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Novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of novel derivative

A kind of technology of octyl phenyl, propylene glycol

Inactive Publication Date: 2014-04-16
ZHENJIANG SAN AN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to overcome the defect in the prior art, provide the novel derivative of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol and application thereof, described The drug activity of derivatives is good, and at the same time, it can solve the problem of bad metabolism of drugs, and the toxic and side effects in the process of medication are small

Method used

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  • Novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of novel derivative
  • Novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of novel derivative
  • Novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of novel derivative

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Preparation of 2-amino-2-[2-(4-octylphenyl)-1,1-difluoroethyl]-1,3-propanediol.

[0020] The preparation of derivatives described in the present invention comprises 3 steps, and synthetic route is as follows:

[0021]

[0022] 1. Preparation of 2-bromo-2,2-difluoro-1-(4-octylphenyl)-ethanone 1-1 by acetylation.

[0023] Under anhydrous, oxygen-free and argon protection, aluminum trichloride, octylbenzene and anhydrous dichloromethane solvent were successively added to a dry flask at room temperature, and cooled to -10°C while stirring. A solution of 2-bromo-2,2-difluoro-acetyl bromide in dichloromethane was added and the mixture was allowed to come to room temperature and stirred overnight. The mixture was slowly poured into ice water, and the aqueous phase was extracted with dichloromethane, the combined organic layers were dried over anhydrous sodium sulfate, and concentrated under reduced pressure to give 2-bromo-2,2-difluoro-1-(4 -octylphenyl)-ethanone 1-1 was ...

Embodiment 2

[0029] Preparation of 2-amino-2-[2-(4-octylphenyl)-1-fluoroethyl]-1,3-propanediol.

[0030]

[0031]The preparation method is the same as in Example 1, except that 2-bromo-2,2-difluoro-acetyl bromide in Example 1 is replaced by 2-bromo-2-fluoro-acetyl bromide.

Embodiment 3

[0033] Preparation of 2-amino-2-[2-(4-octylphenyl)-1,1-difluoro-2,2-dideuterium-ethyl]-1,1,3,3-tetradeuterium-1, 3-Propanediol.

[0034]

[0035] The preparation method is the same as in Example 1, and the sodium borohydride in Example 1 is replaced with sodium borodeuteride.

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Abstract

The invention discloses a novel derivative of 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol and application of the novel derivative. The novel derivative has good medicine activity, can greatly prolong the half-life period of a medicine, prolongs the retention time of the medicine in a human body, and meanwhile, improves the concentration of the medicine in blood; therefore, a better curative effect is achieved. As the half-life period of the medicine is greatly prolonged, the activity concentration of the medicine in the blood can be maintained for a longer period of time; under the cure condition of dose constrain, the curative effect is maintained and the dosage of the medicine is reduced, so that the problem of bad metabolism of the medicine is eliminated, the medicine toxicity is reduced, and the toxic and side effects in the medicine use process are reduced.

Description

technical field [0001] The invention relates to a compound derivative and its application, belonging to the technical field of medicine. Background technique [0002] Multiple sclerosis (MS) is an effect Central Nervous System -brain, spinal cord and optic nerve of chronic self-immune disease. It can impair a person's ability to move, feel, and think, and seriously affect a patient's quality of life. Multiple sclerosis is one of the most common causes of neurological disability in young adults and is more common in women than in men. Multiple sclerosis is often characterized by easy relapses after complete or incomplete recovery. Affects approximately 400,000 Americans, with the relapsing-remitting form being the most common and characterized by progressive deterioration in function followed by a recovery period that is less and less complete over time, leading to progressive decline in function and disability Increase. In October 2010, the US Food and Drug Admini...

Claims

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Application Information

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IPC IPC(8): C07C215/28A61K31/137A61P25/28A61P37/00
Inventor 陈兴海
Owner ZHENJIANG SAN AN PHARMA