A highly efficient kinetic resolution of racemic 2-substituted 1,2-dihydroquinolines via Rh-catalyzed asymmetric hydroarylation has been described for the first time.A variety of arylboronic acids coupled with 2-subst...A highly efficient kinetic resolution of racemic 2-substituted 1,2-dihydroquinolines via Rh-catalyzed asymmetric hydroarylation has been described for the first time.A variety of arylboronic acids coupled with 2-substituted 1,2-dihydroquinolines under mild reaction condition.The transformations into the enantio-enriched 2,3-diaryl-tetrahydroquinolines as well as the recovered chiral 2-aryl-dihydroquinolines were obtained with high yields and excellent enantioselectivities(86%-99% ee,s factor up to 1057).展开更多
An efficient and practical synthesis of heterocyclic nucleosides is developed by a catalyst-free highly regioselective and diastereose-lective[3+2]annulation of a-purine-substituted acrylates with nitrones.The reactio...An efficient and practical synthesis of heterocyclic nucleosides is developed by a catalyst-free highly regioselective and diastereose-lective[3+2]annulation of a-purine-substituted acrylates with nitrones.The reaction operates with excellent functional group toler-ance,very mild reaction conditions,and with the green,sustainable,and eco-friendly 2-methyltetrahydrofuran(2-MeTHF)as sol-vent.Compared with other reactions of electron-deficient olefin dipolarophiles with nitrones,different regioselective cycloaddition products were observed in this work.This 1,3-dipolar cycloaddition reaction gives a series of isoxazolidinyl nucleosides in good to excellent yields with promising applications in biochemistry and medicinal chemistry.展开更多
We designed thenickel-catalyzed enantioselective C(sp^(3))–H arylation of ketones with phenol-derived aryl pyrimidyl ethers via selective cleavage of the C(aryl)–O bond to construct all-carbon quaternary stereocente...We designed thenickel-catalyzed enantioselective C(sp^(3))–H arylation of ketones with phenol-derived aryl pyrimidyl ethers via selective cleavage of the C(aryl)–O bond to construct all-carbon quaternary stereocenters.This method exhibits good functional group compatibility and broad substrate scope.Drug molecule donepezil can directly transform into corresponding highly optically pure derivatives with this developedmethodology.Mechanistic studies reveal that C(aryl)–O cleavage of aryl pyrimidyl ether probably proceeded by means of an anionic organo-Ni(0)intermediate.展开更多
基金the Shenzhen Overseas High-level Talents Innovation Plan of Technical Innovation Project(No.KQJSCX20180319114439973)for financial support.
文摘A highly efficient kinetic resolution of racemic 2-substituted 1,2-dihydroquinolines via Rh-catalyzed asymmetric hydroarylation has been described for the first time.A variety of arylboronic acids coupled with 2-substituted 1,2-dihydroquinolines under mild reaction condition.The transformations into the enantio-enriched 2,3-diaryl-tetrahydroquinolines as well as the recovered chiral 2-aryl-dihydroquinolines were obtained with high yields and excellent enantioselectivities(86%-99% ee,s factor up to 1057).
基金We gratefully acknowledge HKBU RC-Tier 2 Start-up Grant for financial support.
文摘An efficient and practical synthesis of heterocyclic nucleosides is developed by a catalyst-free highly regioselective and diastereose-lective[3+2]annulation of a-purine-substituted acrylates with nitrones.The reaction operates with excellent functional group toler-ance,very mild reaction conditions,and with the green,sustainable,and eco-friendly 2-methyltetrahydrofuran(2-MeTHF)as sol-vent.Compared with other reactions of electron-deficient olefin dipolarophiles with nitrones,different regioselective cycloaddition products were observed in this work.This 1,3-dipolar cycloaddition reaction gives a series of isoxazolidinyl nucleosides in good to excellent yields with promising applications in biochemistry and medicinal chemistry.
基金the National Natural Science Foundation of China(no.NSFC 21902072)and the Guangdong Innovative Program(no.2019BT02Y335)for their financial support.
文摘We designed thenickel-catalyzed enantioselective C(sp^(3))–H arylation of ketones with phenol-derived aryl pyrimidyl ethers via selective cleavage of the C(aryl)–O bond to construct all-carbon quaternary stereocenters.This method exhibits good functional group compatibility and broad substrate scope.Drug molecule donepezil can directly transform into corresponding highly optically pure derivatives with this developedmethodology.Mechanistic studies reveal that C(aryl)–O cleavage of aryl pyrimidyl ether probably proceeded by means of an anionic organo-Ni(0)intermediate.
