β-Boryl amide is a class of high value intermediates in organic chemistry.In this work,a copper-catalyzed carbonylative boroamidation of olefins toward the synthesize ofβ-boryl amides has been developed.Several new ...β-Boryl amide is a class of high value intermediates in organic chemistry.In this work,a copper-catalyzed carbonylative boroamidation of olefins toward the synthesize ofβ-boryl amides has been developed.Several new chemical bonds were constructed in this transformation.A wide range ofβ-boryl amides were produced in excellent regioselectivity and good to excellent yields.Ethylene gas can be successfully transformed under the same standard conditions as well.Notably,with the use of a chiral ligand,the first example of enantioselective carbonylative boroamidation of alkenes was realized.In addition,Piposulfan and Pipobroman,antineoplastic medicines,were prepared by this methodology in a straightforward manner.展开更多
文摘β-Boryl amide is a class of high value intermediates in organic chemistry.In this work,a copper-catalyzed carbonylative boroamidation of olefins toward the synthesize ofβ-boryl amides has been developed.Several new chemical bonds were constructed in this transformation.A wide range ofβ-boryl amides were produced in excellent regioselectivity and good to excellent yields.Ethylene gas can be successfully transformed under the same standard conditions as well.Notably,with the use of a chiral ligand,the first example of enantioselective carbonylative boroamidation of alkenes was realized.In addition,Piposulfan and Pipobroman,antineoplastic medicines,were prepared by this methodology in a straightforward manner.