Cyclobutyl-1-enamine compound, preparation method thereof and application of cyclobutyl-1-enamine compound in medicine

A compound and enamine technology, applied in the field of organic chemical synthesis, can solve the problems of blank research status, high price, unfriendly environment, etc., and achieve the effect of simple post-processing, short reaction path, and environmental friendliness
CN114436918AActive Publication Date: 2022-05-06ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2022-05-06

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Abstract

The invention belongs to the field of organic chemical synthesis, and discloses cyclobutyl-1-enamine compounds, a preparation method thereof and application of the cyclobutyl-1-enamine compounds in antiviral and antitumor drugs. The compound has a structure of a general formula (I), and EWG is selected from alkyl or aryl substituted sulfonyl; r is selected from alkyl, alkoxy, halogen and nitryl. The preparation method comprises the following steps: heating an alkyne amide raw material to a molten state under thermal driving, and carrying out [2 + 2] cycloaddition reaction among molecules to obtain the polysubstituted cyclobutyl-1-enamine compound. The method has the advantages of easily available raw materials, simple steps, no catalyst, no solvent, high yield and the like. The compound has anti-SARS-CoV-2, 5637, Hela, SW480, Hep G2, A549 and MCF-7 activity, and has a good application prospect in the aspect of treating novel coronavirus, bladder cancer, cervical cancer, colon cancer, liver cancer, lung cancer and breast cancer. (I).
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Description

technical field

[0001] The invention relates to the field of organic chemical synthesis, in particular to cyclobut-1-enamine compounds, their preparation methods and their application in antiviral and antitumor drugs. Background technique

[0002] Functionalized cyclobut-1-enamine is an important structural unit present in many pharmaceutically active compounds and natural products. In addition, cyclobut-1-enamine is often used as a reaction substrate to construct other important organic functional group molecules due to the good reactivity endowed by the strain of the four-membered ring. Therefore, the research on the synthesis method of cyclobut-1-enamine compounds has always been a hot spot that chemists pay attention to.

[0003] The traditional construction of cyclobut-1-enamine compounds is realized through the Ficini [2+2] cycloaddition reaction, that is, the [2+2] cycloaddition reaction of alkyne amide and cyclic enone to generate cyclobutan-1 - Enamine. In 2010, ...

Claims

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