A novel and viable palladium-catalyzed sequential cyclization/functionalization of alkynone O-methyloximes with unactivated vinyl ethers under aerobic conditions was described.The structure of the products could be su...A novel and viable palladium-catalyzed sequential cyclization/functionalization of alkynone O-methyloximes with unactivated vinyl ethers under aerobic conditions was described.The structure of the products could be successfully controlled by varying the nature of the substituents of the vinyl ethers.This new approach provides a convenient and straightforward synthetic protocol for the preparation of structurally diverse 4-(1-alkoxyvinyl)-isoxazoles and 4-vinylisoxazoles in moderate to good yields with highly regioselectivity.Remarkably,this protocol can be performed on a gram scale,showing the promising application in synthetic and pharmaceutical chemistry.展开更多
基金We thank the National Natural Science Foundation of China(No.21971072)the Ministry of Science and Technology of the People's Republic of China(No.2016YFA0602900)+1 种基金the Guang Guang dong Natural Science Foundation(No.2018B030308007)the Open Fund of Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates(No.2019B030301003)for financial support.
文摘A novel and viable palladium-catalyzed sequential cyclization/functionalization of alkynone O-methyloximes with unactivated vinyl ethers under aerobic conditions was described.The structure of the products could be successfully controlled by varying the nature of the substituents of the vinyl ethers.This new approach provides a convenient and straightforward synthetic protocol for the preparation of structurally diverse 4-(1-alkoxyvinyl)-isoxazoles and 4-vinylisoxazoles in moderate to good yields with highly regioselectivity.Remarkably,this protocol can be performed on a gram scale,showing the promising application in synthetic and pharmaceutical chemistry.