Preparation and application for compound for treating cerebrovascular disease

A cerebrovascular disease, compound technology, applied in the field of medicine, to achieve the effect of reducing mortality, reversing ischemic damage of vascular endothelial cells, and enhancing normobaric hypoxia tolerance

Inactive Publication Date: 2012-08-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There have been many reports on the use of nitrones for the protection of ischemic brain neurons, and the mechanism is to eliminate the oxidative stress (Bowman, W.C. Pharmacology & Therapeutics 2003, 100, 195-214). The report of ischemic injury of vascular endothelial cells and protective effect of cerebrovascular injury

Method used

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  • Preparation and application for compound for treating cerebrovascular disease
  • Preparation and application for compound for treating cerebrovascular disease
  • Preparation and application for compound for treating cerebrovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Synthesis of α-[2-(2-methoxyphenyl)]phenyl-N-tert-butylnitrone (WS-0426) by chemical synthesis

[0023] step 1:

[0024] The synthesis of o-(2-methoxyphenyl)benzaldehyde: add 1.85 grams (10mmol, 1.0eq) of o-bromobenzaldehyde, 1.82 grams (12mmol, 1.2eq) of 2-methoxy Phenylboronic acid, 3.2 g (12 mmol, 1.2 eq) of potassium phosphate hydrate, 0.23 mg (0.01 mol%) of Pd(OAc) 2 And 25mL of N, N-dimethylacetamide (DMA): H 2 O (4:1), under the protection of nitrogen, heated to 80°C for 24 hours. After the reaction, lower the temperature to room temperature, add 50mL of water and stir for 5 minutes, extract with ethyl acetate (50mL×3), combine the organic phases, and successively use 10mL of 1N sodium hydroxide aqueous solution, 100mL of water and 100mL of saturated saline Wash each once. The organic phase was dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain a crude product. The crude product was separated and purifi...

Embodiment 2

[0028] The synthesis of 2-(2-methoxyphenyl)benzaldehyde: the catalyst Pd(OAc) in the embodiment one step 1 2 The dosage was changed to 2.3 mg (0.1 mol%), and the reaction time was changed to 5 hours to obtain 2.04 g of 2-(2-methoxyphenyl)benzaldehyde with a yield of 96%.

Embodiment 3

[0030] The synthesis of 2-(2-methoxyphenyl)benzaldehyde: the catalyst Pd(OAc) in the embodiment one step 1 2 The dosage was changed to 2.3 mg (0.1 mol%), the reaction temperature was changed to 40° C., and the reaction time was changed to 5 hours to obtain 1.95 g of 2-(2-methoxyphenyl)benzaldehyde with a yield of 92%.

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Abstract

The invention provides application of alpha-[2-(2-metoxybenzene)] phenyl-N-tertiary butyl nitrone (WS-0426) in terms of preparation of medicines for treating a cerebrovascular disease with the pathological feature of vascular endothelial ischemic injury. An aqueous phase system and ligand-free low-capacity palladium catalysis coupling reaction are adopted to synthesize 2-(2- metoxybenzene) benzaldehyde. A pharmacological test shows that the alpha-[2-(2-metoxybenzene)] phenyl-N-tertiary butyl nitrone can effectively reduce mortality of vascular endothelial cells, can reverse ischemic injury of the vascular endothelial cells, strengthens constant-pressure oxygen-deficit tolerance of mice, accordingly relieves ischemic injury of brain tissues, can reduce or stop vascular endothelial cell injury induced by ischemic injury, strengthens anti-hypoxia ability, and is used as a medicine for preventing and curing the cerebrovascular disease with the pathological base of the vascular endothelial cell injury.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the use of a nitrone compound in the preparation of medicines. Especially related to α-[2-(2-methoxyphenyl)]phenyl-N-tert-butylnitrone (WS-0426) used in the preparation of vascular endothelial cell ischemic injury related cerebrovascular disease prevention and The use of therapeutic medicine, and the preparation method of α-[2-(2-methoxyphenyl)]phenyl-N-tert-butylnitrone (WS-0426). Background technique [0002] According to the survey results of the World Health Organization, the incidence of stroke in China ranks first in the world, twice as high as that in the United States. The monitoring results of the past two decades show that the annual death toll of stroke exceeds 2 million, with an annual growth rate of 8.7%. In addition to the high fatality rate, stroke also has the characteristics of high disability rate and high recurrence rate, which seriously threatens the life and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/15C07C251/54C07C249/10A61P9/10
Inventor 吴金龙韩峰卢应梅戴静田允黄继云张根生陶蓉蓉廖美华林本国
Owner ZHEJIANG UNIV
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