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Application of composition of O-(triazolyl) ethyl of Schiglautone A and O-(2-methyl sulfonium ethyl) amido) ethyl derivative in low red blood cell anemia resisting drugs

A low red blood cell and composition technology, applied in the field of preparation and composition, can solve the problems of insufficient hematopoietic raw materials or utilization obstacles

Inactive Publication Date: 2016-12-07
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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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) 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 composition of O-(triazolyl) ethyl of Schiglautone A and O-(2-methyl sulfonium ethyl) amido) ethyl derivative in low red blood cell anemia resisting drugs
  • Application of composition of O-(triazolyl) ethyl of Schiglautone A and O-(2-methyl sulfonium ethyl) amido) ethyl derivative in low red blood cell anemia resisting drugs
  • Application of composition of O-(triazolyl) ethyl of Schiglautone A and O-(2-methyl sulfonium ethyl) amido) ethyl derivative in low red blood cell anemia resisting drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 compound Schiglautone A

[0031] The preparation method of compound Schiglautone A (I) refers to the literature published by Fan-Yu Meng et al. of Schisandra glaucescens. Organic Letters 13 (2011) 1502–1505).

[0032]

Embodiment 2

[0033] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Schiglautone A

[0034] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and 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 8 h. After 8 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=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%...

Embodiment 3

[0039] The synthesis of the O-(triazolyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0040] Compound II (358 mg, 0.5 mmol) was dissolved in 10 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and 1,2,3-triazole (2760 mg, 40 mmol) were added thereto ), the mixture was heated to reflux for 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=100:1.0, v / v), and the light yellow concentrated elution band was collected to obtain compound III as a yellow colloidal solid (245.7mg, 71%) .

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PUM

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Abstract

The invention relates to fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method of the composition and an application of the preparation method in preparing low red blood cell anemia resisting drugs. As is indicated in pharmacological experiment, the composition features in resisting low red blood cell anemia and has the value in development of the low red blood cell anemia resisting drugs.

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] 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 is a bone marrow hematop...

Claims

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Application Information

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IPC IPC(8): A61K31/4192A61K31/195C07D249/04C07C323/25A61P7/06
CPCA61K31/4192A61K31/195C07C323/25C07D249/04A61K2300/00
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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