Synthesize Of α-Ketoamides And β-Hydroxysulfone Under Mild Conditions

α-Ketoamides are widely distributed in natural products,drugs and drug precursors.Their biological activities include anti-HIV,antitumor and anti-inflammatory.Because of its special structure,it can also be used in the field of functional group transformations and total synthesis.Traditionally,the methods of synthesizing α-ketoamides include oxidative coupling,metal catalyzed double carbonylation and coupling of acyl precursors.These methods usually require high temperature,the stoichiometric of peroxides,transition metal catalysts and pre-prepared precursors,which often bring problems in safety and cost,or cumbersome process and difficult storage of raw materials.Therefore,developing a green,convenient and fast method for synthesizing α-ketoamide is of great significance.β-Hydroxysulfone is a kind of important molecular skeleton,and these structure frequently appears in drug molecules and natural products.These structures have great synthetic potential and a wide range of biological characteristics.Traditional methods for synthesizing β-hydroxysulfone usually need to use a large amount of reductant or metal catalysts,which is not conduct the organic synthesis to convenient and efficient.Therefore,the development of synthesizing β-hydroxysulfone via green and efficient method is of great significance.Reviewing the previous works,this paper mainly discusses the following two parts:(1)Electrochemical synthesis of α-ketoamides via radical decarboxylation of α-ketoacids and radical addition with isocyanide.The reaction condition are mild and transformation is efficient,and transition metal catalyst and peroxide are not request in this reaction.The products are easily separated and purified.It is a new method in line with the development of energysaving and environmentally-friendly society for synthesizing α-ketoamides,which have high value in the field of organic synthesis.(2)The method of difunctionalization of olefins for β-hydroxysulfone skeleton without transition metal catalyst and peroxide was studied.The sodium sulfite is used as sulfonyl source,which generates sulfonyl radical under the effect of oxygen and addition to olefins,and then hydrolyzes to obtain β-hydroxysulfone.The method has the advantages of convenience and rapidity,less by-products,and the products are easy to purify.Which has wide scope of substrates,and supports the expansion reaction.This method has a good application prospect in the fields of biomedicine,materials and organic synthesis.