摘要
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
the National Natural Science Foundation of China(Nos.21861007,21702034)
Natural Science Foundation of Guangxi Province(No.2021GXNSFAA075024)
“BAGUI Scholar”Program of Guangxi Province of China
High-Level Innovation Team and Distinguished Scholar Program in Guangxi Colleges and Universities
the Jiangxi Province Science and Technology Project(No.20212BAB213024)。