Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive molecules.In the past decades,these key structures prompted the development of cr...Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive molecules.In the past decades,these key structures prompted the development of creative pharmaceuticals owing to their prominent biological properties,including trypanothione reductase(TryR)inhibitor,Hepatitis B virus(HBV)inhibitive activities,anticancer activities,etc.(Scheme 1A).[1]Notably,the chirality of the C4 atom is crucial for drug design.For example,the DPC-083 is a potent reverse transcriptase inhibitor for the treatment of HIV infection but the undesired enantiomers exhibit virtually no activity.[ia]Therefore,developing synthetic methods for innovative chiral 4-substituted 3,4-dihydroquinazolines is significant and essential for drug discovery.展开更多
A privileged strategy has been developed for the precise construction of enantioenriched azaspiro polycyclic scaffolds.Structurally diverse azaspiro polycycles bearing multiple contiguous stereocenters are obtained wi...A privileged strategy has been developed for the precise construction of enantioenriched azaspiro polycyclic scaffolds.Structurally diverse azaspiro polycycles bearing multiple contiguous stereocenters are obtained with excellent results(up to 99:1 e.r.,>95:5 d.r.) via sequential enantioselective four-component Ugi reactions/post-Ugi transformations with substrates containing prerequisite functional groups in the presence of anionic stereogenic-at-cobalt(Ⅲ) complexes.展开更多
A highly efficient kinetic resolution of racemic thioanilide atropisomers via C(sp^(3))-H arylation has been achieved by a hybrid palladium catalyst bearing an anionic chiral Co^(Ⅲ)-complex and a phosphoramidite liga...A highly efficient kinetic resolution of racemic thioanilide atropisomers via C(sp^(3))-H arylation has been achieved by a hybrid palladium catalyst bearing an anionic chiral Co^(Ⅲ)-complex and a phosphoramidite ligand,leading to both enantioenriched atropisomeric arylation thioanilides(up to 99%ee)and N-Me atropisomeric thioanilides(up to 99%ee),simultaneously.The remained enantioenriched substrates can be arylated again by using an achiral anionic ligand to give the enantiomer with the opposite configuration.展开更多
基金financial support from NSFC(Grant No.92156022)Anhui Provincial Natural Science Funds(Grant Nos.2308085MB43,2308085QB44)Shennong Scholar Program of Anhui Agricultural University,and National Undergraduate Training Program for Innovation and Entrepreneurship.
文摘Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive molecules.In the past decades,these key structures prompted the development of creative pharmaceuticals owing to their prominent biological properties,including trypanothione reductase(TryR)inhibitor,Hepatitis B virus(HBV)inhibitive activities,anticancer activities,etc.(Scheme 1A).[1]Notably,the chirality of the C4 atom is crucial for drug design.For example,the DPC-083 is a potent reverse transcriptase inhibitor for the treatment of HIV infection but the undesired enantiomers exhibit virtually no activity.[ia]Therefore,developing synthetic methods for innovative chiral 4-substituted 3,4-dihydroquinazolines is significant and essential for drug discovery.
基金supported by the National Natural Science Foundation of China (92156022)the Anhui Provincial Natural Science Funds (1908085J07,1908085QB79,2308085MB44,2308085QB44)the Shen-Nong Scholar Program of Anhui Agricultural University。
文摘A privileged strategy has been developed for the precise construction of enantioenriched azaspiro polycyclic scaffolds.Structurally diverse azaspiro polycycles bearing multiple contiguous stereocenters are obtained with excellent results(up to 99:1 e.r.,>95:5 d.r.) via sequential enantioselective four-component Ugi reactions/post-Ugi transformations with substrates containing prerequisite functional groups in the presence of anionic stereogenic-at-cobalt(Ⅲ) complexes.
基金We are grateful for the financial support from NSFC(Grant No.21831007).
文摘A highly efficient kinetic resolution of racemic thioanilide atropisomers via C(sp^(3))-H arylation has been achieved by a hybrid palladium catalyst bearing an anionic chiral Co^(Ⅲ)-complex and a phosphoramidite ligand,leading to both enantioenriched atropisomeric arylation thioanilides(up to 99%ee)and N-Me atropisomeric thioanilides(up to 99%ee),simultaneously.The remained enantioenriched substrates can be arylated again by using an achiral anionic ligand to give the enantiomer with the opposite configuration.
