Journal
ORGANIC LETTERS
Volume 21, Issue 21, Pages 8662-8666Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b03276
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Funding
- Thousand Youth Talents Plan
- NSFC [21672145, 51733007, 21602131]
- STCSM [17JC1403700]
- Drug Innovation Major Project of the Ministry of Science and Technology of China [2018ZX09711001-005-002]
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A versatile dual H-bonds and pi-pi-interaction strategy that enables enantioselective remote C6-selective C-H functionalization of 2,3-disubstituted indoles was first reported. The N-H bond of indole was pivotal to achieve the C6 functionalization with excellent yield and enantioselectivity. Furthermore, this methodology leads to the efficient construction of numerous enantioenriched C6-functionalized indole products under mild reaction conditions employing different electrophiles. Preliminary cell proliferation investigations revealed that the synthesized chiral C6-substituted indole derivatives had potential anticancer activities.
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