The application discloses a novel and efficient electrochemical catalytic synthesis of
sulfone isoxazole derivatives. The method uses beta, gamma-
unsaturated ketone oxime and p-toluenesulfonyl hydrazine as starting materials, under the condition of C(+) / C(-) as an
electrode, a current of 10 mA, and reaction at
room temperature for 4 h, the oxidation sulfonation reaction of the alkenyl
oxime substrate can be smoothly realized, and
sulfone isoxazole derivatives are obtained. The
sulfone radical is generated by anodic
single electron oxidation of p-toluenesulfonyl hydrazine, then the radical addition is carried out on the alkenyl
oxime, the benzyl radical is generated, then the
radical oxidation reaction of the benzyl position and the intramolecular nucleophilic cyclization reaction are further carried out at the
anode to generate the sulfone
isoxazole product. Compared with the traditional synthesis scheme, the application only needs to add
inorganic electrolyte as a conductive medium under mild conditions, without the addition of
metal and additional oxidants, and the sulfone group can be introduced into the skeleton of the isoxazole ring under the electrochemical condition, and the
aryl alkyl sulfone compound constructed is widely used in medicines, biologically active products and materials, and has important biological and synthetic research value.