Biphenyl derivative and preparation method and medical application thereof

A derivative, biphenyl technology, applied in the field of medicine, can solve problems such as limiting clinical application, achieve good therapeutic effect, accurately control ischemia and reperfusion time, and reduce the consumption of vitality

Inactive Publication Date: 2018-01-09
HC SYNTHETIC PHARMA CO LTD
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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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  • Biphenyl derivative and preparation method and medical application thereof
  • Biphenyl derivative and preparation method and medical application thereof
  • Biphenyl derivative and preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1: the preparation of compound I-1

[0057]

[0058] Compound I-1

[0059] 10.0 g of 4'-benzyloxy-3,3',5,5'-tetrakis(1,1,1,3,3,3-hexafluoroisopropyl)biphenyl-4-acetate at room temperature Dissolve in 200mL of methanol, then add 1.0g of 10% palladium carbon, vacuumize, pass through hydrogen, repeat three times, seal and react at room temperature for 17h, filter palladium carbon in the reaction solution, and concentrate the filtrate to dryness. The residue was separated by HPLC to obtain 1.7 g of compound (I-1).

Embodiment 2

[0060] Embodiment 2: the preparation of compound 1-2

[0061]

[0062] Compound I-2

[0063] Add 5 g of 4,4'-dihydroxy-3,3',5,5'-tetrakis(1,1,1,3,3,3-hexafluoroisopropyl)biphenyl into 30 mL of acetic anhydride, Under the protection of nitrogen, after reflux for 3 hours, the reaction solution was cooled to room temperature, and acetic anhydride was removed under reduced pressure. The residue was separated by HPLC to obtain 1.2 g of compound (I-2).

Embodiment 3

[0064] Embodiment 3; The preparation of compound 1-3

[0065]

[0066] Compound I-3

[0067] (1) Take 5g of 4,4'-dihydroxy-3,3',5,5'-tetrakis(1,1,1,3,3,3-hexafluoroisopropyl)biphenyl with anhydrous THF (100 mL) was dissolved, and 2.24 g of NaOH as a solid and 8.185 g of bromochloromethane were added. in N2 Reflux for 2 hours under air protection, cool the reaction solution to room temperature, filter, concentrate, and the residue is separated by HPLC to obtain the intermediate.

[0068] (2) Add 14 mL of triethylamine and 0.5 mL of 85% phosphoric acid to 100 mL of anhydrous acetonitrile in sequence, and add the intermediate obtained in (1) into the acetonitrile solution under stirring conditions, and then react at 65° C. for 2 h. The reaction solution was cooled to room temperature, the solvent was evaporated, the residue was dissolved in 15 mL of water, and the pH was adjusted to 1.5 with 8M HCl; extracted with anhydrous ether, the organic phases were combined, washed wit...

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PUM

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Abstract

The invention relates to a biphenyl derivative and a preparation method and medical application thereof. Specifically, the invention relates to the biphenyl derivative represented in a general formula(I), the preparation method of the biphenyl derivative, a medicinal composition containing the biphenyl derivative and the application of the biphenyl derivative as a therapeutic agent, especially inpreparing medicine for treating ischemic cerebral stroke, wherein definitions of substituents in the general formula (I) are the same as definitions in claims.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a new medicine application. It specifically relates to the application of a biphenyl derivative to the treatment and prevention of 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 currently 7 million surviving patients, 4.5 million of whom have lost the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/63C07C65/105C07C229/08C07C39/367C07F9/09A61K31/222A61K31/225A61K31/194A61K31/198A61K31/05A61K31/661A61P9/10
Inventor 陆华龙
Owner HC SYNTHETIC PHARMA CO LTD
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