Journal
ORGANIC LETTERS
Volume 22, Issue 9, Pages 3397-3401Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c00877
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Funding
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [2018R1A2B2004432]
- Korean Ministry of Education, Science, and Technology [2012M3A7B4049675]
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A Pd(II)-catalyzed C(sp(3))-H/C(sp(2))-H coupling/annulation of anilides and a-dicarbonyl compounds for the synthesis of diverse N-acyl indoles is described. The reaction is achieved by cascade C-H activation, coupling, and intramolecular cyclization. This protocol provides a variety of indoles with high functional group tolerance and excellent regioselectivity. The utility of this protocol is demonstrated by transforming the synthesized compound into diversely functionalized analogues.
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