Main observation and conclusion A new Rh(Ⅲ)-catalyzed direct C—H alkenylation of 2,3-unsubstitued indoles with alkenyl borates through C—H activation followed by transmetallation was described.This protocol provide...Main observation and conclusion A new Rh(Ⅲ)-catalyzed direct C—H alkenylation of 2,3-unsubstitued indoles with alkenyl borates through C—H activation followed by transmetallation was described.This protocol provides an efficient method for the synthesis of terminal C2-alkenylindoles under mild conditions,and also shows broad substrate scope and high functional group tolerance with respect to both components.Furthermore,the C2-alkenylated indole can be easily transformed into carboline derivative,which is an important polycyclic indole moiety in natural products and drug molecules.展开更多
基金We are grateful to the National Natural Science Foundation of China(No.21302064)the Natural Science Foundation of Hubei Province(No.2017CFB690).
文摘Main observation and conclusion A new Rh(Ⅲ)-catalyzed direct C—H alkenylation of 2,3-unsubstitued indoles with alkenyl borates through C—H activation followed by transmetallation was described.This protocol provides an efficient method for the synthesis of terminal C2-alkenylindoles under mild conditions,and also shows broad substrate scope and high functional group tolerance with respect to both components.Furthermore,the C2-alkenylated indole can be easily transformed into carboline derivative,which is an important polycyclic indole moiety in natural products and drug molecules.