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3-aryl amine quinoxalin-2-formamide derivative as well as preparation method and application thereof

A technology of arylaminoquinoxaline and formamides, which is applied in the field of 3-arylaminoquinoxaline-2-carboxamide derivatives and their preparation, can solve the problem of limited synthesis methods, side reactions, and production It can achieve good anti-cancer effect, broad market prospect and high yield.

Active Publication Date: 2020-01-17
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are many kinds of 3-arylaminoquinoxaline-2-carboxamide derivatives, each of which exhibits different biological activities and has a wide range of uses. The synthesis process easily causes side reactions, and the yield is low. very limited

Method used

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  • 3-aryl amine quinoxalin-2-formamide derivative as well as preparation method and application thereof
  • 3-aryl amine quinoxalin-2-formamide derivative as well as preparation method and application thereof
  • 3-aryl amine quinoxalin-2-formamide derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: preparation compound 4a

[0029] Compound 1 and POCl 3 Reaction obtains compound 2; Under electromagnetic stirring, add compound 3 (1.5g, 6.36mmol), compound 2 (1.56g, 12.7mmol) and ethanol (15mL) to the round bottom flask of 50mL successively, under nitrogen protection, heat to 80°C, stirred and reacted for 22h (TLC monitored the reaction progress, developing solvent: V ethyl acetate: V petroleum ether = 1:4), after the reaction was completed, cooled to room temperature, suction filtered, washed with absolute ethanol (2 × 10mL ), drying, to obtain 1.29g brick red solid of compound 4a, productive rate 63%.

[0030] The structural formula of above-mentioned compound 3 is: The structural formula of compound 2 is: The structural formula of compound 1 is: The structural formula of the prepared compound 4a is:

Embodiment 2

[0031] Embodiment 2: preparation compound 4b

[0032] Compound 3 is replaced by The synthesis method was the same as in Example 1, and the compound 4b was obtained with a yield of 40%.

[0033] The structural formula of the prepared compound 4b is:

Embodiment 3

[0034] Embodiment 3: preparation compound 4c

[0035] Compound 3 is replaced by The synthesis method was the same as in Example 1, and the compound 4c was obtained with a yield of 49%.

[0036] The structural formula of the prepared compound 4c is:

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Abstract

The invention relates to a 3-aryl amine quinoxalin-2-formamide derivative as well as a preparation method and application thereof. The 3-aryl amine quinoxalin-2-formamide derivative is synthesized byusing a simple and convenient method, the yield is high, the production cost is low, the obtained 3-aryl amine quinoxalin-2-formamide derivative has a 3-aryl amine quinoxalin-2-formamide parent-nuclear structure, has good antitumor effects both in vivo and in vitro, can be prepared into antitumor medicines of various dosage forms, and has very high medical values and wide market prospects.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a 3-arylaminoquinoxaline-2-carboxamide derivative and a preparation method and application thereof. Background technique [0002] Tumor is a common and frequently-occurring disease, among which malignant tumor has become a major disease that threatens human health, and its morbidity and mortality rank first among all kinds of diseases. In February 2017, the National Cancer Center released the latest cancer data in China. The data shows that about 10,000 people are diagnosed with cancer every day, that is, about 7 people are diagnosed with cancer every minute. Facing this extremely severe situation, it is urgent to continuously develop more There are many new anti-tumor drugs with high efficiency, low toxicity and low price. Quinoxaline is a very important nitrogen-containing heterocycle and a very important advantageous structural unit in medicinal chemistry. Its derivatives h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/44A61P35/00
CPCC07D241/44A61P35/00
Inventor 苏桂发陈南英陆克潘成学袁静梅
Owner GUANGXI NORMAL UNIV