Rh(III)-Catalyzed Direct Access to 2,3-Substituted β-N-Glycosyl Indoles Through C-H Activation/annulation Coupling of β-N-Aryl Glycosides with Substituted Internal Alkynes

29 October 2019, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


An efficient and selective C-H activation/annulation of readily available β-N-aryl glycosides with various alkynes has been established. Using [Cp*RhCl2]2 as a catalyst and AgSbF6 in DCE, this protocol proved to be general to prepare a variety of 2,3-substituted N-glycosyl indoles in good yields with exclusive β-selectivity.


Rh Catalysis
C-H activation/annulation
β-N-aryl glycosides

Supplementary materials

supporting information


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