C7-Indole Amidations and Alkenylations by Ruthenium(II) Catalysis.

ABSTRACT: C7-H-functionalized indoles are ubiquitous structural units of biological and pharmaceutical compounds for numerous antiviral agents against SARS-CoV or HIV-1. Thus, achieving site-selective functionalizations of the C7-H position of indoles, while discriminating among other bonds, is in high demand. Herein, we disclose site-selective C7-H activations of indoles by ruthenium(II) biscarboxylate catalysis under mild conditions. Base-assisted internal electrophilic-type substitution C-H ruthenation by weak O-coordination enabled the C7-H functionalization of indoles and offered a broad scope, including C-N and C-C bond formation. The versatile ruthenium-catalyzed C7-H activations were characterized by gram-scale syntheses and the traceless removal of the directing group, thus providing easy a

SUBMITTER: Choi I 

PROVIDER: S-EPMC7383588 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature