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Application of 3,3',5,5'-tetraisopropyl-4,4'-diphenol in prevention and treatment for ischemic stroke

A technology for ischemic stroke and diphenol, applied in the field of medicine, can solve problems such as limiting clinical application, and achieve the effects of less trauma and accurate control of ischemia and reperfusion time.

Active Publication Date: 2015-04-29
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the general anesthetic effect of propofol itself limits its clinical application in the treatment of ischemic stroke

Method used

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  • Application of 3,3',5,5'-tetraisopropyl-4,4'-diphenol in prevention and treatment for ischemic stroke
  • Application of 3,3',5,5'-tetraisopropyl-4,4'-diphenol in prevention and treatment for ischemic stroke
  • Application of 3,3',5,5'-tetraisopropyl-4,4'-diphenol in prevention and treatment for ischemic stroke

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1, 3,3',5,5'-tetraisopropyl-4,4'biphenol

[0062]

[0063]Weigh 20g of propofol and dissolve it in 100ml of ethyl acetate, then add 24.75g of silver carbonate and 10g of anhydrous magnesium sulfate, stir at room temperature for 2h, and detect that the reaction is complete. Add water to the reaction liquid until no bubbles are generated, filter the solid, wash with ethyl acetate, remove the water phase, dry the ethyl phase with anhydrous sodium sulfate for 1 h, filter, evaporate the filtrate to dryness under reduced pressure, add appropriate amount of Washed with water and methanol to obtain 12.30 g of red crystals. Weigh 7 g of the above-mentioned red solid and dissolve it in 100 mL of ethyl acetate. In addition, dissolve 27.66 g of sodium hydrosulfite in 1 mol / L NaOH, mix the two, stir at room temperature for 1.5 h, and detect that the reaction is complete. The ethyl acetate phase was separated, the aqueous phase was extracted twice with ethyl acetate, drie...

Embodiment 2

[0065] Example 2, 4'-hydroxyl-3,3',5,5'-tetraisopropylbiphenyl-4-acetate

[0066]

[0067] Dissolve 4'-benzyloxy-3,3',5,5'-tetraisopropylbiphenyl-4-acetate (5 g, 10.27 mmol) in 200 mL of methanol at room temperature, and then add 10% palladium carbon ( 570mg), vacuumize, hydrogen, repeat three times, seal and react at room temperature for 10h, filter the palladium carbon in the reaction solution, and evaporate the filtrate under reduced pressure to obtain 4'-hydroxy-3,3',5,5'-tetraiso Propylbiphenyl-4-acetate (3.9 g, 95.73%), white solid.

[0068] white solid; 1 H NMR (300MHz, CDCl 3 )δ7.19 (s, 4H), 4.86 (s, 1H), 3.37-3.32 (m, 4H), 3.16 (s, 3H), 1.20 (d, 24H).

Embodiment 3

[0069] Example 3, 3,3',5,5'-tetraisopropylbiphenyl-4'4-diacetate

[0070]

[0071] Add 4,4'-dihydroxy-3,3',5,5'-tetraisopropylbiphenyl (5g, 14.10mmol) into 30mL of acetic anhydride, under nitrogen protection, reflux for 3h, the reaction solution Cool to room temperature, remove acetic anhydride under reduced pressure, add water (200 mL) to the residue, a white solid appears, wash with 10% cold ethanol (100 mL) and water (200 mL), dry to give 3,3',5,5' - Tetraisopropylbiphenyl-4'4-diacetate (6 g, 95.06%). white solid.

[0072] white solid, 1 H NMR (300MHz, CDCl 3 )δ7.19(s,4H),2.91-2.89(m,4H),2.32(s,6H),1.19(d,24H).

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Abstract

The invention relates to an application of 3,3',5,5'-tetraisopropyl-4,4'-diphenol and pharmaceutical salts, ester compounds or solvent compounds thereof in preparation for traditional Chinese medicines for preventing and treating ischemic stroke. The structure of the diphenol structure is specified in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a new medicine application. In particular, it relates to a new application of biphenol in combating and preventing ischemic stroke. Background technique [0002] In recent years, stroke has become a common disease that seriously threatens the health of human beings, especially middle-aged and elderly people over 50 years old. The characteristics of "four highs and one multiple", stroke patients, due to various predisposing factors, cause cerebral artery stenosis, occlusion or rupture, resulting in acute cerebral blood circulation disorder, clinically manifested as transient or permanent brain dysfunction Symptoms and signs. [0003] According to statistics, 40 million people die of stroke every year in the world, and the number of cases in China alone reaches 2 million every year. There are 7 million surviving patients, 4.5 million of whom have lost their labor force and are una...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61K31/222A61P9/10A61P25/28C07C39/15C07C37/16C07C69/16C07C67/08
CPCA61K31/05A61K31/222C07C37/16C07C67/08C07C39/15C07C69/16A61K9/08A61K9/107A61K9/127A61K9/16A61K9/19A61K9/20A61K9/48A61P9/10C07C37/01
Inventor 王汝涛陈涛安龙赵熠王惟娇郭树攀肖飒庞箐华胡慧静
Owner XIAN LIBANG PHARMA
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