4-pyrroline-2-ketone derivative and preparation method thereof

Abstract

The invention belongs to the technical field of medicine and particularly relates to a 4-pyrroline-2-ketone derivative and a preparation method thereof. The method comprises the following reaction step that a pyrrole compound as shown in the formula (1) reacts in the presence of a solvent, alkali and oxygen, and thus the 4-pyrroline-2-ketone derivative as shown in the formula (2) is obtained. Theraw materials used in the preparation method are easy to obtain, the reaction conditions are mild, the product yield is high, the substrate application range is wide, the reaction specificity is high,post-treatment is easy and environmentally friendly, and thus the synthesis method of the 4-pyrroline-2-one derivative is novel and efficient. The formula (1) and the formula (2) are shown in the description.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a 4-pyrroline-2-one derivative and a preparation method thereof. Background technique [0002] Synthesis of nitrogen-containing heterocycles with diverse structures using simple and readily available raw materials has always been the focus of attention in the field of organic chemistry. Among them, compounds with pyrroline as the core structure are widely used in medicine, and because there are C=C unsaturated bonds in the molecule, they can be used as medicine or organic synthesis intermediates for further functional group reactions, which have anti-inflammatory properties. The modification of pyrrolidone with pharmacological activities such as anti-senile dementia, anti-tumor and anti-HIV plays an important role. 4-Pyrroline-2-one derivatives are an important class of nitrogen-containing heterocyclic compounds with a wide range of biological activities. T...

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Problems solved by technology

[0003] The traditional synthesis of 4-pyrrolin-2-one compounds is mainly to obtain pre-functionalized acyclic substrates through intramolecular or intermolecular cyclization reactions. This synthesis method has the disadvantages of lengthy reaction steps and low reaction efficiency, such as A kind of 1,3-dihydro-2H-pyrrolone compound and its synthesis method of Chinese patent application CN106008304

Even the synthetic strategies based on pyrrole oxidative dearomatization that have been developed in recent years mostly use unfriendly oxidizing reagents such as ozone, hypervalent iodine compounds, singlet oxygen, and electrocatalytic oxidation, and the reaction process is often accompanied by decomposition, polymerization, etc. generation of side reactions

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