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Application of O-(piperazinyl) ethyl derivative of cleistanone to preparation of medicine for resisting erythrocyte hypoplastic anemia

A technology for low erythrocytosis and ethyl derivatives, which is applied in the field of preparation of O-ethyl derivatives of cylindrine, and can solve the problems of insufficient hematopoietic raw materials or utilization obstacles and the like

Active Publication Date: 2015-01-21
冬青南京生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] (3) Anemia caused by insufficient hematopoietic raw materials or utilization disorders
[0019] 1) Folic acid or B vitamins 12 Anemia caused by deficiency or utilization disorder Megaloblastic anemia caused by absolute or relative deficiency or utilization disorder of folic acid or vitamin B12 due to various physiological or pathological factors

Method used

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  • Application of O-(piperazinyl) ethyl derivative of cleistanone to preparation of medicine for resisting erythrocyte hypoplastic anemia
  • Application of O-(piperazinyl) ethyl derivative of cleistanone to preparation of medicine for resisting erythrocyte hypoplastic anemia
  • Application of O-(piperazinyl) ethyl derivative of cleistanone to preparation of medicine for resisting erythrocyte hypoplastic anemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Preparation of Example 1 Compound Cleistanone

[0039] The preparation method of the compound Cleistanone (I) refers to the literature published by Van Trinh Thi Thanh et al. , pages 4108–4111, August 2011).

[0040]

Embodiment 2

[0041] Synthesis of O-bromoethyl derivatives (II) of cleistanone Cleistanone of embodiment 2

[0042]Compound I (440 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.04 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 25 °C for 24 h. After 24 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 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, v / v), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (344 mg, 63%).

[0043] 1H NMR (...

Embodiment 3

[0047] Synthesis of O-(piperazinyl) ethyl derivative (III) of cleistanone Cleistanone of embodiment 3

[0048] Compound II (273mg, 0.5mmol) was dissolved in 30mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 3h. 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=100:1.5, v / v), and the light brown concentrated elution band was collected to obtain compound III as a light brown solid (196.9 mg, 71%).

[004...

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PUM

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Abstract

The invention relates to the fields of organic synthesis and pharmaceutical chemistry, in particular to O-(piperazinyl) ethyl derivative of cleistanone, and a preparation method and the application of the O-(piperazinyl) ethyl derivative to the preparation of medicine for resisting erythrocyte hypoplastic anemia. The invention compounds new O-(piperazinyl) ethyl derivative, and discloses a preparation method thereof. Pharmacology experiments show that the O-(piperazinyl) ethyl derivative has the effect of resisting erythrocyte hypoplastic anemia, and has the value of developing medicine for resisting erythrocyte hypoplastic anemia.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to O-(piperazinyl)ethyl derivatives of cleusenone, a preparation method and uses thereof. Background technique [0002] There are different classifications of anemia based on different clinical features. Such as: acute and chronic anemia according to the progress of anemia; proliferative anemia (such as hemolytic anemia, iron deficiency anemia, megaloblastic anemia, etc.) and hypoplastic anemia (such as aplastic anemia) ). [0003] Clinically, it is often classified from the pathogenesis and etiology of anemia: [0004] 1. Hemorrhagic anemia [0005] According to the rate of blood loss, it can be divided into acute and chronic, and chronic hemorrhagic anemia is often combined with iron deficiency anemia. It can be divided into coagulation diseases (such as idiopathic thrombocytopenic purpura, hemophilia and severe liver disease, etc.) and non-coagulation...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P7/06C07J63/00
CPCA61K31/58C07J63/008
Inventor 皋林朱延通罗东君吴俊华
Owner 冬青南京生物科技有限公司
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