A kind of 3-amino-4-alkylthiomaleimide compound and its preparation and application

Abstract

The invention relates to 3-amino-4-alkylthio maleimide compounds as well as a preparation method and application thereof. The structural formula of the compounds is described in the description, wherein R1 is alkyl or substituted phenyl, NR2R3 is substituted primary amine, secondary amine or cyclic amine, and R4 is H, methyl, benzyl or phenyl. The preparation method comprises the steps of dissolving maleimide, R1SH and amine compounds into an organic solvent, adding a copper salt catalyst, heating up to 80-140 DEG C for carrying out a reaction for 4-8h under the condition of oxygen protection,and purifying to obtain the 3-amino-4-alkylthio maleimide compounds. The 3-amino-4-alkylthio maleimide compounds prepared by the method are a type of novel resistant compounds, and can be used for preventing and treating diseases caused by infection of pathogenic bacteria and the like. The preparation method provided by the invention is high in yield, simple in reaction operation, short in reaction route and less in three wastes and can be used for large-scale production.

Description

technical field [0001] The invention belongs to the field of sulfur amino-substituted maleimide compounds and their preparation and application, in particular to a 3-amino-4-alkylthiomaleimide compound and its preparation and application. Background technique [0002] Since the 21st century, the problem of bacterial resistance to antibiotics has emerged around the world and is becoming increasingly serious. Multidrug-resistant Gram-positive bacteria such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE), vancomycin-resistant enterococci (VRE), and cephalosporin-resistant pneumoniae cocci, etc., caused significantly higher mortality and prolonged hospital stay in infected patients. In 2009, a survey of some hospitals in China found that more than 60% of patients’ Staphylococcus aureus strains were Methicillin-resistant Staphylococcusaureus (MRSA); more than 60% of Pseudomonas aeruginosa strains were multidrug resistant Drugs, includ...

AI Technical Summary

Problems solved by technology

However, it is reported in the literature that the maleimides substituted by thioamino groups are mostly aromatic amines, and the thioaminated products substituted by aliphatic amines have not been reported in the literature, and its synthetic method has many reaction steps, low yield, narrow substrate applicability, serious environmental pollution

Direct realization of maleimide C-H difunctionalization by one-pot method has not been reported in the literature

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