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Application of O-(diethylin) ethyl derivative of Daphmalenine A to preparation of drug for increasing white blood cells

A technology for raising white blood cells by ethyl derivatives, applied in the field of preparation of O-ethyl derivatives, can solve the problems of low safety and high toxicity of white blood cells

Inactive Publication Date: 2015-09-23
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • 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 O-(diethylin) ethyl derivative of Daphmalenine A to preparation of drug for increasing white blood cells
  • Application of O-(diethylin) ethyl derivative of Daphmalenine A to preparation of drug for increasing white blood cells
  • Application of O-(diethylin) ethyl derivative of Daphmalenine A to preparation of drug for increasing white blood cells

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Experimental program
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Effect test

Embodiment 1

[0016] The preparation of embodiment 1 compound Daphmalenine A

[0017] The preparation method of compound Daphmalenine A (I) refers to the literature published by Yu Zhang et al. , 4103–4107) approach.

[0018]

Embodiment 2

[0019] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Daphmalenine A

[0020] Compound I (419 mg, 1.00 mmol) was dissolved in 10 mL of benzene, tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 12 h. After 12 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 four 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=100:1.5, v / v), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (320 mg, 61%).

[0021] 1H NMR (500MHz,...

Embodiment 3

[0025] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Daphmalenine A

[0026] Compound II (263 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and diethylamine (1460 mg, 20 mmol) were added thereto, and the mixture was heated to reflux for 10 h . After the reaction, the reaction solution was poured into ice water, extracted four times 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, v / v), and the yellow concentrated elution band was collected to obtain the O-(diethylamino)ethyl derivative of Daphmalenine A (I...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a Daphmalenine A derivative, a preparation method, and an application of the derivative to preparation of a drug for increasing white blood cells. The new Daphmalenine A derivative is synthesized, and the preparation method of the derivative is disclosed. Pharmacology experiments show that the Daphmalenine A derivative has an effect of increasing the white blood cells and is valuable in developing the drug 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 O-(diethylamino)ethyl derivatives of Daphmalenine A, a preparation method and uses 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 efficie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61P7/00C07D491/107
Inventor 江春平吴俊华
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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