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Composition and application thereof in medicine for increasing leukocyte

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

Inactive Publication Date: 2016-02-10
南京海澳斯生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[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 thereof in medicine for increasing leukocyte
  • Composition and application thereof in medicine for increasing leukocyte
  • Composition and application thereof in medicine for increasing leukocyte

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Artalbicacid

[0011] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).

[0012]

Embodiment 2

[0013] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid

[0014] Compound I (266 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 40 °C for 16 h. After 16 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine for 5 times successively, then dried with anhydrous sodium sulfate, and finally 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 a brown powder of Compound II (272mg, 73%...

Embodiment 3

[0019] Synthesis of O-(piperazinyl) ethyl derivative (III) of embodiment 3 Artalbicacid

[0020] Compound II (187mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 4h. After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted twice with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, 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=100:1.5, v / v), the light brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compoun...

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Abstract

The invention relates to the field of organic synthesis and medical chemistry, particularly relates to a composition, a preparation method of the composition and application of the composition in preparing a medicine for increasing leukocyte, and discloses a composition and a preparation method thereof. Pharmacological experiments indicate that the composition has an effect of increasing leukocyte, and has a value of developing medicines for increasing leukocyte.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Leukopenia is a disease caused by unknown reasons and secondary to other diseases, which can be divided into two categories: primary and secondary. The primary cause is unknown; the secondary cause is believed to be caused by 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 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. [00...

Claims

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Application Information

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IPC IPC(8): A61K31/495C07D295/088C07D233/60A61P7/00A61K31/4166
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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