A Pd(II)-catalyzed C(sp)-H/C(sp)-H coupling/annulation of anilides and α-dicarbonyl compounds for the synthesis of diverse -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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http://dx.doi.org/10.1021/acs.orglett.0c00877DOI Listing

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