This report discloses a distinctive palladium-catalyzed sequential tandem cyclization reaction of two molecular haloalkynes and one molecular N-alkylanilines,leading to the efficient assembly of various 3-halo-1,2,5-t...This report discloses a distinctive palladium-catalyzed sequential tandem cyclization reaction of two molecular haloalkynes and one molecular N-alkylanilines,leading to the efficient assembly of various 3-halo-1,2,5-triarylpyrrole derivatives.Two carbon-carbon tri-ple bonds and one carbon-halogen bond in two molecular haloalkynes are transformed conveniently in one single step,which may involve the aminoalkynylation of haloalkyne and cyclization of the newly formed enyne intermediate.The high chemo-and regiose-lectivities,good functional group tolerance and late-stage modification of the halopyrrole products further illustrate the synthetic value of this strategy.展开更多
A general atom-economical approach for the synthesis of a-halomethyl ketones is demonstrated through Ce(SO4)z/acid co-catalyzed hydration of a wide range of haloalkynes. The reactions are conducted under convenient ...A general atom-economical approach for the synthesis of a-halomethyl ketones is demonstrated through Ce(SO4)z/acid co-catalyzed hydration of a wide range of haloalkynes. The reactions are conducted under convenient conditions and provide products with excellent regioselectivity in good to excellent yields, with broad substrate scope. This protocol is an alternative to conventional a-halogenation of ketones.展开更多
基金The authors thank the National Natural Science Foundation of China(22071063 and 21871095)the Guangdong Basic and Applied Basic Research Foundation(2021B1515020058)the Key-Area Research and Development Program of Guangdong Province(2020B010188001)forfinancialsupport.
文摘This report discloses a distinctive palladium-catalyzed sequential tandem cyclization reaction of two molecular haloalkynes and one molecular N-alkylanilines,leading to the efficient assembly of various 3-halo-1,2,5-triarylpyrrole derivatives.Two carbon-carbon tri-ple bonds and one carbon-halogen bond in two molecular haloalkynes are transformed conveniently in one single step,which may involve the aminoalkynylation of haloalkyne and cyclization of the newly formed enyne intermediate.The high chemo-and regiose-lectivities,good functional group tolerance and late-stage modification of the halopyrrole products further illustrate the synthetic value of this strategy.
文摘A general atom-economical approach for the synthesis of a-halomethyl ketones is demonstrated through Ce(SO4)z/acid co-catalyzed hydration of a wide range of haloalkynes. The reactions are conducted under convenient conditions and provide products with excellent regioselectivity in good to excellent yields, with broad substrate scope. This protocol is an alternative to conventional a-halogenation of ketones.