An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothi...An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothiocyanates,amines and cyclic ethers.This methodology features simple operation,mild reaction conditions,favorable functional group tolerance,easily available starting materials and high efficiency.展开更多
The simultaneous binding/dissociation of multiple bonds in a one-pot manner by multicomponent reactions provide an important approach for developing novel and sustainable pathway in the drug discovery process.Herein w...The simultaneous binding/dissociation of multiple bonds in a one-pot manner by multicomponent reactions provide an important approach for developing novel and sustainable pathway in the drug discovery process.Herein we develop an electrocatalytic three-component reaction to construct multifunctional and valuable isothiourea compounds,which uses thiols,isocyanides and amines as substrates.Compared with the previous work,the organic electrosynthesis technique can avoid the requirement of heavy metal catalysts and stoichiometric oxidants.In addition,using thiol as a substrate to participate in the three-component reaction broadens the source of sulfur,which can also construct more abundant isothiourea derivatives.展开更多
Comprehensive Summary Phthalides serve as core structures pervasive in a wide array of natural products and drug molecules,which display a diverse array of biological activities.We report herein a highly efficient dyn...Comprehensive Summary Phthalides serve as core structures pervasive in a wide array of natural products and drug molecules,which display a diverse array of biological activities.We report herein a highly efficient dynamic kinetic resolution of 3-hydroxyphthalides by chiral isothioureas(ITUs)catalyzed asymmetric acylation,facilitating the effective synthesis of a variety of chiral phthalidyl esters with good yields and enantioselectivities.Notably,this reaction features mild reaction conditions,expansive substrate scope as well as good functional group compatibility.In addition,the practicality of this method is underscored by the large-scale synthesis,reduced catalyst loading experiment and the synthesis of the chiral phthalidyl ester prodrug.展开更多
基金financially supported by Natural Science Foundation of Shandong Province(No.ZR2021MB065)the major innovation fund of Shandong Province(No.2021ZDSYS_(2)3)the National Natural Science Foundation of China(Nos.21976105,22101237).
文摘An additive-free and environmentally friendly strategy has been realized for the construction of S-substituted isothioureas through visible-light-induced multicomponent reaction starting fromα-diazoesters,aryl isothiocyanates,amines and cyclic ethers.This methodology features simple operation,mild reaction conditions,favorable functional group tolerance,easily available starting materials and high efficiency.
基金We thank the financial support from the National Natural Science Foundation of China(Nos.22061003 and 22161008)the Natural Science Foundation of Guangxi Province(Nos.2021GXNSFFA220005 and 2021GXNSFBA196041).
文摘The simultaneous binding/dissociation of multiple bonds in a one-pot manner by multicomponent reactions provide an important approach for developing novel and sustainable pathway in the drug discovery process.Herein we develop an electrocatalytic three-component reaction to construct multifunctional and valuable isothiourea compounds,which uses thiols,isocyanides and amines as substrates.Compared with the previous work,the organic electrosynthesis technique can avoid the requirement of heavy metal catalysts and stoichiometric oxidants.In addition,using thiol as a substrate to participate in the three-component reaction broadens the source of sulfur,which can also construct more abundant isothiourea derivatives.
基金support from the National Natural Science Foundation of China(Grant Nos.22371219,22193011,21971120,21933008 and 22101191)National Science&Technology Fundamental Resource Investigation Program of China(No.2018FY201200)the Fundamental Research Funds for the Central Universities.W.Z.is grateful for the financial support from the program of China Scholarship Council(No.202206240054).
文摘Comprehensive Summary Phthalides serve as core structures pervasive in a wide array of natural products and drug molecules,which display a diverse array of biological activities.We report herein a highly efficient dynamic kinetic resolution of 3-hydroxyphthalides by chiral isothioureas(ITUs)catalyzed asymmetric acylation,facilitating the effective synthesis of a variety of chiral phthalidyl esters with good yields and enantioselectivities.Notably,this reaction features mild reaction conditions,expansive substrate scope as well as good functional group compatibility.In addition,the practicality of this method is underscored by the large-scale synthesis,reduced catalyst loading experiment and the synthesis of the chiral phthalidyl ester prodrug.
