N,O-Spiroaminals have potential biological activities and abilities to modulate the physicochemical and pharmacokinetic properties of drug molecules.However,effective catalytic methods for the efficient construction o...N,O-Spiroaminals have potential biological activities and abilities to modulate the physicochemical and pharmacokinetic properties of drug molecules.However,effective catalytic methods for the efficient construction of N,O-spiroaminals are still limited to date.Herein,we report a novel 1,1,2-trifunctionalization of unactivated alkenes to rapidly and efficiently obtain a diverse array of architecturally intriguing N,O-spiroaminals.This methodology exhibits broad substrate scope,good functional group compatibility,and potential synthetic utility by a scale-up reaction,diverse product derivatizations and late-stage functionalization of complex biorelevant molecule.Notably,this transformation selectively allows for the formation of three new chemical bonds(C–O,C–C,and C–N)and one spiro quaternary carbon center across C-C double bonds.展开更多
基金supported by the National Natural Science Foundation of China(Nos.22101237 and 22171233)Collaborative Fund of Luzhou Government and Southwest Medical University(Nos.2023LZXNYDJ019 and 2024LZXNYDJ050)+1 种基金the Science and Technology Program of Luzhou City(No.2024RCX207)the research fund of Southwest Medical University(Nos.2023QN091 and 2022QN057).
文摘N,O-Spiroaminals have potential biological activities and abilities to modulate the physicochemical and pharmacokinetic properties of drug molecules.However,effective catalytic methods for the efficient construction of N,O-spiroaminals are still limited to date.Herein,we report a novel 1,1,2-trifunctionalization of unactivated alkenes to rapidly and efficiently obtain a diverse array of architecturally intriguing N,O-spiroaminals.This methodology exhibits broad substrate scope,good functional group compatibility,and potential synthetic utility by a scale-up reaction,diverse product derivatizations and late-stage functionalization of complex biorelevant molecule.Notably,this transformation selectively allows for the formation of three new chemical bonds(C–O,C–C,and C–N)and one spiro quaternary carbon center across C-C double bonds.
