The palladium-catalyzed borylative cyclization via C—H activation has been developed.By this chemistry,the indole-fused dihydro-pyrrole motif,which is a kind of important unit in natural products and bio-active molec...The palladium-catalyzed borylative cyclization via C—H activation has been developed.By this chemistry,the indole-fused dihydro-pyrrole motif,which is a kind of important unit in natural products and bio-active molecules,could be constructed and installed with a boric ester group.Furthermore,the utilities of products have been illustrated by the study of further transformations.Importantly,by using chiral ligand,the enantioselectivity of this borylative cyclization reaction could be controlled.Moreover,the borylative mechanism,which should proceed through a Pd(II)/Pd(IV)catalytic cycle,has been proposed based on the DFT calculations.展开更多
基金support is from Tianjin University,State Key Laboratory of Elemento-Organic Chemistry,and the National Natural Science Foundation of China(Nos.21801181,22073066,21503143 and 21975179).
文摘The palladium-catalyzed borylative cyclization via C—H activation has been developed.By this chemistry,the indole-fused dihydro-pyrrole motif,which is a kind of important unit in natural products and bio-active molecules,could be constructed and installed with a boric ester group.Furthermore,the utilities of products have been illustrated by the study of further transformations.Importantly,by using chiral ligand,the enantioselectivity of this borylative cyclization reaction could be controlled.Moreover,the borylative mechanism,which should proceed through a Pd(II)/Pd(IV)catalytic cycle,has been proposed based on the DFT calculations.