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Rhodium‐Catalyzed Selective C−H Alkenylation of Indole at C4 Position
Author(s) -
Wu Qingyi,
Gao Pan,
Yuan Yu
Publication year - 2021
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.202000721
Subject(s) - indole test , chemistry , regioselectivity , catalysis , rhodium , surface modification , benzene , leaving group , combinatorial chemistry , stereochemistry , medicinal chemistry , organic chemistry
The indole motifs play a significant role in the pharmaceutical exploitation and the synthesis of naturel products, and transition metal catalyzed selective C−H bond activation of indoles has received extensive attention. However, the functionalization of C−H bonds on the benzene core is still a great challenge. By installing a bulky protecting group on the nitrogen and under the assistance of an ester directing group, we realized the Rh‐catalyzed alkenylation of indole at C4 position with high efficiency. This catalytic method exhibits satisfactory functional group compatibility and regioselectivity.