • Composition and application of composition to medicine for increasing white blood cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Example 1 Preparation of compound Schiglautone A

[0011] The preparation method of the compound Schiglautone A(I) refers to the method published by Fan-YuMeng et al. (Fan-YuMengetal., 2011.SchiglautoneA, aNewTricyclicTriterpenoidwithaUnique6 / 7 / 9-FusedSkeletonfromtheStemsofSchisandraglaucescens.Organic Letters 13(2011) 1502–1505).

[0012]

Embodiment 2

[0013] Example 2 Synthesis of O-Bromoethyl Derivative (II) of Schiglautone A

[0014] Compound I (502mg, 1.00mmol) was dissolved in 15mL of benzene, tetrabutylammonium bromide (TBAB) (0.08g), 1,2-dibromoethane (7.520g, 40.00mmol) and 6mL of benzene were added to the solution 50% sodium hydroxide solution. The mixture was stirred at 35 degrees Celsius for 8 hours. After 8h, the reaction solution was poured into ice water, immediately extracted twice with dichloromethane, and the organic phase solutions were combined. Then the organic phase solution was washed 3 times with water and saturated brine in turn, and then dried over anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain the crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain the brown powder of co...

Embodiment 3

[0019] Example 3 Synthesis of O-(Diethylamino)ethyl Derivative (III) of Schiglautone A

[0020] Compound II (358mg, 0.5mmol) was dissolved in 10mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and diethylamine (2920mg, 40mmol) were added to it, and the mixture was heated to reflux for 8h . After the reaction, the reaction solution was poured into ice water, extracted twice with the same amount of dichloromethane, and the organic phases were combined. The combined organic phase was washed with water and saturated brine in turn, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain the brown powder of compound III (231.2mg, 66% ).

[0021] 1 HNMR(500...

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PUM

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method of the composition and an application of the composition to preparation of medicine for increasing white blood cells. According to the composition and the preparation method of the composition, pharmacology experiments show that the composition achieves the effect of increasing white blood cells, and has the value for developing the medicine for increasing white blood cells.

Description

Technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to compositions, preparation methods and uses thereof. Background technique [0002] Leukopenia is a disease caused by unknown causes and secondary to other diseases. It is divided into two categories: primary and secondary. The cause of primary patients is unknown; secondary patients believe that the cause can be acute infection, physical and chemical factors, blood system diseases, diseases with splenomegaly, connective tissue diseases, allergic diseases, genetic diseases, etc., acquired or Unexplained neutropenia, etc. [0003] The treatment of leukopenia The existing drugs have the problems of high toxicity and low safety. It is important to find compounds or lead compounds from natural products and modify their structures to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity. [0004] The compound I involved in the ...

Claims

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Application Information

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IPC IPC(8): A61K31/195A61P7/00
Inventor 江春平吴俊华
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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