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Application of atropurpuran derivative composition to medicines for increasing white blood cells

A technology for increasing white blood cells and compositions, which can be used in drug combinations, extracellular fluid diseases, active ingredients of heterocyclic compounds, etc., and can solve problems such as low safety and high toxicity of white blood cells

Inactive Publication Date: 2017-02-22
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Application of atropurpuran derivative composition to medicines for increasing white blood cells
  • Application of atropurpuran derivative composition to medicines for increasing white blood cells
  • Application of atropurpuran derivative composition to medicines for increasing white blood cells

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Experimental program
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Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Atropurpuran

[0011] The preparation method of compound Atropurpuran (I) refers to the literature published by Pei Tang et al. (Pei Tang et al., 2009.Atropurpuran, a novel diterpene with an unprecedented pentacycliccage skeleton, from Aconitum hemsleyanum var.atropurpureum.Tetrahedron Letters50(2009)460-462 )Methods.

[0012]

Embodiment 2

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

[0014] Compound I (312 mg, 1.00 mmol) was dissolved in 10 mL of benzene, 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 35 °C for 6 h. After 6h, 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 three 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 yellow powder of Compound II (309mg, 74%) .

[0...

Embodiment 3

[0019] The synthesis of O-(tetrahydropyrrolyl) ethyl derivative (III) of embodiment 3 Atropurpuran

[0020] Compound II (209 mg, 0.5 mmol) was dissolved in 18 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and pyrrolidine (1420 mg, 20 mmol) were added thereto, and the mixture was heated to reflux for 2 h. After the reaction, the reaction solution was poured into 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=100:1.0, v / v), and the concentrated brown elution band was collected and concentrated to give compound III as a brown solid (125 mg, 61%).

[00...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method thereof and application thereof to preparation of medicines for increasing white blood cells. The invention discloses a composition and a preparation method thereof. Pharmacological experiments indicate that the composition provided by the invention has the effect of increasing the white blood cells and has value of developing the medicines for increasing the white blood cells.

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): A61K31/41C07D257/04C07D295/088A61P7/00A61K31/40
CPCA61K31/41A61K31/40C07D257/04C07D295/088
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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