Method for generating beta-amino ketone compounds through iodine catalysis

Abstract

The invention discloses a method for generating beta-amino ketone compounds by catalyzing 4-hydroxy-2-butanone to react with aromatic amine through iodine. The method comprises the following steps: taking 4-hydroxy-2-butanone and different aromatic amines as reaction substrates, taking iodine as a catalyst, and dimethyl sulfoxide or N,N-dimethyl formamide as a solvent, and reacting at room temperature in a nitrogen atmosphere to obtain the beta-amino ketone compounds, wherein other byproducts are undetected. By adopting the preparation method disclosed by the invention, the beta-amino ketone compounds can be generated by catalyzing 4-hydroxy-2-butanoe to react with aromatic amine through the iodine at room temperature for the first time.

Description

technical field [0001] The invention relates to a synthesis method of β-aminoketone compounds, in particular to a method for generating β-aminoketone compounds by iodine catalysis. Background technique [0002] As an important structural fragment, β-aminoketone exists in many biologically active molecules and drug molecules, and is widely used in the fields of fine chemicals and medicine, such as the synthesis of β-amino acids, β-amino alcohols, 1,3-diamino Alkanes, lactams, nikkomycin, etc. The Mannich reaction is a classic method for the synthesis of β-aminoketones (Formula 2a), but the reaction has disadvantages such as long reaction time, low yield, and harsh conditions. The Aza-Michael addition reaction (conjugate addition of amines to β-unsaturated ketones) is another important method for the synthesis of β-aminoketones (Equation 2b), which has the advantages of simplicity and good atom economy. In recent years, a variety of catalytic systems (Lewis acids, transition...

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In recent years, a variety of catalytic systems (Lewis acids, transition metal catalysts, and organic catalysts) have been report

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