Unlock instant, AI-driven research and patent intelligence for your innovation.

Chemical synthetic method of potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating Alzheimer disease

A technology for Alzheimer's disease and chemical synthesis, which can be used in chemical instruments and methods, organic chemistry, preparation of organic compounds, etc., and can solve problems such as low yields

Active Publication Date: 2013-06-05
上海花之素生命科技有限公司
View PDF2 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

low yield

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Chemical synthetic method of potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating Alzheimer disease
  • Chemical synthetic method of potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating Alzheimer disease
  • Chemical synthetic method of potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating Alzheimer disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0013] Scheme 1, by aryl acrylic acid I a Synthesis of aryl acryloyl activated intermediate I a’ , and then with arylethylamine I b Reaction synthesis target compound II:

[0014] 1.1.1 Weigh 5.00g (33.7mmol) of aryl acrylic acid Ia into a 100ml three-necked flask and measure 30.0ml of DCM, SOCl 2 1 Add 2.20ml (168.1mmol) to the constant pressure dropping funnel, install a condenser tube, dry the tube, and saturate with K 2 CO 3 The solution absorbs the exhaust gas. Add SOCl dropwise at room temperature 2 Heating to reflux for 2.0h reaction after completion, removing the solvent under reduced pressure, measuring 5.0ml DCM and adding it to the concentrated solution to depressurize again to take out the low boiling point fraction. Activated intermediate Ia' 5.58g.

[0015] 1.1.2 Weigh 5.00g (33.7mmol) of aryl acrylic acid Ia into a 100ml three-necked flask, measure 30.0ml of toluene, SOCl 2 Add 2.94ml (40.5mmol) into the constant pressure dropping funnel, install a conde...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention relates to a chemical synthetic method of potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating Alzheimer disease. Aryl acrylic acid and aryl ethylamine serve as origination raw materials. The chemical synthetic method of the potential medicines g x50, g x52, g x 52, g x 180 for preventing and treating the Alzheimer disease is achieved through two reaction paths, wherein one reaction path is that radio-activation intermediate of aryl acryloyl group is combined by the aryl acrylic acid and then reacted with the aryl acrylamide, finally a goal molecule with high yield is obtained, the other path is that the aryl acrylic acid and the aryl ethylamine are reacted directly under the existing conditions of water removing aqua P205 or a molecular sieve and the like, and then a goal composition can be obtained. Pollution can not be caused to environment by the reaction paths.

Description

technical field [0001] The present invention relates to a chemical synthesis method of gx50, gx51, gx52 and gx180, which are potential drugs for preventing and treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a progressive and fatal neurodegenerative disease characterized by progressive deterioration of cognitive and memory functions. At present, it is believed that the accumulation and aggregation of β-amyloid (Aβ) peptide in nerve cells is the central link in the pathogenesis of AD. The α7 nicotinic acetylcholine receptor (α7nAChR) plays a very important role in mediating the apoptosis of nerve cells caused by Aβ, because the specific agonist against α7nAChR can effectively slow down the pathogenesis of Alzheimer's disease and alleviate the disease of patients. Symptoms have become a hot spot for researchers to pursue. We reported in Medicinal Chemistry, 2009, 5, 250-262, using bioinformatics means to...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/22C07C231/02C07D317/60C07C235/34
Inventor 魏冬青马玉坤
Owner 上海花之素生命科技有限公司