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Application of O-(piperidyl)ethyl derivative of Cleistanone in preparation of anti-low erythrocyte anemia drugs

A technology of low red blood cells and ethyl derivatives, which can be used in drug combinations, extracellular fluid diseases, medical preparations containing active ingredients, etc., and can solve problems such as insufficient hematopoietic raw materials or utilization barriers

Active Publication Date: 2014-11-05
谭家湾遗址公园运营管理(桐乡乌镇)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] (3) Anemia caused by insufficient hematopoietic raw materials or utilization disorders
[0017] 1) Anemia caused by folic acid or vitamin B12 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-(piperidyl)ethyl derivative of Cleistanone in preparation of anti-low erythrocyte anemia drugs
  • Application of O-(piperidyl)ethyl derivative of Cleistanone in preparation of anti-low erythrocyte anemia drugs
  • Application of O-(piperidyl)ethyl derivative of Cleistanone in preparation of anti-low erythrocyte anemia drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of Compound Cleistanone

[0039] The preparation method of compound cleistanone Cleistanone (I) refers to the literature published by Van Trinh Thi Thanh et al. Volume2011, Issue22, pages4108–4111, August2011).

[0040]

Embodiment 2

[0041] Example 2 Synthesis of O-Bromoethyl Derivatives (II) of Cleistanone

[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 (500MHz, DMSO-d 6 ...

Embodiment 3

[0047] Example 3 Synthesis of O-(piperidinyl)ethyl derivative (III) of cleistanone Cleistanone

[0048] Compound II (273 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 piperidine (852 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 16 h. After the reaction, the reaction solution was poured into 20 mL of ice water, extracted three 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=100:0.5, v / v), and the yellow concentrated elution band was collected to obtain the yellow color of the O-(piperidinyl)ethyl derivative...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, and in particular relates to an O-(piperidyl)ethyl derivative of Cleistanone, a preparation method thereof and application in preparation of anti-low erythrocyte anemia drugs. The invention synthesizes a new O-(piperidyl)ethyl derivative of Cleistanone and discloses its preparation method. Pharmacological experiments show that the O-(piperidyl)ethyl derivative of Cleistanone provided by the invention has an anti-low erythrocyte anemia effect, and has the value of developing anti-low erythrocyte anemia drugs.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to O-(piperidinyl)ethyl derivatives of cleistanone, 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. Anemia with reduced erythropoiesis [0005] The abnormality of hematopoietic cells, bone marrow hematopoietic microenvironment and hematopoietic raw materials affect erythropoiesis, which can form erythropoietic anemia. [0006] (1) Anemia caused by abnormal hematopoietic stem and progenitor cells [0007] 1) Aplastic anemia (AA) AA ...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P7/06C07J63/00
Inventor 吴俊艺江春平吴俊华
Owner 谭家湾遗址公园运营管理(桐乡乌镇)有限公司
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