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

Synthesis and application of benzotriazole derivatives as rsk2 inhibitors

A kind of technology of use and compound, applied in the field of synthesis of benzotriazole derivatives

Active Publication Date: 2016-02-17
GUANGDONG XTEM BIOTECH CO LTD
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the screening and synthetic development of systematic RSK2 inhibitors have not been reported yet.

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
  • Synthesis and application of benzotriazole derivatives as rsk2 inhibitors
  • Synthesis and application of benzotriazole derivatives as rsk2 inhibitors
  • Synthesis and application of benzotriazole derivatives as rsk2 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0074] synthetic part

[0075] Synthesis of N-((1H-benzo[d][1,2,3]triazole)-1-methyl)aniline (I-1)

[0076]

[0077] Weigh benzotriazole (5mmol, 596mg), aniline (5mmol, 466mg), 40% formaldehyde (5mmol, 375mg) into a 100mL round bottom bottle, add 60mL methanol, stir at room temperature for 2 hours, there are a lot of white solids Precipitate, filter with suction, wash the filter cake with cold methanol, and dry to obtain the target compound. White solid, mass: 1.009 g (yield: 90%). 1 HNMR (400MHz, DMSO-d 6 ): δ8.06(d, J=8.4Hz1H), δ8.01(d, J=8.4Hz1H), δ7.54(t, J=7.6Hz1H), δ7.38(t, J=7.6Hz1H), δ7.27(t, J=7.2Hz1H), δ7.07(t, J=7.6Hz2H), δ6.82(d, J=8Hz2H), δ6.595(t, J=7.2Hz1H), δ6.12 (d, J=7.2Hz2H).

[0078] Synthesis of N-((1H-benzo[d][1,2,3]triazole)-1-methyl)-4-nitroaniline (I-2)

[0079]

[0080] Weigh benzotriazole (5mmol, 596mg), p-nitroaniline (5mmol, 691mg), and 40% formaldehyde (5mmol, 375mg) into a 100mL round bottom bottle, add 60mL of methanol, stir at room ...

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

No PUM Login to View More

Abstract

The invention relates to synthesis of a benzotriazol derivative and its application, specifically to a compound as shown in the following formula II, a pharmaceutical composition containing the compound as shown in the formula II and an application of the compound in preparation of drugs for treating or preventing RSK2-mediated diseases.

Description

technical field [0001] The present invention relates to the synthesis and application of benzotriazole derivatives, in particular to the synthesis of benzotriazole compounds with different substituents and their application as antitumor drugs targeting RSK-2. Background technique [0002] Cancer, namely malignant tumor, is one of the most serious diseases that threaten human life and health. According to statistics, in 2008, 12 million people worldwide were diagnosed with cancer, and 7.6 million people died of cancer. Therefore, the research and development of anticancer drugs is a very challenging and significant field in today's life sciences. [0003] Traditional cytotoxic drugs mainly act on common parts of cells such as DNA, RNA and tubulin, resulting in low selectivity and high toxicity, and their side effects often make patients unable to continue treatment or prevention. On the contrary, new anti-tumor drugs are developed based on the great differences between norm...

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 Patents(China)
IPC IPC(8): A61K31/4192A61P35/00A61P25/00C07D249/18
Inventor 徐玉芳赵振江刘晓峰黄瑾李洪林钟烨卢伟强曹贤文刘康栋
Owner GUANGDONG XTEM BIOTECH CO LTD