期刊
ADVANCED SYNTHESIS & CATALYSIS
卷 358, 期 17, 页码 2714-2720出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201600297
关键词
aldehydes; C-H activation; indoles; indolines; ruthenium
资金
- National Research Foundation of Korea (NRF) - Korea Government (MSIP) [2016R1A4A1011189, 2015R1A2A1A15053033]
The ruthenium(II)- or rhodium(III)-catalyzed pyrimidinyl-directed Grignard-type C-H additions of N-heterocycles with activated aldehydes and ketones are described. A cationic ruthenium catalyst and sodium acetate additive in dichloroethane as solvent were found to be optimal catalytic system for the construction of C-7 alkylated indolines. In sharp contrast, a cationic rhodium complex allows the generation of C-2 alkylated indoles and pyrroles as well as C-1 alkylated carbazoles. The site-selective C-H functionalization of these heterocyclic scaffolds could be an important asset towards the development of novel bioactive compounds.
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