A[3+2]/[2+1]cycloaddition reaction of gem–difluorocyclopropenes is presented,offering a mild and efficient approach to accessing tri-and tetra-substituted 4-fluoropyridines in moderate to good yields with excellent r...A[3+2]/[2+1]cycloaddition reaction of gem–difluorocyclopropenes is presented,offering a mild and efficient approach to accessing tri-and tetra-substituted 4-fluoropyridines in moderate to good yields with excellent regioselectivity.Multiple synthetic applications,including process-scale reactions,modification of bioactive molecules,derivatization reactions and synthesis of the analogue of the PKM2 modulator,are subsequently described.展开更多
A rhodium-catalyzed[4+3]cycloaddition reaction between N-methoxybenzamides and gem–difluorocyclopropenes is described.The reaction offers a mild and efficient approach towards the synthesis of fluorinated 2 H-azepin-...A rhodium-catalyzed[4+3]cycloaddition reaction between N-methoxybenzamides and gem–difluorocyclopropenes is described.The reaction offers a mild and efficient approach towards the synthesis of fluorinated 2 H-azepin-2-ones with broad substrate scope.A consecutive HOAc-assisted C–N bond formation and fluorine elimination are involved as key steps for success as illustrated by detailed DFT studies.展开更多
基金the National Natural Science Foundation of China(Nos.21861007,21702034)Natural Science Foundation of Guangxi Province(No.2021GXNSFAA075024)+2 种基金“BAGUI Scholar”Program of Guangxi Province of ChinaHigh-Level Innovation Team and Distinguished Scholar Program in Guangxi Colleges and Universitiesthe Jiangxi Province Science and Technology Project(No.20212BAB213024)。
文摘A[3+2]/[2+1]cycloaddition reaction of gem–difluorocyclopropenes is presented,offering a mild and efficient approach to accessing tri-and tetra-substituted 4-fluoropyridines in moderate to good yields with excellent regioselectivity.Multiple synthetic applications,including process-scale reactions,modification of bioactive molecules,derivatization reactions and synthesis of the analogue of the PKM2 modulator,are subsequently described.
基金National Natural Science Foundation of China(Nos.21861007,21702034)Natural Science Foundation of Guangxi Province(No.2021GXNSFAA075024)+1 种基金“BAGUI Scholar”Program of Guangxi Province of ChinaHigh-Level Innovation Team and Distinguished Scholar Program in Guangxi Colleges and Universities。
文摘A rhodium-catalyzed[4+3]cycloaddition reaction between N-methoxybenzamides and gem–difluorocyclopropenes is described.The reaction offers a mild and efficient approach towards the synthesis of fluorinated 2 H-azepin-2-ones with broad substrate scope.A consecutive HOAc-assisted C–N bond formation and fluorine elimination are involved as key steps for success as illustrated by detailed DFT studies.
