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作 者:Yuanyuan Ma Qianwen Gao Lan Zhou Shanshan Liu Hong-Gang Cheng Qianghui Zhou
机构地区:[1]Institute for Advanced Studies,Wuhan University,Wuhan,Hubei 430072,ChinaSauvage Center for Molecular Sciences,College of Chemistry and Molecular Sciences at Wuhan University,Wuhan,Hubei 430072,China [2]Institute for Advanced Studies,Wuhan University,Wuhan,Hubei 430072,China
出 处:《Chinese Journal of Chemistry》2022年第6期675-680,共6页中国化学(英文版)
基 金:Weare grateful to the National Natural Science Foundation of China(Grants 21871213,21801193 and 22071189);the start-up funding from Wuhan University for financial support。
摘 要:Flavones and isoflavones are recognized as privileged heterocyclic scaffolds for the preparation of bioactive compounds.Efficient methods to access these heterocycles are in urgent need.Herein,we report diversity-oriented synthesis of flavones and isoflavones from 3-iodochromones via palladium/norbornene cooperative catalysis.The success of this research relies on the use of a unique bridge-head ester modified norbornene derivative as the mediator.Salient features of this include readily available starting materi-als regarding 3-iodochromones,ortho-C-H arylating and alkylating reagents and ipso-terminating reagents,broad substrate scope,good chemoselectivity,good step-economy and scalability.A large number of structurally diversified flavones,isoflavones and 2,3-diarylated chromones can be quickly prepared in a predictable manner.As showcased by the efficient formal synthesis of um-bralisib,this chemistry can be treated as another valuable addition to the toolbox of medicinal chemists.
关 键 词:Diversity-oriented synthesis Oxygen heterocycle PALLADIUM NORBORNENE C-H activation
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